Natural Drug Discovery Group, School of Pharmacy, Queen's University Belfast, Belfast BT9 7BL, Northern Ireland, U.K.
Clinical Trial Center, Beijing Hospital, National Center of Gerontology, Institute of Geriatric Medicine, Chinese Academy of Medical Sciences, Beijing 10073, P.R. China.
Biosci Rep. 2020 May 29;40(5). doi: 10.1042/BSR20200019.
Host-defense antimicrobial peptides (AMPs) from amphibians are usually considered as one of the most promising next-generation antibiotics because of their excellent antimicrobial properties and low cytotoxicity. In the present study, one novel Brevinin-1 type peptide, Brevinin-1GHd, was isolated and characterized from the skin secretion of the frog, Hylarana guentheri. Brevinin-1GHd was found to possess a wide range of antimicrobial activity through penetrating the bacterial membrane within a short time while showing low hemolysis at bactericidal concentrations, even against the resistant strains. It also inhibited and eradicated biofilms that are thought to be closely related to the rise in resistance. Meanwhile, Brevinin-1GHd exhibited wide-spectrum anti-proliferation activity toward human cancer lines. Taken together, these results indicate that Brevinin-1GHd with its excellent antimicrobial and anticancer activities is a promising candidate for a novel antibiotic agent, and study of its structure-activity relationships also provided a rational template for further research and peptide analog design.
宿主防御性抗菌肽(AMPs)通常被认为是最有前途的下一代抗生素之一,因为它们具有出色的抗菌特性和低细胞毒性。在本研究中,从青蛙 Hylarana guentheri 的皮肤分泌物中分离和鉴定出一种新型 Brevinin-1 型肽,命名为 Brevinin-1GHd。Brevinin-1GHd 具有广泛的抗菌活性,能够在短时间内穿透细菌膜,同时在杀菌浓度下显示出低溶血活性,甚至对耐药菌株也有抑制和清除作用。它还能抑制和根除与耐药性上升密切相关的生物膜。同时,Brevinin-1GHd 对人癌细胞系表现出广谱的抗增殖活性。综上所述,Brevinin-1GHd 具有出色的抗菌和抗癌活性,是一种很有前途的新型抗生素候选药物,对其结构-活性关系的研究也为进一步的研究和肽类似物设计提供了合理的模板。