Bioorganic Synthesis, Leiden Institute of Chemistry, Leiden University, PO Box 9502, 2300 RA Leiden, The Netherlands.
Bioorg Med Chem. 2012 Oct 15;20(20):6059-62. doi: 10.1016/j.bmc.2012.08.038. Epub 2012 Aug 31.
A series of gramicidin S derivatives 4-15 are presented that have four ornithine residues as polar protonated side chains and two central hydrophobic amino acids with unaltered turn regions. These peptides were screened against human erthrocytes and our standard panel of Gram negative- and Gram positive bacteria, including four MRSA strains. Based on the antibacterial- and hemolytic data, peptides 13 and 14 have an improved biological profile compared to the clinically applied topical antibiotic gramicidin S.
本文介绍了一系列的短杆菌肽 S 衍生物 4-15，它们具有四个鸟氨酸残基作为极性质子化侧链和两个中央疏水性氨基酸，不变的环区。这些肽被针对人类红细胞和我们的标准革兰氏阴性和革兰氏阳性细菌 panel 进行了筛选，包括四个耐甲氧西林金黄色葡萄球菌 (MRSA) 菌株。根据抗菌和溶血数据，与临床应用的局部抗生素短杆菌肽 S 相比，肽 13 和 14 的生物学特性得到了改善。
