The flavonoid galangin is an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.
The flavonoid galangin is an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.
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类黄酮Galangin是CYP1A1活性的抑制剂，也是芳基烃受体的激动剂/拮抗剂。
DOI：
10.1038/sj.bjc.6690216
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发表时间：
1999-03
影响因子：
8.8
通讯作者：
Yeh, GC
中科院分区：
文献类型：
--
作者：
Ciolino, HP;Yeh, GC
研究了高良姜黄酮对MCF-7人乳腺癌细胞7，12-二甲基苯并[a]蒽（DMBA）代谢、细胞色素P450 1A1（CYP1A1）活性及其表达的影响。通过薄层色谱法测定，高良姜素以剂量依赖性方式抑制DMBA的分解代谢。高良姜素还抑制DMBA-DNA加合物的形成，并阻止DMBA诱导的细胞生长抑制。高良姜素引起了有效的，剂量依赖性抑制CYP1A1活性，测定乙氧基试卤灵-O-脱乙基酶活性，在完整的细胞和DMBA处理的细胞分离的微粒体。通过双倒数图的抑制动力学分析表明，高良姜素以非竞争性方式抑制CYP1A1活性。高良姜素可引起CYP1A1 mRNA水平的增加，表明它可能是一种芳烃受体激动剂，但它可抑制DMBA或2，3，5，7-四氯二苯并-对-二恶英（TCDD）对CYP1A1 mRNA的诱导。高良姜素还抑制DMBA或TCDD诱导的含有CYP1A1启动子的报告载体的转录。因此，高良姜素是DMBA代谢的有效抑制剂和AhR的激动剂/拮抗剂，并且可以证明是有效的化学预防剂。© 1999癌症研究运动
The effect of the dietary flavonoid galangin on the metabolism of 7,12-dimethylbenz[a]anthracene (DMBA), the activity of cytochrome P 450 1A1 (CYP1A1), and the expression of CYP1A1 in MCF-7 human breast carcinoma cells was investigated. Galangin inhibited the catabolic breakdown of DMBA, as measured by thin-layer chromatography, in a dose-dependent manner. Galangin also inhibited the formation of DMBA-DNA adducts, and prevented DMBA-induced inhibition of cell growth. Galangin caused a potent, dose-dependent inhibition of CYP1A1 activity, as measured by ethoxyresorufin-O-deethylase activity, in intact cells and in microsomes isolated from DMBA-treated cells. Analysis of the inhibition kinetics by double-reciprocal plot demonstrated that galangin inhibited CYP1A1 activity in a non-competitive manner. Galangin caused an increase in the level of CYP1A1 mRNA, indicating that it may be an agonist of the aryl hydrocarbon receptor, but it inhibited the induction of CYP1A1 mRNA by DMBA or by 2,3,5,7-tetrachlorodibenzo-p-dioxin (TCDD). Galangin also inhibited the DMBA- or TCDD-induced transcription of a reporter vector containing the CYP1A1 promoter. Thus, galangin is a potent inhibitor of DMBA metabolism and an agonist/antagonist of the AhR, and may prove to be an effective chemopreventive agent. © 1999 Cancer Research Campaign
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