Majerle Andreja, Kidric Jurka, Jerala Roman
Laboratory of Biotechnology, National Institute of Chemistry, Hajdrihova 19, SI-1000 Ljubljana, Slovenia.
J Antimicrob Chemother. 2003 May;51(5):1159-65. doi: 10.1093/jac/dkg219. Epub 2003 Apr 14.
Cationic antibacterial peptides are potentially therapeutic in the treatment of sepsis, because of their amalgamated antibacterial and lipopolysaccharide-binding activities. We prepared acyl analogues of the peptide fragment of human lactoferrin, which originally had weak antibacterial activity. It was found that 12 carbon units constitute the optimal acyl chain length, enhancing the antibacterial activity and binding of lipopolysaccharide by up to two orders of magnitude. Lactoferrin-based lipopeptides approached the activity of polymyxin B, a lipopeptide of natural origin, but were also active against Gram-positive bacteria.
阳离子抗菌肽因其兼具抗菌和脂多糖结合活性，在脓毒症治疗中具有潜在的治疗作用。我们制备了人乳铁蛋白肽片段的酰基类似物，该片段原本抗菌活性较弱。结果发现，12个碳单元构成了最佳的酰基链长度，可将抗菌活性和脂多糖结合能力提高多达两个数量级。基于乳铁蛋白的脂肽接近天然来源的脂肽多粘菌素B的活性，但对革兰氏阳性菌也有活性。
