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别构环素,来自异壁放线菌属的高度氯化安古霉素类化合物。

Allocyclinones, hyperchlorinated angucyclinones from Actinoallomurus.

作者信息

Cruz Joao C S, Maffioli Sonia I, Bernasconi Alice, Brunati Cristina, Gaspari Eleonora, Sosio Margherita, Wellington Elizabeth, Donadio Stefano

机构信息

Ktedogen Srl, Milano, Italy.

School of Life Sciences, University of Warwick, Coventry, UK.

出版信息

J Antibiot (Tokyo). 2017 Jan;70(1):73-78. doi: 10.1038/ja.2016.62. Epub 2016 May 25.

DOI:10.1038/ja.2016.62
PMID:27220409
Abstract

A screening program on a limited number of strains belonging to the Actinoallomurus genus yielded a series of new angucyclinones. NMR and MS analyses established that these compounds are characterized by an unusual lactone ring and present up to four halogens per molecule, with one congener representing the first natural product containing a trichloromethyl substitution on an aromatic system. Remarkably, this family of metabolites seems to be produced by phylogenetically distinct Actinoallomurus isolates. Because of the unique structural features and wide distribution among Actinoallomurus, we have designated these angucyclinones as allocyclinones. Allocyclinones possess interesting activity against different Gram-positive bacteria, including antibiotic-resistant strains, with antibacterial potency increasing with the number of chlorine substituents. The tetrachlorinated compound is the most abundant congener in the allocyclinone complex.

摘要

对属于放线全壁菌属的有限数量菌株进行的筛选程序产生了一系列新的安古环素类化合物。核磁共振(NMR)和质谱(MS)分析表明,这些化合物的特征是具有一个不寻常的内酯环,每个分子中最多含有四个卤素,其中一种同系物是第一种在芳香体系上含有三氯甲基取代基的天然产物。值得注意的是,这一族代谢产物似乎是由系统发育上不同的放线全壁菌分离株产生的。由于其独特的结构特征以及在放线全壁菌中的广泛分布,我们将这些安古环素类化合物命名为别环素类化合物。别环素类化合物对包括耐抗生素菌株在内的不同革兰氏阳性菌具有有趣的活性,其抗菌效力随着氯取代基数量的增加而增强。四氯化化合物是别环素类化合物复合物中含量最丰富的同系物。

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