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Vochysiamides A 和 B:新种大茎点霉产生的两种具有生物活性的新型羧酰胺。

Vochysiamides A and B: Two new bioactive carboxamides produced by the new species Diaporthe vochysiae.

机构信息

Department of Pathology, Universidade Federal do Parana, Av. Coronel Francisco Heráclito dos Santos, 210, CEP: 81531-970 Curitiba, PR, Brazil.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, United States; Department of Genetics, Universidade Federal do Parana, Av. Coronel Francisco Heráclito dos Santos, 210, CEP: 81531-970 Curitiba, PR, Brazil.

出版信息

Fitoterapia. 2019 Oct;138:104273. doi: 10.1016/j.fitote.2019.104273. Epub 2019 Jul 22.

DOI:10.1016/j.fitote.2019.104273
PMID:31344395
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7015639/
Abstract

Endophytic fungi have been considered a rich source for bioactive secondary metabolites with novel chemical structures. A high diverse group of endophytes, isolated from different medicinal plants, belongs to the genus Diaporthe. In a previously study performed by our group the crude extract of strain LGMF1583 showed considerable antibacterial activity mainly against Gram-negative bacteria. Based on ITS phylogeny analysis, strain LGMF1583 was identified as belonging to Diaporthe genus and may represent a new species. In the present study, we described the new species Diporthe vochysiae based on multilocus phylogeny analysis and morphological characteristics. The species name refers to the host, from which strain LGMF1583 was isolated, the medicinal plant Vochysia divergens. In view of the biotechnological potential of strain LGMF1583, we have also characterized the secondary metabolites produced by D. vochysiae. Chemical assessment of the D. vochysiae LGMF1583 revealed two new carboxamides, vochysiamides A (1) and B (2), in addition to the known metabolite, 2,5-dihydroxybenzyl alcohol (3). In the biological activity analysis, vochysiamide B (2) displayed considerable antibacterial activity against the Gram-negative bacterium Klebsiella pneumoniae (KPC), a producer of carbapenemases, MIC of 80 μg/mL. Carbapenemases are considered a major antimicrobial resistance threat, and infections caused by KPC have been considered a public health problem worldwide, and new compounds with activity against this bacterium are nowadays even more required.

摘要

内生真菌被认为是具有新颖化学结构的生物活性次生代谢产物的丰富来源。从不同药用植物中分离出的高度多样化的内生真菌群属于盘菌属。在我们小组之前进行的一项研究中,菌株 LGMF1583 的粗提取物表现出相当大的抗菌活性,主要针对革兰氏阴性菌。基于 ITS 系统发育分析,菌株 LGMF1583 被鉴定为属于盘菌属,可能代表一个新物种。在本研究中,我们根据多基因座系统发育分析和形态特征描述了新物种 Vochysia 盘菌。种名指的是宿主,菌株 LGMF1583 是从药用植物 Vochysia divergens 中分离出来的。鉴于菌株 LGMF1583 的生物技术潜力,我们还对 D.vochysiae 产生的次生代谢产物进行了表征。对 D.vochysiae LGMF1583 的化学评估揭示了两种新的羧酰胺,即 vochysiamide A(1)和 B(2),以及已知代谢物 2,5-二羟基苯甲醇(3)。在生物活性分析中,vochysiamide B(2)对革兰氏阴性菌肺炎克雷伯菌(KPC)表现出相当大的抗菌活性,MIC 为 80μg/mL。碳青霉烯酶被认为是主要的抗菌药物耐药威胁,由 KPC 引起的感染被认为是全球范围内的公共卫生问题,因此,现在甚至更需要具有抗这种细菌活性的新化合物。

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