Bioorganic & Medicinal Chemistry Letters 2010-04-01

Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay.

Yoshihisa Ogawa, Miki Akamatsu, Yudai Hotta, Akifumi Hosoda, Hiroto Tamura

Index: Bioorg. Med. Chem. Lett. 20 , 2111-4, (2010)

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Abstract

The effect of essential oils, such as raspberry ketone, on androgen (AR) receptor was investigated using a MDA-kb2 human breast cancer cell line for predicting potential AR activity. Among them, eugenol had the highest AR antagonistic activity with its IC(50) value of 19 microM. Raspberry ketone, which has threefold higher anti-obese activity than that of capsaicin, also had AR antagonist activity with its IC(50) value of 252 microM. Based on these findings, a more precise CoMFA model was proposed as follows: pIC(50) [log (1/IC(50))]=3.77+[CoMFA field terms] (n=39, s=0.249, r(2)=0.834, s(cv)=0.507, q(2)=0.311 (three components).2010 Elsevier Ltd. All rights reserved.