人参根三醇组皂苷元25-OH-PPT、25-OCH_3-PPT、PPT、PT的HPLC/ELSD法测定及其α-葡萄糖苷酶抑制活性研究  

Simultaneous determination 25-OH-PPT, 25-OCH_3-PPT, PPT, and PT by HPLC-ELSD and its inhibition on α-glycosidase activities

作　　者：徐磊[1,2] 杨宁[3] 关健 崔炯谟[1] 赵余庆[3,4] XU Lei1＇ 2 YANG Ning3 GUAN Jian2 CUI Jiong-mo1 ZHAO Yu-qing3＇.4 1. School ofPharmay Yanbian University Yanji 133000 China 2. Liao ning Xin zhong Modem Pharmaceutical Company Shenyang 110041 China 3. School of Traditional Chinese Materia Medica Shenyang Pharmaceutical University Shenyang 110016 China 4. Key Laboratory of Structure-based Drug Design and Discovery Ministry of Education

机构地区：[1]延边大学药学院,吉林延吉133000 [2]辽宁新中现代医药有限公司,辽宁沈阳110041 [3]沈阳药科大学,辽宁沈阳110016 [4]基于靶点药物设计与研究教育部药物重点实验室,辽宁沈阳110016

出　　处：《药物评价研究》2016年第5期796-799,共4页Drug Evaluation Research

基　　金：基金项目:中药标准提取物的工业化色谱制备平台建设(2009ZX09301-012-105B);天然活性成分的工业化色谱制备公共服务平台(2011412004-7)

摘　　要：目的建立25-OH-PPT、25-OCH_3-PPT、PPT、PT同步检测的方法;从人参根皂苷水解产物中筛选发现具有降血糖活性的三醇组皂苷元。方法采用HPLC-ELSD法测定25-OH-PPT、25-OCH_3-PPT、PPT、PT;采用体外实验测定4种皂苷元对α-葡萄糖苷酶的抑制作用。结果 HPLC-ELSD测定结果表明,25-OH-PPT、25-OCH_3-PPT、PPT、PT在0.05~1.0 mg具有良好的线性关系,回收率分别为95.0%、98.4%、103.3%和96.0%,RSD分别为1.05%（n=4）、1.87%（n=4）、2.15%（n=4）和1.15%（n=4）,质量分数分别为8.07%、4.55%、1.46%和4.53%。4种皂苷元对α-葡萄糖苷酶呈现出不同强度的抑制活性,25-OH-PPT抑制活性强于阿卡波糖。结论 4种皂苷元降血糖活性强弱顺序为25-OH-PPT〉25-OCH_3-PPT〉PPT〉PT。HPLC/ELSD测定方法简单、快速、有效。Objective To determine the inhibitory activity of rare ginsenosides on α-glucosidase, and to select hypoglycemic compounds from ginsenosides. Meanwhile, to establish a method to determinate the contents of ginsenoside 25-OH-PPT, 25-OCH_3-PPT, PPT, and PT in hydrolysis products of total saponins in ginseng roots. Results The inhibitory activity of ginsenosides on α-glucosidase revealed that the inhibitory activities of 25-OH PPT, 25-OCH_3-PPT, PPT, and PT were better than that of positive drug acarbose while PT was worse than acarbose. Meanwhile, HPLC-ELSD results revealed that 25-OH PPT, 25-OCH_3-PPT, PPT, and PT showed good linear relationship in the region of（0.05—1.0） mg/m L. The recoveries were 95.0%, 98.4%, 103.3%, and 96.0%, respectively, RSD values were 1.05%（n = 4）, 1.87%（n= 4）, 2.15%（n = 4）, and 1.15%（n = 4）, respectively, and the content are 8.07%, 4.55%, 1.46%, and 4.53% respectively. Conclusion The order of their hypoglycemic acitivity is 25-OH-PPT 25-OCH_3-PPT PPT PT. Assay method of HPLC/ELSD is simple, fast, and effective.

关 键 词：人参皂苷元 Α-葡萄糖苷酶 HPLC/ELSD 25-OH-PPT 25-OCH3-PPT PPT PT 

分 类 号：R917[医药卫生—药物分析学]