Hyperterpenoids A and B:Two pairs of unprecedented 6/6/4/6/6 polycyclic cyclobutane meroterpenoids with potent neuroprotective and anti-inflammatory activities from Hypericum beanii  

作　　者：Bo Zhen Xinyue Suo Jun Dang Huilan Yue Yanduo Tao Jia-Jia Wang Li Li Ming-Bao Lin Qi Hou Wei-Ping Wang Xiao-Liang Wang Jian-Dong Jiang Teng-Fei Ji 

机构地区：[1]State Key Laboratory of Bioactive Substance and Function of Natural Medicines,Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China [2]Key Laboratory of Tibetan Medicine Research,Northwest Institute of Plateau Biology,Chinese Academy of Sciences,Xining 810008,China

出　　处：《Chinese Chemical Letters》2021年第7期2338-2341,共4页中国化学快报（英文版）

基　　金：financially supported by Projects of International Cooperation and Exchanges NSFC(NSFC-VR,No.81361138020);National Science and Technology Major Projects for"Major New Drugs Innovation and Development",Research and Development of New Drug Varieties from Natural Product Sources and Their Key Innovative Technological Systems(Nos.2018ZX09711001-001-001 and 2018ZX09711001-001-003);the CAMS Innovation Fund for Medical Sciences(CIFMS),the CAMS Initiative for Innovative Medicine(CAMS-I2M,No.2016-I2M-1-010)。

摘　　要：Hyperterpenoid A(1)and B(2),two pairs of enantiomers,with an unprecedented 6/6/4/6/6 polycyclic skeleton,along with one known compoud hypermonone A(3)were isolated from Hypericum beanii.The racemate(±)-1 and(±)-2 were successfully separated into the two optically pure enantiomers(ee>99%)using a preparative HPLC system.Their absolute configurations were elucidated by extensive spectroscopic analyses and single-crystal X-ray diffraction method.The related plausible biogenetic pathways were pre sented.Compound 1-3 showed significant neuroprotective activity and potential antiinflammatory activity.The result that(+)-2 and(-)-2 presented different anti-inflammatory properties,may lead us to new discovery of structure activity relationship between racemates,enantiomers,and diastereomers,as well as further research regarding the binding of drugs to target proteins.

关 键 词：Hypericum beanii MEROTERPENOIDS (±)-Hyperterpenoid A and B Anti-inflammatory activity Neuroprotective activity 

分 类 号：TQ460.1[化学工程—制药化工]