Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon, Republic of Korea.
PLoS One. 2013;8(3):e58997. doi: 10.1371/journal.pone.0058997. Epub 2013 Mar 14.
Concerns over the increasing emergence of antibiotic-resistant pathogenic microorganisms due to the overuse of antibiotics and the lack of effective antibiotics for livestock have prompted efforts to develop alternatives to conventional antibiotics. Antimicrobial peptides (AMPs) with a broad-spectrum activity and rapid killing, along with little opportunity for the development of resistance, represent one of the promising novel alternatives. Their high production cost and cytotoxicity, however, limit the use of AMPs as effective antibiotic agents to livestock. To overcome these problems, we developed potent antimicrobial Escherichia coli displaying multimeric AMPs on the cell surface so that the AMP multimers can be converted into active AMP monomers by the pepsin in the stomach of livestock. Buf IIIb, a strong AMP without cytotoxicity, was expressed on the surface of E. coli as Lpp-OmpA-fused tandem multimers with a pepsin substrate residue, leucine, at the C-terminus of each monomer. The AMP multimers were successfully converted into active AMPs upon pepsin cleavage, and the liberated Buf IIIb-L monomers inhibited the growth of two major oral infectious pathogens of livestock, Salmonella enteritidis and Listeria monocytogenes. Live antimicrobial microorganisms developed in this study may represent the most effective means of providing potent AMPs to livestock, and have a great impact on controlling over pathogenic microorganisms in the livestock production.
由于抗生素的过度使用和缺乏针对家畜的有效抗生素,导致抗生素耐药性致病微生物的不断出现,人们越来越关注这个问题,这促使人们努力开发传统抗生素的替代品。具有广谱活性和快速杀菌作用、耐药性发展机会少的抗菌肽 (AMPs) 是一种很有前途的新型替代品。然而,其高生产成本和细胞毒性限制了 AMP 作为有效抗生素在畜牧业中的应用。为了克服这些问题,我们开发了一种有效的抗菌大肠杆菌,在其表面展示了多聚体 AMP,这样 AMP 多聚体就可以通过家畜胃中的胃蛋白酶转化为活性 AMP 单体。Buf IIIb 是一种没有细胞毒性的强 AMP,作为 Lpp-OmpA 融合串联多聚体表达在大肠杆菌表面,每个单体的 C 末端都有胃蛋白酶底物残基亮氨酸。经胃蛋白酶切割后,AMP 多聚体成功转化为活性 AMPs,释放的 Buf IIIb-L 单体抑制了两种主要的家畜口腔感染病原体——肠炎沙门氏菌和李斯特菌的生长。本研究中开发的活体抗菌微生物可能代表了向家畜提供有效 AMP 的最有效手段,并对控制家畜生产中致病性微生物的过度生长具有重要影响。