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From Chemistry to Medicine DRD 2007
PRICEITE DOES NOT INDUCE GENOTOXICITY IN HUMAN LYMPHOCYTES IN VITRO Hasan TRKEZ, Fatime GEYKOLUAtatrk University, Faculty of Arts and Sciences, Department of Biology, 25240 Erzurum, Turkey
Boron does not exist by itself in nature. This element combines with oxygen and other elements to form boric acid, or inorganic salts called borates. People need borates, too, as an important part of a healthy diet and an essential ingredient in many products necessary for an acceptable standard of living. And borates frequently used in indus-trial, cosmetic, and medical settings. Priceite also (or pandermite = Ca4B10O19.7H2O) is one of the most important commercial boron compounds produced in large. The aim of the present study was to investigate the ability of priceite to induce sister-chromatid exchange (SCE) and micronucleus (MN) in cultured human lymphocytes.
With this aim, whole heparinized blood samples were taken from eight healthy non-smoking donors. Thirteen experimental concen-trations of priceite were used, ranging from 5 to 500 mg/L.
The peripheral blood cultures which were applied 400 and 500 mg/L of priceite was found to be sterile. Treatment with priceite did not cause an increase in the frequency of SCE per cell at all other concentrations. Moreover, there were no significant aneugenic and/or clastogenic effects observed in the micronucleus assay.
Our results firstly indicated that priceite is not a genotoxic agent in human blood cultures and safe for use in medical and cosmetic applications.
THE EFFECTS OF SOME LICHEN SPECIES AGAINST SISTER-CHROMATID EXCHANGE FREQUENCY INDUCED BY TITANIUM DIOXIDE IN HUMAN LYMPHOCYTES Fatime GEYKOLU, Hasan TRKEZAtatrk University, Faculty of Arts and Sciences, Department of Biology, 25240 Erzurum, Turkey
Despite the increasing use of factory-made synthetic drugs, natu-ral healing materials have persisted as the treatment of choice for a multitude of health problems in populations throughout the world. Investigations of genotoxicity and anti-genotoxicity can help evalu-ate the safety and effectiveness of herbal health products. Titanium dioxide (TiO2) is widely used in the pharmaceutical and cosmetic industries. It is also used for sterilization of waste water. The pur-pose of this work was to evaluate the effects of four lichen species (Dermotocopon intestiniformis, Pseudevernia furfuracea, Rhizoplaca melanophthalma and Xanthoparmelia pulla) against the genotoxicity induced by titanium dioxide (TiO2) for the first time.
With this aim, whole heparinized blood samples were taken from three healthy non-smoking donors. TiO2 was added to the cultures in concentrations of 5 and 10 M. After the application of TiO2 and lichen extracts, seperate and together, the sister-chromatid exchange (SCE) test was used to assess DNA damage in lymphocytes.
None of the lichen extracts showed a significant genotoxicity alone. The extract of X. pulla did not show anti-genotoxic activity against the genotoxic effects induced by TiO2. However, D. intestiniformis, P. furfuracea, R. melanophthalma extracts caused significant decreases in titanium-induced SCE frequencies as dose dependent manner. The potency of anti-genotoxic activity was also in the following or-der: P. furfuracea > R. melanophthalma > D. intestiniformis.
Our findings indicated that lichens can be a new resource of therapeu-tic potential as recognized here against to adverse effects of drugs used.
IN VITRO EFFECTS OF ALUMINUM SULPHATE ON SISTER- CHROMATID EXCHANGES AND OXIDATIVE STRESS IN HUMAN BLOOD: PROTECTIVE ROLE OF BISMUTH SUBNITRATE Fatime GEYKOLU, Hasan TRKEZAtatrk University, Faculty of Arts and Sciences, Department of Biology, 25240 Erzurum, Turkey
Aluminum, which is found in several different forms and oxida-tion states, causes acute and chronic adverse health effects. Medici-nally, the treatment methods with bismuth compounds especially bismuth subnitrate (BSN) (as astringents, antacides, antiulcers and antidiarrheals) have been increased. The goal of the present study was to evaluate the genetic and oxidative effects of aluminum sul-phate (Al2(SO4)3) and BSN in human blood in vitro.
The various concentrations of Al2(SO4)3 (10 and 20 g/mL) and BSN (0.75, 1.5, 3 and 5 g/mL) were used. Evaluation of DNA dam-ages was carried out by using Sister-Chromatid Exchange (SCE) method in blood lymphocytes. Oxidative status of erythrocytes was assessed by measuring following oxidative stress markers: reduced glutathione (GSH), superoxide dismutase (SOD), glucose-6- phos-phate dehydrogenase (G6PDH) and catalase (CAT).
The SOD activity increased by Al2(SO4)3 (10 g/mL) exposure but the ratio of SCEs didnt change compared to the controls. On the other hand, the high dose of Al2(SO4)3 (20 g/mL) caused oxidative stress and increased SCE frequency. When the concomitant treat-ment with Al2(SO4)3 of BSN were investigated, BSN exerted an anti-oxidant action at low doses (0.75 and 1.5 g/mL). It also reduced the formation of SCEs.
This study suggests for the first time that BSN may be admin-istered as a potential protective against the effects of Al2(SO4)3 in which oxidative and genetic damages are clearly involved.
GST-CDNB ACTIVITIES IN GILTHEAD SEABREAM (SPARUS AURATA) LIVER CYTOSOL OF DIFFERENT AGES 1Hatice ARDA-AKDOAN, 2Alaattin EN1Pamukkale University, Science and Arts Faculty, Department of Chemistry, 20017 Knkl, Denizli, Turkey2Pamukkale University, Science and Arts Faculty, Department of Biology, 20017 Knkl, Denizli, Turkey
Lipophilic compounds such as polycyclic aromatic hydrocarbons, polychlorinated biphenyls, nitroaromatics, dioxins, drugs, various pesticides and natural residual are readily taken up into the tissues of aquatic organisms where biotransformation via Phase I and Phase II metabolism can in part, determine the fate and toxicity of the xenobiotics. The glutathione S-transferases (GST) represent a ma-jor group of detoxification enzymes. GSTs are a family of phase II detoxification enzymes. It is known that the important changes in drug metabolism occur with ageing because the various factors that have significant influences on xenobiotic metabolizing enzymes are altered by ageing and season.
In this study, gilthead seabream (Sparus aurata) fish liver cytosol of different ages were used as sample. The fish used in this study, Gilthead Seabream (Sparus aurata), were bought from Pinar Fish in zmir, Aegean coast of Turkey. Glutathione S-transferase (GST) were determined from this Gilthead Seabream (Sparus aurata) fish livers cytosoles.
Though various factors that may have a significant impact on drug metabolism are affected by ageing, our results suggest that some im-
May 17-20, 2007
International Symposium on Drug Research and Development
portant age-related differences in xenobiotic metabolism do occur in Gilthead Seabream liver and are substrate specific, which might af-fect obtaining desired actions and/or responses to drugs, hormones and dietary supplements used during breeding.
GST-CDNB activity increased in gilthead seabream (Sparus au-rata) liver cytosol of different ages (ranging from 1.5 to 20 months). 1.5 months of the fish activity is 17,7 0,5 pmol/dakika/mg protein, 20 months of the fish is 690,9 32,0 pmol/dakika/mg protein.
THE PROTECTIVE ROLE OF PSEUDOVERNIA FURFURACEA AGAINST COLLOIDAL BISMUTH SUBCITRATE INDUCED GENOTOXICITY IN HUMAN LYMPHOCYTE CULTURES Hasan TRKEZ, Fatime GEYKOLUAtatrk University, Faculty of Arts and Sciences, Department of Biology, 25240 Erzurum, Turkey
Bismuth compounds, especially, colloidal bismuth subcitrate (CBS) have been actively promoted for the treatment of diarrhoea, peptic and duedonal ulcer diseases. And the therapeutic bismuth compounds are now being marred by episodes of serious adverse reactions. On the other hand, the potential of lichens in cellular ac-tivities remains largely unexplored. The aim of this study was to as-sess the efficacy of the lichen Pseudovernia furfuracea (2.5, 5, 10 and 20 g/mL) on the genotoxicity induced by CBS in the human blood cultures.
With this aim, whole heparinized blood samples were taken from three healthy non-smoking donors. Sister-chromatid exchanges (SCE) and Micronuclei (MN) tests were used for evaluating the ge-notoxicity.
SCEs and MN formations significantly increased by effect of 5 g/mL CBS when compared with the the control group. However, the decreased rates of such formations indicated that P. furfuracea was anti-genotoxic agent. Our results also showed that the protective role of P. furfuracea was dose-related.
On the basis of data, it is thought that this lichen species can pro-vide anti-genotoxic effects as due to their antioxidant defenses al-though there is no evidence for the content of the lichen species in the present investigation.
QSAR MODELING ON SIGMA RECEPTOR LIGANDS Mine YARIM, Ece GRDAL, Dilek EROLYeditepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 34755 stanbul, Trkiye
Sigma () receptors are functional, membrane-bound proteins distributed throughout the brain and peripheral organs. 1 and 2 receptor types are clearly established, and further pharmacologi-cal differentiation may be possible. 1 receptors are implicated in central nervous system (CNS) disorders such as depression, schizo-phrenia and dementia. Further, 1 receptor agonists have value as neuroactive agents, while antagonists may help alleviate cocaine ad-diction. The si