MPCST SPONSORED National Seminar DRUG DISCOVERY s/Archive-2017/March-2017/AIPER... · mpcst sponsored national seminar drug discovery ... pp-37 new eco-friendly titrimetric analysis

MPCST SPONSORED

National Seminar

DRUG DISCOVERY THROUGH REVERSE PHARMACOLOGY & ITS

TRANSFORMATION INTO

MODERN THERAPEUTICS CURRENT STATUS, CHALLENGES & OPPORTUNITIES

27th March 2017

ABSTRACT

BOOK

Organized By

Acropolis Institute of Pharmaceutical Education and Research www.aiper.ac.in

http://www.aiper.ac.in/

Acropolis Institute of Pharmaceutical Education & Research, Indore

Drug Discovery through Reverse Pharmacology & its Transformation into

Modern Therapeutics: Current Status, Challenges & Opportunities

Acropolis Institute of Pharmaceutical Education & Research (AIPER) is nurtured

by Teach for India Education & Research Society having objective of creating state of

art, world class and high quality technical education facilities at Indore. Towards

fulfilment of its objective society established AIPER in the year 2008. AIPER is a

philanthropic organization sprawled in an area of around 2 acres and is committed to

the service of humanity through technological advancement. The institute offers Masters

degree in Pharmaceutics and Bachelor’s degree in Pharmacy. The institute is approved

by AICTE, New Delhi, PCI & CPCSEA and is affiliated to Rajiv Gandhi Technical

University (RGPV), Bhopal.

ABOUT THE INSTITUTE




The seminars, conferences act as a platform for academicians, industrialist, research

scholars and students for sharing knowledge of drug discovery in the area of

Pharmaceuticals, Cosmetics, Neutraceuticals and Allied segments.

I send my greetings and best wishes to the local organizing committee and all the

participants for the grand success of seminar and also the deliberations. I also extend

my best wishes for all the academic lectures and the scientific session.

Mr. Ashish Sojatia

Group Chairman

Acropolis

Indore (M.P.)

I am feeling immense pleasure to know that Acropolis Institute of

Pharmaceutical Education & Research is going to organize

MPCST Sponsored National Seminar on “Drug Discovery

through Reverse Pharmacology & its Transformation into

Modern Therapeutics: Current Status, Challenges &

Opportunities” on 27th March 2017.

GROUP CHAIRMAN’S MESSAGE




There could have not been any more relevant theme for National seminar in

Pharmaceutical sciences to know the proper utilization of traditional knowledge, modern

tools in discovering novel lead molecules from plants by employing Reverse

Pharmacology techniques.

I hope this seminar will open up the discussion to help up the entire participant in the

field of recent development in drug discovery. The seminar will definitely help and open

a new area of research to the researchers by utilizing traditional medicinal knowledge. I

wish the seminar to be a thought provoking, intellectually stimulating event, igniting the

minds of participants for drug discovery and development through Reverse

Pharmacology.

I also take this opportunity in thanking MPCST for sponsoring this event.

Dr. G.N. Darwhekar Principal

AIPER Indore (M.P.)

It gives me immense pleasure in welcoming all the dignitaries,

speakers and delegates to the MPCST Sponsored National Seminar

on “Drug Discovery through Reverse Pharmacology & its

Transformation into Modern Therapeutics: Current Status,

Challenges & Opportunities” on behalf of Acropolis Institute of

Pharmaceutical Education & Research.

PRINCIPAL’S MESSAGE




ABOUT SEMINAR

Reverse pharmacology is the science of integrating documented clinical experiences

and experiential observations into leads by transdisciplinary exploratory studies and

further developing these into drug candidates or formulations through robust preclinical

and clinical research. In recent years the revived scientific interest in plant-derived

natural product-based drug discovery has been observed due to scientific and

technological advances in the relevant research fields. The present seminar will

highlight issues related to the proper utilization of traditional knowledge, modern tools in

discovering novel lead molecules from plants by employing reverse pharmacology

techniques. The seminar will definitely help and open a new area of research to the

researchers by utilizing traditional medicinal knowledge.

OBJECTIVES OF THE SEMINAR

The objective of the proposed seminar is to understand the role of medicinal plants in

discovery of new drugs which will provide a new area of research to understand and

explore the plethora of medicinal plants and traditional knowledge for its transformation

into modern therapeutics to achieve the goal of “Health For All”.

TOPICS TO BE DISCUSSED

Drug Discovery status in India

Country’s contribution in the drug development

Detailed process of drug discovery from lab to market including the time and cost

involved at each stages

Challenges involved in the plant origin drug discovery and its regulatory status

including the patentability

Country’s Scope and opportunity in the current scenario. etc




Dr. Shailendra Saraf

Vice- President, Pharmacy Council of India

Mr. Sanjay Tiwari

Vice President, Sun Pharmaceutical Industries Ltd.

Dr. Swarnalata Saraf

Professor, University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur

(C.G.)

Vice- President, Association of Pharmacy Teachers in India

Dr. Manish Wanjari

Scientist 2, Regional Ayurveda Research Institute for Drug Development, Gwalior,

CCRAS, Ministry of AYUSH, Government of India

Dr. Adnan Naim

Department of Bioscience and Biomedical Engineering, IIT Indore

Dr. C Karthikeyan

Assistant Professor, School of Pharmaceutical Sciences, RGPV Bhopal

CHIEF GUEST

GUEST OF HONOURS & INVITED SPEAKERS




CHIEF PATRONS Shri Ashok Sojatia Shri Ashish Sojatia

PATRONS

Prof. M.K. Dube Dr. Shamsher Singh

TECHNICAL ADVISOR

Dr. D.K. Jain Director, COP, IPS Academy

ORGANIZING CHAIRMAN

Dr. G.N. Darwhekar

CONVENER Mr. Praveen Sharma

CO- CONVENER Mr. Ashish Gupta

REGISTRATION COMITTEE

Mr. Vikas Jain Ms. Ankita Mane

Ms. Archana Patidar

SCIENTIFIC COMMITTEE

Ms. Lata Sharma Ms. Ritu Soudawat

Ms. Akanksha Dwivedi Ms. Rakhi Khabiya

STAGE COMMITTEE

Mr. Mukul Sharma Ms. Anamika Singh

HOSPITALITY COMMITTEE

Mr. Ravi Sharma Mr. Anupam Mishra

WEB & MEDIA Dr. Kunjbihari Sulakhiya

Ms. Priyanka Joshi Ms. Priyanka Mishra

Organizing Institute Acropolis Institute of Pharmaceutical Education & Research, Indore

ORGANIZING COMMITTEE





MPCST SPONSORED

National Seminar on Drug Discovery through Reverse Pharmacology & its Transformation into Modern Therapeutics: Current Status, Challenges &

Opportunities

TIME EVENT

8:30AM-9:30AM REGISTRATION & BREAKFAST

9:30AM-10:30AM PREINAUGRAL SESSION

10:30AM-11:30AM INAUGURAL CEREMONY

11:30AM-12:30PM SCIENTIFIC SESSION I

12:30PM- 1:30PM SCIENTIFIC SESSION II

1:30PM-2:00PM LUNCH

2:00PM-3:00PM SCIENTIFIC SESSION III

3:00PM-4:00PM POSTER PRESENTATION

4:00PM-5:00PM VALEDICTORY

5:00PM-5:30PM HIGH TEA

SEMINAR PROCEEDINGS




Acropolis Institute of Pharmaceutical Education & Research, Indore Page 1



INDEX

ABSTRACT NO.

TITLE PRESENTING AUTHOR

PP-01 PREDICTION OF SITE OF METABOLISM FOR CYTOCHROME P450 1A2 LIGANDS AND VIRTUAL SCREENING MODELS

Dr. Elangovan Manivannan

PP-02 DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF 3-(2-OXO-2-ARYLETHYLIDENE)INDOLIN-2-ONES AS POTENTIAL ANTI-BREAST CANCER AGENTS

Dr. C. Karthikeyan

PP-03 RATIONALIZATION OF MOLECULAR DESCRIPTORS OF CYCLIC-UREA DERIVATIVES AS HIV PROTEASE INHIBITORS: A QSAR STUDIES

Dr. M.C.Sharma

PP-04 EFFECT OF ACACIA NILOTICA L. ON DRUG INDUCED SEXUAL DYSFUNCTION IN MALE RATS.

Dr. Neelesh Malviya

PP-05

STRUCTURE-BASED VIRTUAL SCREENING AND IN-SILICO ADMET PROFILING ON PTP1B RECEPTOR FOR IDENTIFICATION OF POTENTIAL CELL PERMEABLE INHIBITORS OF NOVEL ANTI DIABETIC AGENT

Mr. Neelesh Maheshwari

PP-06 3D-QSAR STUDIES OF 3-[4-(1H-IMIDAZOL-1-YL) PHENYL] PROP-2-EN-1-ONES AS ANTILEISHMANIAL AGENTS

Ms. Ritu Soudawat

PP-07 FORMULATION AND EVALUATION OF PLURONIC LECITHIN ORGANOGEL OF LORNOXICAM FOR TOPICAL DELIVERY.

Ms. Prerana Mishra

PP-08 SPECTROPHOTOMETRIC ESTIMATION OF TOTAL TANNIN CONTENT IN SOME AYURVEDIC EYE DROPS

Dr. Vishal Soni

PP-09 IN-VITRO ANTIUROLITHIATIC ACTIVITY OF ALCOHOLIC AND HYDROALCOHOLIC EXTRACTS OF KALANCHOE PINNATA LEAVES

Dr. Priyanka Soni

PP-10 IN VITRO SCREENING OF ETOPOSIDE HYDROGEL FOR ITS PROPERTY AGAINST MELANOMA (B16F10) & LUNG (L-132) CANCER CELL LINES

Mr. Anupam Mishra

PP-11 HIGH POTENTIAL ACTION OF AGOMELATINE FOR THE TREATMENT OF OBSESSIVE COMPULSIVE DISORDER

Dr. Shaily Chaudhary

PP-12 ANTI INFLAMMATORY & ANTI ULCER ACTIVITY OF JASMINUM SAMBAC IN WISTAR RATS.

Mr. Anupam Mishra

PP-13 REVERSE PHARMACOLOGY: A NEW APPROACH TO DRUG DISCOVERY AND DEVELOPMENT AND ALSO AMELIORATES PROCESS.

Mr. Vikas Kumar Jain

PP-14 APPROACHES IN THE DEVELOPMENT OF QUALITY PARAMETERS OF MEDICINAL PLANTS WITH REFERENCE TO ENDANGERED MEDICINAL PLANTS

Dr. Sumeet Dwivedi

PP-15 MODELING OF CARBONIC ANHYDRASE INHIBITOR-I (CA-I) WITH LOG KI (NANOMOLAR AFFINITY)

Ms. Sarla Biloniya,




PP-16 DRUG DISCOVERY: JOURNEY FROM CONCEPT TO MARKET Ms. Saloni Kakkar

PP-17 FORMULATION & EVALUATION OF BERBERINE NANOPARTICLES FOR ADMINISTRATION THROUGH NASAL ROUTE

Ms. Ankita Mane

PP-18 NETWORK P[HARMACOLOGY Ms. Anamika Singh

PP-19 SOLID DISPERSION: A REVIEW Mr. Abhishek

Yaduvanshi

PP-20 ANTIDEPRESSANT ACTIVITY OF HYDROALCOHOLIC EXTRACT OF BUCHANANIA LANZAN

Ms. Aashruti Agrawal

PP-21 HERBAL PLANTS CONTAINING CHOLINESTERASE INHIBITORS ACTIVITY APPROACH FOR MEMORY ENHANCING

Mr Aman Mourya

PP-22 A REVIEW: ON MEDICATED TAPE Mr. Ankit Gupta

PP-23 CARBON NANOTUBES : A REVIEW Mr. Avinash Sharma

PP-24 ANTIPARASITIC ACTIVITY OF NYCTANTHES ARBOR-TRISTIS LINN. IN MALARIA: "REVERSE PHARMACOLOGY"

Mr. A. Nigam

PP-25 A REVIEW : ON FAST DISINTEGRATING TABLETS Mr. Beerendra

Vishwakarma

PP-26 HIGH THROUGHPUT SCREENING IN DRUG DISCOVERY PROCESS AND FUTURE ASPECTS

Mr. Farhan Qureshi

PP-27 ANTI-ANEMIC ACTIVITY OF HYDRO-ALCOHOLIC LEAF EXTRACT OF TAMARINDUS INDICA IN PHENYLHYDRAZINE INDUCED ANEMIC RATS

Ms. Deepanshu Gupta

PP-28 WNT/Β-CATENIN PATHWAY AS NOVEL TARGET FOR ANTICANCER DRUG DISCOVERY

Mr. Abhishek Rai

PP-29 IDENTIFICATION OF NOVEL ANTI-INFLAMMATORY AGENTS FOR PREVENTION OF CHRONIC DISEASES: "REVERSE PHARMACOLOGY"

Ms. H.Sayyed

PP-30 ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF JUGLANS CINEREA

Mr. Someshver Sirvi

PP-31 DEVELOPING AN ANTI-MALARIAL PHYTOMEDICINE THROUGH REVERSE PHARMACOLOGY

Ms. Manobhi Maltare

PP-32 TARGETING THE MDM2-P53 PROTEIN-PROTEIN INTERACTION FOR NEW CANCER THERAPEUTICS

Ms. Neha Trivedi

PP-33 AN ARCHETYPE SHIFT FOR MODERN DRUG DEVELOPMENT: AN APPROACH FOR CLINICAL CANDIDATE USING REVERSE PHARMACOLOGY.

Ms. Varnika Pagare

PP-34 COMBINATORIAL CHEMISTRY: “A NOVEL AND EFFICIENT APPROACH IN DRUG DISCOVERY”

Mr. Palash Prajapati

PP-35 DIURETIC ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF NYCTANTHES ARBORTRISTIS IN ALBINO RATS

Mr. Pawan Goud

PP-36 SUBLINGUAL TABLETS : AN OVERVIEW Ms. Sheetal Sem

PP-37 NEW ECO-FRIENDLY TITRIMETRIC ANALYSIS OF ASPIRIN Ms. Smriti Mishra




TABLETS USING MIXED HYDROTROPIC SOLUBILISATION

PP-38 TREATMENT OF TUBERCULOSIS FROM DRUG DEVELOPED THROUGH SOIL BACTERIA

Ms. Soniya Pillai

PP-39 PILOT PLANT DEVELOMENT OF MARIJUANA TAMPONS Ms. Sunayna Joshi

PP-40 DESIGN AND DEVELOPMENT OF MICROEMULSION DRUG DELIVERY SYSTEM OF FELODIPINE FOR IMPROVEMENT OF ORAL BIOAVAILABILITY’’

Ms. Rinku Verma

PP-41 NEW ECO-FRIENDLY APPLICATION OF MIXED HYDROTROPIC SOLUBILISATION FOR TITRIMETRIC ANALYSIS OF ACECLOFENAC TABLETS

Mr. Sunil Goyal

PP-42 MEMORY ENHANCING ACTIVITY OF BUCHANANIA LANZAN BY SCOPOLAMINE INDUCED AMNESIA IN RATS

Mr. Priyanshu Shekar

PP-43 A REVIEW: ON GASTRORESISTENT MICROPARTICLES CONTAINING SODIUM-PANTOPRAZOLE: STABILITY STUDIES AND IN-VIVO ANTIULCER ACTIVITY

Ms. Priyanka Yadav

PP-44 5 ACETIC ACID PEPTIDE HYBRID DERIVATIVES AS POTENT ANTIDIABETIC AGENTS "REVERSE PHARMACOLOGY"

Mr. R. Sharma

PP-45 NOVEL CARBAZOLE TETHERED PYRROLE DERIVATIVES AS POTENT INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS "REVERSE PHARMACOLOGY"

Mr. R. Adhav

PP-46 ANTI-DIABETIC EFFECT OF MAHANIMBINE FROM MURRAYA KOENIGII: REVERSE PHARMACOLOGY

Ms. Supriya Shidhaye

PP-47 NATURAL GUMS AS SUPERDISINTEGRANTS IN FORMULATION OF MOUTH DISSOLVING TABLETS- A REVIEW

Mr. Sovran S Thakur

PP-48 ADR IN HERBAL MEDICATION WITH MAINSTREAM MEDICAL THERAPIES

Ms. Garima Sharma

PP-49

ISOLATION OF AMYLASE PRODUCING BACTERIA FROM SOIL AND ITS OPTIMIZATION OF PRODUCTION PARAMETERS BY SHAKE FLASK CULTURE METHOD

Ms. Nidhi Nair

PP-50 CUTTING EDGE IN DRUG DISCOVERY AND DEVELOPMENT – REVERSE PHARMACOLOGY

Ms. Mehazabeen Kachchawala

PP-51

INHIBITION OF MATRIX METALLOPROTEINASE – 2 (MMP) IN DMH INDUCED COLON CANCER IN SD RATS IN THE PRESENCE OF DIETARY SUPPLEMENTS AND CHEMOTHERAPY: A MECHANISM AND PROBLEMS BASED APPROACH

Mr. Taha Hakimi

PP-52 IN VITRO ANTI OXIDANT ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF CAESALPINIA BONDUC

Ms. Sweta S Koka




PREDICTION OF SITE OF METABOLISM FOR CYTOCHROME P450 1A2 LIGANDS AND VIRTUAL

SCREENING MODELS

Elangovan Manivannan*and N.S. Hari Narayanan Moorthy

School of Pharmacy, Devi Ahilya Vishwavidyalaya, Indore-452001 (M.P.)

Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak-484887

[email protected]

ABSTRACT

Cytochrome P450 (CYP) 3A4, 2D6, 2C9, 2C19, and 1A2 are the most important drug-metabolizing

enzymes. Understanding of which parts of a drug molecule are subject to metabolic reactions catalyzed

by these enzymes is crucial for drug design. With the availability of large number of high resolution crystal

structures of human cytochrome P450 enzymes made possible the utility of structure-based molecular

modeling tools to study cytochrome P450. In the present study we explore the possibilities of employing

docking and scoring functions on cytochrome P450 1A2. An Attempt has been made to address the

issues like prediction of binding orientations and conformations for various substrates, a virtual screening

with satisfactory enrichment rates. The results show that docking and scoring can be used successfully to

address the issues. Results of the structure-based modeling were compared to experimental data. The

possibilities and limitations of using structure-based drug design tools for cytochrome P450 1A2 are

discussed in detail.

Keywords: Cytochrome P450 (CYP), metabolism, ligands, screening models.

PP - 01

mailto:[email protected]




DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF 3-(2-OXO-2-ARYLETHYLIDENE)

INDOLIN-2-ONES AS POTENTIAL ANTI-BREAST CANCER AGENTS

C. Karthikeyan1*, H. Lee2, M. R. Mustafa3 and P. Trivedi1

1Schoool of Pharmaceutical Sciences,Rajiv Gandhi Proudyogiki Vishwavidyalaya, Bhopal-462033, India.

2Advanced Medical Research Institute of Canada, Sudbury, Ontario P3E 5J1, Canada.

3Department of Pharmacology, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia.

[email protected]

ABSTRACT

Breast cancer is one of the most commonly diagnosed cancers among women and it is the second

leading cause of cancer deaths in women worldwide. The present study describes discovery of a novel

series of 3-(2-oxo-2-arylethylidene) indolin-2-ones as potential antibreast cancer agents. Fourteen 3-(2-

oxo-2-phenylethylidene) indolin-2-ones designed employing molecular hybridization approach were

synthesized and evaluated for growth inhibitory activity against three breast cancer cell lines (MDA-

MB231, MDA-MB468 and MCF-7) and one non-cancer breast epithelial cell line (184B5) using SRB

protocol. The results indicated that most of the compounds showed promising anticancer activity (<20

µM) against the studied cancer cell lines. Compound 3m bearing a 5- chloro substituent in the benzo ring

of the Isatin moiety and 3, 4-dimethoxy substitution in the phenyl ring was found to be the most active in

the series with IC50 values of 8.54, 4.76 and 3.59 against MDA-MB231, MDA-MB468 and MCF-7 cells,

respectively. The mechanism of cytotoxicity of 3m was studied in MCF-7 cells and the results revealed

that 3m induces intracellular ROS generation, which causes DNA damage, increased membrane

permeability and activation of a mitochondria-dependent caspase cascade resulting in apoptosis. Overall,

the findings of the mechanistic studies highlight 3m as a potential new lead molecule for the development

of novel anticancer agents with potential therapeutic benefits in breast cancer.

Keywords: Breast cancer, molecular hybridization, anticancer, apoptosis.

PP - 02




RATIONALIZATION OF MOLECULAR DESCRIPTORS OF CYCLIC-UREA DERIVATIVES AS HIV

PROTEASE INHIBITORS: A QSAR STUDIES

Sharma M.C.*

*School of Pharmacy, Devi Ahilya University, Khandwa Road, Indore (M.P) - 452 001, India

[email protected]

ABSTRACT

Herein described is quantitative structure activity analysis of a series of cyclic-urea derivatives were taken

as HIV protease inhibitors with inhibitory HIV were developed. The best quantitative structure activity

relationship model was selected having a correlation coefficient (r2) of 0.7562, cross-validated correlation

coefficient (q2) of 0.7218. The model selected emphasized the importance of Highest Occupied

Molecular Orbital, and lowest unoccupied molecular orbital energy suggest that a good percentage of the

total variance in biological activity. Based on the findings of the QSAR study, novel compounds for HIV

protease inhibitors can be synthesized.

Keywords: QSAR, multiple linear regressions, cyclic-urea, Chem‐Office 8.0, HIV protease inhibitors

PP - 03




EFFECT OF ACACIA NILOTICA L. ON DRUG INDUCED SEXUAL DYSFUNCTION IN MALE RATS

Neelesh Malviya*

Department of Pharmacognosy

Smriti College of Pharmaceutical Education, Indore, M.P.

[email protected]

ABSTRACT

Acacia nilotica L. commonly known as babool is one of the most widely used medicinal plants in Indian

system of medicine and traditionally used as antiplasmodial, anti-inflammatory, analgesic and antipyretic.

It has been reported to have antidiabetic, antioxidant and considerable inhibitory effects against HIV-1

protease. In traditional system of medicines, stem of Acacia nilotica is often recommended for the

management and treatment of Male sexual dysfunctions. However, convincing scientific data to support

the aforesaid claim is lacking. Thus in the absence of any scientific evidence, in the present study an

attempt was taken to investigate the effect of alcoholic extract of Acacia nilotica L. stem on male rat

sexual behavior and its effects on androgenic hormones in paroxetine induced reproductive dysfunction in

experimental male rat model. Alcoholic extract of stem of Acacia nilotica at the dose of 500mg/kg body

weight was administered in male rats and mount frequency, intromission frequency, ejaculatory

frequency, mount latency, intromission latency, ejaculatory latency and post-ejaculatory interval, sperm

profile, testes weight, testicular index, hormones level and histoarchitecture of reproductive organs were

the parameters observed and compared during the study. Results observed from the study revealed that

the alcoholic extract of stem of Acacia nilotica at the dose of 500mg/kg body weight, significantly restore

the sexual behaviour in paroxetine induced reproductive dysfunction in experimental male rat model.

Keywords: Indian system of medicine, Male Sexual Dysfunction, Acacia nilotica, Paroxetine, Medicinal

Plant

PP - 04




STRUCTURE-BASED VIRTUAL SCREENING AND IN-SILICO ADMET PROFILING ON PTP1B

RECEPTOR FOR IDENTIFICATION OF POTENTIAL CELL PERMEABLE INHIBITORS OF NOVEL

ANTI DIABETIC AGENT

Maheshwari Neelesh#1, Karthikeyan Chandrabose1, Trivedi Piyush1 Moorthy N. S. Hari Narayana2

1 School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Bypass Road,

Gandhi Nagar, Bhopal, Madhya Pradesh.

2Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, Madhya Pradesh

[email protected]

ABSTRACT

Abstract: Protein tyrosine phosphatases (PTPs) and protein tyrosine kinases (PTKs) maintain a balance

of protein activity through the dephosphorylation and phosphorylation of proteins in a signalling pathway

and regulate virtually all aspects of cellular functions. An imbalance of PTP and PTK activities can lead to

abnormalities which causes of human diseases, such as cancers, diabetes and obesity. PTP1B is an

important member of PTP family which has been implicated as key regulators of intracellular signalling

cascades and involved in various important pathways related with diabetes and obesity. Hence, it has

been acknowledged as an outstanding therapeutic target for the treatment of cancer, diabetes along with

obesity. The aim of this study was to screen a library of small molecules In-silico for discovery of some

inhibitors of PTP1B with increased cell permeability. The molecular docking based virtual screening

results showed that compounds possessed good docking score and interacted well with the active site

residues as well as secondary aryl phosphate binding site of PTP1B enzyme. In-silico ADME prediction

studies on these hits were also found to be promising. Non-charged compounds identified as hits may act

as novel leads for PTP1B inhibitors.

Keywords: PTP1B, Diabetes and obesity, Docking, ADME prediction

PP - 05


http://igntu.nic.in/




3D-QSAR STUDIES OF 3-[4-(1H-IMIDAZOL-1-YL) PHENYL] PROP-2-EN-1-ONES AS

ANTILEISHMANIAL AGENTS

Soudawat Ritu 1, Kaskhedikar, S.G. 2

1Acropolis Institute of Pharmaceutical Education and Research, Indore, M.P.

2 Department of Pharmacy, Shri G. S. Institute of Technology & Science, Indore.

[email protected]

ABSTARCT

Leishmaniasis, a disease caused by obligate intracellular protozoa of the genus Leishmania, is an old but

largely unknown disease that afflicts the world’s large populations. WHO estimates the worldwide

prevalence to be approximately 12 million cases, with annual mortality of about 60 000. The size of the

population at risk is about 350 million. Currently the drugs used for the treatment of Leishmaniasis are

limited and are very expensive and highly toxic. The recently reported series of 3-[4-(1H-Imidazol-1-yl)

Phenyl] Prop-2-en-1-ones have activity in the range of 0.63 to 1.11 µg against Leishmania major

promastigotes and may rise another class of therapeutic agents. The molecular modeling study was

performed using P-IV processor CS Chemoffice version 8.0 and regression analysis were carried out on

VALSTAT. The various statistical parameters of the selected model are: The correlation coefficient (r)

=0.865, R-squared the coefficient of determination (r2) = 0.788, Fisher test value F=82.72, the standard

deviation of regression (SD) - 0.148, bootstrapping r2 (r2bs) - 0.798 & Q2-0.624.

Keywords: Leishmaniasis, QSAR, Antileishmanial Agents, molecular modeling.

PP - 06





FORMULATION AND EVALUATION OF PLURONIC LECITHIN ORGANOGEL OF LORNOXICAM FOR

TOPICAL DELIVERY.

Prerana Mishra*, D P Chatterjee

Mittal Institute of Pharmacy, Bhopal (M. P.)

[email protected]

ABSTRACT

Pluronic Lecithin Organogels (PLO gels) are commonly used as transdermal vehicles in compounding

pharmacies to provide customized medication for pain management as well as for other therapies. The

purpose of this research is to formulate and evaluate the suitability of pluronic lecithin organogels

containing lornoxicam for topical application. Eleven formulations were developed using lornoxicam,

soya-lecithin, Pluronic F127, isopropyl myristate, PEG-400, sorbic acid and potassium sorbate were

coded as F-1to F-11. Concentration of Pluronic F127 and soya-lecithin was varied in these formulations.

The optimized organogels were evaluated for appearance and feel rheologically, in vitro diffusion study,

drug content, viscosity and pH. Release of lornoxicam from all formulations was monitored via dialysis

membrane-70 and Wistar rat skin as a semipermeable membrane into phosphate buffer saline (0.2 M, pH

7.4) using Keshary-Chien diffusion cell. The viscosities of different formulations were determined by using

Brookfield Viscometer at 25°. An attempt has been made to explore the potential of pluronic lecithin

organogels for topical delivery of lornoxicam.

Keywords: Pluronic Lecithin Organogels, transdermal.

PP - 07





SPECTROPHOTOMETRIC ESTIMATION OF TOTAL TANNIN CONTENT IN SOME AYURVEDIC EYE

DROPS

Soni Vishal*, Soni Priyanka, Mali Tarun

Department of Herbal Drug Research, B.R. Nahata College of Pharmacy, Research Centre, Mhow

Neemuch Road, Mandsaur 458001, India

ABSTRACT

Ayurvedic eye drops preparation contains aqueous extracts of different herbs. Ethnobotanical survey

shows that plants used in Ayurvedic eye drops formulation are rich source of tannin and tannin like

compounds. Tannins are responsible for antimicrobial and antioxidant properties of Ayurvedic eye drops.

The present study was designed with the aim to determine the tannin content in two different brands of

Ayurvedic eye drops, by colorimetric method using Folin-denis reagent. The tannin content of both the

brands was found to be A-725.23 and B-556.00 μg/ml. The results obtained are reproducible with

coefficient of variation less than 0.99 %. The present approach can be used as one of the parameters for

the standardization of Ayurvedic eye drop preparations.

Keywords: Tannin estimation, antimicrobial activity, Ayurvedic eye drops, standardization etc

PP - 08




IN-VITRO ANTIUROLITHIATIC ACTIVITY OF ALCOHOLIC AND HYDROALCOHOLIC EXTRACTS

OF KALANCHOE PINNATA LEAVES

Soni Priyanka, , Soni Vishal, Chhipa Abu Sufiyan

Department of Herbal Drug Research, B.R. Nahata College of Pharmacy and Research Centre

Mhow Neemuch Road, Mandsaur 458 001, India

[email protected]

ABSTRACT

The objective of this research was to find the efficiency of alcoholic and hydroalcoholic extracts of

Kalanchoe pinnata leaves in dissolution of calcium oxalate crystals by using in-vitro dissolution model.

in-vitro dissolution model was prepared by using semi permeable membranes obtained from eggs that

served as dissolution bags for the investigation. Dissolution bags containing calcium oxalate and

different extracts were suspended in conical flasks containing TRIS buffer. Percentage dissolution of

calcium oxalate by different extracts was evaluated by titrimetry. Hydroalcoholic extract of leaves of

Kalanchoe pinnata showed more dissolution of calcium oxalate as compared to alcoholic extract.

Although the dissolution of calcium oxalate by hydroalcoholic extract was less than that of standard

drug. Results obtained from this research work indicated promising effects of Kalanchoe pinnata leaves

in dissolution of calcium oxalate. Extracts of Kalanchoe pinnata leaves can be used for the effective

treatment of urolithiasis.

Keywords: Kalanchoe pinnata, antiurolithiatic activity, calcium oxalate, hydroalcoholic, alcoholic,

cystone.

PP - 09




IN VITRO SCREENING OF ETOPOSIDE HYDROGEL FOR ITS PROPERTY AGAINST MELANOMA

(B16F10) & LUNG (L-132) CANCER CELL LINES

Mishra Anupam*1, N Ganesh2, Soni Govind2, Yadav Khushwant S2., Dhote Vipin V2

1Acropolis institute of pharmaceutical education and research, Indore

2VNS faculty of pharmacy, Bhopal

[email protected]

ABSTRACT

The present study was designed to investigate the in vitro screening of the Etoposide Hydrogel for its

property against Melanoma (B16F10) and Lung (L-132) Cancer Cell Lines.

Viability of cancer cell lines is determined by trypan blue exclusion method, in this method 10µl of cell line

& 10µl of 0.4% trypan blue stain was added thoroughly and allows staining for 5 min and to observing

under microscope. Cytotoxicity study of cancer cell lines against hydrogels of etoposide and other

anticancer drugs was determined by M.T.T assay. Cells were seeded into 96-well plate and subjected on

hydrogel treatments. 24 h before the end of experiment, 30μl of M.T.T was added and cells were

incubated at 37°C. Then medium was removed and the residue was dissolved in DMSO. The absorbance

of each well was read at 490 nm with ELISA reader. Thermosensitive Hydrogel of Etoposide showed

Anticancer activity and was found to be statistically very significant when compared to normal control with

a p value of <0.05 and <0.001 on treatment with lung cancer (L132) and Melanoma (B16F10) cell lines

respectively. The present study is a comparative study between old conventional therapeutic regimen and

modern approach of sustain release of drug i.e. hydrogels. It demonstrates that the hydrogel of etoposide

have effectively approach the cancerous cells to inhibit its potentiality. Such drug delivery is in demand in

the field of oncomedicine where the conventional drug causes huge number of cellular as well as organ

toxicity. The present study will not only approach the cancerous cells but could be able to protect normal

cell cellularity & morphology.

Keywords: Lung cancer, Melanoma, Thermosensitive Hydrogels of Etoposide, Cell lines, M.T.T assay.

PP - 10




HIGH POTENTIAL ACTION OF AGOMELATINE FOR THE TREATMENT OF OBSESSIVE

COMPULSIVE DISORDER

Shaily Chaudhary*1,Khuswant Singh Yadav1 and Nikunjana Patel2

1Smriti College of Pharmaceutical Education, 4/1, Pipliya Kumar Kakkad, MR-11, Indore, Madhya

Pradesh, India.

2Faculty of Pharmacy, Shree S. K. Patel College of Pharmaceutical Education &Research,

Ganpat University,Ganpat Vidyanagar, Gujarat, India.

[email protected]

ABSTRACT

In the present work, a randomized, double-blind, placebo-controlled trial was performed to check the

efficacy of agomelatine in treatment of anxiety disorder, prompting its therapeutic potential in treatment of

obsessive compulsive disorder (OCD). The effect of acute and chronic administration of agomelatine on

the marble burying behavior (MBB) of mice, which is reported to be an index of anticompulsive behavior,

was performed. In addition, to rule out the role of enhanced serotonergic neurotransmission, studies were

carried out in p-chlorophenylamine (PCPA). Results indicated a potent and dose dependent influence of

agomelatine on MBB of mice. However, the higher doses were found to be locomotor depressant. In

conclusion, agomelatine administration reduces the MBB in mice, which should be explored for its

potential use in the treatment of OCD.

Keywords: Agomelatine, obsessive compulsive disorder (OCD), marble-burying behavior (MBB),

melatonin.

PP - 11




ANTI INFLAMMATORY & ANTI ULCER ACTIVITY OF JASMINUM SAMBAC IN WISTAR RATS.

Mishra Anupam1*, Dangi Uma2, Sheikh Saima2, Kawadkar Manisha2, Dhote Vipin V2.

1Acropolis institute of pharmaceutical education and research, Indore

2VNS faculty of pharmacy, Bhopal

[email protected]

ABSTRACT

The present study was designed to investigate the Antiulcer activity following indomethacin induced

ulceration & Anti-inflammatory activity following histamine induced paw edema of Jasminum sambac in

rats.Adult wistar rats (180-250gm) were exposed to inflammation by using Histamine induced paw

edema. Rat received histamine (0.1ml) in saline solution for 7 days in sub-planater region of left hind paw.

Ethenolic extract of jasminum sambac leaf (400mg/kg, p.o.) given & following parameter were estimated

like percentage inhibition paw volume and Antioxidant parameters like S.O.D & L.P.O. Jasminum sambac

was evaluated for Anti-ulcer activity; ulcer was induced using indomethacin induced model. Animal were

treated with indomethacin (5mg/kg, p.o.) for 5 days for induction. Aqueous extract of jasminum sambac

stem (500mg/kg, p.o.) was administered & ulceration was evaluated by estimating ulcer index and

percentage (%) ulcer inhibition. Jasminum sambac leaf extract showed significant (*P<0.05) Reduction in

paw volume percentage inhibition, SOD activity (P<0.001) were significantly enhanced while LPO levels

(P<0.001) significantly reduced with treatment of jasminum sambac. Jasminum sambac stem extract

showed significant reduction (*P<0.05) in ulcer index & percentage ulcer inhibition as compare to control

group. Jasminum sambac showed potent Anti-ulcer & Anti-inflammatory activity which could be mediated

by antioxidant, analgesic & antispasmodic. These activities could be attributed to the presence of

glycosides like sambicin, jasminin and flavonoides. The optimum dose of Jasminum sambac which

produced gastro protective activity was found to be 500mg/kg & anti-inflammatory activity was found to be

400mg/kg in this experimental study.

Keywords: Anti-inflammatory, anti-ulcer.

PP - 12




REVERSE PHARMACOLOGY: A NEW APPROACH TO DRUG DISCOVERY AND DEVELOPMENT

AND ALSO AMELIORATES PROCESS.

Jain Vikas Kumar*, Darwhekar G N

Acropolis institute of pharmaceutical education and research, Indore

[email protected]

ABSTRACT

“Historically modern drug therapy has developed from the herbal and folklore medicine of the past with its

mixture of magic, empirical pharmacology and faith of the patient in the doctor.” Natural products of

ayurveda offer a vast potential for novel phytomolecules with clinical activity. In India, ayurveda is availed

of by more than 70% of the population. There has been a renaissance in scientific exploration of

medicinal plants with therapeutic activity. New methods have been proposed and developed for such

exploration. Ayurvedic pharmacoepidemiology, observational therapeutics and reverse Pharmacology

paths have led to significant hits, leads and drug candidates for several diseases. The active phyto-

molecules will also provide novel scaffolds for medicinal chemists to enhance efficacy and reduce toxicity.

In case of conventional R & D expenses have risen enormously in last decade but surprisingly it has not

led to a corresponding increase in the number and efficacy of new drugs. Alternatively, reverse

pharmacology also known as target base drug discovery is now becoming a popular option in the field of

drug discovery and development from bedside observations on drug effects to bench-side experiments.

This approach generates evidence of safety and efficacy at different levels of biological organization,

ranging from cell to community. Eventually the innovative integration of research methods will be

translated back to the bedside as a new drug. The article also discusses the Reverse Pharmacology

approach for natural products used for treatment of various diseases.

Keywords: Reverse Pharmacology, Ayurveda, Drug discovery and development, R&D

PP - 13





APPROACHES IN THE DEVELOPMENT OF QUALITY PARAMETERS OF MEDICINAL PLANTS WITH

REFERENCE TO ENDANGERED MEDICINAL PLANTS

Shriwas Shweta, Dwivedi Sumeet*, Dubey Raghvendra

College of Pharmacy, Dr. APJ Abdul Kalam University, Indore, (M.P.), India

[email protected]

ABSTRACT

India is among the important mega biodiversity centers of the world with nearly 45,000 known plant

species. This diversity coupled with a rich heritage of traditional knowledge in

Ayurveda, Siddha and Unani. Herbal medicines, however, are associated with a number of shortcomings

including uniform efficacy and lack of appropriate quality control measures at various stages of product

development. The present paper intends to outline the importance of development of quality parameters

towards standardization and manufacturing of botanicals especially endangered medicinal plants. The

previous finding highlights that there have been constant efforts for developing state of the art

technologies in the field of herbal research. Sincere efforts were to be taken to ensure safety, purity and

efficacy of herbal medicines by the Govt. authorities and researcher.

Keywords: India, quality control, regulations, standardization, traditional medicine

PP - 14




MODELING OF CARBONIC ANHYDRASE INHIBITOR-I (CA-I) WITH LOG KI (NANOMOLAR

AFFINITY)

Biloniya Sarla, Verma R.G., Solanki Aruna

Government Science College, Dewas

[email protected]

ABSTRACT

This paper deals with a QSAR study on a large set of carbonic anhydrase inhibitor-I using a combination

of topological descriptor. The regression analysis has been carried out assuming linear relationship

between LogKi nd topological descriptor. The analysis of the data has indicated that an excellent model is

obtained. The obtained model is further supported through cross validation.

Keywords: QSAR/ topological descriptor/ carbonic anhydrase inhibitor-I/LogKi

PP - 15

mailto:[email protected],




DRUG DISCOVERY: JOURNEY FROM CONCEPT TO MARKET

Kakkar Saloni 1*, Tahlan Sumit 1

1Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana

[email protected]

ABSTRACT

Drug development takes around 10-15 years and is an expensive, long and high-risk business.

Before a drug is deemed suitable for patients, it has to go through rigorous testing and cost-effectiveness

analyses. The need for new drugs is because of medical reasons, disease prevalence and the

likelihood of success. Before any drug can be administered to humans, it involves refining the

molecular properties until a compound is suitable. The major sources for the development of drug

candidate have always been natural compounds from plants, fungi or marine animals but nowadays focus

has shifted to genetics and proteins to create new molecules using computers. Any drug candidate has

to undergo extensive range of in vitro and in vivo test procedures prior to its administration to

humans. One of the regulatory requirements is that the drug is to be administered to animals as well

to assess its safety which is known as Pre-clinical trial. Clinical trials includes phase I in which

healthy volunteers participate to assess primarily pharmacokinetics, safety and toleration, phase II

involves the patients with the target disease to establish efficacy and dose-response relationship

and large-scale phase III studies to confirm safety and efficacy. Each drug is required to outweigh

its benefits over its risks before it will be approved by the regulatory agencies. The pre -clinical and

clinical trials as well as the manufacturing of pharmaceutical products are required to follow the

regulatory standards. The assessment of the new medicinal product’s safety continues beyond the

initial drug approval through post-marketing monitoring of adverse events.

Keywords: Drug discovery, Pre-clinical trial, Clinical trial, Safety and efficacy.

PP - 16





FORMULATION & EVALUATION OF BERBERINE NANOPARTICLES FOR ADMINISTRATION

THROUGH NASAL ROUTE

Mane Ankita, Darwhekar G.N, Gupta Ashish


[email protected]

ABSTRACT

Berberine is a protoberberine type, isoquinoline alkaloid, derived from medicinal plants such as Hydrastis

Canadensis L, Coptis rhizome & barberry plants (Berberis vulgaris). Berberine is used in indian & chinese

medicines as an antimicrobial, stomachic & in treatment of cancer, diabetes mellitus & neurodegenerative

diseases. Literature review shows that berberine distributes readily in various tissues and hence very low

amount of berberine reach to the systemic circulation which accounts for its low bioavailability (0.68 %).

Bioavailability of berberine can be improved by formulating it as nanoparticles.

Present study aims to prepare & evaluate nanoparticles containing berberine using chitosan as polymer

and administration of this nanoparticle preparation through nasal route so as to improve its bioavailability.

The nanoparticles were prepared by ionic gelation method and evaluated for particle size, zeta potential,

entrapment efficiency, In-vitro drug release & drug release kinetics.

The formulation A5 showed particle size – 104.52 nm, zeta potential – 32.40 mV and entrapment

efficiency – 30.05 %. In-vitro release studies showed improved bioavailability of 80.23 %. The drug

release kinetic studies showed that berberine nanoparticle formulation followed Higuchi & Korsmeyer-

peppas model of drug release.

Keywords: Nanoparticle, antimicrobial, bioavailability, nasal route.

PP - 17





NETWORK PHARMACOLOGY: A NOVEL APPROACH FOR DRUG DEVELOPMENT

Singh Anamika*, Darwhekar G. N.

Acropolis Institute of Pharmaceutical Education and Research, Indore

[email protected]

ABSTRACT

Network pharmacology is a distinctive new approach to drug discovery. It involves application of

network analysis to determine the set of proteins most critical in any disease, and then chemical biology

to identify molecules capable of targeting that set of proteins. It is a novel approach which works on the

principle of “multiple targets, multiple effects, complex disease” instead of the conventional principle of

“one gene, one target, one disease”. System biology is a recent trend in bioscience research which

focuses on the complex interactions in biological systems from a holistic perspective rather than altering

the single molecular component. The process of network pharmacology research includes data collection

and validation followed by network analysis and visualization. Network pharmacology can make an

impact at two main approaches in the drug development process. One is to establish a pragmatic network

model and predict the drug target based on public databases or available data of earlier researches.

Subsequently, the mechanism of functional drug should be explored for the network equilibrium principle.

The advantage of network pharmacology includes regulation of the signaling pathway with multiple

channels, increase in drug efficacy, reduction of side effects, increase in the success rates of clinical trials

and decrease in the costs of drug discovery. The advancements in systems biology and bioinformatics

and the concept of network pharmacology will undoubtedly bring about a conceptual move in drug

discovery.

Keywords: Network Pharmacology, Drug Discovery, System Biology

PP - 18





SOLID DISPERSION: A REVEW

Yaduvanshi Abhishek*, Darwhekar G.N., Gupta Ashish, Sharma Ravi


[email protected]

ABSTRACT

Upto 40 percent of new chemical entities are poorly water soluble or lipid soluble. Drugs that followes

dissolution rate limited gastrointestinal absorption results in better dissolution and good bio availability

due to decressed particle size. However reduction of particle size of drug may cause aggregation and

agglomeration those results in poor wettability. Development of solid dispersion is an effective approach

to improve bioavailability of poorly water soluble drugs by overcoming the limitations of other approaches

like formation of salt, reduction of particle size. Solid Dispersion is a novel phenomenon to overcome

these problems and to enhance the dissolution by making the solid dispersion of water soluble carriers

with poorly water soluble drugs. The overall review emphasis on bioavailablity enhancement of poorly

aqueous soluble drugs by solid dispersion technolgy which utilizes to develop various dosage forms in

convinent way.

Keywords: Solid Dispersion, Bioavailablity, Solubility, Techniques

PP - 19




ANTIDEPRESSANT ACTIVITY OF HYDROALCOHOLIC EXTRACT OF BUCHANANIA LANZAN

Agrawal Aashruti*, Joshi Ankur, Malviya Sapna, & Kharia Anil

Modern institute of Pharmaceutical Sciences, Indore

(Shri Prabhat Chandra Kharia Research and Educational Society)

Alwasa, Behind Rewti Range, Sanwer Road, Dist Indore (MP) Pin 453111

[email protected]

ABSTRACT

The present study was design to evaluate the effect of Buchanania lanzan hydro-alcoholic extract as well

as its interaction with conventional anxiolytic and antidepressant drugs using tail suspension test and

forced swim test (FST) and to evaluate the possible mechanisms involved in its actions. The rhizomes of

Buchanania lanzan were collected and authenticated. Extraction of dried rhizomes was carried out using

soxhlet apparatus to obtain its Hydro alcoholic extract. The extract of Buchanania lanzan showed the

significant antidepressant activity comparable to the standard drug. The oral administration of Buchanania

lanzan extract at 150 mg/ kg and 300 mg/kg respectively as compared to the control treated group

showed an antidepressant activity comparable to that of standard drug. The antidepressant effects of

Buchanania lanzan extract seem to be mainly associated with the activation of dopamineergic system

and possess potential anxiolytic and antidepressant activities.

Keywords: Antidepressant activity, Buchanania lanzan, forced swimming test, tail suspension test.

PP - 20




HERBAL PLANTS CONTAINING CHOLINESTERASE INHIBITORS ACTIVITY APPROACH FOR

MEMORY ENHANCING

Mourya Aman*, Joshi Ankur, Malviya Sapna, & Kharia Anil




[email protected]

ABSTRACT

Learning is the process of acquisition of information and skills, while subsequent retention of that

information is called memory. Learning and memory together called as cognition. Also, memory is a

process involving encoding, storing, and recalling information. Thus, memory records various facts and

events, make it available for further use, and hence can be considered as most valuable health asset. To

elucidate the biochemical and molecular mechanisms underlying learning and memory could be

considered as one of the challenging tasks for neuroscientists. Poor memory, lower retention, and slow

recall are common problems in today’s stressful and competitive world, especially with associated ageing

process. Neurotransmitter modification is an important method for the treatment of memory loss or

amnesia. Inhibition of acetylcholinesterase (AChE), the key enzyme in the breakdown of acetylcholine, is

considered as a promising strategy for the treatment of neurological disorder Amnesia. A potential source

of AChE inhibitors is certainly provided by the abundance of plants in nature. This article aims to provide f

plants having AChE inhibitory activity. Numerous phytoconstituents and promising plant species as AChE

inhibitors are described in this.

Keywords: Acetylcholinesterase, Phytoconstituents, Amnesia

PP - 21




A REVIEW: ON MEDICATED TAPE

Gupta Ankit*, Darwhekar G.N.


[email protected]

ABSTRACT

Medicated tape (bandage) is the popular for its self-application property. Due to its adhesive property,

dose at the site will adhere longer. Medicated tape is widely uses for the wound healing and as a

analgesics. The medicated tape is the topical drug delivery system which improves the bioavailability of

drug with the help of hydration of skin. Medicated tape has advantage over the non-conscious patients

and its self-applicability. Several advantages are their related to medicated tape easy to application, self-

application and long duration of action are major advantages. Removal of medicated tape from skin is

painful it is a major disadvantage of medicated tape. Medicated tape with controlled amount of drug in

each medicated tape is helpful to cure the disease. Medicated tape with lignocaine will reduce the

stinging and burning topically which happens by some other drugs.

Keywords: Medicated tape, Medicated tape containing lignocaine, Bandage of lignocaine, Lignocaine

PP - 22




CARBON NANOTUBES: A REVIEW

Sharma Avinash*, Sharma Praveen, Darwhekar G.N.


[email protected]

ABSTRACT

The Carbon nanotubes (CNT) are one of the most unique in the field of nanotechnology during last

decade. The cylindrical carbon molecules possess novel properties that make them quite useful for many

applications in nanotechnology. Carbon nanotubes lie between fullerenes and graphite as a quite new

member of allotropes. These allotropes of carbon derived from graphene sheet which exhibit unusual

mechanical strength i.e. toughness, elasticity. Nanotubes are classified as single-walled nanotubes and

multiple nanotubes. Generally CNTs rolled graphene with SP2 Hybridization. CNTs applied in many field

of nanotechnology, nanomedicies, nanoelectronics and biotechnology. Not only in the field of

Therapeutics but as well as these CNTs are feasible to the diagnosis purposes. There are various

technologies recently developed to synthesize CNTs including Chemical vaporize deposition (CVD), the

laser ablation method and sol gel method. Overall CNTs have shown a wide glimpse in the future of

nanotechnology and other fields of material science.

Keywords: Carbon nanotubes, synthesis, Single and multiple walled nanotubes.

PP - 23




ANTIPARASITIC ACTIVITY OF NYCTANTHES ARBOR-TRISTIS LINN. IN MALARIA: "REVERSE

PHARMACOLOGY"

A. Nigam*, M. Zaveri, G. Jain, N. Kawathekar

Dept. of Pharmacy, Shri G.S. Institute of Technology and Science,

23-Park Road, Indore (M.P)-452003, India

[email protected]

ABSTRACT

An unceasing threat of drug resistance continuously poses demand for new antimalarial drugs. A

scientific assessment of traditionally used antimalarial plants through reverse pharmacology is crucial for

a fast track drug discovery. Herbal plant Nyctanthes arbor-tristis Linn. (Parijat) is being used in clinical

practice and had shown antimalarial activity, with a parasite clearance in 76.6% of 120 patients, in an

earlier clinical study. The objective of this study is to further explore antimalarial potential of the plant

through additional objective markers.

Keywords: Malaria, anti-parasitic activity, drug resistance.

PP - 24




A REVIEW: ON FAST DISINTEGRATING TABLETS

Vishwakarma Beerendra*, Sharma Ravi, Darwhekar G.N.

Acropolis institute of Pharmaceutical Education And Research, Indore

[email protected]

ABSTRACT

Tablet is the most popular among all dosage existing today because of its convenience of self

administration, compactness easy administration and manufacturing and fast onset of action is required

for conventional therapy. Pharmaceutical research is focused on designing a fast disintegrating tablet is a

novel drug delivery system with improved patient compliance and increase bioavailability of poorly water

soluble drug. FDTs is solid unit dosage forms which disintegrate or dissolve in saliva within a few second

when put on tongue of without need of water. FDTs provide advantages particularly for bedridden,

psychiatric, pediatric and geriatric patient. Dysphagia is the most common disadvantages of conventional

tablets. The review describe the various formulation aspects superdisintegrants, conventional technology,

new patented technology, evaluation test, marketed formulation, suitability of drug candidates and future

prospects.

Keywords: Fast disintegrating tablet, conventional technique, superdisintegrants.

PP - 25




HIGH THROUGHPUT SCREENING IN DRUG DISCOVERY PROCESS AND FUTURE ASPECTS

Qureshi Farhan*, Mule Preeti, Malviya Sapna, Kharia Anil

Modern Institute of Pharmaceutical Sciences, Indore

[email protected]

ABSTRACT

High Throughput Screening (HTS) is a drug-discovery process widely used in the pharmaceutical

industry. It leverages automation to quickly assay the biological or biochemical activity of a large number

of drug-like compounds. It is a useful for discovering ligands for receptors, enzymes, ion-channels or

other pharmacological targets, or pharmacologically profiling a cellular or biochemical pathway of interest.

Typically, HTS assays are performed in "automation-friendly". It is a way of rapidly assessing a large

number of candidate compounds or genetic modulators to identify active compounds, antibodies or genes

which modulate a particular biomolecular pathway. An HTS system generally includes robotic microplate

and labware handling systems, liquid handling systems, colony pickers and laboratory instrument control

software. The wells in the microplates are filled via the liquid handling systems, and sensors are used to

evaluate the samples in the microplate, often after a period of incubation. Laboratory automation

software choreographs the entire process, ensuring accuracy within the process and repeatability

between processes. High-throughput screening (HTS) allows researchers to quickly and cost-effectively

process thousands and even hundreds of thousands (ultra-high-throughput screening, or uHTS) of

compounds, which in turn enables them to zero in on hits (compounds that display the desired

characteristic) to be advanced into the next stages of drug discovery and development. Ultra-high-

throughput screening (uHTS) is an automated methodology for conducting hundreds of thousands of

biological or chemical screening tests per day. The cut-off between high-throughput screening (HTS) and

uHTS is somewhat arbitrary. The advent of automated plate-handling and reading instrumentation, and

the replacement of radiolabeling assays with luminescence- and fluorescence-based screens, created the

opportunity for the several-hundredfold improvement in throughput represented by uHTS.

Keywords: HTS, uHTS, Microplate, fluorescence

PP - 26

http://hudsonrobotics.com/products/colony-picking/

http://hudsonrobotics.com/products/microplate-handling

http://hudsonrobotics.com/products/microplate-handling


http://hudsonrobotics.com/products/liquid-handling




ANTI-ANEMIC ACTIVITY OF HYDRO-ALCOHOLIC LEAF EXTRACT OF TAMARINDUS INDICA IN

PHENYLHYDRAZINE INDUCED ANEMIC RATS

Gupta Deepanshu*, Joshi Ankur, Malviya Sapna, & Kharia Anil




[email protected]

ABSTRACT

The aim of the present study is to evaluate the anti-anemic activity of hydro-alcoholic leaf extract of

Tamarindus indica against phenylhydrazine induced hemolytic anemia in rats. Phenylhydrazine

(60mg/kg) was administered intraperitoneally for 2 days to induce anemia in rats. The animals were

divided in to four groups of 6 animals each. Group I served as normal control, group II as anemic control,

group III as reference control administered with Vitamin B12 and group IV animals were treated with

200mg/kg, of hydro-alcoholic leaf extract of Tamarindus indica. All the test drugs were administered once

daily for 28 days through oral route. On 29th day blood was withdrawn, through tail puncture under

phenobarbitone anesthesia and subjected to the estimation of RBC, Hb and percentage Hematocrit. Both

the hydro-alcoholic leaf extract of Tamarindus indica and Vitamin B12 significantly increased the RBC, Hb

and Hematocrit levels which conclude that, Tamarindus indica leaf extract exhibits anti-anemic activity.

Keywords: Anemia, Anti-anemic activity, Tamarindus indica and Vitamin B12.

PP - 27





WNT/Β-CATENIN PATHWAY AS NOVEL TARGET FOR ANTICANCER DRUG DISCOVERY

Rai Abhishek*, Karthikeyan C., Jain Deepti

School of Pharmaceutical Sciences, Rajiv Gandhi Technical University, Bhopal.

[email protected]

ABSTRACT

The Wnt/β-catenin pathway plays crucial role in regulating several features of cell cycle progression,

apoptosis and the EMT process in many types of cancer cells. Deregulation of Wnt/β-catenin pathway

has clear implications in the process of tumorigenesis, CSC, tumor cell invasion and metastasis hence

aberrant Wnt/ β-catenin signaling has been implicated in different cancers including familial adenomatous

polyposis, sporadic colorectal cancer, hepatocellular carcinomas, pancreatic cancer, prostate cancer,

medulloblastoma, hematologic malignancies, breast and pancreatic cancer and sarcomas. Implication of

Wnt/β-catenin pathway in such a broad spectrum of cancers defines its importance in anticancer drug

discovery. The intricate regulation of β-catenin provides alternative points for therapeutic interventions.

Wnt/β-catenin pathway has been targeted at different levels including extracellular and cell membrane

level, cytoplasmic level, and nuclear levels. Targeting Wnt/β-catenin pathway for anticancer activity has

armed us with some very potent and effective molecules including LGK974, IPWs, NSC668036, OMP-

18R5, IWR1, JW55, JW74, XAV939, IWRs, PKF222-815, iCRT5, ICG-001, AVI-4126, and CCI-779 out of

which some are in clinical trials and others have shown promising activities in animal trials and cell line

studies.

Keywords: Wnt/β-catenin pathway, Cancer, embryonic pathway, Cancer stem cells.

PP - 28





IDENTIFICATION OF NOVEL ANTI-INFLAMMATORY AGENTS FOR PREVENTION OF CHRONIC

DISEASES: "REVERSE PHARMACOLOGY"

H.Sayyed*, M. Zaveri, G. Jain, N. Kawathekar

Dept. of Pharmacy, Shri G.S. Institute of Technology and Science,

23-Park Road, Indore (M.P)-452003, India

[email protected]

ABSTRACT

Inflammation, although first characterized by Cornelius Celsus, Extensive research within last three

decades has confirmed these observations and identified the molecular basis for most chronic diseases

and for the associated inflammation. The transcription factor, Nuclear Factor-kappaB (NF-kappaB) that

controls over 500 different gene products, has emerged as major mediator of inflammation. Thus agents

that can inhibit NF-kappaB and diminish chronic inflammation have potential to prevent or delay the onset

of the chronic diseases and further even treat them. In an attempt to identify novel anti-inflammatory

agents which are safe and effective, in contrast to high throughput screen, we have turned to "reverse

pharmacology" approach. We found that, a science of long life, can serve as a "goldmine" for novel anti-

inflammatory agents used for centuries to treat chronic diseases. The current review is an attempt to

provide description of various Herbal plants currently used for treatment, their active chemical

components, and the inflammatory pathways that they inhibit.

Keywords: Inflammation, transcription factor, reverse pharmacology.

PP - 29




ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF

JUGLANS CINEREA

Sirvi Someshver*, Joshi Ankur, Pathak Vishwas, Malviya Sapna, & Kharia Anil




[email protected]

ABSTRACT

Analgesic and antipyretic effects of hydroalcholic extract of fruits of Juglans cinerea (Juglandaceae) were

investigated at doses 150mg/kg b.w. and 300mg/kg b.w. using acetic-acid induced writhing, hot- plate,

tail-clip, formalin and yeast-induced pyrexia tests. Oral administration Juglans cinerea hydro-alcholic

extract produced significant (P<0.0001) reduction in no. of writhes induced by acetic-acid. Moreover, in

hot-plate test, Juglans cinerea hydro-alcholic extract significantly (P<0.0001) raised the pain threshold at

different time of observation (0-60min) in comparison with control. In tail-clip test also the extract caused a

significant (P<0.0001) inhibition of pain at both the doses used. There was a significant dose-dependent

inhibition of both phases of the formalin induced pain response in mice. Tested on yeast-induced pyrexia

in rats, Juglans cinerea hydro-alcholic extract significantly (P<0.0001) reversed hyperthermia at either

dose. The results of pharmacological tests performed in the present study suggest that Juglans cinerea

hydro-alcholic extract possesses potent analgesic and antipyretic effects.

Keywords: Juglans cinerea, Analgesic activity, Antipyretic activity.

PP - 30





DEVELOPING AN ANTI-MALARIAL PHYTOMEDICINE THROUGH REVERSE PHARMACOLOGY

Maltare Manobh*, Singh Anamika, Darwhekar G.N.


[email protected]

ABSTRACT

Reverse pharmacology is the science of integrating documented clinical/experimental hits into leads by

transdisciplinary exploratory studies and further developing these into drug candidates by experimental

and clinical research. MALARIA elimination efforts will lead to much wider use of the few currently

effective anti-malarial drugs such as artesunate .There is already discussion about intermittent treatment

of infants, pregnant women. Resistances already exist to amodiaquine and sp, and will probably increase

as a result of increase drug pressure. In this cortex it is important to maximize the lifespan of anti-malarial

and for its development the Anti-malarial Phytomedicines are used. A reverse pharmacology approach to

developing an anti-malarial phytomedicine was designed and implemented in Mali, resulting in new

standardized herbal anti-malarial after six years of research. The first step was to select a remedy for

development, through a retrospective treatment-outcome study. The second step was dose escalating

clinical trial that showed a dose-response phenomenon and helped select and most efficacious dose. The

third step was randomized controlled trial to compare the phytomedicine to standard first-line treatment.

The last step was to identify active compounds which can be used as markers for standardization and

quality control. This example of reverse pharmacology for an anti-malarial phytomedicine is developed

faster, long term and more cheaply than conventional drugs.

Keywords: Reverse pharmacology, Anti-malarial, phytomedicine.

PP - 31





TARGETING THE MDM2-P53 PROTEIN-PROTEIN INTERACTION FOR NEW CANCER

THERAPEUTICS

Trivedi Neha, Karthikeyan Chandrabose, Trivedi Piyush, Maheshwari Neelesh

School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Bypass Road,

Gandhi Nagar, Bhopal, Madhya Pradesh.

[email protected]

ABSTRACT

The p53 tumor suppressor protein is a transcriptional factor that plays a key role in regulation of several

cellular processes, including the cell cycle, apoptosis, DNA repair, and angiogenesis. The murine double

minute 2 (MDM2) protein is the primary cellular inhibitor of p53, functioning through direct interaction with

p53. Design of non-peptide, small-molecule inhibitors that block the MDM2-p53 interaction has been

sought as an attractive strategy to activate p53 for the treatment of cancer and other human diseases.

Major advances have been made in the design of small-molecule inhibitors of the MDM2-p53 interaction

in recent years, and several compounds have moved into advanced preclinical development or clinical

trials.

Keywords: HDM2 • Inhibitors • MDM2 • Protein-protein interactions.

PP - 32





AN ARCHETYPE SHIFT FOR MODERN DRUG DEVELOPMENT: AN APPROACH FOR CLINICAL

CANDIDATE USING REVERSE PHARMACOLOGY.

Pagare Varnika*, Soni Priyanka, Patidar Archana, Darwhekar G. N.

Acropolis Institute of pharmaceutical Education and Research, Indore.

[email protected]

ABSTRACT

A trans-disciplinary endeavor in the field of drug discovery called reverse pharmacology, also known as

target-based drug discovery (TDD), is a hypothesis that involves modulation of the activity of a specific

protein target. The approach leverages on chemical and biological information about ligands and/or

biological targets to identify and optimize new drugs. This has been made possible by increase

identification of molecular targets, elucidation of the 3D structures by X- ray crystallography and nuclear

magnetic resonance (NMR), availability of commercial, private or public data bases (of biological targets

and ligands) and availability of computer-aided drug design software. Targeting the protein and

involvement of CADD is highly beneficial starting point for drug discovery. CADD employs the use of in

silico filters to identify hits (active drug candidates), eliminate compounds with undesirable properties

(poor activity and/or poor Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET), selects

the most promising candidates for further evaluation, and optimizes these leads i.e. transform biologically

active compounds into suitable drugs by improving their physicochemical, pharmaceutical, ADMET/PK

(pharmacokinetic) properties. It involves Screening of chemical libraries of small molecules which is used

to identify compounds that bind with high affinity to the target. The hits from these screens are then used

as starting points for desired clinical candidate. Differently than the classical (forward) pharmacology, with

the reverse pharmacology approach in vivo efficacy of identified active (lead) compounds is usually

performed in the final drug discovery stages.

Keywords: Reverse pharmacology, X- ray crystallography, CADD, data bases.

PP - 33


https://en.wikipedia.org/wiki/Biological_target

https://en.wikipedia.org/wiki/Drug_discovery

https://en.wikipedia.org/wiki/High-throughput_screening

https://en.wikipedia.org/wiki/Lead_compound

https://en.wikipedia.org/wiki/Small_molecule

https://en.wikipedia.org/wiki/Chemical_library

https://en.wikipedia.org/wiki/Classical_pharmacology




COMBINATORIAL CHEMISTRY: “A NOVEL AND EFFICIENT APPROACH IN DRUG DISCOVERY”

PrajapatiPalash*, Muley Preeti, MalviyaSapna, Kharia Anil


[email protected]

ABSTRACT

Combinatorial Chemistry is defined as the systematic and repetitive covalent connection of a set of

different ‘building blocks’ of varying structures to each other to yield a large array of diverse molecular

entities (libraries) simultaneously. Combinatorial chemistry involves the rapid synthesis or the computer

simulation of a large number of different but often structurally related molecules or materials.

Combinatorial chemistry is especially common in CADD (Computer Added Drug Design).The logical

development of receptor technology is closely connected with the changes in strategy of chemical

synthesis. High Throughput Screening provides the most promising substances. The vast number of

chemical compounds produced by Combinatorial Chemistry and the possibility of testing many

compounds, including natural products, in a short period of time by HTS attracted attention of many

workers. It has become possible to use solid- or solution-phase syntheses with different chemistries and

scaffolds to produce libraries tailor-made for finding or optimizing a lead directed at almost any class of

target. Various detection techniques like Fluorescence resonance energy transfer (FRET), Homogeneous

time resolved fluorescence (HTRF), etc are available, and the screening of more than 100,000 samples is

per day possible. With the introduction of robotics, automation and miniaturization techniques, it has

become feasible to screen 50,000 compounds a day with complex work-stations. Today, Cell-based

assays are used in more than half of all High throughput drug screening for target validation and ADMET

(Absorption, Distribution, Metabolism, Elimination and Toxicity) in the early stage of drug discovery.

Keywords: Combinatorial chemistry, HTS (High throughput screening), Libraries, Cell-based assays,

Miniaturization

PP - 34




DIURETIC ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF NYCTANTHES ARBORTRISTIS IN

ALBINO RATS

Goud Pawan*, Joshi Ankur, Malviya Sapna, & Kharia Anil


[email protected]

ABSTRACT

In the present study hydro-alcoholic extract of Nyctanthes arbortristis was prepared using soxhlets

apparatus. Albino rats were divided into 5 groups of 6 rats each. Group-I (Control) received distilled

water 25ml/kg orally. Group-II (Standard). received Furosemide 20mg/kg orally. Group-III received

hydro-alcoholic extract of Nyctanthes arbortristis 100 mg/kg, Group-IV received hydro-alcoholic extract

of Nyctanthes arbortristis 200 mg/kg and Group-V received hydro-alcoholic extract of Nyctanthes

arbortristis 400 mg/kg. The urine samples were collected for all the groups upto 5 hours after dosing

and urine volume was measured. Urine was analysed for electrolytes (Na+, K+ and Cl-). ANOVA,

Dunnet’ s test and p-values were measured and data was analysed. hydro-alcoholic extract of

Nyctanthes arbortristis exhibited significant diuretic activity by increasing urine volume and also by

enhancing elimination of Sodium (Na+), Potassium (K+) and Chloride (Cl-) at doses of 100 and

200mg/kg. hydro-alcoholic extract of Nyctanthes arbortristis possesses significant diuretic activity.

Keywords: Diuretics, Nyctanthes arbortristi, Furosemide,

PP - 35




SUBLINGUAL TABLETS: AN OVERVIEW

Sem Sheetal, Gupta Ashish, Darwhekar G.N.


[email protected]

ABSTRACT

The Demand of Sublingual tablets are growing rapidly now a days for geriatric and pediatric patients

suffering from dysphagia. Sublingual administration is most convenient providing ease of administration,

painless, enhancing bioavailability. Drug delivery via sublingual route is one of the most promising

alternatives that is useful for rapid onset of action with better patient compliance than orally ingested.

Sublingual means “under the tongue”, which refers that administering drug through mouth in such a way

that the substance is rapidly absorbed via blood vessels under tongue. The mechanism involved in drug

transfer across the oral mucosa is majorly passive diffusion. Then the drug further diffuses into venous

capillary and eventually reaches to the systemic circulation via the jugular vein. In permeability concept,

most preferable is sublingual area which is more permeable than buccal and palatal area. The portion of

drug which is absorbed through sublingual route avoid hepatic first pass metabolism and enhance the

bioavailability of drug. Several techniques can be used to formulate sublingual tablets. The review

emphasize on sublingual tablets, factors affecting sublingual absorption, advantages and various

evaluation parameters with available marketed formulations.

Keywords: Sublingual tablets, Oral cavity, Enhanced bioavailability, Dysphagia.

PP - 36




NEW ECO-FRIENDLY TITRIMETRIC ANALYSIS OF ASPIRIN TABLETS USING MIXED

HYDROTROPIC SOLUBILISATION

Mishra Smriti *, Maheshwari R.K., Likhar Sumit

Department of Pharmacy, Shri G.S. Institute of Technology and Science, Indore-452003, India

[email protected]

ABSTRACT

In the present study, a blend of 15% w/v sodium salicylate, 5%w/vniacinamide, 5%w/vsodium acetate and

5% w/v sodium citrate is prepared to carry out estimation of aspirin tablets. The solubility of aspirin in

distilled water at room temperature was found to be 1.31 mg/ml. The solubility of aspirin was significant in

this mixed hydrotropic blend (133.9 mg/ml). The crushed powder of tablets of aspirin were extracted using

this blend. The analysis of the drug was done by titrimetric analysis in 0.5M hydrochloric acid. Various

organic solvents like methanol, chloroform, dimethyl formamide and ethanol have been employed for

solubilisation of poorly water soluble drugs to conduct their titrimetric analysis. This proposed method for

analysis is recommended because it eliminates the use of toxic solvents and it is a novel, rapid, accurate

and reproducible method that is economic as well. Statistical data proved accuracy, precision and

reproducibility of the proposed analytical method.

The proposed method uses the concept of mixed hydrotropy and provides an alternative method of

analysis where the toxicity of solvents can be eliminated.

Keywords: Mixed hydrotropy, titrimetry, aspirin, sodium salicylate, niacinamide, sodium acetate, sodium

citrate.

PP - 37





TREATMENT OF TUBERCULOSIS FROM DRUG DEVELOPED THROUGH SOIL BACTERIA

Pillai Soniya*, Mishra Priya, Dwivedi Akanksha, Khabiya Rakhi, Darwhekar GN


[email protected]

ABSTRACT

Tuberculosis is very deadly and severely spreading infectious disease, caused by Mycobacterium

tuberculosis. In 2015 an estimated 4,80,000 cases were unresponsive to the two major drugs used to

treat tuberculosis. It is estimated more than 2,50,000 tuberculosis deaths were from drug resistant

infection. Mycobacterium tuberculosis is becoming increasingly resistant to current therapies, indicating

an urgent need to develop new and effective tuberculosis drugs.

The review describes the rapid synthesis of analogues of the sansanmycin uridylpeptide natural product.

The sansanmycin are produced by the soil bacterium streptomyces species and has a number of

interesting structural features that are unique to uridylpeptide natural product family. These natural

product analogues disrupt the activity of mycobacterium tuberculosis phospho-MurNAc pentapeptide

translocase, the integral membrane enzyme responsible for the biosynthesis of Lipid-I, a key intermediate

in mycobacterial peptidoglycan synthesis. These analogs inhibit the action of a key protein needed to

build a protective cell wall around the bacterium. Without the cell wall, the bacterium dies. This wall –

building protein is not targeted by currently available tuberculosis drugs. Thus through soil bacteria

economic and effective treatment of tuberculosis is achievable.

Keywords: Tuberculosis, soil bacteria, sansanmycin uridylpeptide.

PP - 38




PILOT PLANT DEVELOMENT OF MARIJUANA TAMPONS

Joshi Sunayna *, Dwivedi Akanksha, Darwhekar G.N.

Acropolis Institute of Pharmaceutical Education & Research, Indore. Madhya Pradesh, India.

[email protected]

ABSTRACT

Marijuana is progressively more recognized as an effective medicinal product by both the common public

and medical professionals. This abstract is about development of pilot plant of marijuana tampons. They

aren’t typically considered as tampons, but they can be used as modified tampons inserted in the form of

suppositories. Women who suffer from painful menstrual cramps sympathize with the debilitating

discomfort that arrives monthly like clockwork. However, now there’s apparently a new remedy for cramps

marijuana tampons Makers of marijuana-infused personal lubricant, created “relief suppositories” made

out of Marijuana .these suppositories “maximize the muscle relaxing and pain relieving properties of

cannabis without inducing a psychotropic ‘high’. Primary focus is on relieving pain, with an intention to

“share the powerful medicinal properties of this plant while utilizing modern extraction techniques to

standardize purity and potency.” Creating a tampon, rather than a pill, helps deliver the medicine directly

to where it is needed most. These tampons, which cost $44 for a 4-pack, are made with only three

ingredients: cocoa butter, distilled THC Oil and CBD Isolate (99.99%) from organically-grown hemp. CBD

Isolate is one of “two key active cannabinoid compounds found in cannabis,” the other being THC.

Reviewer of the suppositories claims that the pill “smells like cookie dough and cocoa butter.”There’s a

catch though—the tampons are only available in for residents of Colorado and for residents of California

with a medical marijuana card or physician’s recommendation letter. Manufacturing of marijuana

tampons can be achieved at laboratory scale and by feting local entrepreneurs and organizing awareness

camps about the effectiveness of these tampons could be briefed. Marketing and selling of marijuana

tampons could be started which would ultimately lead a good starter in local markets of India

Keywords: Marijuana tampons, Pain-killing activity, menstrual cramps, organic farming, domestic market.

PP - 39





DESIGN AND DEVELOPMENT OF MICROEMULSION DRUG DELIVERY SYSTEM OF FELODIPINE

FOR IMPROVEMENT OF ORAL BIOAVAILABILITY

Verma Rinku, Darwhekar G.N., Gupta Ashish, Sharma Praveen

Acropolis Institute of Pharmaceutical Education and Research

[email protected]

ABSTRACT

Microemulsion drug delivery system is a novel and versatile approach for overcoming the formulation

difficulties of drugs with poor aqueous solubility. The main purpose of this work was to develop an oral

microemulsion formulation for enhancing the bioavailability of felodipine. Felodipine is an antihypertensive

drug a calcium channel blocker it belongs to BCS classⅡ. It shows extensive first pass metabolism. The

bioavailability of felodipine is 15% hence it was suitable candidate for design microemulsion.

The solubility of drug was determined in various oils, surfactants and cosurfactants for selection of

components of formulations. Pseudo ternary phase diagram is a useful and important tool to study the

phase behaviour of microemulsions Pseudo-ternary phase diagrams were constructed to obtain the

appropriate components and their concentration ranges that result in large existence area of

microemulsion.

Microemulsion was prepared with 6%Isopropyl Myristate (IPM), 30% Tween 80&10% PEG-400 and54%

water respectively. Phase behaviour of the selected components was investigated by construction of

ternary phase diagrams. Optimized formulation was evaluated for drug content, zeta potential, droplet

size, pH, viscosity, in-vitro drug release profile and stability study. Globule size of optimize batch F3 was

found to be 77.57nm. In vitro release study had shown 85.34% drug release from microemulsion which

was more compared to pure drug suspension (55.1%).

Keywords: Microemulsion, antihypertensive, pseudo-ternary.

PP - 40





NEW ECO-FRIENDLY APPLICATION OF MIXED HYDROTROPIC SOLUBILISATION FOR

TITRIMETRIC ANALYSIS OF ACECLOFENAC TABLETS

Goyal Sunil *, Shah Mitali, Maheshwari, R.K.

Department of Pharmacy, Shri G.S. Institute of Technology and Science, Indore-452003, India

[email protected]

ABSTRACT

In the present study, a blend of 20% w/v sodium benzoate and 10% w/v niacinamideis prepared to carry

out estimation of aceclofenac tablets. The solubility of aceclofenac in distilled water at room temperature

was found to be0.11 mg/ml. The solubility of aceclofenac was significant in this mixe hydrotropic blend

(108.8 mg/ml). The crushed powder of the tablets of aceclofenac were extracted using this blend. The

analysis of the drug was done by titrimetric analysis in 0.1 N NaOH solution. Various organic solvents like

methanol, chloroform, dimethyl formamide and ethanol have been employed for solubilisation of poorly

water soluble drugs to conduct their titrimetric analysis. This proposed method for analysis is

recommended because it eliminates the use of toxic solvents and it is a novel, rapid, accurate and

reproducible method that is economic as well. Statistical data proved accuracy, precision and

reproducibility of the proposed analytical method.

The proposed method uses the concept of mixed hydrotropy and provides an alternative method of

analysis where the toxicity of solvents can be eliminated.

Keywords: Mixed hydrotropic solubilsation, titrimetry, aceclofenac, sodium benzoate, niacinamide.

PP - 41




MEMORY ENHANCING ACTIVITY OF BUCHANANIA LANZAN BY SCOPOLAMINE INDUCED

AMNESIA IN RATS

Shekar Priyanshu*, Joshi Ankur, Malviya Sapna, & Kharia Anil


[email protected]

ABSTRACT

The present study was undertaken to investigate the effect of Buchanania lanzan on cognitive functions,

total cholesterol levels and cholinesterase (ChE) activity in scopolamine-induced amnesia in rats. The

paste of Buchanania lanzan was administered orally at three doses (150, 300 and 600 mg/kg) for 7 and

14 consecutive days to the respective groups of rats. Piracetam (200 mg/kg) was used as a standard

nootropic agent. Learning and memory parameters were evaluated using elevated plus maze (EPM),

passive avoidance and motor activity paradigms. Brain ChE activity and serum biochemical parameters

like total cholesterol, total triglycerides and glucose were evaluated. It was observed that Buchanania

lanzan at the above-mentioned doses after 7 and 14 days of administration in the respective groups

significantly reversed scopolamine (1 mg/kg i.p.)-induced amnesia, as evidenced by a decrease in the

transfer latency in the EPM task and step-down latency in the passive avoidance task. Buchanania

lanzan reduced the brain ChE activity in rats. Buchanania lanzan also exhibited a remarkable cholesterol

and triglyceride lowering property and slight increase in glucose levels in the present study.

Keywords: Alzheimer’s disease, amnesia, Buchanania lanzan, scopolamine

PP - 42




A REVIEW: ON GASTRORESISTENT MICROPARTICLES CONTAINING SODIUM-PANTOPRAZOLE:

STABILITY STUDIES AND IN-VIVO ANTIULCER ACTIVITY

Yadav Priyanka, Darwhekar G.N.

Acropolis institute of Pharmaceutical Education And Research, Indore

[email protected]

ABSTRACT

The aim of the present work was to verify the in-vivo capability of pantoprazole –loaded microparticles to

protect the gastric mucosa against ulcer formulation and evaluate their stability under accelerated

conditins. Pentoprazole is a proton pump inhibitor used in the treatment of gastric ulcer,

gastroesophageal reflux disease and Helicobactor pylori infections associated to other diseases and the

pantoprazole-loaded microparticles were prepared by spray-drying in pilot scale, using Eudragit® S100

as polymer. Transparent glass vials containing drug-loaded microparticals were stored for 6 months at

40˚C and 75% RH. Photostabilty was tested under UVA light. Ulcers were induced by the oral

administration of absolute ethanol to rats. Regarding the drug content during the accelerate stability

study, samples showed complete encapsulation efficiency and were considered stable. The

microencapsulation of pantoprazole reduced its photodegradation. The in vivo evaluation showed that the

microparticles presented ulcers index lower than the solutions. Enteric microparticles had acceptable

stability under accelerated conditions and were efficient in protecting the stomach against ulceration

caused by ethanol.

Keywords: proton pump inhibitor, Helicobactor pylori, enteric microparticles.

PP - 43




5 ACETIC ACID PEPTIDE HYBRID DERIVATIVES AS POTENT ANTIDIABETIC AGENTS "REVERSE

PHARMACOLOGY"

Sharma R*, Zaveri M., Kawathekar N, Jain G

Department of Pharmacy, Shri G. S. Institute of Technology & Sciences,

[email protected]

ABSTRACT

The present investigation is concerned with the docking study of Thiazolidinedione 5acetic acid peptide

hybrid derivative, with the aim of discovering novel and potent anti-diabetic agent. In this study the flexible

ligand docking simulation was performed on Thiazolidinedione 5 acetic acid peptide hybrid derivative

against PPAR-ϒ agonist with PDB ID – 2POB using Glide v 5.6 of Schrodinger and LLC. All the

compounds show good Glide score compared to the class of thiazolidinedione (Rosiglitazone) as

standard drug. The derivative of 5 acetic acid peptide hybrid shows highest GLIDE score (-10.072)

compared to standard drug (-9.321). The designed compound shows Hydrogen bond interaction via Val

95 and Tyr 95 residues were found to play significant role in binding.

Keywords: reverse pharmacology, anti-diabetic agent, Thiazolidinedione, PPAR-ϒ.

PP - 44




NOVEL CARBAZOLE TETHERED PYRROLE DERIVATIVES AS POTENT INHIBITORS OF

MYCOBACTERIUM TUBERCULOSIS "REVERSE PHARMACOLOGY"

Adhav Rohit, Zaveri M, Jain G, Kawathekar N

Department of Pharmacy, Shri G.S. Institute of Technology and Science,

[email protected]

ABSTRACT

Tuberculosis (TB) is a highly dangerous infectious disease caused by the bacterial pathogen

Mycobacterium tuberculosis (Mtb). Amongst the worldwide health threats, TB continued to remain as

second leading cause of mortality from a single infectious disease. In 2012 alone, nearly 1.3 million

fatalities are due to TB and over 95% of them are occurred in low- and middle income countries. Further

TB threat has acquired a new dimension with the emergence of both multidrug- resistant TB (MDR-TB)

and extensively drug-resistant TB (XDR-TB).Recent focus in the tubercular drug research is on the

development of agents inhibiting the enzyme targets involved in potential role in the life cycle of the

pathogen. Inh A, the enoyl acyl carrier protein reductase from Mycobacterium tuberculosis is one of the

key enzymes involved in the mycobacterial fatty acid elongation cycle and has been considered as a

promising target in antitubercular screening. Inhibition of Inh A disrupts the biosynthesis of the mycolic

acids that are central constituents of the mycobacterial cell wall. Docking was performed against enoyl

acyl carrier protein reductase protein (PDB ID: 4TZK) and enoyl acyl carrier protein reductase

transpeptidase (PDB ID: 2H7M) using the GLIDE molecular docking tool implemented in the Schrodinger

software.

Keywords: Tuberculosis, multidrug- resistant TB, Inh A, Docking, pyrrole

PP - 45




ANTI-DIABETIC EFFECT OF MAHANIMBINE FROM MURRAYA KOENIGII: REVERSE

PHARMACOLOGY

Shidhaye Supriya*, Mishra Kamlendra, Mahajan S. C.

Mahakal Institute of Pharmaceutical Studies, Ujjain

[email protected]

ABSTRACT

Reverse pharmacology is defined as the modern technique of drug discovery, which integrates

documented clinical/experimental data into leads by transdisciplinary exploratory studies and further

develops it into promising drug candidate and then in form of formulation by experimental and clinical

research. RP is comparatively safer and better way of drug discovery because it is based on the

knowledge of traditional, folk and ayurvedic use of medicinal plants. Traditional knowledge can help to

eliminate three main hurdles in drug development these are time, money and safety/toxicity. In general,

path of drug discovery starts with research in laboratory and ends with the effect in human volunteer but

in reverse pharmacology westarts from patient and then go to the laboratory for finding the

pharmacologically active molecule. There is need to understand and execute the basic principles of

ayurveda in a scientific manner that is RP, in order to integrate safe, effective and promising use of

medicinal plants. Here we discus reverse pharmacological approach for treatment of diabetes with special

reference to antidiabetic molecule mahanimbine from medicinal plant Murraya koenigii.

Keywords: Reverse pharmacology, ayurveda, antidiabetic, Murraya koenigii.

PP - 46




NATURAL GUMS AS SUPERDISINTEGRANTS IN FORMULATION OF MOUTH DISSOLVING

TABLETS- A REVIEW

Thakur Sovran S *, Niranjan Swatantra, Verma Kaushilya, Chatterjee D. P.

Mittal Institute of Technology, Bhopal

[email protected]

ABSTRACT

The aim is to study the use of natural gums as natural superdisintegrants in formulation of mouth

dissolving tablets. Fast disintegrating tablet have received ever-increasing demand during the last

decade, and the field has become a rapidly growing area in the pharmaceutical area. Particularly the fast

dissolving drug delivery systems formulated with natural polymers have more demand because natural

materials like gums and mucilage have been extensively used in the field of drug delivery for their easy

availability, ease of administration, non-toxicity, non-irritant nature, biodegradability etc. Mouth dissolving

tablets with natural gums and mucilage generally show better disintegrating property as well as release

profile. Tablets which needs rapid disintegration, the inclusion of the right disintegrant is a prerequisite for

optimal bioavailability. So superdisintegrants are used to improve the efficacy of such solid dosage forms.

Use of natural gums as such disintegrants is rapidly increasing nowadays. Hence it can be concluded that

natural gums can be efficiently used as natural superdisintegrants with many advantages over synthetic

superdisintegrants in formulation of mouth dissolving tablets.

Keywords: natural gums, superdisintegrants, mouth dissolving tablets, drug delivery.

PP - 47





ADR IN HERBAL MEDICATION WITH MAINSTREAM MEDICAL THERAPIES

Sharma Garima *, Chhajed Mahavir, Prachand Sumeet, Jain Sanjay

Indore Institute of Pharmacy, Indore

[email protected]

ABSTRACT

Natural health products (NHPs) are sold over-the-counter and are often perceived to be safe, despite

potential risks. In India and China and some other countries, the use of herbal medication is to large

extent because of their easy availability, no expert consultation needed, and considered safe to use and

also because primary health care services fall short to the peoples need. Proper reporting of suspected

ADR of herbal medicines is of great significance. The marketed Ayurvedic and other CAM medicines

should be FDA approved and need to increase public awareness about pros and cons of their uses. We

need to focus on the common belief that anything natural is safe is a fallacious statement. The

manufacturers of herbal medicines are not required to submit the proof of safety and efficacy with

rigorous analysis to the FDA before marketing. For this reason, the adverse effects and drug interactions

associated with herbal remedies are largely unknown. Thus, some of the adverse effects and drug

interactions reported for herbal products could be caused by impurities (e.g., allergens, pollen and

spores). Ginkgo biloba extract, has been reported to cause spontaneous bleeding, and it may interact

with anticoagulants and antiplatelet agents, and as a matter of fact Green Tea also have Stimulant drugs

speed up the nervous system. Caffeine (contained in green tea) and ephedrine are both stimulant drugs.

Taking green tea along with ephedrine might cause too much stimulation and sometimes serious side

effects and heart problems. So Perception that natural safe should be seen in a new light Interest and

information on alternative therapies is also need to be explore more due to lack of regulation &Information

on use of these therapies must be specifically elicited from patients

Keywords: Natural health products, Ayurvedic & CAM medicines, drug interactions.

PP - 48




ISOLATION OF AMYLASE PRODUCING BACTERIA FROM SOIL AND ITS OPTIMIZATION OF

PRODUCTION PARAMETERS BY SHAKE FLASK CULTURE METHOD

Nair Nidhi *, Chhajed Mahavir, Khambete Hemant, Jain Sanjay

Indore Institute of Pharmacy Indore

[email protected]

ABSTRACT

The effects of various production parameters such as pH, temperature, incubation time and sources of

carbon were tested in submerged fermentation process by shake flask culture method in production of

amylase by bacteria isolated from groundnut field soil. The production medium with provision of glucose

as carbon source, incubated for 48 h, maintained with pH of 6.5 at 39oC, was found optimal for production

of amylase.

Keywords: amylase, shake flask culture, starch agar plate, fermentation.

PP - 49




CUTTING EDGE IN DRUG DISCOVERY AND DEVELOPMENT – REVERSE PHARMACOLOGY

Kachchawala Mehazabeen*, Chhajed Mahavir, Dumbwani Jacky, Jain Sanjay

Indore Institute of Pharmacy, Indore

[email protected]

ABSTRACT

A synthetic discovery is always a first recognition of an event, a phenomenon, process, or a state of

affairs not previously recognized or known. Most of the stirring and deeply influential discoveries of

science come under this heading. Reverse pharmacology is the science of integrating documented

clinical/experimental hits, into leads by trans-disciplinary exploratory studies and further developing these

into drug candidates by experimental and clinical research. To discover and develop numerous novel

therapeutic agents for the treatment of a wide spectrum of diseases, scientists launched a significant and

noticeable effort aimed at improving the integration of discovery technologies, chemical sourcing for route

selection/delivery of active pharmaceutical ingredients. However, recent trends indicate that this model

may no longer ensure high growth rates. R&D expenses have risen enormously in last decade but

surprisingly it has not led to a corresponding increase in the number and efficacy of new drugs. And so

numbers of approved new chemical/molecular entities are declining. The extremely time consuming,

complex and capital- intensive process makes companies ‘target rich’ but ‘lead poor’. Alternatively,

Reverse Pharmacology also known as Target base Drug Discovery (TDD) is now becoming a popular

option in the field of drug discovery where a hypothesis is first made that modulation of the activity of a

specific protein target will have beneficial therapeutic effects. Screening of chemical libraries of small

molecules is then used to identify compounds that bind with high affinity to the target. The hits from these

screens are then used as starting points for drug discovery. This method became popular after the

sequencing of the human genome which allowed rapid cloning and synthesis of large quantities of

purified proteins.

Keywords: drug discovery, reverse pharmacology, Target base Drug Discovery, chemical libraries

PP - 50




INHIBITION OF MATRIX METALLOPROTEINASE – 2 (MMP) IN DMH INDUCED COLON CANCER IN

SD RATS IN THE PRESENCE OF DIETARY SUPPLEMENTS AND CHEMOTHERAPY: A

MECHANISM AND PROBLEMS BASED APPROACH

Hakimi Taha *, Gupta Saurabh, Chhajed Mahavir, Patidar Shivangi

Indore institute of Pharmacy, Indore

[email protected]

ABSTRACT

Naringenin (NRG), chemically flavonoid is potentially antioxidant and chemoprotective agent. In

abundance, this molecule found in citrus fruits like Citrus paradise and Citrus Sinensis. NRG evaluated

against paclitaxel (PCT) and cisplatin (CPT) in inhibiting Matrix Metalloproteinase-2 (MMP-2) and

angiogenesis along with oxidative stress, nephrotoxicity and bone marrow toxicity in colon cancer induced

SD rats. The tested drugs ({PCT (6mg/kg) CPT (4mg/kg)} PCT.CPT, {PCT (6mg/kg) CPT (4mg/kg) NRG

(40mg/kg)} PCT.CPT.NRG and NRG (40mg/kg)) were administered p.o. at 50th day after the challenge of

40mg/kg p. o. Di –Methyl Hydrazine (DMH) schedule. Different haematological parameters like

Hemoglobin, total and differential leucocytes count, blood urea nitrogen were estimated in Blood. The

other parameters, lipid Peroxidation (LPO), Malonaldehyde (MDA), Superoxide Dismutase (SOD) and

Clastogenic activity by Micronuclei assay are estimated in kidney. Further, MMP-2 estimation was done in

colon tissue preparation. The results reveal a significant increase in hemoglobin, total and differential

leucocytes count, blood urea nitrogen in PCT.CPT.NRG treated group. The present investigations

suggest that naringenin showed to have protected against the toxic effects of paclitaxel and cisplatin at

tested doses. The chemoprotective effect of these compounds could be due to antioxidant mechanism.

Further, research in MMP-2 expression with probable scope to quantify the extent of expression of the

gene and to identify the relationship with angiogenesis in the tumor.

Keywords: Naringenin, Paclitaxel, Cisplatin and Matrix Metalloproteinase-2.

PP - 51




IN VITRO ANTI OXIDANT ACTIVITY OF HYDRO-ALCOHOLIC EXTRACT OF CAESALPINIA BONDUC

Koka Sweta S *, Bankar Amit

LNCP, Indore

[email protected]

ABSTRACT

Present study deals with the In vitro Anti oxidant activity of hydro alcoholic extract of Caesalpinia bonduc

commonly known as sagargota belongs to the family. Hydro alcoholic extract of Caesalpinia bondu

c was subjected to In vitro antioxidant activity screening models such as DPPH, ABTS radical

scavenging activity, inhibition of Lipid peroxidation where Gallic acid, Butylated Hydroxy Toulene (BHT)

and Ascorbic acid were used as the standards. In all the models studied, hydro alcoholic extract of

Caesalpinia bonduc showed nearly equal activities to standards used. In conclusion, the present study

approved that the Caesalpinia bonduc extract have promising In- vitro antioxidant activity.

Keywords: Caesalpinia bonduc, DPPH, ABTS, Lipid peroxidation.

PP - 52

www.aiper.ac.in

ACROPOLIS INSTITUTE OF PHARMACEUTICAL EDUCATION & RESEARCH

Acropolis Institute of Pharmaceutical Education & Research (AIPER) is nurtured by Teach

For India Education & Research Society having objective of creating state of art, world

class, high quality technical education facilities at Indore. Towards fulfilment of its

objective society established AIPER in the year 2008.AIPER is a philanthropic

organization sprawled in an area of around 2 acres and is committed to the service of

humanity through technological advancement. The institute offers Masters degree in

Pharmaceutics and Bachelor’s degree in Pharmacy. The institute is approved by AICTE,

New Delhi , PCI, CPCSEA and is affiliated to Rajiv Gandhi Technical University (RGPV),

Bhopal.

Acropolis Institute of Pharmaceutical Education and Research

Indore Dewas Bypass Road, Manglia Square, Indore, M.P. 453771

Email Id: [email protected]

Contact Details: 0731-4730091, 9630080804

http://www.aiper.ac.in/


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