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Design, synthesis and biological evaluation of vincamine derivatives as potential pancreatic beta-cells protective agents for the treatment of type 2 diabetes mellitus

文献类型：期刊论文

作者Wang, Junwei1; Lv, Xue2; Xu, Jiawen1; Liu, Xinpeng1; Du, Te2,3; Sun, Guanglong2,3; Chen, Jing2,3; Shen, Xu1; Wang, Jiaying1; Hu, Lihong1,2,3
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2020-02-15
卷号188页码:17
关键词Type 2 diabetes mellitus Pancreatic beta-cells protective agents Vincamine derivatives Structural modifications Structure-activity relationships
ISSN号0223-5234
DOI10.1016/j.ejmech.2019.111976
通讯作者Wang, Jiaying(wangjy@njucm.edu.cn) ; Hu, Lihong(lhhu@njucm.edu.cn)
英文摘要A series of vincamine derivatives were designed, synthesized and evaluated as pancreatic beta-cells protective agents for type 2 diabetes mellitus. Most of the compounds displayed potent pancreatic beta-cells protective activities and five derivatives were found to exhibit 20-50-fold higher activities than vincamine. Especially for compounds Vin-C01 and Vin-F03, exhibited a remarkable EC50 value of 0.22 mu NI and 0.27 mu M, respectively. Their pancreatic beta-cells protective activities increased approximately 2 times than vincamine. In cell viability assay, compounds Vin-001 and Vin-F03 could effectively promote beta-cell survival and protect beta-cells from STZ-induced apoptosis. Further cellular mechanism of action studies demonstrated that their potent protective activities were achieved by regulating IRS2/Pl3K/Akt signaling pathway. The present study evidently showed that compounds Vin-C01 and Vin-F03 were two more potent pancreatic beta-cells protective agents compared to vincamine and might serve as promising lead candidates for the treatment of type 2 diabetes mellitus. (C) 2019 Elsevier Masson SAS. All rights reserved.
WOS关键词APOPTOSIS
资助项目National Natural Science Foundation of China[81773596] ; Natural Science Foundation of Jiangsu Province[BK20180826] ; Natural science foundation of Jiangsu Higher Education Institutions[17KJA360004] ; Natural science foundation of Jiangsu Higher Education Institutions[18KJB350008] ; Program for Outstanding Scientific and Technological Innovation Team of Jiangsu Higher Education Institutions ; Priority Academic Program Development of Jiangsu Higher Education Institutions
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000515428100018
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/281464]  
专题新药研究国家重点实验室
通讯作者Wang, Jiaying; Hu, Lihong
作者单位1.Nanjing Univ Chinese Med, Stake Key Lab Cultivat Base TCM Qual & Efficacy, Jiangsu Collaborat Innovat Ctr Chinese Med Resour, Jiangsu Key Lab Funct Subst Chinese Med,Sch Pharm, Nanjing 210023, 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, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Junwei,Lv, Xue,Xu, Jiawen,et al. Design, synthesis and biological evaluation of vincamine derivatives as potential pancreatic beta-cells protective agents for the treatment of type 2 diabetes mellitus[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2020,188:17.
APA Wang, Junwei.,Lv, Xue.,Xu, Jiawen.,Liu, Xinpeng.,Du, Te.,...&Hu, Lihong.(2020).Design, synthesis and biological evaluation of vincamine derivatives as potential pancreatic beta-cells protective agents for the treatment of type 2 diabetes mellitus.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,188,17.
MLA Wang, Junwei,et al."Design, synthesis and biological evaluation of vincamine derivatives as potential pancreatic beta-cells protective agents for the treatment of type 2 diabetes mellitus".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 188(2020):17.

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来源：上海药物研究所

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