Posted by admin on Apr 1, 2013 in |
Protein tyrosine kinases (PTKs) are key players in cellular signal transduction events and have essential roles in cell growth, survival, differentiation and migration. Perturbations in protein tyrosine kinase activity have been implicated in a number of abnormalities, particularly cancer. Selective small molecule inhibitors are potential therapeutic agents targeting protein kinases involved in cancer and other diseases. The most dramatic clinical responses have been observed in cancer types that are strictly dependent on oncogenic kinases. In this case, targeting these kinases seems to be sufficient to provoke apoptotic response, thus limiting the process of tumorigenesis. Among tyrosine kinase inhibitors, imatinib mesylate (Gleevec®; Novartis) has demonstrated magnificent clinical efficacy in more than one type of cancer and received FDA approval for treatment of chronic myeloid leukemia (CML) and gastrointestinal stromal tumor (GIST). Imatinib has set a paradigm for the treatment and management of CML as BCR-ABL kinase inhibitor. It binds kinase domain of PTK as an ATP-competitive inhibitor thus preventing the interaction with effector proteins and subsequent signaling pathway. Imatinib has...
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Posted by admin on Apr 1, 2013 in |
Heliotropium indicum Linn., commonly known as ‘Indian heliotrope’ is very common in India with a long history of traditional medicinal uses in many countries in the world. The plant is reported to possess antibacterial, antitumor, uterine stimulant effect, antifertility, wound healing, anti-inflammatory, antinociceptive and diuretic activities. Several pyrrolizidine alkaloids have been isolated from this species. The active principle Indicine-N-oxide has reached Phase 1 clinical trials in advanced cancer patients. But severe toxic side-effects showed that a therapy with indicine-N-oxide was not justified. Most of the alkaloids are hepatoxic and therefore internal use of Heliotropium species is not recommended. External application to promote wound healing and to fight infections seems to be less hazardous, but more research is needed. The comprehensive account of the chemical constituents and the biological activities are presented in this review such that the potential use of this plant in various traditional medicines can be systematically...
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Posted by admin on Mar 1, 2013 in |
The different fractions of crude methanol extract of stem of Stephania japonica (Thunb.) Miers (Menispermaceae) was screened for its analgesic and antidiarrhoeal activities. The different fractions of crude extract produced significant writhing inhibition in acetic acid induced writhing in mice at the dose of 250 and 500 mg/kg body weight comparable to the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight. When tested for its antidiarrhoeal effects on castor oil induced diarrhea in mice, it increased mean latent period and decreased the frequency of defecation significantly at the dose of 250 and 500 mg/kg body weight comparable to the standard drug loperamide at the dose of 50 mg/kg of body weight. The overall results suggest the analgesic and antidiarrhoeal activities of the different fractions of crude extract. Among all the fractions Ethyl acetate soluble fraction showed most significant analgesic activity and Petroleum ether soluble fraction showed the most significant antidiarrhoeal...
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Posted by admin on Mar 1, 2013 in |
Obesity is a chronic disease and a major health problem which require long term treatment in developed and affluent society of developing countries. Pharmacotherapies for obesity have to be given for a long duration with lifestyle modifications. Anti-obesity drugs acts through various targets in the body which reduce the food intake, decrease absorption and increase metabolism. Many drugs were approved and used in the past but were removed or abandoned in the later stages due to the various adverse drug reactions associated with the drugs. At present orlistat is the only approved drugs but it’s also associated with steatorrhoea and other side effects. Lorcaserin and the combination of phentermine and topiramate have shown to reduce greater weight loss and fewer side effects than orlistat. There are new combinations from existing drugs are in various phase of clinical trials like bupropion/naltrexone, bupropion/zonisamide and pramlintide/metreleptin. Many single agents like tesofensine, liraglutide, cetilistat, etc are in various phases of clinical trials and have shown promise to be in the league of the...
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Posted by admin on Mar 1, 2013 in |
A new, simple, precise, rapid, accurate and stability-indicating RP-HPLC method has been developed for the determination of Entacapone in presence of its degradation products or other pharmaceutical excipients. Stress studies were performed on Entacapone tablets and it was found that it degrades sufficiently in acidic, alkaline and oxidation conditions, while negligible degradation was observed in thermal, photolytic and humidity conditions. The peaks of the degradation products were not observed in the chromatogram due to the nonchromophoric nature of the degradation moiety formed. The separations were carried out on a Hypersil BDS C8, 150 mm x 4.6 mm 5µm particle size column with a mobile phase consisting of Acetonitrile: 0.01% Orthophosphoric acid pH 2.5 at a flow rate of 1.0 ml/min. Detection wavelength was 210nm. The retention time of Entacapone was 7.0minutes. The developed method was validated in terms of specificity, forced degradation, linearity, precision, intermediate precision (ruggedness), accuracy, range and robustness. The calibration curve for Entacapone was linear (correlation coefficient 0.99995) from range of 50µg/ml to 150µg/ml. Relative standard...
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