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Abstract
Artocarpus 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, Clindamycin (MIC 0.03 μg/mL) indicating their potential as anti-acne agents.
Acne is one of the major skin diseases that are visualized prominently at the age groups 14–20 years. It is recommended to treat acne at their early stages before they form the wounds or further worsen which leads to depression. 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. Medications derived from phytochemicals are becoming reliable due to their safety, tolerability and efficacy. Due to the medicinal value of Artocarpus species, this study is intended to isolate the chemical components present in stem wood extract of A. hirsutus, to synthesize new derivatives and to evaluate their anti-acne potential. Among the isolated compounds, cudraflavone A, cycloartocarpin and artocarpin showed significant in vitro anti-acne activity comparable with commercially available anti-acne agent tea tree oil and standard antibiotic, Clindamycin.
Competing Interests
The authors declare no competing interest.
Acknowledgements
The author(s) thank Dr N. Kalyanam, Dr S. Natarajan, Dr Samuel Manoharan T., Dr Rajendran R., Mr Anand Desai and Analytical team of SLL for their valuable support.
Additional information
Notes on contributors
A. Nagarajan
A. 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. He has three years post-doctoral research experience at the University of Oklahoma, USA in the area of organometallic and organic chemistry. 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.
