| 论文题目: | A novel class of alpha-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A(y) mice |
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| 作者: | Wang Kai , Bao Li , Ma Ke , Zhang Jinjin , Chen Baosong , Han Junjie , Ren Jinwei , Luo Huajun , and Liu Hongwei*. |
| 联系作者: | |
| 刊物名称: | European Journal of Medicinal Chemistry |
| 期: | |
| 卷: | 127 |
| 页: | 1035-1046 |
| 年份: | 2017 |
| 影响因子: | 3.982 |
| 论文下载: | 下载地址 |
| 摘要: | Three new meroterpenoids, ganoleucin A-C (1-3), together with five known meroterpenoids (4-8), were isolated from the fruiting bodies of Ganoderma leucocontextum. The structures of the new compounds were elucidated by extensive spectroscopic analysis, circular dichroism (CD) spectroscopy, and chemical transformation. The inhibitory effects of 1-8 on HMG-CoA reductase and a-glucosidase were tested in vitro. Ganomycin I (4), 5, and 8 showed stronger inhibitory activity against HMG-CoA reductase than the positive control atorvastatin. Compounds 1, and 3-8 presented potent noncompetitive inhibitory activity against alpha-glucosidase from both yeast and rat small intestinal mucosa. Ganomycin 1(4), the most potent inhibitor against both a-glucosidase and HMG-CoA reductase, was synthesized and evaluated for its in vivo bioactivity. Pharmacological results showed that ganomycin I (4) exerted potent and efficacious hypoglycemic, hypolipidemic, and insulin-sensitizing effects in KK-A(y) mice. (C) 2016 Elsevier Masson SAS. All rights reserved. |
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