Potent modification of inducible CYP1A1 expression by flavonoids.
Potent modification of inducible CYP1A1 expression by flavonoids.
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DOI：
10.1248/bpb.33.1698
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发表时间：
2010-10
影响因子：
2
通讯作者：
W. Chatuphonprasert;Sachiko Kondo;K. Jarukamjorn;Yuki Kawasaki;T. Sakuma;N. Nemoto
中科院分区：
文献类型：
--
作者：
W. Chatuphonprasert;Sachiko Kondo;K. Jarukamjorn;Yuki Kawasaki;T. Sakuma;N. Nemoto
本研究观察了黄酮类化合物对原代培养小鼠肝细胞中β-萘啶酮（β-NF）诱导的细胞色素P450 1A 1（CYP 1A 1）表达的影响。部分黄酮类化合物（芹菜素、白杨素、黄酮、二氢黄酮、高良姜素、木犀草素和柚皮素）单独诱导CYP 1A 1 mRNA表达，尤其是黄酮类化合物的诱导作用比β-NF更强。对β-NF诱导的CYP 1A 1 mRNA表达的影响各不相同，即累加、抑制或两者兼而有之。加性效应后，观察到与黄烷酮，柚皮素，白杨素联合治疗，而山奈酚，杨梅素，槲皮素降低CYP 1A 1水平。芹菜素、白杨素、高良姜素、木樨草素和桑色素在24 h协同增强β-NF诱导的CYP 1A 1表达，但在9 h显著抑制。黄酮类化合物作为诱导剂或抑制剂影响CYP 1A 1表达的构效关系进行了讨论。目前的观察结果表明，需要揭示的机制，CYP 1A 1的表达被类黄酮修饰的风险评估，因为CYP 1A 1激活环境致癌的多环烃类化合物和类黄酮是食品中的主要成分。
The present study examined modifications of β-naphthoflavone (β-NF)-induced cytochrome P450 1A1 (CYP1A1) expression by flavonoids in mouse hepatocytes in primary culture. Some flavonoids (apigenin, chrysin, flavone, flavanone, galangin, luteolin, and naringenin) by themselves induced CYP1A1 mRNA expression, especially flavone which was even more effective than β-NF. The effect on β-NF-induced CYP1A1 mRNA expression was varied, namely additive, suppressive, or both. An additive effect was observed after combined treatment with flavanone, naringenin, and chrysin, whereas kaempferol, myricetin, and quercetin decreased CYP1A1 levels. Apigenin, chrysin, galangin, luteolin, and morin synergistically enhanced β-NF-induced CYP1A1 expression at 24 h, but considerably suppressed it at 9 h. The structure-activity relationship of flavonoids affecting CYP1A1 expression as inducers or inhibitors is discussed. The present observations suggest the need to reveal the mechanism by which CYP1A1 expression is modified by flavonoids for risk assessment, since CYP1A1 activates environmental carcinogenic polycyclic hydrocarbons and flavonoids are major constituents in food.