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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：在从放线菌代谢产物中筛选抗肿瘤药物的过程中，发现了两种新的4'-乙酰化金霉素类似物。通过标准光谱分析确定了它们的结构和物理化学性质。针对一组癌细胞系和微生物评估了它们的细胞毒性和抗菌活性。乙酰化增强了金霉素B的细胞毒性，但削弱了金霉素A的活性。金霉素A及其乙酰化类似物对大多数IC（50）s小于10 ng ml（-1）的癌细胞显示出较高的细胞毒性。4'-乙酰基金霉素A主要在可观察到自发荧光的浓度下的细胞核中观察到。金霉素对革兰氏阳性菌有效。4'-乙酰化金霉素A和B对包括MRSA和VRE在内的革兰氏阳性细菌的MIC分别为0.5-2μg ml（-1）和2-64μg ml（-1）。

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