Curcumin derivatives inhibit testicular 17beta-hydroxysteroid dehydrogenase 3.

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.

• Authors: Guo-Xin Hu, Guang Liang, Yanhui Chu, Xiaokun Li, Qing-Quang Lian, Han Lin, Yi He, Yadong Huang, Dianne O Hardy, Ren-Shan Ge
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 8 Pg. 2549-51 (Apr 15 2010) ISSN: 1464-3405 [Electronic] England
• PMID: 20346654 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright 2010 Elsevier Ltd. All rights reserved.

Chemical References

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

Topics

• 17-Hydroxysteroid Dehydrogenases (antagonists & inhibitors)
• Animals
• Curcumin (analogs & derivatives, pharmacology)
• Enzyme Inhibitors (pharmacology)
• Humans
• Male
• Rats
• Testis (drug effects, enzymology)