Selective inhibition of human type-5 17β-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis

…, O El-Kabbani, N Toyooka, S Ohta, A Hara

Index: El-Kabbani, Ossama; Scammells, Peter J.; Gosling, Joshua; Dhagat, Urmi; Endo, Satoshi; Matsunaga, Toshiyuki; Soda, Midori; Hara, Akira Journal of Medicinal Chemistry, 2009 , vol. 52, # 10 p. 3259 - 3264

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Citation Number: 25

Abstract

The human aldo-keto reductase (AKR) 1C3, also known as type-5 17β-hydroxysteroid dehydrogenase and prostaglandin F synthase, has been suggested as a therapeutic target in the treatment of prostate and breast cancers. In this study, AKR1C3 inhibition was examined by Brazilian propolis-derived cinnamic acid derivatives that show potential antitumor activity, and it was found that baccharin (1) is a potent competitive inhibitor (K i ...