Jelinkova Pavlina, Splichal Zbynek, Jimenez Ana Maria Jimenez, Haddad Yazan, Mazumdar Aninda, Sur Vishma Pratap, Milosavljevic Vedran, Kopel Pavel, Buchtelova Hana, Guran Roman, Zitka Ondrej, Richtera Lukas, Hegerova Dagmar, Heger Zbynek, Moulick Amitava, Adam Vojtech
Department of Chemistry and Biochemistry, Mendel University in Brno, Zemedelska, Brno, Czech Republic,
Central European Institute of Technology, Brno University of Technology, Purkynova, Brno, Czech Republic,
Infect Drug Resist. 2018 Oct 12;11:1807-1817. doi: 10.2147/IDR.S160975. eCollection 2018.
Increase in vancomycin (Van)-resistant bacterial strains including vancomycin-resistant (VRSA) and lack of new effective antibiotics have become a formidable health problem.
We designed a new conjugate composed of Van and a peptide Hecate (Hec; Van/Hec), and its potential antimicrobial activity was evaluated.
Results from disk diffusion test, time-kill assay, determination of minimum inhibitory concentration (MIC), microscopy, and comet assay showed strong antimicrobial effects of Van/Hec against wild-type, methicillin-resistant (MRSA) and VRSA. Microscopy revealed that the exposure to Van/Hec results in disruption of bacterial cell integrity in all tested strains, which was not observed in case of Van or Hec alone.
Overall, we showed that the preparation of conjugates from antibiotics and biologically active peptides could help us to overcome the limitation of the use of antibiotic in the treatment of infections caused by multidrug-resistant bacteria.
包括耐万古霉素金黄色葡萄球菌（VRSA）在内的耐万古霉素细菌菌株的增加以及缺乏新的有效抗生素已成为一个严峻的健康问题。
我们设计了一种由万古霉素（Van）和一种肽赫卡特（Hec；Van/Hec）组成的新型缀合物，并评估了其潜在的抗菌活性。
纸片扩散试验、时间杀菌试验、最低抑菌浓度（MIC）测定、显微镜检查和彗星试验的结果表明，Van/Hec对野生型、耐甲氧西林金黄色葡萄球菌（MRSA）和VRSA具有强大的抗菌作用。显微镜检查显示，暴露于Van/Hec会导致所有测试菌株的细菌细胞完整性遭到破坏，而单独使用Van或Hec时未观察到这种情况。
总体而言，我们表明由抗生素和生物活性肽制备缀合物有助于我们克服抗生素在治疗多重耐药菌引起的感染方面的使用限制。
