虎杖中α-葡萄糖苷酶抑制剂的高分辨筛选研究  

High-resolution screening ofα-glucosidase inhibitors from Polygoni Cuspidate Rhizoma et Radix

作　　者：陈文龙 何健 陶柒琪 陈智超 周灵佳 陈芝蓄 江正瑾 张婷婷 CHEN Wen-long;HE Jian;TAO Qi-qi;CHEN Zhi-chao;ZHOU Ling-jia;CHEN Zhi-xu;JIANG Zheng-jin;ZHANG Ting-ting(Institute of Pharmaceutical Analysis,College of Pharmacy,Jinan University,Guangzhou 510632,China;China Resources Sanjiu Medical&Pharmaceutical Co.,Ltd.,Shenzhen 518110,China)

机构地区：[1]暨南大学药学院药物分析研究中心,广州510632 [2]华润三九医药股份有限公司,深圳518110

出　　处：《药物分析杂志》2025年第1期81-91,共11页Chinese Journal of Pharmaceutical Analysis

基　　金：广东省大学生创新创业训练计划支持项目(S202310559152)。

摘　　要：目的:研究中药虎杖通过抑制α-葡萄糖苷酶活性发挥降糖功效的作用物质基础。方法:整合高效液相色谱系统、微流分收集装置、活性检测通道和高分辨质谱仪4大模块,搭建高通量活性轮廓分析平台;并引入制备液相色谱对虎杖提取液进行分段富集,通过优化色谱分离条件、微流分收集参数和多孔板中的酶活性检测方法等,实现虎杖中α-葡萄糖苷酶抑制剂的快速筛选。结果:从虎杖中筛出28个α-葡萄糖苷酶抑制剂,其中儿茶素-3-O-没食子酰基和原花青素B_(2)-3''-O-没食子酸酯的抑制活性IC_(50)达到了(9.49±1.93)μmol·L^(-1)和(69.94±8.14)μmol·L^(-1)。结论:本研究实现了中药中α-葡萄糖苷酶抑制剂的高通量与高分辨筛选,为阐明虎杖降糖的活性物质基础和作用机制提供了有力工具。Objective:To study the bioactive components of the hypoglycemic effect of the traditional Chinese medicine Polygoni Cuspidate Rhizoma et Radix through its ability to inhibitα-glucosidase activity.Methods:Four modules:high-performance liquid chromatography system,the nanofraction collector,the channel of bioassay and high-resolution mass spectrometry were integrated to build a high-throughput bioassay profiling analysis platform.The preparative liquid chromatography was introduced to apply segmented enrichment to the extract of Polygoni Cuspidate Rhizoma et Radix,and the rapid screening ofα-glucosidase inhibitors from Polygoni Cuspidate Rhizoma et Radix was realized by optimizing the chromatographic separation conditions,microfluidic fractionation collection parameters and bioassaying of enzyme activity in multi-well plates.Results:28α-glucosidase inhibitors were identified from Polygoni Cuspidate Rhizoma et Radix.The inhibitory activities of catechin-3-O-galloyl and procyanidin B_(2)-3''-O-gallate were determined with the IC_(50)values of(9.49±1.93)μmol·L^(-1)and(69.94±8.14)μmol·L^(-1),respectively.Conclusion:This study has enabled high-throughput and high-resolution screening ofα-glucosidase inhibitors in traditional Chinese medicine,providing a valuable tool for elucidating the active components and mechanisms of Polygoni Cuspidate Rhizoma et Radix to lower hyperglycemia.

关 键 词：虎杖 活性轮廓分析平台 糖尿病 Α-葡萄糖苷酶抑制剂 活性成分筛选 作用物质基础 

分 类 号：R917[医药卫生—药物分析学]