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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