目的:对金线莲(Anoectochilus roxburghii(Wall.)Lindl.)中分离到的两个丁酸苷类化合物进行PTP1B抑制活性研究。方法:采用比色法间接测定游离磷酸根的量,来评价PTP1B的去磷酸化活性。结果:体外PTP1B抑制活性筛选结果表明化合物Ⅰ(kinsenoside)对PTP1B有显著的抑制作用,抑制活性明显强于阳性对照和化合物Ⅱ(methyl4-β-D-glucopyranosyl-butanoate)。结论:kinsenoside有望作为潜在的PTP1B抑制剂或活性先导化合物,用于治疗Ⅱ型糖尿病和肥胖症,值得进一步研究和开发。
Objective:In order to investigate the inhibiting effects on PTP1B of two butanoic acid glycosides isolated from Anoectochilus roxburghii(Wall.) Lindl.Methods:Colorimetric assay was employed to determine free phosphate radical,which is used to measure the dephosphorylation activity of PTP1B.Results:Notable inhibiting effect of Ⅰ(kinsenoside) on PTP1B was observed,which was much more significant than the positive control and compound Ⅱ(methyl 4-β-D-glucopyranosyl-butanoate).Conclusion:Based on the significant inhibiting effect of kinsenoside on PTP1B,it may be a potential PTP1B inhibitor or leading compound for treating diabetesⅡand obesity.