Antimicrobial activity of (KLAKLAK)–NH2 analogs against pathogenic microbial strains

IF 3.6 Q2 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Current Research in Biotechnology Pub Date : 2024-01-01 DOI:10.1016/j.crbiot.2024.100236
Sirine Jaber , Yana Evstatieva , Veronica Nemska , Dilyana Nikolova , Emilia Naydenova , Nelly Georgieva , Dancho Danalev
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Abstract

Many microorganisms pose a threat to human health due to the ever-increasing bacterial resistance to conventional drugs. Nowadays, searching for new alternatives to conventional antibiotics to fight bacterial resistance is a main task. Thus, natural molecules such as amino acids and peptides arise as possible solutions to the problem. The antimicrobial activity of targeted compounds was studied by the agar-diffusion method, using the prepared working solutions of the targeted peptides with the corresponding concentrations. The results of the antimicrobial activity against different test pathogens show specificity, as antimicrobial activity against the used test microorganisms was not found in the investigated short-chain synthetic peptides Si6, Si3 and Si13. Antimicrobial activity against Bacillus cereus, Staphylococcus aureus, Staphylococcus epidermidis, Propionibacterium acnes, Escherichia coli, Pseudomonas aeruginosa, and the yeasts Malassezia furfur and Candida albicans was established for the long-chain synthetic peptides Si1, Si5 and Si16, except Si5 which does not show activity against pathogenic fungal strain C. albicans. The compound Si16 where natural Leu in (KLAKLAK)2-NH2 is replaced by unnatural Nle is the best candidate for medical drug due to the combined antibacterial and antiproliferative effect as well as long hydrolytic stability.

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(KLAKLAK)-NH2类似物对病原微生物菌株的抗菌活性
由于细菌对传统药物的耐药性不断增加,许多微生物对人类健康构成威胁。如今,寻找传统抗生素的新替代品来对抗细菌耐药性已成为一项主要任务。因此,氨基酸和肽等天然分子成为解决问题的可能方案。通过琼脂扩散法,使用制备的相应浓度的目标肽工作溶液研究了目标化合物的抗菌活性。针对不同测试病原体的抗菌活性结果显示出特异性,因为所研究的短链合成肽 Si6、Si3 和 Si13 没有发现针对所用测试微生物的抗菌活性。长链合成肽 Si1、Si5 和 Si16 对蜡样芽孢杆菌、金黄色葡萄球菌、表皮葡萄球菌、痤疮丙酸杆菌、大肠杆菌、铜绿假单胞菌、糠秕马拉色菌和白色念珠菌等酵母菌具有抗菌活性,只有 Si5 对致病真菌白色念珠菌没有活性。在化合物 Si16 中,(KLAKLAK)2-NH2 中的天然 Leu 被非天然 Nle 所取代,由于该化合物具有抗菌和抗增殖的综合效果以及较长的水解稳定性,因此是医疗药物的最佳候选化合物。
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来源期刊
Current Research in Biotechnology
Current Research in Biotechnology Biochemistry, Genetics and Molecular Biology-Biotechnology
CiteScore
6.70
自引率
3.60%
发文量
50
审稿时长
38 days
期刊介绍: Current Research in Biotechnology (CRBIOT) is a new primary research, gold open access journal from Elsevier. CRBIOT publishes original papers, reviews, and short communications (including viewpoints and perspectives) resulting from research in biotechnology and biotech-associated disciplines. Current Research in Biotechnology is a peer-reviewed gold open access (OA) journal and upon acceptance all articles are permanently and freely available. It is a companion to the highly regarded review journal Current Opinion in Biotechnology (2018 CiteScore 8.450) and is part of the Current Opinion and Research (CO+RE) suite of journals. All CO+RE journals leverage the Current Opinion legacy-of editorial excellence, high-impact, and global reach-to ensure they are a widely read resource that is integral to scientists' workflow.
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