Gray B H, Haseman J R, Mayo K H
Department of Biochemistry, University of Minnesota, Minneapolis 55455, USA.
Biochim Biophys Acta. 1995 May 11;1244(1):185-90. doi: 10.1016/0304-4165(95)00004-u.
Human neutrophil bactericidal protein (B/PI) is known for its ability to kill bacteria and to neutralize the action of endotoxin. Short linear peptides derived from residues 80-109 have been synthesized and their bactericidal and endotoxin neutralizing activities have been assayed. A series of 'walk-through' decapeptides, overlapping 3 to 4 residues, indicates that endotoxin neutralizing and partial bactericidal activities can be localized within the N- and C-terminal portions, respectively, of the 80-109 sequence. Bactericidal activity toward Pseudomonas aeruginosa was localized in central peptides of the walk-through series and greatest in peptide 90-99. By using longer peptides, residues 86-104 and 82-108, both bactericidal and endotoxin neutralizing activities are significantly enhanced. Bactericidal activity of peptide 82-108 is now only 6-fold less than that of parent B/PI and 9-fold more potent than peptide 86-104. The 82-108 peptide was 7-fold more active at endotoxin neutralization than 86-104 but showed less enhanced activity, being approx. 470-times less active than B/PI. Cyclized 82-108 peptide retained bactericidal activity but did not improve in capacity to neutralize endotoxin.
人中性粒细胞杀菌蛋白（B/PI）以其杀灭细菌和中和内毒素作用的能力而闻名。已合成了源自80 - 109位残基的短线性肽，并测定了它们的杀菌和内毒素中和活性。一系列重叠3至4个残基的“穿梭”十肽表明，内毒素中和活性和部分杀菌活性可分别定位在80 - 109序列的N端和C端部分。对铜绿假单胞菌的杀菌活性定位在穿梭系列的中间肽段，在肽段90 - 99中活性最强。通过使用更长的肽段，即86 - 104和82 - 108，杀菌活性和内毒素中和活性均显著增强。肽段82 - 108的杀菌活性现在仅比亲本B/PI低6倍，比肽段86 - 104强9倍。82 - 108肽在内毒素中和方面的活性比86 - 104高7倍，但增强活性较小，约比B/PI低470倍。环化的82 - 108肽保留了杀菌活性，但在内毒素中和能力上没有提高。
