Naphtho-Gamma-Pyrones (NγPs) with Obvious Cholesterol Absorption Inhibitory Activity from the Marine-Derived Fungus Aspergillus niger S-48 |
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Authors: | Chang-Zheng Wu Xiao-Ping Peng Gang Li Qi Wang Hong-Xiang Lou |
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Institution: | 1.Department of Natural Medicinal Chemistry and Pharmacognosy, School of Pharmacy, Qingdao University, Qingdao 266021, China; (C.-Z.W.); (X.-P.P.); (G.L.); (Q.W.);2.Key Laboratory of Chemical Biology of Ministry of Education, Department of Natural Product Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China |
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Abstract: | Eight naphtho-gamma-pyrones (NγPs) (1–8), together with four known biosynthetically related coumarin derivatives (9–12), were isolated from the potato dextrose agar media of a marine-derived fungus Aspergillus niger S-48. Among them, natural compounds 1 and 2 were tentatively subjected to benzohydrazide reaction to evaluate the importance of pyran rings in NγPs. Their structures were elucidated by extensive 1D and 2D NMR spectroscopic data and MS spectra. Compounds 1–4 showed obvious activity for reducing cholesterol absorption verging on ezetimibe. This work highlighted the potential of natural NγPs as NPC1L1 inhibitors. |
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Keywords: | Aspergillus niger natural products naphtho-gamma-pyrones (Nγ Ps) Niemann-Pick C1-Like 1 cholesterol |
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