Synthesis and glucose-stimulate insulin secretion (GSIS) evaluation of vindoline derivatives |
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| Authors: | Chengqian Xiao Yunan Tian Min Lei Fanglei Chen Xianwen Gan Xingang Yao Xu Shen Jing Chen Lihong Hu |
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| Institution: | 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 |
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| Abstract: | It is demonstrated that natural product vindoline can enhance the glucose-stimulated insulin secretion (GSIS) in MIN6 cells with the EC50 value of 50.2 μM. 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 12.7 μM, respectively) than vindoline. |
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| Keywords: | Vindoline Natural product Glucose-stimulate insulin secretion (GSIS) Structure–activity relationships (SARs) |
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