Proansamycin B derivatives from the post-PKS modification gene deletion mutant of Amycolatopsis mediterranei S699

IF 2.1 4区医学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY

Journal of Antibiotics Pub Date : 2024-02-26 DOI:10.1038/s41429-024-00708-4

Xinyu Ma, Feng Ye, Xiaochun Zhang, Zhan Li, Yanjiao Ding, Chunhua Lu, Yuemao Shen

引用次数: 0

Abstract

Ten new proansamycin B congeners (1–10) together with one known (11) were isolated and characterized on the basis of 1D and 2D NMR spectroscopic and HRESIMS data from the Amycolatopsis mediterranei S699 ΔPM::rifR+rif-orf19 mutant. Compounds 8 and 9 featured with six-membered ring and five-membered ring hemiketal, respectively. Compounds 1, 2, and 9 displayed antibacterial activity against MRSA (methicillin-resistant Staphylococcus aureus), with the MIC (minimal inhibitory concentration) values of 64, 8, and 128 µg/mL, respectively. Compound 1 showed significant cytotoxicity against MDA-MB-231, HepG2 and Panc-1 cell lines with IC50 (half maximal inhibitory concentration) values of 2.3 ± 0.2, 2.5 ± 0.3 and 3.8 ± 0.5 μM, respectively.

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Amycolatopsis mediterranei S699 的后 PKS 修饰基因缺失突变体产生的原安塞霉素 B 衍生物。

根据来自Amycolatopsis mediterranei S699 ΔPM::rifR+rif-orf19突变体的一维和二维核磁共振光谱及HRESIMS数据，分离并鉴定了10个新的原安山霉素B同系物（1-10）和一个已知的同系物（11）。化合物 8 和 9 分别具有六元环和五元环 hemiketal 特征。化合物 1、2 和 9 对 MRSA（耐甲氧西林金黄色葡萄球菌）具有抗菌活性，其 MIC（最小抑菌浓度）值分别为 64、8 和 128 µg/mL。化合物 1 对 MDA-MB-231、HepG2 和 Panc-1 细胞株具有明显的细胞毒性，其 IC50（半最大抑制浓度）值分别为 2.3 ± 0.2、2.5 ± 0.3 和 3.8 ± 0.5 μM。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Antibiotics 医学-免疫学

CiteScore

6.60

自引率

3.00%

发文量

审稿时长

1 months

期刊介绍： The Journal of Antibiotics seeks to promote research on antibiotics and related types of biologically active substances and publishes Articles, Review Articles, Brief Communication, Correspondence and other specially commissioned reports. The Journal of Antibiotics accepts papers on biochemical, chemical, microbiological and pharmacological studies. However, studies regarding human therapy do not fall under the journal’s scope. Contributions regarding recently discovered antibiotics and biologically active microbial products are particularly encouraged. Topics of particular interest within the journal''s scope include, but are not limited to, those listed below: Discovery of new antibiotics and related types of biologically active substances Production, isolation, characterization, structural elucidation, chemical synthesis and derivatization, biological activities, mechanisms of action, and structure-activity relationships of antibiotics and related types of biologically active substances Biosynthesis, bioconversion, taxonomy and genetic studies on producing microorganisms, as well as improvement of production of antibiotics and related types of biologically active substances Novel physical, chemical, biochemical, microbiological or pharmacological methods for detection, assay, determination, structural elucidation and evaluation of antibiotics and related types of biologically active substances Newly found properties, mechanisms of action and resistance-development of antibiotics and related types of biologically active substances.