7种黄酮类化合物对重组人促肝细胞再生磷酸酶-3活性的影响

Effect of Seven Kinds of Flavonoids on Recombinant Human Protein Tyrosine Phosphatase

目的:观察7种黄酮类化合物对重组人促肝细胞再生磷酸酶-3(PRL-3)活性的影响。方法:利用基因工程技术获得重组人PRL-3;通过测定PRL-3水解底物DiFMUP中磷酸基团生成DiFMU的荧光强度,探讨黄酮类化合物对重组人PRL-3活性的抑制作用,并采用半数效量概率单位法计算其IC50。结果:杨梅素和印棉黄素能显著抑制PRL-3的活性,其IC50分别为55.54、68.86μmol/L。槲皮素、木犀草素及7,8-二羟基黄酮对PRL-3的抑制作用较弱,其IC50分别为113.38、151.56、249.49μmol/L;而3-羟基黄酮和6-羟基黄酮对PRL-3酶的活性无明显影响。构效分析表明:黄酮母核C4位、C7位上羟基可能是抑制PRL-3的必需基团,且随着黄酮骨架上羟基数目的增多,抑制效果越强。结论:杨梅素和印棉黄素是2种较强的PRL-3抑制剂。

Objective：To observe the effects of seven kinds of flavonoids on recombinant human phosphatase of regenerating liver-3 activity.Methods：The inhibitory effect of flavonoids was tested by DiFMUP assay.Calculation of IC50 values was performed according to the law of semi-effect-probit.Results：Myricetin and gossypin could significantly inhibit recombinant PRL-3 activity in a concentration dependent manner with IC50 values of 55.54 and 68.86 μmol/L,respectively.Quercetin,luteolin and 7,8-Dihydroxyflavone had a weak inhibitory effect with IC50 values of 113.38,151.56 and 249.49 μmol/L.respectively.While 3-hydroxyflavone and 6-hydroxyflavone had no significant effect on PRL-3 activity.Structure activity study indicated that C4 and C7 hydroxyls on the flavone skeleton were key functional groups to influencing PRL-3 inhibotory activity.The inhibitory effect of flavonoids on PRL-3 was increased with the number of hydroxyl group.Conclusion：Myricetin and gossypin were two strong inhibitors on recombinant human protein tyrosine phosphatase PRL-3.