Vincamine as a GPR40 agonist improves glucose homeostasis in type 2 diabetic mice
文献类型：期刊论文
| 作者 | Du, Te2,3; Yang, Liu2,3; Xu, Xu4; Shi, Xiaofan2,3; Xu, Xin2,3; Lu, Jian4; Lv, Jianlu4; Huang, Xi4; Chen, Jing2,3 ; Wang, Heyao2,3
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| 刊名 | JOURNAL OF ENDOCRINOLOGY
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| 出版日期 | 2019-02 |
| 卷号 | 240期号:2页码:195-214 |
| 关键词 | vincamine GPR40 beta-cell function insulin secretion type 2 diabetes |
| ISSN号 | 0022-0795 |
| DOI | 10.1530/JOE-18-0432 |
| 文献子类 | Article |
| 英文摘要 | Vincamine, a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle, is clinically used for the treatment of cardio-cerebrovascular diseases, while also treated as a dietary supplement with nootropic function. Given the neuronal protection of vincamine and the potency of beta-cell amelioration in treating type 2 diabetes mellitus (T2DM), we investigated the potential of vincamine in protecting it-cells and ameliorating glucose homeostasis in vitro and in vivo. Interestingly, we found that vincamine could protect INS-832/13 cells function by regulating G-protein-coupled receptor 40 (GPR40)/cAMP/Ca2+/IRS2/PI3K/Akt signaling pathway, while increasing glucosestimulated insulin secretion (GSIS) by modulating GPR40/cAMP/Ca2+/CaMKII pathway, which reveals a novel mechanism underlying GPR40-mediated cell protection and GSIS in INS-832/13 cells. Moreover, administration of vincamine effectively ameliorated glucose homeostasis in either HFD/STZ or db/db type 2 diabetic mice. To our knowledge, our current work might be the first report on vincamine targeting GPR40 and its potential in the treatment of T2DM. |
| WOS关键词 | PANCREATIC BETA-CELL ; PROTEIN-COUPLED RECEPTORS ; INSULIN-SECRETION ; DRUG TARGET ; IN-VITRO ; CALCIUM ; APOPTOSIS ; STREPTOZOTOCIN ; GLUCOKINASE ; INHIBITION |
| 资助项目 | National Natural Science Foundation of China[81473141] ; National Natural Science Foundation of China[81773596] ; NSFC-TRF collaboration project[NSFC81561148011] ; Key Laboratory of Receptor Research of the Chinese Academy of Sciences[SIMM1606YZZ-04] ; Priority Academic Program Development of Jiangsu Higher Education Institutions (Integration of Chinese and Western Medicine)[00000000] |
| WOS研究方向 | Endocrinology & Metabolism |
| 语种 | 英语 |
| WOS记录号 | WOS:000453043400010 |
| 出版者 | BIOSCIENTIFICA LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279456]  |
| 专题 | 药物安全性评价中心 |
| 通讯作者 | Chen, Jing; Hu, Lihong; Shen, Xu |
| 作者单位 | 1.RMIT Univ, Sch Hlth & Biomed Sci, Melbourne, Vic, Australia 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai, Peoples R China; 3.Univ Chinese Acad Sci, Sch Pharm, Beijing, Peoples R China; 4.Nanjing Univ Chinese Med, Sch Med & Life Sci, Nanjing, Jiangsu, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Du, Te,Yang, Liu,Xu, Xu,et al. Vincamine as a GPR40 agonist improves glucose homeostasis in type 2 diabetic mice[J]. JOURNAL OF ENDOCRINOLOGY,2019,240(2):195-214. |
| APA | Du, Te.,Yang, Liu.,Xu, Xu.,Shi, Xiaofan.,Xu, Xin.,...&Shen, Xu.(2019).Vincamine as a GPR40 agonist improves glucose homeostasis in type 2 diabetic mice.JOURNAL OF ENDOCRINOLOGY,240(2),195-214. |
| MLA | Du, Te,et al."Vincamine as a GPR40 agonist improves glucose homeostasis in type 2 diabetic mice".JOURNAL OF ENDOCRINOLOGY 240.2(2019):195-214. |
入库方式： OAI收割
来源：上海药物研究所
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