Anti-Androgenic Curcumin Analogues as Steroid 5-Alpha Reductase Inhibitors

    March 2017 in “ Medicinal Chemistry Research ”
    Jukkarin Srivilai, Karma Rabgay, Nantaka Khorana, Neti Waranuch, Nitra Nuengchamnong, Wudtichai Wisuitiprot, Thipphawan Chuprajob, Chatchawan Changtam, Apichart Suksamrarn, Warinthorn Chavasiri, Nilubon Sornkaew, Kornkanok Ingkaninan
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    TLDR Some curcumin-like compounds can effectively and safely block the enzyme linked to hair loss and other conditions related to male hormones.
    In the 2017 study, researchers evaluated the anti-androgenic activity of 33 curcumin analogues as inhibitors of steroid 5-alpha reductase (S5αR), which is implicated in conditions like androgenic alopecia. They discovered that compounds 1, 4, and 5 were the most potent, with IC50 values of 13.4 ± 0.4, 15.3 ± 3.1, and 8.9 ± 0.9 µM, respectively, and that specific structural features such as the unsaturated enone moiety and particular substitutions were key for activity. The analogues also demonstrated low cytotoxicity on human dermal papilla cells, suggesting a good safety profile. The study provided insights for designing new curcumin analogs with enhanced potency and safety for treating hair loss and other androgen-related conditions.
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