首页> 外文期刊>Journal of natural products >Production of 8-Demethylgeldanamycin and 4,5-Epoxy-8-demethylgeldanamycin from a Recombinant Strain of Streptomyces hygroscopicus.
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Production of 8-Demethylgeldanamycin and 4,5-Epoxy-8-demethylgeldanamycin from a Recombinant Strain of Streptomyces hygroscopicus.

机译:从吸水链霉菌的重组菌株生产8-去甲基格尔德霉素和4,5-环氧-8-去甲基格尔德霉素。

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摘要

Two new geldanamycin derivatives produced by genetic engineering of Streptomyces hygroscopicus strain K309-27-1 were isolated and characterized. Removal of the 8-methyl group of geldanamycin was achieved by replacing the AT4 domain of the polyketide synthase with a malonyl AT domain. The resulting strain produced 8-demethyl geldanamycin (2) and 4,5-epoxy-8-demethylgeldanamycin (3). The structures of both molecules were elucidated through interpretation of 1D and 2D NMR data as well as comparison with authentic geldanamycin derivatives. Compounds 2 and 3 displayed moderate cytotoxicity against the human breast cancer cell line SK-BR-3.
机译:分离并鉴定了由吸水链霉菌菌株K309-27-1的基因工程产生的两种新的格尔德霉素衍生物。通过用丙二酰基AT结构域代替聚酮化合物合酶的AT4结构域来实现格尔德霉素的8-甲基的去除。所得菌株产生8-去甲基格尔德霉素(2)和4,5-环氧-8-去甲基格尔德霉素(3)。通过解释1D和2D NMR数据以及与真实的格尔德霉素衍生物进行比较,阐明了两种分子的结构。化合物2和3显示出对人乳腺癌细胞系SK-BR-3的中等细胞毒性。

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