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布福菌素 I 是传统抗生素的替代品:抗菌性能、稳定性和安全性评估。

Buforin I an alternative to conventional antibiotics: Evaluation of the antimicrobial properties, stability, and safety.

机构信息

Department of Food Science and Technology, Faculty of Agriculture, Ferdowsi University of Mashhad, Mashhad, Iran.

Department of Animal Science, Faculty of Agriculture, Ferdowsi University of Mashhad, Mashhad, Iran; Stem Cell Biology and Regenerative Medicine Research Group, Research Institute of Biotechnology, Ferdowsi University of Mashhad, Mashhad, Iran.

出版信息

Microb Pathog. 2021 Dec;161(Pt B):105301. doi: 10.1016/j.micpath.2021.105301. Epub 2021 Nov 22.

DOI:10.1016/j.micpath.2021.105301
PMID:34822969
Abstract

Cationic antimicrobial peptides are being developed as a promising class of antimicrobial sub-stances. The introduction of a new antibiotic component requires a comprehensive study of its properties so that it can be relied upon to continue laboratory procedures and clinical trials on laboratory animals or human volunteers. Antimicrobial activity of buforin I was evaluated against 15 of the most important pathogenic bacterial and fungal strains. This was followed by assessing anti-biofilm activity, time-dependent inhibitory, thermal stability, plas-ma stability, hemolysis, and cytotoxic activities. The range of obtained MICs was between 4 and 16 μg/mL. The most resistant and most sensitive microbial strains were S. salivarius and C. perfringens, respectively. Buforin I not only inhibited biofilm formation, but also showed a high biofilm radiation activity. Buforin I was stable in human plasma and also at different temperatures including 40, 60, and 80 °C. Although no significant anti-cancer properties were observed for buforin I, the lack of cytotoxicity as well as the lack of hemolytic activity confirm its safety. The high therapeutic index indicated that buforin I has a considerable pharmaceutical potential and can be a reasonable candidate to replace antibiotics or administered in combination with antibiotics to increase the effectiveness as well as reduce the dose of antibiotics.

摘要

阳离子抗菌肽作为一种很有前途的抗菌物质类别正在被开发。引入一种新的抗生素成分需要对其性质进行全面研究,以便能够依靠它继续在实验室动物或人类志愿者身上进行实验室程序和临床试验。我们评估了蜂毒素 I 对 15 种最重要的致病细菌和真菌菌株的抗菌活性。然后评估了抗生物膜活性、时间依赖性抑制、热稳定性、血浆稳定性、溶血和细胞毒性活性。获得的 MIC 范围在 4 到 16μg/mL 之间。最耐药和最敏感的微生物菌株分别是唾液链球菌和产气荚膜梭菌。蜂毒素 I 不仅抑制生物膜形成,而且还表现出高的生物膜辐射活性。蜂毒素 I 在人血浆中稳定,并且在包括 40、60 和 80°C 的不同温度下稳定。尽管蜂毒素 I 没有表现出显著的抗癌特性,但缺乏细胞毒性以及缺乏溶血活性证实了其安全性。高治疗指数表明蜂毒素 I 具有相当大的药物潜力,可以作为替代抗生素的合理候选物,或者与抗生素联合使用,以提高有效性并减少抗生素剂量。

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