摘要
目的糖尿病并发症与糖代谢的多元醇通路有关,而醛糖还原酶(aldose reductase,AR)是该通路的关键限速酶。本研究拟分析不同类型人参皂苷对AR的抑制作用,探讨其在糖尿病并发症治疗中的潜在应用价值。方法采用分光光度法测定不同类型人参皂苷对AR的抑制作用,并依据动力学曲线计算其半数抑制浓度((IC50));通过双倒数作图法确定人参皂苷对AR抑制作用的类型。结果人参皂苷Rb1、Rd、Rg1和Rg2对AR具有抑制作用,而人参皂苷Rb2、Rb3、Rc和Re的抑制作用不明显。进一步分析表明,人参皂苷Rd、Rg1和Rg2对AR的抑制作用强于"依帕司他",而Rb1的抑制作用较弱;另外,人参皂苷的浓度与其对AR的抑制作用正相关,且抑制类型均为反竞争性抑制。结论人参皂苷Rg2、Rg1、Rd对该AR具有较强的抑制作用,在糖尿病并发症治疗方面具有潜在的应用价值。
Aim To explore the inhibitory effect of different types of ginsenoside on AR,and provide an insight into the potential application of ginsenoside in the treatment of diabetic complications.Methods The spectrophotometry was used to determinate the inhibitory effect of ginsenoside on AR,and the 50% inhibitory concentraton（IC50） was calculated based on the inhibitory kinetic curve;the inhibition types were characterized by Lineweaver-Burk method.Results The inhibitory effects of ginsenoside Rb1,Rd,Rg1 and Rg2 on AR were detected,while no obvious inhibition of Rb2,Rb3,Rc and Re was observed.The further analysis showed that the inhibitory effects of ginsenoside Rd,Rg1 and Rg2 were significantly stronger than those of epalrestat,while that of the ginsenoside Rb1 was relatively lower.Moreover,the inhibitory effects on AR were increased along with concentrations of ginsenoside Rd,Rg1 and Rg2,and they were all uncompetitive inhibition.Conclusion The ginsenoside Rd,Rg1 and Rg2 have stronger inhibitory effect on aldose reductase（AR）,which implies their potential application prospects of treating diabetic complications.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2011年第6期827-830,共4页
Chinese Pharmacological Bulletin
基金
吉林省科技发展计划重点项目(No20060902)
关键词
人参皂苷
醛糖还原酶
糖尿病并发症
糖代谢
分光光度法
双倒数作图法
反竞争性抑制
ginsenoside
aldose reductase
diabetic complications
glucose metabolism
spectrophotometry
line weaver-burk method
uncompetitive inhibition
