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首页> 外文期刊>RSC Advances >Synergistic bactericide and antibiotic effects of dimeric, tetrameric, or palindromic peptides containing the RWQWR motif against Gram-positive and Gram-negative strains
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Synergistic bactericide and antibiotic effects of dimeric, tetrameric, or palindromic peptides containing the RWQWR motif against Gram-positive and Gram-negative strains

机译：含有RWQWR基序的二聚体，四聚或回文肽的协同杀菌剂和抗生素效果含有革兰氏阳性和革兰氏阴性菌株

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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)(Pal): RWQWRWQWR were obtained by means of the SPPS-Fmoc/tBu methodology. The antibacterial activity of these molecules was evaluated against Escherichia coli (ATCC 25922 and ATCC 11775), Staphylococcus aureus (ATCC 25923), Enterococcus faecalis (ATCC 29212), and Pseudomonas aeruginosa (ATCC 27853). The dimer LfcinB (20-25)(2): (RRWQWR)(2)K-Ahx, the tetramer LfcinB (20-25)(4): (RRWQWR)(4)K-2-Ahx(2)-C-2, and the palindromic sequence LfcinB (21-25)(Pal) 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)(2) and LfcinB (20-25)(4) exhibited bacteriostatic and bactericidal activity against E. coli, P. aeruginosa, and S. aureus strains; additionally, this dimer and this tetramer combined with ciprofloxacin exhibited a synergistic antibacterial effect against E. coli ATCC 25922 and P. aeruginosa, respectively. Furthermore, the peptides LfcinB (20-30)(4), LfcinB (20-25)(4), and LfcinB (21-25)(Pal) combined with vancomycin exhibited a synergistic antibacterial effect against S. aureus and E. faecalis, 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.
机译：二聚和自LfcinB衍生的四聚体的肽（20-25）：RRWQWR，LfcinB（20-30）：RRWQWRMKKLG，LfcinB（17-31）：FKARRWQWRMKKLGA或回文序列LfcinB（21-25）（PAL）：RWQWRWQWR获得由SPPS-的Fmoc / TBU方法的装置。这些分子的抗菌活性对大肠杆菌进行评估（ATCC 25922和ATCC 11775），金黄色葡萄球菌（ATCC 25923），粪肠球菌（ATCC 29212），和铜绿假单胞菌（ATCC 27853）。二聚体LfcinB（20-25）（2）：（RRWQWR）（2）K-AHX，四聚体LfcinB（20-25）（4）：（RRWQWR）（4）K-2-AHX（2）-C -2，回文序列LfcinB（21-25）（PAL）表现出对所测试的细菌菌株的最高的抗菌活性。在所有情况下，其抗菌活性依赖于肽浓度。多价分子LfcinB（20-25）（2）和LfcinB（20-25）（4）表现出对大肠杆菌，铜绿假单胞菌和金黄色葡萄球菌菌株的抑菌和杀菌活性;另外，此二聚体和四聚体本环丙沙星表现出协同抗菌分别针对大肠杆菌ATCC 25922及铜绿假单胞菌，效果相结合。此外，所述肽LfcinB（20-30）（4），LfcinB（20-25）（4），和LfcinB（21-25）（PAL）用万古霉素组合表现出抗金黄色葡萄球菌和粪肠球菌的协同抗菌作用， 分别。这项研究表明，从LfcinB推导出多价肽表现出显著的抗菌活性，这表明这些肽可能有治疗应用。此外，我们的研究结果表明，多价合成肽可考虑作为获得承诺抗菌分子的创新和可行的策略。

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