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海洋来源真菌 sp. 的 Sortase A 抑制代谢产物

Sortase A-Inhibitory Metabolites from a Marine-Derived Fungus sp.

机构信息

Natural Products Research Institute, College of Pharmacy, Seoul National University, Seoul 08826, Korea.

Department of Agricultural Biotechnology, College of Agriculture and Life Sciences, Seoul National University, Seoul 08826, Korea.

出版信息

Mar Drugs. 2020 Jul 13;18(7):359. doi: 10.3390/md18070359.

Abstract

Seven alkaloidal compounds (-) and one polyketide () were isolated from a semisolid rice culture of the marine-derived fungus sp. F452. Structures of the isolated compounds were elucidated based on spectroscopic data and comparisons with previously reported data. The alkaloidal compounds (-) displayed weak to moderate inhibitory activities against -derived sortase A (SrtA) without affecting cell viability. Aspermytin A () strongly inhibited SrtA activity, with an IC value of 146.0 μM, and significantly reduced bacterial adherence to fibronectin-coated surfaces. The present results indicate that the underlying mechanism of action of compound is associated with the inhibition of SrtA-mediated . adhesion to fibronectin, thus potentially serving as an SrtA inhibitor.

摘要

从海洋来源真菌 sp. F452 的半固态大米培养物中分离得到 7 种生物碱化合物(-)和 1 种聚酮化合物()。基于光谱数据和与先前报道数据的比较,确定了分离化合物的结构。生物碱化合物(-)对 - 衍生的 sortase A(SrtA)显示出弱至中等的抑制活性,而不影响细胞活力。Aspermytin A()强烈抑制 SrtA 活性,IC 值为 146.0 μM,并显著减少细菌对纤维连接蛋白涂层表面的黏附。这些结果表明,化合物的作用机制与抑制 SrtA 介导的黏附有关,因此可能作为 SrtA 抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba50/7401278/f6dbdc7a4ee8/marinedrugs-18-00359-g001.jpg

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