Antileishmanial phenylpropanoids from Alpinia galanga (Linn.) Willd.

Hexane, chloroform and ethyl acetate extracts (100 µg/ml) of Alpinia galanga rhizomes exhibited significant activity in vitro against promastigotes of L. donovani. Twelve compounds namely, methyleugenol (1), p-coumaryl diacetate (2), 1'-acetoxychavicol acetate (3), 1'-acetoxyeugenol acetate (4), trans-p-acetoxycinnamyl alcohol (5), trans-3,4-dimethoxycinnamyl alcohol (6), p-hydroxybenzaldehyde (7), p-hydroxycinnamaldehyde (8), trans-p-coumaryl alcohol (9), galangin (10), trans-p-coumaric acid (11) and galanganol B (12) were isolated from these extracts. Of these, compounds 2, 3, 4 and 5 were found most active in vitro against promastigotes of L. donovani with IC50 values of 39.3, 32.9, 18.9 and 79.9 µM respectively. This is the first report of antileishmanial activity of the extracts and isolated constituents of A. galanga.

Synthesis, biological evaluation and molecular docking of aryl hydrazines and hydrazides for anticancer activity.

Aryl hydrazine and hydrazide analogues were synthesized based on p-tolyl hydrazine, isolated as a breakdown product of a secondary metabolite from the mushroom, Agaricus bisporus, and tested to be highly active molecule than 5-fluorouracil in in vitro anticancer studies. The synthesized analogues were tested for anticancer activity using NCI protocol. Anolgues 12 and 15 emerged as molecules with significant in vitro anticancer activity. Molecular docking study revealed the binding orientations of aryl hydrazines and hydrazides analogues in the active sites of thymidylate synthase.

Natural products drug discovery research in India: Status and appraisal.

Discovery of a new drug is time consuming and laborious process. Natural products have long been a thriving source for the discovery of new drugs due to their chemical diversity and ability to act on various biological targets. The phytochemical exploration of indigeneous flora has contributed to some extent in this race for the discovery of new drugs. The traditional Indian systems of medicine has been a part of our lifestyle since ages and the classical texts like Ayurveda and Charak Samhita have served as materia medica for this purpose. This review focuses on the contributions made from India in the drug discovery and development process and provides future directions in the area.