Bioassay-guided isolation of α-Glucosidase inhibitory constituents from Hypericum sampsonii

作     者：TAO Linlan XU Shuangyu ZHANG Zizhen LI Yanan YANG Jue GU Wei YI Ping HAO Xiaojiang YUAN Chunmao TAO Linlan;XU Shuangyu;ZHANG Zizhen;LI Yanan;YANG Jue;GU Wei;YI Ping;HAO Xiaojiang;YUAN Chunmao

作者机构：State Key Laboratory of Functions and Applications of Medicinal PlantsGuizhou Medical UniversityGuiyang 550014China School of Pharmaceutical SciencesGuizhou Medical UniversityGuiyang 550025China Natural Products Research Center of Guizhou ProvinceGuiyang 550014China State Key Laboratory of Phytochemistry and Plant Resources in West ChinaKunming Institute of BotanyChinese Academy of SciencesKunming 650201China 

出 版 物：《Chinese Journal of Natural Medicines》 (中国天然药物（英文版）)

年 卷 期：2023年第21卷第6期

页      面：443-453页

核心收录：

学科分类：1008[医学-中药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

基　　金：supported by the National Natural Science Foundation of China(No.32270413,U1812403) the Science and Technology Department of Guizhou Province(No.QKH 2020-1Z076) the 13th batch of Outstanding Young Scientific and Technological Talents in Guizhou Province(No.QKHPTRC5633) Cultivation project of National Natural Science Foundation of Guizhou Medical University(No.19NSP003) the Education Department of Guizhou Province(No.QJH KY189) the Natural Science Foundation of Guizhou Province(No.QKHZYD4015) High-level Innovative Talents in Guizhou Province(Thousand Levels of Talent for Chunmao Yuan in 2018) “Light of the West”Talent Cultivation Program of Chinese Academy of Sciences for Chunmao Yuan(No.RZ82) 

主　　题：Hypericum sampsonii Chemical constituents Structure elucidation α-Glucosidase Molecular docking 

摘      要：This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic *** sampsonii was investigated,leading to the isolation of two highly modified seco-polycyclic polyprenylated acylphloroglucinols(PPAPs)(1 and 2),eight phenolic derivatives(3-10),and four terpene derivatives(11-14).The structures of compounds 1 and 2,featuring an unprecedented octahydro-2H-chromen-2-one ring system,were fully characterized using extensive spectroscopic data and quantum chemistry *** compounds(1,5-7,9,and 14)exhibited potential inhibitory effects against α-glucosidase,with IC_(50) values ranging from 0.050±0.0016 to 366.70±11.08μg·mL^(-1).Notably,compound 5(0.050±0.0016μg·mL^(-1))was identified as the most potential α-glucosidase inhibitor,with an inhibitory effect about 6900 times stronger than the positive control,acarbose(IC_(50)=346.63±15.65μg·mL^(-1)).A docking study was conducted to predict molecular interactions between two compounds(1 and 5)and α-glucosidase,and the hypothetical biosynthetic pathways of the two unprecedented seco-PPAPs were proposed.