Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 127, Issue -, Pages 1035-1046Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.11.015
Keywords
Ganoderma leucocontextum; Meroterpenes; HMG-CoA reductase inhibition; alpha-Glucosidase inhibition; Anti-diabetic activities
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Funding
- National Nature Science Foundation [21472233]
- Ministry of Science and Technology of China [2014CB138304]
- Youth Innovation Promotion Association of Chinese Academy of Sciences [2014074]
- Open Fund of Hubei Key Laboratory of Natural Products Research and Development [2016NP09]
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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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