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海洋来源真菌 S-48 中具有明显胆固醇吸收抑制活性的萘并-γ-吡喃酮(NPs)。

Naphtho-Gamma-Pyrones (NPs) with Obvious Cholesterol Absorption Inhibitory Activity from the Marine-Derived Fungus S-48.

机构信息

Department of Natural Medicinal Chemistry and Pharmacognosy, School of Pharmacy, Qingdao University, Qingdao 266021, China.

Key Laboratory of Chemical Biology of Ministry of Education, Department of Natural Product Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.

出版信息

Molecules. 2022 Apr 13;27(8):2514. doi: 10.3390/molecules27082514.

Abstract

Eight naphtho-gamma-pyrones (NPs) (-), together with four known biosynthetically related coumarin derivatives (-), were isolated from the potato dextrose agar media of a marine-derived fungus S-48. Among them, natural compounds and were tentatively subjected to benzohydrazide reaction to evaluate the importance of pyran rings in NPs. Their structures were elucidated by extensive 1D and 2D NMR spectroscopic data and MS spectra. Compounds - showed obvious activity for reducing cholesterol absorption verging on ezetimibe. This work highlighted the potential of natural NPs as NPC1L1 inhibitors.

摘要

从一株海洋来源真菌 S-48 的马铃薯葡萄糖琼脂培养基中分离得到了 8 个萘并-γ-吡喃酮(NPs)(-)和 4 个已知的生物合成相关的香豆素衍生物(-)。其中,天然化合物(-)被初步进行苯甲酰肼反应,以评估 NPs 中吡喃环的重要性。通过广泛的 1D 和 2D NMR 光谱数据和 MS 谱确定了它们的结构。化合物(-)表现出明显的降低胆固醇吸收的活性,接近于依泽替米贝。这项工作突出了天然 NPs 作为 NPC1L1 抑制剂的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/91aa/9029069/09d552d3feea/molecules-27-02514-g001.jpg

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