Spiromastixones A-O, Antibacterial Chlorodepsidones from a Deep-Sea-Derived Spiromastix sp Fungus
Spiromastixones A-O, Antibacterial Chlorodepsidones from a Deep-Sea-Derived Spiromastix sp Fungus
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DOI：
10.1021/np5000457
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发表时间：
2014-04-01
影响因子：
5.1
通讯作者：
Lin, Wenhan
中科院分区：
文献类型：
--
作者：
Niu, Siwen;Liu, Dong;Lin, Wenhan
从深海spiromastitix sp.真菌发酵液中分离到15个新的以depsidone为基础的类似物，命名为spiromastixones a - o（1-15）。它们的结构是在广泛的核磁共振和质谱分析的基础上与化学转化相关联的。根据C环相对于A环的取向将螺马替酮A- o分为两个亚型，而A环和C环上的n-丙基取代基在天然产物中很少见到。大多数类似物被不同数目的氯原子取代。所有化合物对金黄色葡萄球菌、苏云金芽孢杆菌和枯草芽孢杆菌等革兰氏阳性菌均有明显的抑制作用，MIC值在0.125 ~ 8.0 μ g/mL之间。此外，化合物6 ~ 10对耐甲氧西林的金黄色葡萄球菌（MRSA）和表皮葡萄球菌（MRSE）均有较强的抑制作用，对耐万古霉素的粪肠球菌（Enterococcus faecalis）和粪肠球菌（E. faecium）也有抑制作用。讨论了结构活性关系。
Fifteen new depsidone-based analogues named spiromastixones A-O (1-15) were isolated from the fermentation broth of a deep-sea Spiromastix sp. fungus. Their structures were elucidated on the basis of extensive NMR and mass spectroscopic analysis in association with chemical conversion. Spiromastixones A-O are classified into two subtypes based on the orientation of ring C relative to ring A, while the n-propyl substituents on rings A and C are rarely seen in natural products. Most analogues are substituted by various numbers of chlorine atoms. All compounds exhibited significant inhibition against Gram-positive bacteria including Staphylococcus aureus, Bacillus thuringiensis, and Bacillus subtilis with MIC values ranging from 0.125 to 8.0 mu g/mL. In addition, compounds 6-10 displayed potent inhibitory effects against methicillin-resistant bacterial strains of S. aureus (MRSA) and S. epidermidis (MRSE), while 10 also inhibited the growth of the vancomycin-resistant bacteria Enterococcus faecalis and E. faecium (VRE). The structure activity relationships are discussed.