Alvarez-Bravo J, Kurata S, Natori S
Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Biochem J. 1994 Sep 1;302 ( Pt 2)(Pt 2):535-8. doi: 10.1042/bj3020535.
Previously, we identified a core undecapeptide of sapecin B having antimicrobial activity. Based on the structure of this peptide, we systematically synthesized peptides consisting of terminal basic motifs and internal oligo-leucine sequences and examined their antimicrobial activities. Of these peptides, RLKLLLLLRLK-NH2 and KLKLLLLLKLK-NH2 were found to have potent microbicidal activity against Staphylococcus aureus, Escherichia coli, methicillin-resistant S. aureus and Candida albicans in liquid medium. We also synthesized the D-enantiomer of KLKLLLLLKLK-NH2. This enantiomer was resistant to tryptic digestion and persisted longer in the culture medium, showing greater antimicrobial activity than the original peptide.
此前，我们鉴定出了具有抗菌活性的杀佩菌素B的核心十一肽。基于该肽的结构，我们系统地合成了由末端碱性基序和内部寡聚亮氨酸序列组成的肽，并检测了它们的抗菌活性。在这些肽中，发现RLKLLLLLRLK-NH2和KLKLLLLLKLK-NH2在液体培养基中对金黄色葡萄球菌、大肠杆菌、耐甲氧西林金黄色葡萄球菌和白色念珠菌具有强大的杀菌活性。我们还合成了KLKLLLLLKLK-NH2的D-对映体。该对映体对胰蛋白酶消化具有抗性，并且在培养基中持续时间更长，显示出比原始肽更强的抗菌活性。
