Diarylheptanoid-flavanone Hybrids as Multiple-target Antidiabetic Agents from Alpinia katsumadai  

作　　者：Xiao-Feng He Ji-Jun Chen Tian-Ze Li Jing Hu Xiao-Yan Huang Xue-Mei Zhang Yuan-Qiang Guo Chang-An Geng 

机构地区：[1]State Key Laboratory of Phytochemistry and Plant Resources in West China,Kunming Institute of Botany,Chinese Academy of Sciences,Yunnan Key Laboratory of Natural Medicinal Chemistry,Kunming,Yunnan,650201 China [2]College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research,Nankai University,Tianjin,300071 China [3]University of Chinese Academy of Sciences,Beijing,100049 China

出　　处：《Chinese Journal of Chemistry》2021年第11期3051-3063,共13页中国化学（英文版）

基　　金：This work was financially supported by the Yunnan Wanren Project(YNWR-QNBJ-2018-061);the Fund of State Key Laboratory of Phytochemistry and Plant Resources in West China(P2020-KF05);the Postdoctoral Oriented Training Program of Yunnan Province(E131821261);the Special Research Assistant Project of Chinese Academy of Sciences(E12D9211Q1);the Yunnan Science Fund for Excellent Young Scholars(2019FI017);the Reserve Talents of Young and Middle-aged Academic and Technical Leaders in Yunnan Province.

摘　　要：The EtOAc fraction of Alpinia katsumadai seeds showed significant inhibition on glycogen phosphorylase a(GPa)with inhibitory ratios of 97.9%and 64.6%at concentrations of 200 and 100μg/mL,respectively.Bioactivity-guided isolation afforded 15 new diarylheptanoid-flavanone hybrids,katsumadainols B_(1)-B_(15)(1-15),together with eight known ones(16-23).Compounds 4-10 and 12-21 exhibited activity against GPa with IC_(50) values of 10.1-95.4μmol/L;compounds 4,5,16,and 17 displayed inhibitory effects onα-glucosidase with IC_(50) values of 7.1,12.4,7.2,and 8.3μmol/L,obviously higher than acarbose(IC_(50),209.1μmol/L);compounds 4-6,14,16-20,22,and 23 were PTP1B/TCPTP selective inhibitors with IC_(50) values of 40.7-95.8μmol/L;compounds 4,5,16,and 17 showed DPP4 inhibitory effects with inhibitory ratios of 50.0%-54.2%(200μmol/L).Diarylheptanoid-flavanone hybrids(4,5,16,and 17)with a p-hydroxybenzyl at C-6 position represent a promising class of multiple-target antidiabetic agents inhibiting GPa,α-glucosidase,PTP1B,and DPP4.

关 键 词：Alpinia katsumadai Katsumadainols Bx-B_(15) Natural products Structure elucidation Biological activity 

分 类 号：O62[理学—有机化学]