从人LL-37衍生的新型抗菌肽作为角膜炎潜在抗菌剂的硅片设计和体外评价。

IF 1.8 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Arsalan Pashapour, Soroush Sardari, Parastoo Ehsani
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引用次数: 1

摘要

人体产生两类抗菌肽(AMPs),即防御素和抗菌肽。本研究利用生物信息学工具设计了一种基于人抗菌肽(LL-37)的新型十肽(Catoid)及其二聚体(Dicatoid),用于治疗细菌性角膜炎。选择合成肽序列后,对标准菌株和耐药菌株铜绿假单胞菌和金黄色葡萄球菌进行抑菌活性评价。为了进行更准确的比较,本试验采用LL-37、庆大霉素、环丙沙星、阿米卡星和青霉素。此外,还研究了指定化合物对成纤维细胞和牛角膜内皮细胞的细胞毒性水平。结果表明,与LL-37相比,所设计的肽对铜绿假单胞菌具有更强的抑菌活性;而Catoid对金黄色葡萄球菌的抑菌效果较好。此外,与初始设计模型LL-37相比,Catoid和Dicatoid对人皮肤成纤维细胞系和牛角膜内皮细胞的毒性水平非常低,这是一个重要的成就。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

<i>In Silico</i> Design and In Vitro Evaluation of Some Novel AMPs Derived From Human LL-37 as Potential Antimicrobial Agents for Keratitis.

<i>In Silico</i> Design and In Vitro Evaluation of Some Novel AMPs Derived From Human LL-37 as Potential Antimicrobial Agents for Keratitis.

<i>In Silico</i> Design and In Vitro Evaluation of Some Novel AMPs Derived From Human LL-37 as Potential Antimicrobial Agents for Keratitis.

In Silico Design and In Vitro Evaluation of Some Novel AMPs Derived From Human LL-37 as Potential Antimicrobial Agents for Keratitis.

The human body produces two classes of antimicrobial peptides (AMPs), namely defensins and cathelicidins. In this study, a novel decapeptide (Catoid) and its dimer (Dicatoid) based on human cathelicidin (LL-37) have been designed by bioinformatics tools to be used in the treatment of bacterial keratitis. After the selection and synthesis of peptide sequences, their antimicrobial activities against the standard and resistant strains of Pseudomonas aeruginosa and Staphylococcus aureus were evaluated. This test was performed with LL-37, gentamicin, ciprofloxacin, amikacin, and penicillin for a more accurate comparison. Furthermore, the cytotoxicity levels of the specified compounds on fibroblast cells and bovine corneal endothelial cells were investigated. The results demonstrated that the designed peptides had a superior antimicrobial activity on P. aeruginosa, compared to LL-37; however, Catoid had a better effect on the S. aureus strain. Additionally, a significant achievement is the very low toxicity level of Catoid and Dicatoid on the human skin fibroblast cell line and bovine corneal endothelial cells, compared to that of LL-37 as the initial design model.

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来源期刊
CiteScore
3.40
自引率
6.20%
发文量
52
审稿时长
2 months
期刊介绍: The Iranian Journal of Pharmaceutical Research (IJPR) is a peer-reviewed multi-disciplinary pharmaceutical publication, scheduled to appear quarterly and serve as a means for scientific information exchange in the international pharmaceutical forum. Specific scientific topics of interest to the journal include, but are not limited to: pharmaceutics, industrial pharmacy, pharmacognosy, toxicology, medicinal chemistry, novel analytical methods for drug characterization, computational and modeling approaches to drug design, bio-medical experience, clinical investigation, rational drug prescribing, pharmacoeconomics, biotechnology, nanotechnology, biopharmaceutics and physical pharmacy.
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