Department of Biology, San Diego State University, San Diego, CA 92182-4614, USA.
Antimicrob Agents Chemother. 2010 May;54(5):1888-99. doi: 10.1128/AAC.01610-09. Epub 2010 Feb 22.
The hexapeptide WRWYCR was previously identified on the basis of its ability to inhibit bacteriophage lambda integrase-mediated recombination by trapping and preventing resolution of the Holliday junction intermediate. This peptide inhibits several unrelated DNA repair enzymes that bind to and process Holliday junctions and branched DNA substrates. WRWYCR and its d stereoisomer, wrwycr, are bactericidal against both Gram-positive and Gram-negative bacteria, causing the accumulation of DNA breaks, chromosome segregation defects, and the filamentation of cells. DNA repair is a novel target of antibiotics. In the present study, we examined the ability of the peptides to inhibit the growth of Salmonella in mammalian cells. J774A.1 macrophage-like cells and murine peritoneal macrophages were infected with Salmonella enterica serovar Typhimurium and grown in the presence or absence of peptide. We found that peptide wrwycr reduced the number of Salmonella cells recovered after 24 h growth in J774A.1 cells by 100 to 1,000 times, depending on the multiplicity of infection. The peptide also inhibited Salmonella growth in peritoneal macrophages, and although higher doses were required, these were not toxic to the host cells. The apparent lower level of potency of the peptide paralleled the lower level of replication of Salmonella and the lower level of permeation of the peptide in the peritoneal macrophages than in the J774.1 cells. Treatment with peptide wrwycr elicited the SOS response in a significant fraction of the intracellular bacteria, as would be expected if the mechanism of bacterial killing was the same in pure culture and in host cells. These results represent a proof of principle of the antimicrobial activities of compounds that target DNA repair.
六肽 WRWYCR 此前因其能够通过捕获和阻止霍利迪结中间体的解析来抑制噬菌体 λ 整合酶介导的重组而被鉴定。该肽抑制几种与结合和处理霍利迪结和分支 DNA 底物的几种不相关的 DNA 修复酶。WRWYCR 和它的 d 对映异构体 wrwycr 对革兰氏阳性和革兰氏阴性细菌都具有杀菌作用,导致 DNA 断裂、染色体分离缺陷和细胞丝状化的积累。DNA 修复是抗生素的一个新靶点。在本研究中,我们研究了肽抑制哺乳动物细胞中沙门氏菌生长的能力。J774A.1 巨噬细胞样细胞和鼠腹膜巨噬细胞被感染了肠炎沙门氏菌血清型 Typhimurium,并在存在或不存在肽的情况下生长。我们发现,肽 wrwycr 减少了 J774A.1 细胞中 24 小时生长后回收的沙门氏菌细胞数量 100 到 1000 倍,具体取决于感染复数。该肽还抑制了腹膜巨噬细胞中的沙门氏菌生长,尽管需要更高的剂量,但这些剂量对宿主细胞没有毒性。肽的效力明显降低与沙门氏菌的复制水平降低以及肽在腹膜巨噬细胞中的渗透水平低于 J774.1 细胞相平行。用肽 wrwycr 处理会引起细胞内细菌的 SOS 反应,这与在纯培养物和宿主细胞中杀菌机制相同的情况下是一致的。这些结果代表了靶向 DNA 修复的化合物的抗菌活性的原理证明。