黄酮与黄酮醇类化合物对HepG2细胞中CYP1A1mRNA表达的影响

Effects of flavones and flavonols on CYP1A1 mRNA expression in HepG2 cells

目的观察15种黄酮与黄酮醇类化合物对细胞色素P450酶(cytochrome P450,CYP)1A1基因表达的影响。方法采用实时定量PCR技术检测HepG2细胞中各CYP1A1mRNA的表达。结果黄酮、6-羟基黄酮、槲皮素、黄芩素、野黄芩苷、野黄芩素和白杨黄素是CYP1A1的强诱导剂,50uM浓度时诱导超过10倍;黄芩苷是中等程度诱导剂,诱导倍数为7.68;桑黄素、木犀草素、汉黄芩素和山萘酚是CYP1A1弱诱导剂,诱导倍数在2-3倍左右。而7-羟基黄酮、漆黄素、芹菜黄素是CYP1A1的弱抑制剂,抑制倍数在2-3倍。结论黄酮与黄酮醇类化合物对CYP1A1的诱导作用存在很大的差异,其诱导作用的强弱与其结构有关。黄酮与黄酮醇类化合物对CYP1A1表达的强诱导作用,能加速一些前致癌物转化为致癌物,我们的研究为黄酮制剂的安全性提供了实验数据。

Objective Study the effects of fifteen kinds of flavones and flavonols on cytochrome P450 enzymes （CYP） 1A1 mRNA expression.Methods The mR.NA expression level of CYP 1A1 was determined by quantitative reverse-transeriptase polymerase chain reaction in HepG2 cells. Results Favone, 6-hydroxyfalvone, quercetin, baicalein, scutellarin, scutellarein and chrysin are strongly CYP1A1-inducing agents, whose inducing folds are more than ten at 50 uM; Baicalin is moderately inducing agent, whose inducing folds are 7.68 at 50 uM; Morin, luteolin, wogonin and kaempferol are weakly inducing agent, whose inducing folds are about 2 - 3;7-hydroxyflavone, fisetin and apigenin are weakly inhibiting agent, whose inhibiting folds are about 2- 3. Conclusion There are largely differences on the effect of flavones and flavonols on CYP1A1 mRNA expression.Their inducing effects are associated with their structures. The inducing effects of flavones and flavonols on CYP1A1 expression might induce proearcinogen to carcinogen, which would give the evidence for the safety of flavones and flavonols.