Flavonoids from the roots and rhizomes of Sophora tonkinensis and their in vitro anti-SARS-CoV-2 activity  

作　　者：LI Zhuo XIE Hang TANG Chunping FENG Lu KE Changqiang XU Yechun SU Haixia YAO Sheng YE Yang 

机构地区：[1]School of Chinese Materia Medica,Nanjing University of Chinese Medicine,Nanjing 210023,China [2]State Key Laboratory of Drug Research,and Natural Products Chemistry Department,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China [3]School of Pharmacy,University of Chinese Academy of Sciences,Beijing 100049,China [4]Drug Discovery and Design Center,CAS Key Laboratory of Receptor Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China [5]School of Pharmaceutical Science and Technology,Hangzhou Institute for Advanced Study,University of Chinese Academy of Sciences,Hangzhou,China

出　　处：《Chinese Journal of Natural Medicines》2023年第1期65-80,共16页中国天然药物（英文版）

基　　金：This work was supported from the National Natural Science Foundation of China(Nos.82173696 and 21920102003);the Science and Technology Commission of Shanghai Municipality(Nos.20431900200 and 20430780300);the Strategic Priority Research Program of Chinese Academy of Sciences(Nos.SIMM010110 and SIMM040302);the Sustainable Development of Precious Traditional Chinese Medicine Resources(No.2060302-2001-01).

摘　　要：Acute respiratory infection caused by severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)had caused a global pandemic since 2019,and posed a serious threat to global health security.Traditional Chinese medicine(TCM)has played an indispensable role in the battle against the epidemic.Many components originated from TCMs were found to inhibit the production of SARS-CoV-23C-like protease(3CLpro)and papain-like protease(PLpro),which are two promising therapeutic targets to inhibit SARS-CoV-2.This study describes a systematic investigation of the roots and rhizomes of Sophora tonkinensis,which results in the characterization of 12 new flavonoids,including seven prenylated flavanones(1−7),one prenylated flavonol(8),two prenylated chalcones(9−10),one isoflavanone(11),and one isoflavan dimer(12),together with 43 known compounds(13−55).Their structures including the absolute configurations were elucidated by comprehensive analysis of MS,1D and 2D NMR data,and time-dependent density functional theory electronic circular dichroism(TDDFT ECD)calculations.Compounds 12 and 51 exhibited inhibitory effects against SARS-CoV-23CLpro with IC_(50) values of 34.89 and 19.88μmol·L^(−1),repectively while compounds 9,43 and 47 exhibited inhibitory effects against PLpro with IC_(50) values of 32.67,79.38,and 16.74μmol·L^(−1),respectively.

关 键 词：Sophora tonkinensis Flavonoid Anti-SARS-CoV-2 activity SARS-CoV-23CLpro SARS-CoV-2 PLpro 

分 类 号：R284[医药卫生—中药学] R965[医药卫生—中医学]