Antimicrobial and Antibiofilm Activity of UP-5, an Ultrashort Antimicrobial Peptide Designed Using Only Arginine and Biphenylalanine.
Antimicrobial and Antibiofilm Activity of UP-5, an Ultrashort Antimicrobial Peptide Designed Using Only Arginine and Biphenylalanine.
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DOI：
10.3390/ph11010003
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发表时间：
2018-01-02
期刊：
影响因子：
--
通讯作者：
Al-Balas Q
中科院分区：
文献类型：
--
作者：
Almaaytah A;Qaoud MT;Khalil Mohammed G;Abualhaijaa A;Knappe D;Hoffmann R;Al-Balas Q
最近，全球社区中多重耐药细菌（MDRB）的激增已成为全球卫生专业人员和人类面临的最严峻挑战之一。阳离子超短抗菌肽（USAMP）是一组有前途的分子，满足新型抗菌药物开发所需的标准。 UP-5 是一种新型五肽，对各种标准和临床分离的 MDRB 表现出显着的抗菌活性。 UP-5 对革兰氏阳性菌和革兰氏阴性菌的 MIC 值分别在 (10–15 μM) 和 (55–65 μM) 范围内。此外，UP-5 显示出抗生物膜活性，最小生物膜根除浓度 (MBEC) 值相当于 MIC 值的两倍。在相同的抑制浓度下，UP-5对人类红细胞和哺乳动物细胞表现出非常低或可以忽略不计的毒性。将 UP-5 与传统抗生素联合使用会产生协同或相加的作用模式，导致某些抗生素的 MIC 值降低 99.7%，同时肽的 MIC 值也显着下降。在小鼠全血浆和血清中评估了 UP-5 的稳定性，结果表明血浆中的模式更稳定。目前的研究表明，USAMP 是一种很有前途的抗菌剂，可以避免传统抗菌肽的负面特征。此外，USAMP 对 MDRB 表现出良好至中等的活性、可忽略不计的毒性以及与传统抗菌药物组合的协同效果。
The recent upsurge of multidrug resistant bacteria (MDRB) among global communities has become one of the most serious challenges facing health professionals and the human population worldwide. Cationic ultrashort antimicrobial peptides (USAMPs) are a promising group of molecules that meet the required criteria of novel antimicrobial drug development. UP-5, a novel penta-peptide, displayed significant antimicrobial activities against various standard and clinical isolates of MDRB. UP-5 displayed MICs values within the range of (10–15 μM) and (55–65 μM) against Gram-positive and Gram-negative bacteria, respectively. Furthermore, UP-5 displayed antibiofilm activity with minimum biofilm eradication concentration (MBEC) value as equal to twofold higher than MIC value. At the same inhibitory concentrations, UP-5 exhibited very low or negligible toxicity toward human erythrocytes and mammalian cells. Combining UP-5 with conventional antibiotics led to a synergistic or additive mode of action that resulted in the reduction of the MIC values for some of the antibiotics by 99.7% along a significant drop in MIC values of the peptide. The stability profile of UP-5 was evaluated in full mouse plasma and serum with results indicating a more stable pattern in plasma. The present study indicates that USAMPs are promising antimicrobial agents that can avoid the negative characteristics of conventional antimicrobial peptides. Additionally, USAMPs exhibit good to moderate activity against MDRB, negligible toxicity, and synergistic outcomes in combination with conventional antimicrobial agents.
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