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

被引：25
|
作者：
Ogawa, Yoshihisa [1 ]
Akamatsu, Miki [2 ]
Hotta, Yudai [1 ]
Hosoda, Akifumi [1 ]
Tamura, Hiroto [1 ]
机构：
[1] Meijo Univ, Dept Environm Biosci, Nagoya, Aichi 4688502, Japan
[2] Kyoto Univ, Grad Sch Agr, Kyoto 6068502, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 07期
关键词：
Androgen; Antagonist; Essential oil; CoMFA; Drug design; RECEPTOR AGONISTS; ANDROGEN; ANTAGONISTS; BINDING; MDA-KB2; COMFA;
D O I：
10.1016/j.bmcl.2010.02.059
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 IC50 value of 19 mu M. Raspberry ketone, which has threefold higher anti-obese activity than that of capsaicin, also had AR antagonist activity with its IC50 value of 252 mu M. Based on these findings, a more precise CoMFA model was proposed as follows: pIC(50) [log (1/IC50)] = 3.77 + [CoMFA field terms] (n = 39, s = 0.249, r(2) = 0.834, s(cv) = 0.507, q(2) = 0.311 (three components). (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2111 / 2114
页数：4
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