Synthesis and glucose-stimulate insulin secretion (GSIS) evaluation of vindoline derivatives
| Autor: | Xin-gang Yao, Min Lei, Fanglei Chen, Chengqian Xiao, Xianwen Gan, Yunan Tian, Lihong Hu, Jing Chen, Xu Shen |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
endocrine system
Clinical Biochemistry Pharmaceutical Science 030209 endocrinology & metabolism Stimulation Vinblastine 01 natural sciences Biochemistry Cell Line 03 medical and health sciences chemistry.chemical_compound Inhibitory Concentration 50 Mice 0302 clinical medicine Insulin-Secreting Cells Drug Discovery Insulin Secretion Animals Hypoglycemic Agents Insulin Insulin secretion Molecular Biology Natural product Molecular Structure 010405 organic chemistry Organic Chemistry 0104 chemical sciences Glucose chemistry Molecular Medicine Vindoline |
| Zdroj: | Bioorganicmedicinal chemistry letters. 27(5) |
| ISSN: | 1464-3405 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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