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Dimeric styrylpyrones with stimulating GLP-1 secretion activities from Alpinia kwangsiensis

文献类型：期刊论文

作者Wu, Meng-Zhen3,5; GongPan, Pian-Chou4; Dai, Meng -Yuan2; Sun, Peng4; Xiao, Chun-Fen4; Li, Jia1,3,5; Sun, Yi-Li1,3; Ji, Kai-Long4
刊名TETRAHEDRON
出版日期2022-08-13
卷号120页码:7
ISSN号0040-4020
关键词Glucagon-like peptide-1 Type 2 diabetes Alpinia kwangsiensis Dimeric styrylpyrones
DOI10.1016/j.tet.2022.132901
通讯作者Sun, Yi-Li(yilisun@simm.ac.cn) ; Ji, Kai-Long(kl14ji@163.com)
英文摘要Stimulating glucagon-like peptide-1 (GLP-1) secretion is an important approach for the treatment of type 2 diabetes. Chemical investigation of Alpinia kwangsiensis rhizomes produced six dimeric styrylpyrones (1-6), including two new degraded ones (1 and 2). Compounds 1-4 were identified as four pairs of enantiomers and successfully prepared by chiral HPLC separation. These compounds incorporate the distinctive cyclobutane moiety via [2 + 2] cycloaddition, a key step in the biosynthetic pathway. The bioactivities of isolates in stimulating GLP-1 secretion in STC-1 cells were evaluated. Results showed that compounds (+)-1, (+)-2, (-)-2, (-)-4, 5 and 6 significantly increased GLP-1 secretion, and compound (+)-1 exhibited the strongest activity with EC50 value of 6.51 mM. In addition, compounds (+)-2, (-)-4 and 5 promoted GLP-1 secretion by increasing intracellular calcium concentration dependent on the PKA pathway, which could provide a chemical basis for the development of diabetes drugs especially that directly promote GLP-1 secretion.
WOS关键词GLUCAGON-LIKE PEPTIDE-1
资助项目Yunnan Fundamental Research Projects[202101AU070148] ; Yunnan Fundamental Research Projects[202101AT070055] ; National Natural Science Foundation of China[81903682] ; National Natural Science Foundation of China[82104268] ; Shanghai Science and Technology Committee[19YF1410200] ; Shanghai Municipal Science and Technology Major Project[TM202101H001] ; Lingang Laboratory[LG202103-03-04]
WOS研究方向Chemistry
语种英语
出版者PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号WOS:000877768600015
源URL[http://119.78.100.183/handle/2S10ELR8/302891]  
专题新药研究国家重点实验室
通讯作者Sun, Yi-Li; Ji, Kai-Long
作者单位1.Bohai Rim Adv Res Inst Drug Discovery, Yantai 264000, Shandong, Peoples R China
2.Yunnan Acad Agr Sci, Ind Crop Res Inst, Kunming 650223, Yunnan, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China
4.Chinese Acad Sci, CAS Key Lab Trop Plant Resources & Sustainable Use, Xishuangbanna Trop Bot Garden, 88 Xuefu Rd, Kunming 650223, Yunnan, Peoples R China
5.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Jiangsu, Peoples R China
推荐引用方式
GB/T 7714		 Wu, Meng-Zhen,GongPan, Pian-Chou,Dai, Meng -Yuan,et al. Dimeric styrylpyrones with stimulating GLP-1 secretion activities from Alpinia kwangsiensis[J]. TETRAHEDRON,2022,120:7.
APA Wu, Meng-Zhen.,GongPan, Pian-Chou.,Dai, Meng -Yuan.,Sun, Peng.,Xiao, Chun-Fen.,...&Ji, Kai-Long.(2022).Dimeric styrylpyrones with stimulating GLP-1 secretion activities from Alpinia kwangsiensis.TETRAHEDRON,120,7.
MLA Wu, Meng-Zhen,et al."Dimeric styrylpyrones with stimulating GLP-1 secretion activities from Alpinia kwangsiensis".TETRAHEDRON 120(2022):7.

入库方式： OAI收割

来源：上海药物研究所

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