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Structures and biological activities of novel 4'-acetylated analogs of chrysomycins A and B.
The Journal of Antibiotics ( IF 3.3 ) Pub Date : 2017-Nov-01 , DOI: 10.1038/ja.2017.99
Shun-ichi Wada , Ryuichi Sawa , Fumiki Iwanami , Miho Nagayoshi , Yumiko Kubota , Kiyoko Iijima , Chigusa Hayashi , Yuko Shibuya , Masaki Hatano , Masayuki Igarashi , Manabu Kawada

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 IC50s 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 μg ml-1 and 2 to greater than 64 μg ml-1, respectively, toward Gram-positive bacteria including MRSA and VRE.

中文翻译:

金霉素A和B的新型4'-乙酰化类似物的结构和生物学活性。

在从放线菌代谢物中筛选抗肿瘤药物时,发现了两个新的霉素霉素的4'-乙酰化类似物。通过标准光谱分析确定它们的结构和理化性质。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Chrysomycin B的细胞毒性,但减弱了Chrysomycin A的活性。ChrysomycinA及其乙酰化类似物对大多数癌细胞表现出高细胞毒性,IC 50 s小于10 ng ml -1。主要在细胞核中观察到自发荧光的浓度下观察到4'-乙酰-霉素霉素A。金霉素对革兰氏阳性细菌有效。的0.5-2微克毫升4'-乙酰化chrysomycin甲乙具有的MIC -1和2至大于64微克毫升-1,分别朝向革兰氏阳性菌,包括MRSA和VRE。
更新日期:2017-09-06
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