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KMID : 0603820130190020147
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Journal of Experimental & Biomedical Science
2013 Volume.19 No. 2 p.147 ~ p.152
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Inhibitory Effects of Curcuminoids on 17β-hydroxysteroid Dehydrogenase Type 1 Activity in Animal Livers
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Lee Sung-Eun
Park Byeoung-Soo
Kim Hye-Jin
Lee Eun-Woo
Yum Jong-Hwa
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Abstract
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17-β-hydroxysteroid dehydrogenase type 1 (17β-HSD type 1) mediates the reaction of 17β-estradiol (E2) production from estrone (E1). Inhibitory effects of curcuminoids on 17β-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 (IC50 = 2.7 μM) on mouse 17β-HSD type 1. Curcuminoids also displayed their inhibitory effects on the production of 17α-estradiol which is a carcinogenic metabolite produced by the enzyme. Bisdemethoxycurcumin (IC?? = 1.3 μM) showed potent inhibitory effect on the 17α-estradiol production by chicken 17β-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 17β-HSD type 1 activity.
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KEYWORD
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Curcuminoids, 17β-hydroxysteroid dehydrogenase type 1, 17β-estradiol, 17α-estradiol, Demethoxycurcumin
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