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海洋放线菌诺卡氏菌 SCA30 来源的二酮哌嗪衍生物具有抗耐甲氧西林金黄色葡萄球菌(MRSA)的抗菌活性。

Diketopiperazine derivative from marine actinomycetes Nocardiopsis sp. SCA30 with antimicrobial activity against MRSA.

机构信息

Department of Microbiology, University of Mysore, Mysore, 570006, India.

Department of Microbiology, Faculty of Life Sciences, JSS Academy of Higher Education and Research, Mysore, 570015, India.

出版信息

Arch Microbiol. 2021 Dec;203(10):6173-6181. doi: 10.1007/s00203-021-02582-2. Epub 2021 Oct 10.

Abstract

Actinobacteria isolated from marine sources are a potential source of novel natural products. In this study, we report isolation, biological activity and characterization of secondary metabolites from strain Nocardiopsis sp. SCA30, isolated from marine sediments of Havelock Islands, Andaman and Nicobar, India. The ethyl acetate extracts of the isolate on screening for biological activity demonstrated antibacterial potency and antiproliferative activity. The extracts showed anticancer activity in a panel of cell lines, including HCT 15, HT 29, MCF 7 and MDA-MB 468, at concentrations ranging from 62.5 to 1000 µg/ml. A dose-dependent reduction in cell viability was observed in all the tested cell lines. The extract at 15 µg/ml and 30 µg/ml inhibited growth of methicillin-resistant Staphylococcus aureus ATCC NR-46071 and NR-46171 with MIC's of 15.62 and 7.81 µg/ml, respectively. LC-MS and NMR studies revealed that the antibacterial and anticancer compound isolated from Nocardiopsis sp. SCA30 is 1-acetyl-4-4(hydroxyphenyl)piperazine.

摘要

从海洋来源分离出的放线菌是新型天然产物的潜在来源。在这项研究中,我们报告了从印度安达曼和尼科巴群岛哈夫洛克群岛的海洋沉积物中分离出的枝孢菌 SCA30 次生代谢产物的分离、生物活性和特性。该分离物的乙酸乙酯提取物在筛选生物活性时表现出抗菌活力和抗增殖活性。提取物在包括 HCT 15、HT 29、MCF 7 和 MDA-MB 468 在内的一系列细胞系中显示出抗癌活性,浓度范围为 62.5 至 1000μg/ml。在所有测试的细胞系中,均观察到细胞活力呈剂量依赖性降低。在 15μg/ml 和 30μg/ml 时,提取物对耐甲氧西林金黄色葡萄球菌 ATCC NR-46071 和 NR-46171 的生长具有抑制作用,MIC 分别为 15.62 和 7.81μg/ml。LC-MS 和 NMR 研究表明,从枝孢菌 SCA30 中分离出的具有抗菌和抗癌活性的化合物是 1-乙酰基-4-4(羟基苯基)哌嗪。

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