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合理设计的抗菌肽的抗菌活性

Antibacterial Activity of Rationally Designed Antimicrobial Peptides.

作者信息

Tincho Marius B, Morris Thureyah, Meyer Mervin, Pretorius Ashley

机构信息

Bioinformatics Research Group (BRG), DST/Mintek Nanotechnology Innovation Centre-Biolabels Node, Department of Biotechnology, Faculty of Natural Sciences, University of the Western Cape, Bellville 7535, South Africa.

Food Toxicology Laboratory, Department of Medical Bioscience, Faculty of Natural Sciences, University of the Western Cape, Bellville 7535, South Africa.

出版信息

Int J Microbiol. 2020 Apr 8;2020:2131535. doi: 10.1155/2020/2131535. eCollection 2020.

DOI:10.1155/2020/2131535
PMID:32322274
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7168710/
Abstract

Many infectious diseases are still prevalent in the world's populations since no effective treatments are available to eradicate them. The reasons may either be the antibiotic resistance towards the available therapeutic molecules or the slow rate of producing adequate therapeutic regimens to tackle the rapid growth of new infectious diseases, as well as the toxicity of current treatment regimens. Due to these reasons, there is a need to seek and develop novel therapeutic regimens to reduce the rapid scale of bacterial infections. Antimicrobial Peptides (AMPs) are components of the first line of defense for prokaryotes and eukaryotes and have a wide range of activities against Gram-negative and Gram-positive bacteria, fungi, cancer cells, and protozoa, as well as viruses. In this study, peptides which were initially identified for their HIV inhibitory activity were further screened for antibacterial activity through determination of their kinetics as well as their cytotoxicity. From the results obtained, the MICs of two AMPs (Molecule 3 and Molecule 7) were 12.5 g/ml for (ATCC 700603) and 6.25 g/ml for . (ATCC 22108). The two AMPs killed these bacteria rapidly , preventing bacterial growth within few hours of treatment. Furthermore, the cytotoxic activity of these two peptides was significantly low, even at an AMP concentration of 100 g/ml. These results revealed that Molecule 3 and 7 have great potential as antibacterial drugs or could serve as lead compounds in the design of therapeutic regimens for the treatment of antibiotic-resistant bacteria.

摘要

许多传染病在世界人口中仍然普遍存在,因为目前没有有效的治疗方法来根除它们。原因可能是现有治疗分子存在抗生素耐药性,或者是针对新出现的传染病快速增长研发足够治疗方案的速度缓慢,以及现有治疗方案存在毒性。由于这些原因,需要寻找和开发新的治疗方案,以减少细菌感染的快速蔓延。抗菌肽(AMPs)是原核生物和真核生物第一道防线的组成部分,对革兰氏阴性菌和革兰氏阳性菌、真菌、癌细胞、原生动物以及病毒都有广泛的活性。在本研究中,最初因其对HIV的抑制活性而被鉴定的肽,通过测定其动力学以及细胞毒性,进一步筛选其抗菌活性。从获得的结果来看,两种抗菌肽(分子3和分子7)对粪肠球菌(ATCC 700603)的最低抑菌浓度(MIC)为12.5μg/ml,对金黄色葡萄球菌(ATCC 22108)的MIC为6.25μg/ml。这两种抗菌肽能迅速杀死这些细菌,在治疗后数小时内就能阻止细菌生长。此外,即使在抗菌肽浓度为100μg/ml时,这两种肽的细胞毒性也显著较低。这些结果表明,分子3和分子7作为抗菌药物具有很大潜力,或者可以作为设计治疗耐抗生素细菌治疗方案的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/53d5/7168710/e9c31a7516a1/IJMICRO2020-2131535.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/53d5/7168710/d096b0744d37/IJMICRO2020-2131535.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/53d5/7168710/cbdf4b921f8c/IJMICRO2020-2131535.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/53d5/7168710/e9c31a7516a1/IJMICRO2020-2131535.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/53d5/7168710/d096b0744d37/IJMICRO2020-2131535.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/53d5/7168710/cbdf4b921f8c/IJMICRO2020-2131535.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/53d5/7168710/e9c31a7516a1/IJMICRO2020-2131535.003.jpg

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