International Journal of Drug Discovery

Number 1, 2010

1-7
INDUCTION OF APOPTOSIS BY THE AQUEOUS AND ETHANOLIC LEAF EXTRACT OF VITEX NEGUNDO L. IN MCF-7 HUMAN BREAST CANCER CELLS

Authors: Arulvasu C., Prabhu D., Manikandan R., Srinivasan P., Dinesh D., Babu G., Sellamuthu S.

Abstract

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The aim of this investigation was to evaluate the anti-proliferative potential of aqueous and ethanolic extract from Vitex negundo against human breast cancer cell (MCF-7). The aqueous and ethanol extract from V. negundo potently inhibited growth of MCF-7 in a concentration-dependent manner. V. negundo pretreatment resulted in deferential cell viability and IC50 value were observed in MCF-7 cell line but not in control cell line. The above result suggested that V. negundo has a potential benefits in breast cancer cells.

8-16
FORMULATION AND EVALUATION OF INDOMETHACIN MICROSPHERES USING NATURAL AND SYNTHETIC POLYMERS AS CONTROLLED RELEASE DOSAGE FORMS

Authors: Chinna Gangadhar B., Shyam Sunder R., Vimal Kumar Varma. M., Sleeva Raju M., Sai Kiran M.

Abstract

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Purpose: The aim of this study was to formulate and evaluate microspheres as controlled release preparations of a highly water-insoluble drug, Indomethacin, using natural polymer, Egg albumin; semi synthetic polymer, Ethyl cellulose and Synthetic polymer, Meth acrylic acid esters (Eudragit L 100) as the retardant materials. Methods: Microspheres were prepared by solvent evaporation method using an acetone / liquid paraffin system and Phase separation co-acervation method using petroleum ether and coconut oil as dispersion and continuous phase systems. Magnesium stearate was used as the droplet stabilizer and n-hexane was added to harden the microspheres. The prepared microspheres were evaluated for their micromeritic properties, drug content and encapsulation efficiency and characterized by Fourier transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM). The in vitro release studies was performed by buffer change method to mimic Gas Intestine Tract(GIT) environment in pH 1.2, carbonate buffer (acidic) and pH 7.4, phosphate buffer (Alkaline). Results: The prepared microspheres were pale yellow, free flowing and spherical in shape. The mean particle size of the microspheres was found in the range of 150 to 400Î¼m. The drug-loaded microspheres showed 70-86% of entrapment and release was extended up to 6 to 8 h releasing 86% of the total drug from the microspheres. The infrared spectra showed stable character of Indomethacin in the drug-loaded microspheres and revealed the absence of drug-polymer interactions. Scanning electron microscopy study revealed that the microspheres were spherical and porous in nature. Conclusion: The best-fit release kinetics was achieved with Koresmeyer-Peppas plot followed by zero order and First order. The release of Indomethacin was influenced by the drug to polymer ratio and particle size & was found to be both diffusion and dissolution controlled.

17-25
STUDY OF NEW DEVELOPMENTS IN BIRCH REDUCTION PROCESS AND THEIR APPLICATIONS FOR THE SYNTHESIS AND CNS DEPRESSANT ACTIVITY OF 3- AMINOCYCLOHEXA-1,4-DIENE-1-CARBOXYLIC ACID AND 3-[5-SUBSTITUTED 1,3,4-THIADIAZOLE-2-YL]-2-STYRYL 5,8-DIHYDROQUINAZOLINE-4 (3H)-ONES

Authors: Charbe N.B., Mehere A.P., Shende S.G., Mohod V.S., Gautam D.T., Madusudhan M., Chaitanya Ch

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Meta nitro benzoic acid has been reduced to 3-aminocyclohexa-1,5-diene-1-carboxylic acid with three different Birch like reduction condition (Method I, II, III) to 3-aminocyclohexa-1,4-diene-1-carboxylic acid. 3-aminocyclohexa-1,4-diene-1-carboxylic acid is found to be structurally more super impossible on gama-amino butyric acid (GABA) and hence the synthesized compounds was tested for the CNS depressant and muscle relaxant activities. A series of new 3-[5-substituted phenyl-1,3,4-thiadiazole-2-yl]-2- styryl 5,8-dihydroquinazoline-4 (3H)-ones were synthesized and evaluated for anticonvulsant, sedativehypnotic and CNS depression activities. Various derivatives of 3-[5-substituted phenyl-1,3,4-thiadiazole-2- yl]-2-styryl 5,8-dihydroquinazoline-4 (3H)-ones were examined in the maximal electroshock (MES) induced seizures and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. Rotorod method was employed to determine the neurotoxicity. Out of 9 compounds only 3 compounds showed anticonvulsant activity in one or more test models. All except compound (a) exhibited significant sedativehypnotic activity via actophotometer screen. Forced swim pool method to determine CNS depressant activity resulted in some potent compounds. It can be concluded that synthesized compounds exhibited better sedative-hypnotic and CNS depressant activities than anticonvulsant activity.