Bandeira Izabel Cristina Justino, Bandeira-Lima Danya, Mello Clarissa Perdigão, Pereira Ticiana Praciano, De Menezes Ramon Róseo Paula Pessoa Bezerra, Sampaio Tiago Lima, Falcão Cláudio Borges, Rádis-Baptista Gandhi, Martins Alice Maria Costa
Programa de Pós-Graduação em Ciências Farmacêuticas,Universidade Federal do Ceará,Fortaleza,CE,Brasil.
Departamento de Fisiologia e Farmacologia,Faculdade de Medicina,Universidade Federal do Ceará,Fortaleza,CE,Brasil.
Parasitology. 2018 Jul;145(8):1059-1064. doi: 10.1017/S0031182017001846. Epub 2017 Dec 6.
Cathelicidins are antimicrobial peptides produced by humans and animals in response to various pathogenic microbes. Crotalicidin (Ctn), a cathelicidin-related vipericidin from the South American Crotalus durissus terrificus rattlesnake's venom gland, and its fragments have demonstrated antimicrobial and antifungal activity, similarly to human cathelicidin LL-37. In order to provide templates for the development of modern trypanocidal agents, the present study evaluated the antichagasic effect of these four peptides (Ctn, Ctn[1-14], Ctn[15-34] and LL-37). Herein, Ctn and short derived peptides were tested against the epimastigote, trypomastigote and amastigote forms of Trypanosoma cruzi Y strain (benznidazole-resistant strain) and cytotoxicity in mammalian cells was evaluated against LLC-MK2 lineage cells. Ctn inhibited all T. cruzi developmental forms, including amastigotes, which is implicated in the burden of infection in the chronic phase of Chagas disease. Moreover, Ctn showed a high selective index against trypomastigote forms (>200). Ctn induced cell death in T. cruzi through necrosis, as determined by flow cytometry analyses with specific molecular probes and morphological alterations, such as loss of membrane integrity and cell shrinkage, as observed through scanning electron microscopy. Overall, Ctn seems to be a promising template for the development of antichagasic agents.
防御素是人和动物在应对各种致病微生物时产生的抗菌肽。响尾蛇防御素(Ctn)是一种来自南美杜氏响尾蛇毒腺的与防御素相关的蝰蛇毒素,与其片段一样,已证明具有抗菌和抗真菌活性,类似于人类防御素LL-37。为了为现代杀锥虫剂的开发提供模板,本研究评估了这四种肽(Ctn、Ctn[1-14]、Ctn[15-34]和LL-37)的抗恰加斯病作用。在此,测试了Ctn和短衍生肽对克氏锥虫Y株(苯硝唑耐药株)的前鞭毛体、锥鞭毛体和无鞭毛体形式的作用,并评估了对LLC-MK2细胞系的哺乳动物细胞的细胞毒性。Ctn抑制了所有克氏锥虫的发育形式,包括无鞭毛体,而无鞭毛体与恰加斯病慢性期的感染负担有关。此外,Ctn对锥鞭毛体形式显示出高选择性指数(>200)。通过使用特异性分子探针的流式细胞术分析以及通过扫描电子显微镜观察到的形态学改变,如膜完整性丧失和细胞收缩,确定Ctn通过坏死诱导克氏锥虫细胞死亡。总体而言,Ctn似乎是开发抗恰加斯病药物的一个有前景的模板。