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来自具有广泛抗菌活性的蝎子斑点瓦乔蝎的肽。

Peptides from the scorpion Vaejovis punctatus with broad antimicrobial activity.

作者信息

Ramírez-Carreto Santos, Jiménez-Vargas Juana María, Rivas-Santiago Bruno, Corzo Gerardo, Possani Lourival D, Becerril Baltazar, Ortiz Ernesto

机构信息

Departamento de Medicina Molecular y Bioprocesos, Instituto de Biotecnología, Universidad Nacional Autónoma de Mexico. Avenida Universidad, 2001, Colonia Chamilpa, Apartado Postal 510-3, Cuernavaca, Morelos 62210, Mexico.

Medical Research Unit-Zacatecas, Mexican Institute of Social Security IMSS, Zacatecas, Mexico.

出版信息

Peptides. 2015 Nov;73:51-9. doi: 10.1016/j.peptides.2015.08.014. Epub 2015 Sep 4.

Abstract

The antimicrobial potential of two new non-disulfide bound peptides, named VpAmp1.0 (LPFFLLSLIPSAISAIKKI, amidated) and VpAmp2.0 (FWGFLGKLAMKAVPSLIGGNKSSSK) is here reported. These are 19- and 25-aminoacid-long peptides with +2 and +4 net charges, respectively. Their sequences correspond to the predicted mature regions from longer precursors, putatively encoded by cDNAs derived from the venom glands of the Mexican scorpion Vaejovis punctatus. Both peptides were chemically synthesized and assayed against a variety of microorganisms, including pathogenic strains from clinical isolates and strains resistant to conventional antibiotics. Two shorter variants, named VpAmp1.1 (FFLLSLIPSAISAIKKI, amidated) and VpAmp2.1 (FWGFLGKLAMKAVPSLIGGNKK), were also synthesized and tested. The antimicrobial assays revealed that the four synthetic peptides effectively inhibit the growth of both Gram-positive (Staphylococcus aureus and Streptococcus agalactiaea) and Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria, with MICs in the range of 2.5-24.0 μM; yeasts (Candida albicans and Candida glabrata) with MICs of 3.1-50.0 μM; and two clinically isolated strains of Mycobacterium tuberculosis-including a multi-drug resistant one- with MICs in the range of 4.8-30.5 μM. A comparison between the activities of the original peptides and their derivatives gives insight into the structural/functional role of their distinctive residues.

摘要

本文报道了两种新的非二硫键结合肽VpAmp1.0(LPFFLLSLIPSAISAIKKI,酰胺化)和VpAmp2.0(FWGFLGKLAMKAVPSLIGGNKSSSK)的抗菌潜力。它们分别是19和25个氨基酸长的肽,净电荷分别为+2和+4。其序列对应于较长前体的预测成熟区域,推测由墨西哥蝎子Vaejovis punctatus毒腺来源的cDNA编码。两种肽均通过化学合成,并针对多种微生物进行了检测,包括临床分离的致病菌株和对传统抗生素耐药的菌株。还合成并测试了两个较短的变体,命名为VpAmp1.1(FFLLSLIPSAISAIKKI,酰胺化)和VpAmp2.1(FWGFLGKLAMKAVPSLIGGNKK)。抗菌试验表明,这四种合成肽能有效抑制革兰氏阳性菌(金黄色葡萄球菌和无乳链球菌)和革兰氏阴性菌(大肠杆菌和铜绿假单胞菌)的生长,最小抑菌浓度(MIC)在2.5 - 24.0μM范围内;对酵母(白色念珠菌和光滑念珠菌)的MIC为3.1 - 50.0μM;对两株临床分离的结核分枝杆菌菌株(包括一株耐多药菌株)的MIC在4.8 - 30.5μM范围内。对原始肽及其衍生物活性的比较有助于深入了解其独特残基的结构/功能作用。

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