A southern Australian soil isolate, Amycolatopsis sp. MST-108494, was subjected to a panel of fermentation and media optimization trials, supported by analytical chemical profiling, to detect and enhance production of a rare class of secondary metabolites. Chemical fractionation of two complementary fermentations yielded three new polyketides, identified by detailed spectroscopic analysis as the glycosylated macrolactones, amycolatopsins A (1), B (2) and C (3), closely related to the ammocidins and apoptolidins. Amycolatopsins 1 and 3 selectively inhibited growth of Mycobacterium bovis (BCG) and Mycobacterium tuberculosis (H37Rv) when compared with other Gram-positive or Gram-negative bacteria, with 3 exhibiting low levels of cytotoxicity toward mammalian cells. Thus, our data reveal promising structure activity relationship correlations where the antimycobacterial properties of amycolatopsins are enhanced by hydroxylation of the 6-Me (that is, 1 and 3), whereas mammalian cytotoxicity is decreased by hydrolysis of the disaccharide moiety (that is, 3).

中文翻译：

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Amycolatopsins AC：来自澳大利亚土壤Amycolatopsis sp。的抗分枝杆菌糖基化聚酮大环内酯类。MST-108494。

澳大利亚南部的土壤分离株，Amycolatopsis sp.。对MST-108494进行了一系列发酵和培养基优化试验，并通过分析化学分析进行了分析，以检测和增强稀有类次生代谢产物的产生。两种互补发酵的化学分级分离产生了三种新的聚酮化合物，通过详细的光谱分析鉴定为糖基化大内酯，即淀粉酶类蛋白A（1），B（2）和C（3），与氨苄青霉素和细胞凋亡素密切相关。与其他革兰氏阳性或革兰氏阴性细菌相比，支链淀粉酶1和3选择性抑制牛分枝杆菌（BCG）和结核分枝杆菌（H37Rv）的生长，其中3种对哺乳动物细胞的毒性低。因此，