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Spirobiflavonoid stereoisomers from the endangered conifer Glyptostrobus pensilis and their protein tyrosine phosphatase 1B inhibitory activity

文献类型：期刊论文

作者Xiong, Juan1; Hu, Chang-Ling1; Wang, Pei-Pei4; Gao, Ding-Ding3; Huang, Fang2; Li, Jia4; Hu, Jin-Feng1
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2020-02-15
卷号30期号:4页码:4
关键词Glyptostrobus pensilis Cupressaceae Endangered conifer Spirobiflavonoids PTP1B inhibition
ISSN号0960-894X
DOI10.1016/j.bmcl.2019.126943
通讯作者Li, Jia(jli@simm.ac.cn) ; Hu, Jin-Feng(jfhu@fudan.edu.cn)
英文摘要Six spirobiflavonoid stereoisomers including two new ones, spiropensilisols A (1) and B (2), were isolated from a mass-limited trunk barks of Glyptostrobus pensilis, an endangered conifer endemic to China. The new structures featuring a benzofuran-containing spirolactone and their absolute configurations were determined by extensive spectroscopic methods. All the isolates showed significant inhibitory activities against the human protein tyrosine phosphatase 1B (PTP1B) enzyme, a potential therapeutic target for diabetes and obesity, with IC50 values ranging from 3.3 to 17.1 mu M. A preliminary SAR analysis with assistance of the molecular modeling approach was performed for the most potent compound (i.e., 1), to understand the nature of interactions governing the binding mode of spirobiflavonids within the active site of the PTP1B enzyme.
WOS关键词PHENOLIC-COMPOUNDS ; A-C ; DITERPENOIDS ; BARK
资助项目NSFC[21937002] ; NSFC[21772025] ; NSFC[81773599] ; MOST[2019ZX09735-002]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000507987200035
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/282366]  
专题新药研究国家重点实验室
通讯作者Li, Jia; Hu, Jin-Feng
作者单位1.Fudan Univ, Sch Pharm, Dept Nat Prod Chem, Shanghai 201203, Peoples R China
2.Shanghai Acad Landscape Architecture Sci & Planni, Shanghai 200232, Peoples R China
3.Shanghai Univ Tradit Chinese Med, Innovat Res Inst IRI Tradit Chinese Med, Shanghai 201203, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Xiong, Juan,Hu, Chang-Ling,Wang, Pei-Pei,et al. Spirobiflavonoid stereoisomers from the endangered conifer Glyptostrobus pensilis and their protein tyrosine phosphatase 1B inhibitory activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2020,30(4):4.
APA Xiong, Juan.,Hu, Chang-Ling.,Wang, Pei-Pei.,Gao, Ding-Ding.,Huang, Fang.,...&Hu, Jin-Feng.(2020).Spirobiflavonoid stereoisomers from the endangered conifer Glyptostrobus pensilis and their protein tyrosine phosphatase 1B inhibitory activity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,30(4),4.
MLA Xiong, Juan,et al."Spirobiflavonoid stereoisomers from the endangered conifer Glyptostrobus pensilis and their protein tyrosine phosphatase 1B inhibitory activity".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 30.4(2020):4.

入库方式： OAI收割

来源：上海药物研究所

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