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Isolation and properties of cytotoxic polyene antibiotics produced by Myxococcus stipitatus JW117

机译:粘球菌JW117产生的细胞毒性多烯抗生素的分离及性质

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Drug resistance is one of the most significant impediments to successful chemotherapy of cancer. Multidrug-resistance (MDR) is characterized by decreased cellular sensitivity to anticancer agents due to the overexpression of P-glycoprotein. By employing adriamycin-resistance CL02 cancer cells, we undertook the screening for agents which were effective to multidrug-resistant cancer cells. As a result, a myxobacterial strain JW117 was selected for study since the solvent extract of cell mass of the Strain was found to exhibit significant activity against the CL02 cancer cells. Cytotoxicity-guided chromatographic fractionation led to the isolation of phenalamides A_1, A_2 and A_3. The producing organism was identified as Myxococcus stipitatus by taxonomic comparison with type strains of Myxococcus sp. as well as its morphological and physiological characteristics. Phenalamides A_1, A_2 and A_3 were as active against drug-resistant cancer cells CL02 and CP70 as against the corresponding sensitive cells with IC_(50) values ranging from 0.23-0.57 #mu#g/ml.
机译:耐药性是成功进行癌症化学疗法的最重要障碍之一。多药耐药性(MDR)的特征在于,由于P-糖蛋白的过度表达,导致细胞对抗癌药的敏感性降低。通过采用抗阿霉素的CL02癌细胞,我们筛选了对多药耐药癌细胞有效的药物。结果,选择了粘细菌菌株JW117进行研究,因为发现该菌株细胞团的溶剂提取物表现出对CL02癌细胞的显着活性。细胞毒性引导的色谱分离导致苯乙酰胺A_1,A_2和A_3的分离。通过与Myxococcus sp。的类型菌株的分类学比较,将生产生物鉴定为S. sixitatus。以及它的形态和生理特征。酚酰胺A_1,A_2和A_3对耐药癌细胞CL02和CP70的活性与对相应敏感细胞的活性相同,IC_(50)值为0.23-0.57#mu#g / ml。

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