Synthesis and glucose-stimulate insulin secretion (GSIS) evaluation of vindoline derivatives

Bioorg Med Chem Lett. 2017 Mar 1;27(5):1316-1318. doi: 10.1016/j.bmcl.2016.09.064.

Chengqian Xiao ¹, Yunan Tian ², Min Lei ³, Fanglei Chen ¹, Xianwen Gan ¹, Xingang Yao ², Xu Shen ², Jing Chen ⁴, Lihong Hu ⁵

Affiliations

1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai, PR China.
2 CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai, PR China.
3 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai, PR China. Electronic address: mlei@simm.ac.cn.
4 CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai, PR China. Electronic address: jingchen@simm.ac.cn.
5 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai, PR China. Electronic address: lhhu@simm.ac.cn.

PMID: 28162858 DOI: 10.1016/j.bmcl.2016.09.064

Abstract

It is demonstrated that natural product vindoline can enhance the glucose-stimulated Insulin secretion (GSIS) in MIN6 cells with the EC₅₀ value of 50.2μM. In order to improve the activities, a series of vindoline derivatives are synthesized and evaluated in MIN6 cells. Compounds 4, 8, 17 and 24 show about 4.5 times more effective stimulation Insulin secretion ability (EC₅₀: 10.4, 14.2, 11.0 and 12.7μM, respectively) than vindoline.

Keywords

Glucose-stimulate insulin secretion (GSIS); Natural product; Structure–activity relationships (SARs); Vindoline.

Name
Email *

	Sorry, but the email address you supplied was invalid.