Title |
Induction of apoptosis by the aqueous and ethanolic leaf extract of Vitex negundo L. in MCF-7 human breast cancer cells |
| Int J Drug Discov Vol:2 Iss:1 (2010-06-15) : 1-7 |
Authors |
Arulvasu C., Prabhu D., Manikandan R., Srinivasan P., Dinesh D., Babu G., Sellamuthu S. |
Published on |
15 Jun 2010 Pages : 1-7 Article Id : BIA0000172 Views : 1038 Downloads : 1083 |
DOI | http://dx.doi.org/10.9735/0975-4423.2.1.1-7 |
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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.
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Title |
Formulation and Evaluation of Indomethacin Microspheres using natural and synthetic polymers as Controlled Release Dosage Forms |
| Int J Drug Discov Vol:2 Iss:1 (2010-06-15) : 8-16 |
Authors |
Chinna Gangadhar B., Shyam Sunder R., Vimal Kumar Varma. M., Sleeva Raju M., Sai Kiran M. |
Published on |
15 Jun 2010 Pages : 8-16 Article Id : BIA0000173 Views : 1023 Downloads : 1217 |
DOI | http://dx.doi.org/10.9735/0975-4423.2.1.8-16 |
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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 400μm. 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.
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Title |
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 |
| Int J Drug Discov Vol:2 Iss:1 (2010-06-15) : 17-25 |
Authors |
Charbe N.B., Mehere A.P., Shende S.G., Mohod V.S., Gautam D.T., Madusudhan M., Chaitanya Ch |
Published on |
15 Jun 2010 Pages : 17-25 Article Id : BIA0000174 Views : 1015 Downloads : 1218 |
DOI | http://dx.doi.org/10.9735/0975-4423.2.1.17-25 |
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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.
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