Hong S Y, Park T G, Lee K H
Department of Biochemistry, Yonsei University, 134 Shinchon-Dong, Seodaemun-Gu, Seoul 120-749, South Korea.
Peptides. 2001 Oct;22(10):1669-74. doi: 10.1016/s0196-9781(01)00502-2.
By using short linear antimicrobial peptides as a model system, the effect of peptide charge on the specificity between Candida albicans (fungi) and Gram-positive bacteria was investigated. In a present study, we added and/or deleted lysine residue(s) at the C-terminal and/or N-terminal end(s) of an antimicrobial peptide (KKVVFKVKFK-NH(2)) and synthesized the peptides that had similar alpha helical structures in a lipid membrane mimic condition. The increase of peptide charge improved antifungal activity without the change of antibacterial activity. Structure-activity relationship study about the peptides revealed that the net positive charge must play an important role in the specificity between C. albicans and Gram-positive bacteria and the increase of the net positive charge without the moderate change of secondary structure could improve activity for C. albicans rather than Gram-positive bacteria.
通过使用短线性抗菌肽作为模型系统，研究了肽电荷对白色念珠菌（真菌）与革兰氏阳性菌之间特异性的影响。在本研究中，我们在抗菌肽（KKVVFKVKFK-NH₂）的C端和/或N端添加和/或缺失赖氨酸残基，并在脂质膜模拟条件下合成了具有相似α螺旋结构的肽。肽电荷的增加提高了抗真菌活性，而抗菌活性没有改变。对这些肽的构效关系研究表明，净正电荷在白色念珠菌与革兰氏阳性菌之间的特异性中必定起重要作用，并且在二级结构没有适度变化的情况下净正电荷的增加可提高对白色念珠菌而非革兰氏阳性菌的活性。
