生物可利用的甲基化黄酮对芳香化酶的抑制作用。
Aromatase inhibition by bioavailable methylated flavones.
作者信息
Ta Nga, Walle Thomas
机构信息
Department of Cell and Molecular Pharmacology & Experimental Therapeutics, Medical University of South Carolina, 173 Ashley Avenue, Charleston, SC 29425, USA.
出版信息
J Steroid Biochem Mol Biol. 2007 Oct;107(1-2):127-9. doi: 10.1016/j.jsbmb.2007.01.006. Epub 2007 Jun 6.
Abstract
Previous studies have shown chrysin, 7-hydroxyflavone and 7,4'-dihydroxyflavone to be the most potent flavonoid inhibitors of aromatase. However, very poor oral bioavailability is a major limitation for the successful use of dietary flavonoids as chemopreventive agents. We have recently shown that methylated flavones, including 5,7-dimethoxyflavone, 7-methoxyflavone and 7,4'-dimethoxyflavone, are much more resistant to metabolism than their unmethylated analogs and have much higher intestinal absorption. In this study, we examined these fully methylated flavones as potential aromatase inhibitors for the prevention and/or treatment of hormone-dependent cancers. Whereas 5,7-dimethoxyflavone had poor effect compared to its unmethylated analog chrysin, 7-methoxyflavone and 7,4'-dimethoxyflavone were almost equipotent to their unmethylated analogs with IC(50) values of 2-9 microM. Thus, some fully methylated flavones appear to have great potential as cancer chemopreventive/chemotherapeutic agents.
摘要
先前的研究表明，白杨素、7-羟基黄酮和7,4'-二羟基黄酮是最有效的芳香化酶类黄酮抑制剂。然而，口服生物利用度极低是膳食类黄酮作为化学预防剂成功应用的主要限制因素。我们最近发现，包括5,7-二甲氧基黄酮、7-甲氧基黄酮和7,4'-二甲氧基黄酮在内的甲基化黄酮比其未甲基化类似物对代谢的抵抗力更强，且肠道吸收更高。在本研究中，我们研究了这些完全甲基化的黄酮作为预防和/或治疗激素依赖性癌症的潜在芳香化酶抑制剂。与未甲基化类似物白杨素相比，5,7-二甲氧基黄酮效果不佳，而7-甲氧基黄酮和7,4'-二甲氧基黄酮与其未甲基化类似物几乎等效，IC(50)值为2-9微摩尔。因此，一些完全甲基化的黄酮作为癌症化学预防/化疗药物似乎具有巨大潜力。
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本文引用的文献
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2
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