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Unusual ent-Labdane Diterpenoid Dimers and their Selective Activation of TRPV Channels

文献类型：期刊论文

作者Gao, Suyu6; Wang, Dun6; Chai, Hao2,3,4; Xu, Jiamin6; Li, Tianyu2,3,4; Niu, Yingxue6; Chen, Xinxin6; Qiu, Feng1,7; Li, Yang2,3,4; Li, Hua5,6
刊名JOURNAL OF ORGANIC CHEMISTRY
出版日期2019-11-01
卷号84期号:21页码:13595-13603
ISSN号0022-3263
DOI10.1021/acs.joc.9b01864
通讯作者Qiu, Feng(fengqiu20070118@163.com) ; Li, Yang(liyang@simm.ac.cn) ; Li, Hua(li_hua@hust.edu.cn) ; Chen, Lixia(syzyclx@163.com)
英文摘要Five unusual dimers of ent-labdane diterpenoids (1-5) were isolated and identified from Andrographis paniculata, a famous medicinal plant. Bisandrographolide E (1) represents the first example of a labdane dimer possessing an unprecedent tricyclic system that comprised a spiroketal moiety fused with a ketal-gamma-lactone unit in its skeleton. Its biosynthetically related intermediates, all four stereoisomers at C-12 and C-15', bisandrographolides F (2, a new compound) and A-C (3-5), were obtained at the same time. The steric configurations of the newly formed asymmetric carbons in 1-5 were first solved by single-crystal X-ray diffraction of the diacetone derivatives of 2-4 and ECD and NMR calculations of 1. More importantly, bisandrographolides 1-5, with different chemical structures or absolute configurations at C-12 and C-15', selectively activated different TRPV1 -4 channels and protected cardiomyocytes from hypoxia-reoxygenation injury. Among them, 5 with 12R/15'S configuration activated TRPV1 most effectively and displayed the best cardiomyocyte protection.
WOS关键词SECONDARY METABOLITES ; AERIAL PARTS ; PREDICTION
资助项目National Natural Science Foundation of China[81773594] ; National Natural Science Foundation of China[81202426] ; National Natural Science Foundation of China[81473254] ; National Natural Science Foundation of China[81773637] ; Liaoning Province Natural Science Foundation[2019-MS-299] ; Liaoning Revitalization Talents Program[XLYC1807182] ; Program for Liaoning Innovation Talents in University[LR2016002]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000494562600034
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/281922]  
专题新药研究国家重点实验室
通讯作者Qiu, Feng; Li, Yang; Li, Hua; Chen, Lixia
作者单位1.Tianjin Univ Tradit Chinese Med, Sch Chinese Mat Med, Tianjin 300193, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, Shanghai 201203, Peoples R China
5.Huazhong Univ Sci & Technol, Tongji Med Coll, Sch Pharm, Wuhan 430030, Hubei, Peoples R China
6.Shenyang Pharmaceut Univ, Wuya Coll Innovat, Sch Pharmaceut Engn, Key Lab Struct Based Drug Design & Discovery,Mini, Shenyang 110016, Liaoning, Peoples R China
7.Tianjin Univ Tradit Chinese Med, Tianjin State Key Lab Modern Chinese Med, Tianjin 300193, Peoples R China
推荐引用方式
GB/T 7714		 Gao, Suyu,Wang, Dun,Chai, Hao,et al. Unusual ent-Labdane Diterpenoid Dimers and their Selective Activation of TRPV Channels[J]. JOURNAL OF ORGANIC CHEMISTRY,2019,84(21):13595-13603.
APA Gao, Suyu.,Wang, Dun.,Chai, Hao.,Xu, Jiamin.,Li, Tianyu.,...&Chen, Lixia.(2019).Unusual ent-Labdane Diterpenoid Dimers and their Selective Activation of TRPV Channels.JOURNAL OF ORGANIC CHEMISTRY,84(21),13595-13603.
MLA Gao, Suyu,et al."Unusual ent-Labdane Diterpenoid Dimers and their Selective Activation of TRPV Channels".JOURNAL OF ORGANIC CHEMISTRY 84.21(2019):13595-13603.

入库方式： OAI收割

来源：上海药物研究所

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