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首页> 外文期刊>Peptides: An International Journal >Peptide conjugates of lactoferricin analogues and antimicrobials-Design, chemical synthesis, and evaluation of antimicrobial activity and mammalian cytotoxicity
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Peptide conjugates of lactoferricin analogues and antimicrobials-Design, chemical synthesis, and evaluation of antimicrobial activity and mammalian cytotoxicity

机译：乳叶苷素类似物和抗微生物设计，化学合成和抗菌活性和哺乳动物细胞毒性评价的肽缀合物

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摘要

Eight new peptide conjugates composed of modified bovine lactoferricin truncated analogues (LFcinB) and one of the three antimicrobials - ciprofloxacin (CIP), levofloxacin (LVX), and fluconazole (FLC) - were synthesized. Four different linkers were applied to connect a peptide and an antimicrobial agent. The FLC-containing peptidic conjugates were synthesized using the "click chemistry" method. This novel approach is reported here for the first time. Unlike their components, CIP- and LVX-based conjugates exerted activity against Candida yeast. Similarly to the constituent peptides, synthesized conjugates showed activity against Gram-positive bacteria, especially S. epidermidis. The most active were the conjugates containing CIP linked to the peptide by the redox-sensitive disulfide bridge. Our results show a significant role of a linker between antimicrobial agent and a peptide. This was also confirmed by the lack of synergistic effects on the antimicrobial activity of the constituent compounds. Moreover, cytotoxicity assays revealed that the proposed conjugates cause a comparatively low cytotoxic effect in reference to antibiotics widely used in therapies. Therefore, they can be deliberated as attractive leading structures for the development of drugs.
机译：合成了八种新的肽缀合物，由改性牛乳叶蛋白截短的类似物（LFCINB）和三种抗微生物 - 环丙沙星（CIP），左氧氟沙星（LVX）和氟康唑（FLC）之一组成。施用四种不同的接头以连接肽和抗微生物剂。使用“咔哒化学”方法合成含FLC的肽缀合物。这部新方法是第一次报告。与他们的组成部分不同，基于CIP和LVX的共轭物施加对念珠菌酵母的活动。与组成肽类似，合成的缀合物显示针对革兰氏阳性细菌的活性，尤其是S.表皮。最活跃的是通过氧化还原敏化二硫桥含有连接到肽的CIP的缀合物。我们的结果表明抗微生物剂和肽之间的接头的重要作用。这也通过对组分化合物的抗微生物活性缺乏协同作用来证实。此外，细胞毒性测定揭示了所提出的缀合物引起相对低的细胞毒性效应，参考疗法广泛使用的抗生素。因此，它们可以被审议为有吸引力的领先结构以发展毒品。

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