Abstract
AbstractArtocarpus hirsutus Lam., one of the species of Artocarpus, is not well studied. The present study is intended to isolate the chemical constituents present in stem wood extract of A. hirsutus, to synthesize their new derivatives and to evaluate their activity against Propionibacterium acnes. Three major flavonoids, cudraflavone A, cycloartocarpin and artocarpin were isolated from the stem wood extract and cudraflavone A was isolated for the first time from this plant. New prenyl ether and acetate derivatives of isolated flavonoids have been synthesized. This is the first to report on the evaluation of in vitro anti-acne potential of crude extracts, isolated flavonoids and their new synthetic derivatives. The crude extracts (MIC values 2, 4 and 15.6 μg/mL) and the isolated constituents (MIC values 2, 0.5 and 0.25 μg/mL) showed significant in vitro anti-acne activity against P. acnes which was comparable with commercially available anti-acne agent, tea tree, oil and a standard antibiotic, Clindamyci...
Highlights
Artocarpus hirsutus Lam. plant grows mostly in India, especially in heavy rainfall area of Western Ghat, Kerala and is commonly used as a traditional medicine
All new molecules were characterized from their spectroscopic analysis
It was revealed that new acetates and prenyl ether derivatives possessed almost negligible activity against P. acnes with respect to their parent molecules
Summary
Nagarajan is the Vice president R&D of Sami Labs and associated with the company for the last 22 years He obtained his PhD in Organic Chemistry from the University of Madras. His research interests include synthetic methodology, synthesis of chiral molecules and bioactive natural products and to study their significance on biological system. He has more than 30 years of research experience in the field of Organic Chemistry and has published more than 15 articles in reputed journals. Despite commercial viability of topical and oral medications in controlling acne, it is significant to discover precise drug molecules possessing better potency, minimal toxicity and capable of specific delivery onto disease site.
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