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Biotransformation is a process by which organic compounds are transformed from one form to another, aided by organisms such as bacteria, fungi and enzymes. It plays a major role and determines the fate of the prospective drugs. Biotransformation must take place only after the drugs reach their specific target site and produce the desired effects. In addition, the nature of the metabolites produced from the drug, must be thoroughly studied; otherwise, the drugs would be rejected during the screening process. Hence, drug metabolism is a major criterion in the highthroughput screening of prospective drugs.Biotransformation has an important role in the determination of the pharmacokinetic parameters like oral bioavailability, drug-drug interaction, clearance and the half-life of the entity within the cell. It is very essential in the toxicity studies too. Biotransformation is used as a valuable strategy to build molecules, similar to parent drug in the drug discovery programme. It can play an important role in identifying factors underlying the problems, facilitate the optimal selection of compounds for further development, provide information on metabolites for possible improvement in drug design, and contribute to the identification of the appropriate animal species for subsequent toxicity testing. Hence, some of the metabolites of biotransformation were already developed as a drug and are currently in clinical use.pharmacologically inactive compounds to pharmacologically active metabolites. These reactions are usually mediated by a broad class of hydrolytic enzymes, such as esterases, amidases and phosphotases, although the conversion of a prodrug to the corresponding active drug can also occur non-enzymatically [3][4][5][6]. Methods for generation of metabolitesIn vitro methods Subcellular fractions: Subcellular fractions prepared from organs expressing drug metabolizing enzymes include the cytosolic fraction, the S9 fraction and microsomes. Organs such as intestine, liver, kidney, lung, and skin are known to mediate xenobiotic metabolism. Liver is the major site of drug metabolism. As a result, liver subcellular fractions are often employed for studying metabolic reactions and generation of metabolites. Subcellular fractions can be used to prepare metabolites formed by a number of enzymes such as CYP, FMO, myeloperoxidase, ketoreductase, alcohol dehydrogenase, sulfotransferase, etc. [7]. Primary cell-based systems:Intact cells such as primary hepatocytes, contain both soluble and membrane-bound enzymes including the relevant cofactors at or near the appropriate physiological concentrations. As a result, they have greater physiological relevance and can mediate both phase I and phase II metabolism. Cryopreserved J o u rn al of D r u g M etaboli s m & T ox icol o g y

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Background: In addition to resistance against drugs, no new drugs have reached the market during the last decade for malaria treatment. This implies the urgent need to search for new drugs from different sources. Medicinal plants are one of such sources for novel drugs. Therefore, the aim of the current study was to investigate antimalarial activity of crude extract of leaves of Moringa oleifera Lam (Moringaceae) in Plasmodium berghei in a mice model. Methods:The acute toxicity test was used as per standard guidelines. To determine parasite inhibition, 4-day Peter's suppressive test was done. Curative and prophylactic tests were done by applying standard methods. Windows SPSS version 16 was used to analyse the data and analysis of variance (ANOVA) followed by Post Hoc Tukey's HSD to compare results between groups. Results: Death was not observed up to a dose of 2000 mg/kg of the plant extract. In all mice treated with the extract, the level of parasitaemia was significantly reduced in comparison with the control group (P < 0.001) and also a very significant difference was observed in comparison with the chloroquine treated group (P < 0.0001) with lower doses. Mean survival time was significantly increased at all treatment doses. It reduced parasitemia in a dose-dependent manner in both curative and prophylactic activity tests resulting in a significant (P < 0.05) reduction of parasitaemia in comparison with the control group. Conclusions:The result of the current study revealed that the extract possessed significant anti-plasmodial activity as displayed by its ability to suppress P. berghei infection in mice. The present study can be considered as confirmation for traditionally claimed use of the plant against malaria treatment.

AbstractÖz Purpose: A considerable number of individuals in developing countries do not attend physicians for their illnesses; instead they commonly use self-medication. Although responsible self-medication with over the counter (OTC) drugs is often acceptable and promoted as one form of self-care, self-medication with prescription drugs is inappropriate and should always be discouraged. The aim of this study was to determine prevalence of selfmedication and associated factors in Sire town, West Ethiopia. Material and Methods: A community based crosssectional study was conducted on 423 households, which were selected systematically. Data was collected by using semi-structured questionnaire. Results: Two hundred forty three individuals in 230 households perceived illness two weeks prior to the study. Out of them, 66 (27.16%) used self-medication. The practice of self-medication was not significantly associated with sex, educational status, occupation and income of the patients or caregivers. The most frequent illness reported for self-medication was headache (37.89%). Most (84.84%) of the drugs used for self-medication were obtained from drug stores. The relatively lower cost was the major, 21 (31.82%), reason for using self-medication. Analgesics were the largest category of medicinal agents used for self-medication 34(40.96%), followed by antibiotics 20(24.10%), traditional medicines 17(20.48%), antimalarials 4(4.71%), and anthelminthics 3(3.53%). Conclusion: Self-medication was practiced by considerably large number of the study participants. The prevalence of self-medication with prescription drugs like antimicrobials was also high. Self-medication with these drugs without medical consultation may lead to inappropriate use and thereby contribute to emergence of drug resistance. Amaç:Gelişmekte olan ülkelerde bireylerin büyük kısmı, hastalıkları için doktora gitmek yerine kendi kendine tedavi yöntemlerini kullanmaktadır. Kendi kendine tedavide genelde reçetesiz ilaçlar kullanılmakta ve kişisel bakımın bir formu olarak desteklenmekteysede reçeteli ilaçlar kişisel tedaviye uygun olmayıp desteklenmemelidir. Bu çalışmanın amacı Batı Etiyopya'nın Sire şehrinde kendi kendine tedavi ve ilgili faktörlerin sıklığının saptanmasıdır. Gereç ve Yöntem: Toplum tabanlı bu kesitsel çalışma, sistematik olarak seçilmiş 423 aile ile yapılmıştır. Çalışmada veriler yarı yapılandırılmış anket ile toplanmıştır. Bulgular: İkiyüz otuz aileden 243 bireyde, çalışmadan 2 hafta öncesinde hastalık farkedilmiştir, onların dışında, 66 birey (%27.16) kendi kendine tedavi kullanmıştır. Kendi kendine tedavi uygulaması ile hasta ve hasta bakıcısının cinsiyet, eğitim seviyesi, meslek ve kazancı arasında anlamlı bir ilişki saptanmamıştır. Kendi kendine tedavi için en sık karşılaşılan hastalık başağrısıdır. (%37.89). Kendi kendine tedavi için kullanılan ilaçların çoğu (84.84%) eczanelerden sağlanmaktadır. Kendi kendine tedavi uygulamasının en önemli nedeni düşük fiyattır, 21 (%31.82). Tıbbi ajanlar arasında en fazla kullanılanlar analjeziklerdir 34...