短杆菌肽 S 的脯氨酸残基修饰的聚阳离子类似物，对革兰氏阳性菌和革兰氏阴性菌均具有高抗菌活性且溶血活性低。

Proline residue-modified polycationic analogs of gramicidin S with high antibacterial activity against both Gram-positive and Gram-negative bacteria and low hemolytic activity.

作者信息

Kawai M, Yamamura H, Tanaka R, Umemoto H, Ohmizo C, Higuchi S, Katsu T

机构信息

Graduate School of Engineering, Nagoya Institute of Technology, Nagoya 466-8555, Japan.

出版信息

J Pept Res. 2005 Jan;65(1):98-104. doi: 10.1111/j.1399-3011.2004.00204.x.

DOI:10.1111/j.1399-3011.2004.00204.x

PMID:15686540

Abstract

Novel polycationic analogs of the cyclic decapeptide antibiotic, gramicidin S, possessing NH(2), D/L-Phe-NH or L-Lys-NH groups at the 4alpha- or 4beta-positions of the L-Pro residues, were synthesized. While L-Pro(4alpha/beta-NH(2))-containing analogs exhibited much weaker antibacterial activity, the D/L-Phe and L-Lys-substituted analogs exhibited higher antibacterial activity against Gram-negative bacteria than the parent gramicidin S. All of these additional amino group-containing analogs showed substantially reduced toxicity against human blood cells.

摘要

合成了环十肽抗生素短杆菌肽S的新型聚阳离子类似物，这些类似物在L-脯氨酸残基的4α-或4β-位具有NH₂、D/L-苯丙氨酸-NH或L-赖氨酸-NH基团。虽然含L-脯氨酸（4α/β-NH₂）的类似物表现出弱得多的抗菌活性，但D/L-苯丙氨酸和L-赖氨酸取代的类似物对革兰氏阴性菌的抗菌活性高于母体短杆菌肽S。所有这些含额外氨基的类似物对人血细胞的毒性都大幅降低。