title: The intracellular mechanism of action on Escherichia coli of BF2-A/C, two analogues of the antimicrobial peptide Buforin 2.
abstract: In the present study, the antimicrobial peptides BF2-A and BF2-C, two analogues of Buforin 2, were chemically synthesized and the activities were assayed. To elucidate the bactericidal mechanism of BF2-A/C and their different antimicrobial activities, the influence of peptides to E. coli cell membrane and targets of intracellular action were researched. Obviously, BF2-A and BF2-C did not induce the influx of PI into the E. coli cells, indicating nonmemebrane permeabilizing killing action. The FITC-labeled BF2-A/C could penetrate the E. coli cell membrane and BF2-C penetrated the cells more efficiently. Furthermore, BF2-A/C could bind to DNA and RNA respectively, and the affinity of BF2-C to DNA was powerful at least over 4 times than that of BF2-A. The present results implied that BF2-A and BF2-C inhibited the cellular functions by binding to DNA and RNA of cells after penetrating the cell membranes, resulting in the rapid cell death. The structure-activity relationship analysis of BF2-A/C revealed that the cell-penetrating efficiency and the affinity ability to DNA were critical factors for determining the antimicrobial potency of both peptides. The more efficient cell-penetrating and stronger affinity to DNA caused that BF2-C displayed more excellent antimicrobial activity and rapid killing kinetics than BF2-A.
authors.affiliation: College of Life Science and Technology, Southwest University for Nationalities, ChengDu 610041, Sichuan Province, P. R. China.
authors.forename: Gang
authors.initials: G
authors.lastname: Hao
authors.forename: Yong-Hui
authors.initials: YH
authors.lastname: Shi
authors.forename: Ya-Li
authors.initials: YL
authors.lastname: Tang
authors.forename: Guo-Wei
authors.initials: GW
authors.lastname: Le
mesh_terms: D023181:Antimicrobial Cationic Peptides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects / Q000378:metabolism; D004926:Escherichia coli / Q000737:chemistry / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D050296:Microbial Viability / Q000187:drug effects; D011506:Proteins / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D023181:Antimicrobial Cationic Peptides; D011506:Proteins; C097849:buforin II