ANTICANCER ACTIVITY OF INDOLE-3-CARBINOL [I3C]

DERIVATIVES

SUBHRADIP ROYCHOWDHURY* & SATARUPA BHATTACHARJEE**

*M.PHARM 1ST YEAR [PHARMACEUTICAL CHEMISTRY] DEPT. OF PHARM. SC. BIRLA INSTITUTE OF TECHNOLOGY, MESRA-835215

** B.PHARM 4TH YEAR GURU NANAK INSTITUTE OF PHARMACEUTICAL SCIENCE AND TECHNOLOGY, KOLKATA-114

DEFINITION , TYPES AND CAUSES OF CANCER Cancer known medically as a malignant neoplasm, is a broad group of diseases involving uncontrolled , abnormal cell

proliferation

GENESIS OF CANCER

HISTORICAL BACKGROUND OF USE OF I3C

“If a cancerous ulcer appears upon the breasts, apply a crushed cabbage leaf

and it will make it well.”

- Roman statesman, Cato the Elder [234-149 BC]

Crushing or chewing cabbage leaves causes 72% reduction in risk of breast

cancer and also reduces developing prostate and pancreatic cancer.

SOURCES OF I3C

Primarily found in

cruciferous

vegetables.

Family : Cruciferae.

Genus : Brassica.

DERIVATIVES OF I3C

CHEMICAL PROFILE OF I3C

Oral consumption of Cruciferous vegetables Glucobrassicin ,a

glucosinolate Indole-3-glucosinolate Myrosinase in plant cell

Acid autohydrolysis in stomach Condensed oligomeric derivatives

majorly DIM,ICZ & LTr1

Modulates the metabolism of carcinogens, such as Benzopyrene, Aflatoxin B1.

Inhibits activation of various transcription factors.

Anticancer agent for both hormone responsive and triple negative breast

tumors.

PROTEIN TARGETS OF I3C DERIVATIVE DIM

ACTIVITIES ASSIGNED TO I3C

DIM Di Indolyl Methane

ESTROGEN METABOLISM, CANCER AND I3C

I3C increases the urinary excretion ratio of 2-hydroxyestrone to 16 alpha

hydroxyestrone.

Inhibits the 4-hydroxylation of estradiol.

Increases 2-hydroxylation keeping away 16 alpha hydroxylation of

estradiol via induction of two isoenzymes CYP4501A1 and CYP4501A2.

DISEASES THAT CAN BE TREATED WITH I3C

Breast cancer

Lung cancer

Liver cancer

Leukaemia

Cervical cancer

Prostate cancer

Colon cancer

Hepatotoxicity

Systemic lupus

erythematosus

In management

of HSV

Recurrent

respiratory

papillomatosis

DOSE AND SAFETY DATA OF I3C DERIVATIVES

PREGNANCY AND LACTATION : Safety has not been established.

DRUG INTERACTION :

Tamoxifen [Synergistic in Breast Cancer]

Antacids and PPI are contraindicated [As they will prevent acid

condensation to form ICZ]

DOSE : Dosage ranges from 400 mg to 800 mg daily.

CONCLUSION

So from here it can be concluded that

Consumption of Indole-3-carbinol, a component of cruciferous

vegetables, has incredible potential both for prevention

and for treatment of cancer.

While being cytoprotective for the normal cells, it is an

apoptotic agent for the tumor cells.

This potential of Indole-3-carbinol should be further

explored both alone and in combination with various

chemotherapeutic agents for the treatment of cancer.

REFERENCESAggarwal et al; Molecular Targets and Anticancer Potential of Indole-3-

Carbinol and Its Derivatives; [Cell Cycle 4:9, 1201-1215; September

2005];2005 Landes Bioscience.

farmacists.blogspot.in/2009/05/indole-3-carbinol-novel-approach-to.html cited

on 26.09.2013

Bardlow H.L. et al; Long-term responses of women to indole-3-carbinol or a

high fibre diet; Cancer Epidemiol Biomarkers Prev 1994;3:591-595.

cancerres.aacrjournals.org/content/67/16/7815.long cited on 26.09.2013

ncbi.nlm.nih.gov/pubmed/22110194 cited on 26.09.2013

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