一种新型的、无两亲性构象的短杆菌肽S抗菌活性类似物。

A novel, antimicrobially active analog of gramicidin S without amphiphilic conformation.

作者信息

Tamaki Makoto, Sawa Kenta, Kikuchi Sho, Shindo Mitsuno, Uchida Yoshiki

出版信息

J Antibiot (Tokyo). 2006 Jun;59(6):370-2. doi: 10.1038/ja.2006.54.

DOI:10.1038/ja.2006.54

Abstract

A novel gramicidin S analog, cyclo(-Val-Leu-Leu-Orn-Leu-D-Phe-Pro-)2, was synthesized, its antibiotic activity compared with gramicidin S and shown to be as potent as gramicidin S when compared with the susceptibility toward five Gram-positive microorganisms. It exceeded the activity of gramicidin S against Bacillus megaterium ATCC 19213 by a factor of two. Circular dichroism and NMR data suggested this analog to adopt an antiparallel beta-sheet conformation without amphiphilic character.

摘要

合成了一种新型短杆菌肽S类似物环（-缬氨酸-亮氨酸-亮氨酸-鸟氨酸-亮氨酸-D-苯丙氨酸-脯氨酸-）2，将其抗生素活性与短杆菌肽S进行了比较，结果表明，与对五种革兰氏阳性微生物的敏感性相比，其活性与短杆菌肽S相当。它对巨大芽孢杆菌ATCC 19213的活性比短杆菌肽S高出两倍。圆二色性和核磁共振数据表明，该类似物采用了无两亲性特征的反平行β-折叠构象。