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

Lee, Sung-Eun (Division of Applied Biosciences, Kyungpook National University)
Park, Byeoung-Soo (Research Station, Nanotoxtech Inc.)
Kim, Hye Jin (Department of Dental Hygiene, College of Nursing and Healthcare Sciences, Dong-eui University)
Lee, Eun-Woo (Department of Life Science and Biotechnology, College of Natural Sciences, Dong-eui University)
Yum, Jong Hwa (Department of Clinical Laboratory Science, College of Nursing and Healthcare Sciences)
Abstract
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.
Keywords
Curcuminoids; $17{\beta}$-hydroxysteroid dehydrogenase type 1; $17{\beta}$-estradiol; $17{\alpha}$-estradiol; Demethoxycurcumin;
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