Curcumin Derivatives Inhibit Testicular 17β-Hydroxysteroid Dehydrogenase 3

    March 2010 in “ Bioorganic & Medicinal Chemistry Letters ”
    Guoxin Hu, Guang Liang, Yanhui Chu, Xiaokun Li, Qing-Quang Lian, Han Chieh Lin, Yi He, Yadong Huang, Dianne O. Hardy, Ren-Shan Ge
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    TLDR Curcumin and its derivatives can block an enzyme important for making testosterone, with one derivative being particularly strong.
    The study from April 2010 examined the effects of curcumin and its derivatives on the enzyme 17β-hydroxysteroid dehydrogenase 3 (17β-HSD3), which is important for testosterone production. Curcumin inhibited the enzyme with IC50 values of 9.0 ± 1.0 µM in rat Leydig cells, 2.3 ± 1.2 µM in rat testis microsomes, and 67.3 ± 11.9 µM in human testis microsomes. One derivative, compound C3, was significantly more effective, with an IC50 of 0.1 µM against human 17β-HSD3. The results indicated that curcumin derivatives could be more potent inhibitors of 17β-HSD3 than curcumin itself, with varying effectiveness between species, suggesting their potential use in anti-androgenic therapies.
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