地中海拟无枝酸菌 S699 的聚酮化合物后修饰基因缺失突变株来源的普罗卡酰胺 B 衍生物。
Proansamycin B derivatives from the post-PKS modification gene deletion mutant of Amycolatopsis mediterranei S699.
机构信息
Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong, 250012, China.
Department of Pharmacy, Shandong Second Provincial General Hospital, Jinan, Shandong, 250022, China.
出版信息
J Antibiot (Tokyo). 2024 May;77(5):278-287. doi: 10.1038/s41429-024-00708-4. Epub 2024 Feb 26.
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 IC (half maximal inhibitory concentration) values of 2.3 ± 0.2, 2.5 ± 0.3 and 3.8 ± 0.5 μM, respectively.
从地中海链霉菌 S699ΔPM::rifR+rif-orf19 突变株中，基于 1D 和 2D NMR 光谱和 HRESIMS 数据，分离并鉴定了 10 个新的普罗沙姆霉素 B 同系物（1-10）和 1 个已知化合物（11）。化合物 8 和 9 分别具有六元环和五元环半缩酮。化合物 1、2 和 9 对 MRSA（耐甲氧西林金黄色葡萄球菌）表现出抗菌活性，MIC（最小抑菌浓度）值分别为 64、8 和 128μg/mL。化合物 1 对 MDA-MB-231、HepG2 和 Panc-1 细胞系表现出显著的细胞毒性，IC（半最大抑制浓度）值分别为 2.3±0.2、2.5±0.3 和 3.8±0.5μM。
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