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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Structures and biological activities of novel 4 '-acetylated analogs of chrysomycins A and B
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Structures and biological activities of novel 4 '-acetylated analogs of chrysomycins A and B

机译：新型4'-乙酰化蛹A和B的乙酰化类似物的结构和生物学活性

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摘要

Two new 4'-acetylated analogs of chrysomycin were discovered during the screening for antitumor agents from the metabolites of actinomycetes. Their structures and physicochemical properties were determined by standard spectrometric analyses. Their cytotoxicities and antimicrobial activities were evaluated against a panel of cancer cell lines and microbes. While acetylation reinforced the cytotoxicity of chrysomycin B, it weakened the activity of chrysomycin A. Chrysomycin A and its acetylated analog showed high cytotoxicity toward most of the cancer cells with IC(50)s less than 10 ng ml(-1). The 4'-acetyl-chrysomycin A was predominantly observed in nuclei at concentrations where the autofluorescence was observable. Chrysomycins were effective toward Gram-positive bacteria. The 4'-acetylated-chrysomycin A and B had MICs of 0.5-2 mu g ml(-1) and 2 to greater than 64 mu g ml(-1), respectively, toward Gram-positive bacteria including MRSA and VRE.
机译：在筛选抗肿瘤剂的抗肿瘤来自放线菌的抗肿瘤剂期间发现了两种新的4'-乙酰化类似物。 它们的结构和物理化学性质通过标准光谱分析确定。 他们对癌细胞系和微生物面板评估了它们的细胞毒性和抗微生物活性。 虽然乙酰化增强了蛹B的细胞毒性，但它削弱了蛹A的活性。蛹A及其乙酰化类似物向大多数癌细胞显示出高细胞毒性，IC（50）S小于10ng（-1）。 在可观察到自发荧光的浓度下，在核中主要观察到4'-乙酰基 - 糠霉素A. 蛹对革兰氏阳性细菌有效。 4'-乙酰化 - 蛹A和B分别具有0.5-2μgml（-1）和2至大于64μgml（-1）的麦克风，朝向包括MRSA和VE的革兰氏阳性细菌。

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