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一种来自光滑盾甲蝎的新型无半胱氨酸毒液肽,对耐抗生素病原体具有强大的抗菌活性。

A novel cysteine-free venom peptide with strong antimicrobial activity against antibiotics-resistant pathogens from the scorpion Opistophthalmus glabrifrons.

作者信息

Bao Aorigele, Zhong Jie, Zeng Xian-Chun, Nie Yao, Zhang Lei, Peng Zhao Feng

机构信息

Department of Biological Science and Technology, School of Environmental Studies, State Key Laboratory of Biogeology and Environmental Geology, China University of Geosciences, Wuhan, 430074, China.

出版信息

J Pept Sci. 2015 Oct;21(10):758-64. doi: 10.1002/psc.2801. Epub 2015 Aug 6.

DOI:10.1002/psc.2801
PMID:26251012
Abstract

Antibiotic-resistant bacteria, such as methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus, pose serious threat to human health. The outbreak of antibiotic-resistant pathogens in recent years emphasizes once again the urgent need for the development of new antimicrobial agents. Here, we discovered a novel antimicrobial peptide from the scorpion Opistophthalmus glabrifrons, which was referred to as Opisin. Opisin consists of 19 amino acid residues without disulfide bridges. It is a cationic, amphipathic, and α-helical molecule. Protein sequence homology search revealed that Opisin shares 42.1-5.3% sequence identities to the 17/18-mer antimicrobial peptides from scorpions. Antimicrobial assay showed that Opisin is able to potently inhibit the growth of the tested Gram-positive bacteria with the minimal inhibitory concentration (MIC) values of 4.0-10.0 μM; in contrast, it possesses much lower activity against the tested Gram-negative bacteria and a fungus. It is interesting to see that Opisin is able to strongly inhibit the growth of methicillin- and vancomycin-resistant pathogens with the MICs ranging from 2.0 to 4.0 μM and from 4.0 to 6.0 μM, respectively. We found that at a concentration of 5 × MIC, Opisin completely killed all the cultured methicillin-resistant Staphylococcus aureus. These results suggest that Opisin is a promising therapeutic candidate for the treatment of the antibiotic-resistant bacterial infections.

摘要

耐抗生素细菌,如耐甲氧西林金黄色葡萄球菌和耐万古霉素肠球菌,对人类健康构成严重威胁。近年来耐抗生素病原体的爆发再次凸显了开发新型抗菌剂的迫切需求。在此,我们从蝎子光滑眼疣蛛中发现了一种新型抗菌肽,命名为Opisin。Opisin由19个氨基酸残基组成,无二硫键。它是一种阳离子、两亲性且呈α螺旋的分子。蛋白质序列同源性搜索显示,Opisin与来自蝎子的17/18聚体抗菌肽的序列同一性为42.1 - 5.3%。抗菌试验表明,Opisin能够有效抑制受试革兰氏阳性菌的生长,最小抑菌浓度(MIC)值为4.0 - 10.0 μM;相比之下,它对受试革兰氏阴性菌和一种真菌的活性要低得多。有趣的是,Opisin能够强烈抑制耐甲氧西林和耐万古霉素病原体的生长,其MIC分别为2.0至4.0 μM和4.0至6.0 μM。我们发现,在5×MIC的浓度下,Opisin能完全杀死所有培养的耐甲氧西林金黄色葡萄球菌。这些结果表明,Opisin是治疗耐抗生素细菌感染的一个有前景的治疗候选物。

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