摘要
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.
出处
《中药药理与临床》
CAS
CSCD
北大核心
2010年第4期16-18,共3页
Pharmacology and Clinics of Chinese Materia Medica
基金
国家自然科学基金(30400585)
教育部新世纪优秀人才支持计划(NCET-08-0224)
国家中医药管理局中医药科学技术研究专项(04-05ZQ03)
华中科技大学自主创新基金重点项目(09514009)
