Effects of emetine on insulin secretion in rat islets through GLP-1R
- VernacularTitle:吐根碱通过GLP-1R促进大鼠胰岛组织胰岛素分泌作用的研究
- Author:
Huan XUE
1
;
Zhi-Hong LU
;
Bin WANG
;
Si-Ting YU
;
Xi ZHANG
;
Bin HU
;
Qing-Xuan ZENG
;
Yi ZHANG
Author Information
- Keywords: glucagon-like peptide-1 receptor; molecu-lar docking; type 2 diabetes mellitus; emetine; insulin secretion; small molecular compound
- From: Chinese Pharmacological Bulletin 2024;40(7):1267-1272
- CountryChina
- Language:Chinese
- Abstract: Aim To study the effect of emetine on in-sulin secretion through glucagon-like peptide-1 receptor(GLP-1R).Methods Isolating rat islets were used to carry out insulin secretion experiment.Islets were incubated with different concentrations of emetine(2,10,50 μmol·L-1),different concentrations of glu-cose solution(2.8,11.1,16.7 mmol·L-1)or spe-cific GLP-1R antagonist Exendin(9-39).The amount of insulin secretion in the supernatant of each group was determined by an enzyme-linked radioimmunoas-say.Small molecule compounds were docked to GLP-1R(PDB code:5NX2)using SYBYL-X2.0 software.Results Emetine could promote insulin secretion in high glucose(11.1 mmol·L-1)in a dose-dependent manner.In low glucose(2.8 mmol·L-1),insulin secretion did not change after intervention of emetine.But in high glucose(11.1,16.7 mmol·L-1),insu-lin secretion significantly increased under the treatment of emetine in a glucose-dependent manner.The doc-king score of emetine and GLP-1R was Total Score=6.82,C Score=5,indicating that emetine had a good binding affinity with GLP-1R.Using Exendin(9-39)to block GLP-1R,the insulinotropic effect of emetine was reduced.Conclusion Emetine could promote in-sulin secretion,which is related to the activation of GLP-1R.
