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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Chlorinated bis-indole alkaloids from deep-sea derived Streptomyces sp. SCSIO 11791 with antibacterial and cytotoxic activities
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Chlorinated bis-indole alkaloids from deep-sea derived Streptomyces sp. SCSIO 11791 with antibacterial and cytotoxic activities

机译:来自深海衍生的链霉菌SP的氯化双吲哚生物碱。 SCSIO 11791具有抗菌和细胞毒性活动

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摘要

Two new chlorinated bis-indole alkaloids, dionemycin (1) and 6-OMe-7 ',7 ''-dichorochromopyrrolic acid (2), along with seven known analogs 3-9, were isolated from the deep-sea derived Streptomyces sp. SCSIO 11791. Their structures were elucidated by extensive HRESIMS, and 1D and 2D NMR data analysis. In vitro antibacterial and cytotoxic assays revealed that, compound 1, shows anti-staphylococcal activity with an MIC range of 1-2 mu g/mL against six clinic strains of methicillin-resistant Staphylococcus aureus (MRSA) isolated from human and pig. Additionally, compound 1 displayed cytotoxic activity against human cancer cell lines NCI-H460, MDA-MB-231, HCT-116, HepG2, and noncancerous MCF10A with an IC50 range of 3.1-11.2 mu M. Analysis of the structure-activity relationship reveals that the chlorine atom at C-6 '' could be pivotal for conferring their bioactivities, thus providing hints on chemical modifications on bis-indole alkaloid scaffold in drug design.
机译:两种新的氯化双吲哚生物碱,二硫嘧啶(1)和6-OME-7',7' - 二巯基吡咯酸(2)以及七种已知的类似物3-9,从深海衍生的链霉菌SP中分离出来。 SCSIO 11791。通过广泛的Hresims和1D和2D NMR数据分析阐明了它们的结构。 体外抗菌和细胞毒性测定显示,化合物1显示抗葡葡萄球菌活性,其麦克风范围为1-2μg/ ml,其六个临床型甲氧西林耐金黄色葡萄球菌(MRSA)中分离出来的人和猪。 另外,化合物1针对人癌细胞系NCI-H460,MDA-MB-231,HCT-116,HepG2和非癌变的MCF10A显示了细胞毒性活性,IC50范围为3.1-11.2μm。结构 - 活动关系的分析显示 C-6''的氯原子可以是赋予其生物活性的枢转,从而为药物设计中的双吲哚生物碱支架上的化学修饰提供了暗示。

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    Chinese Acad Sci RNAM Ctr Marine Microbiol South China Sea Inst Oceanol CAS Key Lab Trop Marine;

    Chinese Acad Sci RNAM Ctr Marine Microbiol South China Sea Inst Oceanol CAS Key Lab Trop Marine;

    Sun Yat Sen Univ Key Lab Trop Dis Control Minist Educ Guangzhou 510080 Peoples R China;

    Chinese Acad Sci RNAM Ctr Marine Microbiol South China Sea Inst Oceanol CAS Key Lab Trop Marine;

    Sun Yat Sen Univ Key Lab Trop Dis Control Minist Educ Guangzhou 510080 Peoples R China;

    Southern Univ Sci &

    Technol Hosp 2 Peoples Hosp Shenzhen 3 Natl Clin Res Ctr Infect Dis;

    Chinese Acad Sci RNAM Ctr Marine Microbiol South China Sea Inst Oceanol CAS Key Lab Trop Marine;

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  • 正文语种 eng
  • 中图分类 药学;
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