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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >The isolation of tetrangomycin from terrestrial Streptomyces sp CAH29: evaluation of antioxidant, anticancer, and anti-MRSA activity
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The isolation of tetrangomycin from terrestrial Streptomyces sp CAH29: evaluation of antioxidant, anticancer, and anti-MRSA activity

机译:从地面链霉菌CAH29中分离出丁霉素:评估抗氧化剂,抗癌和抗MRSA活性

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摘要

A rhizosphere isolate Streptomyces sp. CAH29 was found to possess potent antibacterial and antifungal activity against a variety of test organisms. Based on 16S ribosomal ribonucleic acid sequence homology studies, this strain was found to be similar to Streptomyces stramineus (gene sequence similarity 99 %). The major bioactive metabolite produced by Streptomyces sp. CAH29 isolate was extracted, purified andidentified by nuclear magnetic resonance as tetrangomycin. This known anthraquinone-exhibited antimicrobial activity against Staphylococcus aureus, Streptococcus pyogenes, methicillin resistant Staphylococcus aureus and Candida albicans with inhibition zones of 14, 10, 12 and 8 mm, respectively. Docking results demonstrate that tetrangomycin has a similar mode of action and a comparable docking score to bind to the dehydrosqualene synthase (CrtM) enzyme of methicillin resistant Staphylococcus aureus compared to the current inhibitor. Hence, this suggests that tetrangomycin has a potential to be used as an anti-methicillin resistant Staphylococcus aureus agent. Tetrangomycin also showed moderate free radical scavenging activity with 1,1-diphenyl-2-picryl-hydrazil. Tetrangomycin apparently decreased all of the studied cytokine (pro-inflammatory: interleukin 1B, interleukin 2, tumor necrosis factor and interleukin L6 and anti-inflammatory: interleukin 10) expression levels at IC50 concentrations in A459 (adenocarcinomic human alveolar basal epithelial) and LNCAP (human prostate adenocarcinoma) cell lines. In addition, it reduced Caspase 8 and 3 mRNA levels in LNCAP and A549 cells. This study describes for the first time novel in vitro immunosuppressive function of tetrangomycin by reducing the transcription of cytokine genes.
机译:根际分离链霉菌。发现CAH29具有针对多种测试生物的有效抗菌和抗真菌活性。根据16S核糖体核糖核酸序列同源性研究,发现该菌株与Streptomyces stramineus相似(基因序列相似性为99%)。链霉菌产生的主要生物活性代谢物。提取,纯化并通过核磁共振法鉴定CAH29分离物为丁霉素。这种已知的蒽醌对金黄色葡萄球菌,化脓性链球菌,耐甲氧西林的金黄色葡萄球菌和白色念珠菌的抗菌活性分别为14、10、12和8 mm。对接结果表明,与目前的抑制剂相比,丁霉素具有相似的作用方式和相当的对接分数,可与耐甲氧西林的金黄色葡萄球菌的脱氢角鲨烯合酶(CrtM)酶结合。因此,这表明丁霉素具有用作抗甲氧西林的金黄色葡萄球菌剂的潜力。土霉素还显示出对1,1-二苯基-2-吡咯-肼具有适度的自由基清除活性。在A459(腺癌人类肺泡基底上皮)和LNCAP(A459)中,IC50浓度下,四环霉素明显降低了所有研究的细胞因子(促炎:白介素1B,白介素2,肿瘤坏死因子和白介素L6和抗炎:白介素10)表达水平。人前列腺腺癌)细胞系。此外,它降低了LNCAP和A549细胞中的Caspase 8和3 mRNA水平。这项研究首次通过减少细胞因子基因的转录描述了丁霉素的新型体外免疫抑制功能。

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