Inhibitory Effects of Curcuminoids on $17{\beta}$-hydroxysteroid Dehydrogenase Type 1 Activity in Animal Livers

• Published in: Journal of experimental & biomedical sciences Vol. 19; no. 2; pp. 147 - 152
• Main Authors: Lee, Sung-Eun, Park, Byeoung-Soo, Kim, Hye Jin, Lee, Eun-Woo, Yum, Jong Hwa
• Format: Journal Article
• Language: Korean
• Published: 2013
• Subjects: Demethoxycurcumin; 17{\beta}$-estradiol; Curcuminoids; 17{\alpha}$-estradiol; 17{\beta}$-hydroxysteroid dehydrogenase type 1
• ISSN: 1738-3226

17-${\beta}$-hydroxysteroid dehydrogenase type 1 ($17{\beta}$-HSD type 1) mediates the reaction of $17{\beta}$-estradiol (E2) production from estrone (E1). Inhibitory effects of curcuminoids on $17{\beta}$-HSD type 1 activity were investigated to find a lead compound for treating estrogen-dependent diseases including breast cancer. Among curcuminoids, demethoxycurcumin showed potent inhibitory effect ($IC_{50}=2.7{\mu}M$) on mouse $17{\beta}$-HSD type 1. Curcuminoids also displayed their inhibitory effects on the production of $17{\alpha}$-estradiol which is a carcinogenic metabolite produced by the enzyme. Bisdemethoxycurcumin ($IC_{50}=1.3{\mu}M$) showed potent inhibitory effect on the $17{\alpha}$-estradiol production by chicken $17{\beta}$-HSD type 1. Curcuminoids did not inhibit ERE transcriptional activity with and without E2. Taken together, curcuminoids can be used for treating and preventing E2-dependent diseases via inhibition on $17{\beta}$-HSD type 1 activity.