Vargas-Casanova Yerly, Rodríguez-Mayor Andrea Verónica, Cardenas Karen Johanna, Leal-Castro Aura Lucía, Muñoz-Molina Liliana Constanza, Fierro-Medina Ricardo, Rivera-Monroy Zuly Jenny, García-Castañeda Javier Eduardo
Biotechnology Institute, Universidad Nacional de Colombia Carrera 45 No 26-85 Bogotá 11321 Colombia.
Chemistry Department, Universidad Nacional de Colombia Carrera 45 No 26-85, Building 450, Office 213 Bogotá 11321 Colombia.
RSC Adv. 2019 Mar 5;9(13):7239-7245. doi: 10.1039/c9ra00708c. eCollection 2019 Mar 1.
Dimeric and tetrameric peptides derived from LfcinB (20-25): RRWQWR, LfcinB (20-30): RRWQWRMKKLG, LfcinB (17-31): FKARRWQWRMKKLGA, or the palindromic sequence LfcinB (21-25): RWQWRWQWR were obtained by means of the SPPS-Fmoc/Bu methodology. The antibacterial activity of these molecules was evaluated against (ATCC 25922 and ATCC 11775), (ATCC 25923), (ATCC 29212), and (ATCC 27853). The dimer LfcinB (20-25): (RRWQWR)K-Ahx, the tetramer LfcinB (20-25): (RRWQWR)K-Ahx-C, and the palindromic sequence LfcinB (21-25) exhibited the highest antibacterial activity against the tested bacterial strains. In all cases, the antibacterial activity was dependent on peptide concentration. The polyvalent molecules LfcinB (20-25) and LfcinB (20-25) exhibited bacteriostatic and bactericidal activity against , , and strains; additionally, this dimer and this tetramer combined with ciprofloxacin exhibited a synergistic antibacterial effect against ATCC 25922 and , respectively. Furthermore, the peptides LfcinB (20-30), LfcinB (20-25), and LfcinB (21-25) combined with vancomycin exhibited a synergistic antibacterial effect against and , respectively. This study showed that polyvalent peptides derived from LfcinB exhibit significant antibacterial activity, suggesting that these peptides could have a therapeutic application. Furthermore, our results suggest that polyvalent peptide synthesis could be considered as an innovative and viable strategy for obtaining promising antimicrobial molecules.
通过固相肽合成法（SPPS-Fmoc/Bu方法）获得了源自乳铁传递蛋白B（LfcinB）（20 - 25）的二聚体和四聚体肽：RRWQWR、LfcinB（20 - 30）：RRWQWRMKKLG、LfcinB（17 - 31）：FKARRWQWRMKKLGA，或回文序列LfcinB（21 - 25）：RWQWRWQWR。评估了这些分子对金黄色葡萄球菌（ATCC 25922和ATCC 11775）、大肠杆菌（ATCC 25923）、粪肠球菌（ATCC 29212）和白色念珠菌（ATCC 27853）的抗菌活性。二聚体LfcinB（20 - 25）：（RRWQWR）K - Ahx、四聚体LfcinB（20 - 25）：（RRWQWR）K - Ahx - C和回文序列LfcinB（21 - 25）对测试的细菌菌株表现出最高的抗菌活性。在所有情况下，抗菌活性均取决于肽的浓度。多价分子LfcinB（20 - 25）和LfcinB（20 - 25）对金黄色葡萄球菌、大肠杆菌和粪肠球菌菌株表现出抑菌和杀菌活性；此外，该二聚体和该四聚体与环丙沙星联合使用时，分别对金黄色葡萄球菌ATCC 25922和粪肠球菌表现出协同抗菌作用。此外，肽LfcinB（20 - 30）、LfcinB（20 - 25）和LfcinB（21 - 25）与万古霉素联合使用时，分别对粪肠球菌和金黄色葡萄球菌表现出协同抗菌作用。这项研究表明，源自LfcinB的多价肽具有显著的抗菌活性，表明这些肽可能具有治疗应用价值。此外，我们的结果表明多价肽合成可被视为获得有前景的抗菌分子的一种创新且可行的策略。
