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Activity Guided Purification Identifies Lupeol, a Pentacyclic Triterpene, As a Novel Agent Targeting Multiple Pathogenic Factors of Acne.

J Invest Dermatol. 2015 Feb 3;

Authors: Hoon Kwon H, Young Yoon J, Yong Park S, Min S, Kim YI, Yong Park J, Lee YS, Thiboutot DM, Hun Suh D

Acne vulgaris is a nearly universal cutaneous disease characterized by multifactorial pathogenic processes. Because current acne medications have various side effects, investigating new pharmacologically active molecules is important for treating acne. As natural products generally provide various classes of relatively safe compounds with medicinal potentials, we performed activity guided purification after a series of screenings from the extracts of five medicinal plants to explore novel acne medications. Lupeol, a pentacyclic triterpene, from the hexane extract of Solanum melongena L was identified after instrumental analysis. Lupeol targeted most of the major pathogenic features of acne with desired physicochemical traits. It strongly suppressed lipogenesis by modulating IGR-1R/PI3K/Akt/SREBP-1 signaling pathway in SEB-1 sebocytes, and reduced inflammation by suppressing the NF-κB pathway in SEB-1 sebocytes and HaCaT keratinocytes. Lupeol exhibited a marginal effect on cell viability and may have modulated dyskeratosis of epidermis. Subsequently, histopathological analysis of human patients' acne tissues after applying lupeol for 4 weeks demonstrated that lupeol markedly attenuated levels of both the number of infiltrated cells and major pathogenic proteins examined in vitro around comedones or sebaceous glands, providing solid evidence for suggested therapeutic mechanisms. These results demonstrate the clinical feasibility of applying lupeol for the treatment of acne.Journal of Investigative Dermatology accepted article preview online, 03 February 2015. doi:10.1038/jid.2015.29.

PMID: 25647437 [PubMed - as supplied by publisher]

http://www.ncbi.nlm.nih.gov/pubmed/25647437?dopt=Abstract = URL to article

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