Curcumin derivatives inhibit testicular 17beta-hydroxysteroid dehydrogenase 3

Guo-Xin Hu; Guang Liang; Yanhui Chu; Xiaokun Li; Qing-Quang Lian; Han Lin; Yi He; Yadong Huang; Dianne O Hardy; Ren-Shan Ge

doi:10.1016/j.bmcl.2010.02.089

Curcumin derivatives inhibit testicular 17beta-hydroxysteroid dehydrogenase 3

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2549-51. doi: 10.1016/j.bmcl.2010.02.089. Epub 2010 Mar 1.

Authors

Guo-Xin Hu¹, Guang Liang, Yanhui Chu, Xiaokun Li, Qing-Quang Lian, Han Lin, Yi He, Yadong Huang, Dianne O Hardy, Ren-Shan Ge

Affiliation

¹ School of Pharmacy, Wenzhou Medical College, Wenzhou 325000, PR China.

PMID: 20346654
DOI: 10.1016/j.bmcl.2010.02.089

Abstract

Non-steroidal compounds that inhibit 17beta-hydroxysteroid dehydrogenase isoform 3 (17beta-HSD3), an enzyme catalyzing the final step in testosterone biosynthesis in Leydig cells, are under development for male contraceptive or treatment of androgen dependent diseases including prostate cancer. A series of curcumin analogues with more stable chemical structures were compared to curcumin as inhibitors of 17beta-HSD3 in rat intact Leydig cells as well as rat and human testis microsomes.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

17-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
Animals
Curcumin / analogs & derivatives*
Curcumin / pharmacology
Enzyme Inhibitors / pharmacology*
Humans
Male
Rats
Testis / drug effects*
Testis / enzymology

Substances

Enzyme Inhibitors
17-Hydroxysteroid Dehydrogenases
17beta-hydroxysteroid dehydrogenase type 3
Curcumin