Wang Hui, He Haoyang, Chen Xiaoling, Zhou Mei, Wei Minjie, Xi Xinping, Ma Chengbang, Du Qiang, Chen Tianbao, Shaw Chris, Wang Lei
School of Pharmacy, China Medical University, Shenyang 110001, China.
Natural Drug Discovery Group, School of Pharmacy, Queen's University Belfast, Belfast BT9 7BL, Northern Ireland, UK.
Biology (Basel). 2020 Jul 2;9(7):148. doi: 10.3390/biology9070148.
Amphibian skin secretions are remarkable sources of novel bioactive peptides. Among these, antimicrobial peptides have demonstrated an outstanding efficacy in killing microorganisms via a general membranolytic mechanism, which may offer the prospect of solving specific target-driven antibiotic resistance. Here, the discovery of a novel defensive peptide is described from the skin secretion of the African frog, Named kassinatuerin-3, it was identified through a combination of "shot-gun" cloning and MS/MS fragmentation sequencing. Subsequently, a synthetic replicate was subjected to biofunctional evaluation. The results indicated that kassinatuerin-3 possessed antimicrobial activity against Gram-positive bacteria but no effect against Gram-negative bacteria. Additionally, it was active in biofilm eradication on and MRSA and in the antiproliferation of selected cancer cell lines. Moreover, it had a very mild hemolytic effect, which demonstrated a high therapeutic index for kassinatuerin-3. Collectively, although kassinatuerin-3 did not demonstrate remarkable bioactivities compared with other natural or synthetic antimicrobial peptides (AMPs), it offered a new insight into the design of antimicrobial derivatives.
两栖动物的皮肤分泌物是新型生物活性肽的重要来源。其中，抗菌肽已通过一般的膜溶解机制在杀灭微生物方面展现出卓越功效，这可能为解决特定靶点驱动的抗生素耐药性问题带来希望。在此，描述了一种从非洲青蛙皮肤分泌物中发现的新型防御肽。它被命名为kassinatuerin-3，是通过“鸟枪法”克隆和串联质谱（MS/MS）片段测序相结合的方法鉴定出来的。随后，对其合成复制品进行了生物功能评估。结果表明，kassinatuerin-3对革兰氏阳性菌具有抗菌活性，但对革兰氏阴性菌无效。此外，它在消除耐甲氧西林金黄色葡萄球菌（MRSA）生物膜以及所选癌细胞系的抗增殖方面具有活性。而且，它具有非常轻微的溶血作用，这表明kassinatuerin-3具有较高的治疗指数。总体而言，尽管与其他天然或合成抗菌肽（AMPs）相比，kassinatuerin-3并未表现出显著的生物活性，但它为抗菌衍生物的设计提供了新的思路。
