The effect of lupeol, a pentacyclic triterpene, on the treatment of acne

Abstract

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 screened various medicinal plants to explore the novel acne medication. Among them, lupeol, a pentacyclic triterpene, from the hexane extract of Solanum melongena L was identifed. Lupeol targeted most of the major pathogenic factors of acne with desired physicochemical traits. It strongly suppressed lipogenesis by modulating IGF-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 only a minimal effect on cell viability and possibly modulated dyskeratosis of epidermal keratinocyte. It also decreased the viability of P. acnes. Finally, lupeol improved facial acne and was well tolerated in a 4-week double-blind, randomized, split-face, small-scale clinical trial. These results provide a therapeutic rationale for the use of lupeol in acne treatment.