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海洋来源真菌中具有 -葡萄糖苷酶抑制活性的新型二苯并-吡喃酮衍生物。

New Dibenzo--pyrone Derivatives with -Glucosidase Inhibitory Activities from the Marine-Derived Fungus .

机构信息

State Key Laboratory of Mycology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China.

University of Chinese Academy of Sciences, Beijing 100049, China.

出版信息

Mar Drugs. 2022 Dec 14;20(12):778. doi: 10.3390/md20120778.

Abstract

Three new dibenzo--pyrone derivatives, alternolides A-C (-), and seven known congeners (-) were isolated from the marine-derived fungus of LW37 assisted by the one strain-many compounds (OSMAC) strategy. The structures of - were established by extensive spectroscopic analyses, and their absolute configurations were determined by modified Snatzke's method and electronic circular dichroism (ECD) calculations. Compounds and showed good 1,1-diphenyl-2-picrylhydrazyl (DPPH) antioxidant scavenging activities with IC values of 83.94 ± 4.14 and 23.60 ± 1.23 µM, respectively. Additionally, , and exhibited inhibitory effects against -glucosidase with IC values of 725.85 ± 4.75, 451.25 ± 6.95 and 6.27 ± 0.68 µM, respectively. The enzyme kinetics study indicated and were mixed-type inhibitors of -glucosidase with values of 347.0 and 108.5 µM, respectively. Furthermore, the interactions of , and with -glucosidase were investigated by molecular docking.

摘要

从海洋来源真菌 LW37 中分离得到三种新的二苯并-吡喃酮衍生物(alternolides A-C (-))和七种已知同系物(-),通过单菌株多产物(OSMAC)策略辅助。通过广泛的光谱分析确定了-的结构,其绝对构型通过改良的 Snatzke 法和电子圆二色性(ECD)计算确定。化合物和显示出良好的 1,1-二苯基-2-苦基肼(DPPH)抗氧化清除活性,IC 值分别为 83.94 ± 4.14 和 23.60 ± 1.23 μM。此外,、和对 -葡萄糖苷酶表现出抑制作用,IC 值分别为 725.85 ± 4.75、451.25 ± 6.95 和 6.27 ± 0.68 μM。酶动力学研究表明和是 -葡萄糖苷酶的混合型抑制剂,值分别为 347.0 和 108.5 μM。此外,通过分子对接研究了、和与 -葡萄糖苷酶的相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9e92/9785194/fa20fc8afe0a/marinedrugs-20-00778-g001.jpg

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