Department of Chemistry, Faculty of Science, Fukuoka University, Jonan-ku, Fukuoka, Japan.
J Pept Sci. 2010 Apr;16(4):171-7. doi: 10.1002/psc.1217.
A series of Trp and Arg analogs of antibacterial indolicidin (Ind) was synthesized and the antimicrobial and hemolytic activities were investigated. [L(9)]Ind, [L(11)]Ind, [K(8),L(9)]Ind and [K(6, 8),L(9)]Ind showed desirable characteristics, exhibiting negligible hemolytic activity while keeping strong antibacterial activity. The results indicated that the Trp residue at position 11 essentially contributes to both activities and one can not be exchanged for the other, whereas the Trp residues at positions 4 and 9 play important roles in antimicrobial and hemolytic activities, respectively. The Trp residues at positions 6 and 8 play no important roles in biological activities. We then found that the retro analog of Ind showed higher antibacterial activity than Ind against both Gram-positive and Gram-negative bacteria but remarkably lower hemolytic activity than that of Ind.
合成了一系列抗菌吲哚素（Ind）的色氨酸和精氨酸类似物，并研究了它们的抗菌和溶血活性。[L(9)]Ind、[L(11)]Ind、[K(8),L(9)]Ind 和 [K(6,8),L(9)]Ind 表现出良好的特性，溶血活性可忽略不计，而抗菌活性保持较强。结果表明，第 11 位的色氨酸残基对这两种活性都有重要贡献，不能相互替换，而第 4 位和第 9 位的色氨酸残基分别在抗菌和溶血活性中起重要作用。第 6 位和第 8 位的色氨酸残基在生物活性中不起重要作用。然后我们发现，吲哚素的反向类似物对革兰氏阳性菌和革兰氏阴性菌的抗菌活性均高于吲哚素，但溶血活性明显低于吲哚素。
