Lima Dânya Bandeira, Mello Clarissa Perdigão, Bandeira Izabel Cristina Justino, Pessoa Bezerra de Menezes Ramon Róseo Paula, Sampaio Tiago Lima, Falcão Cláudio Borges, Morlighem Jean-Étienne R L, Rádis-Baptista Gandhi, Martins Alice Maria Costa
Faculty of Pharmacy, Department of Clinical and Toxicological Analysis, Federal University of Ceará, Rua Capitão Francisco Pedro 1210, 60430-372 Fortaleza/CE, Brazil.
Program of Post-Graduation in Pharmaceutical Sciences, Faculty of Pharmacy, Federal University of Ceará, Rua Capitão Francisco Pedro 1210, 60430-372 Fortaleza/CE, Brazil.
Biol Chem. 2018 Jan 26;399(2):187-196. doi: 10.1515/hsz-2017-0198.
The crude venom of the giant ant Dinoponera quadriceps is a cocktail of polypeptides and organic compounds that shows antiparasitic effects against Trypanosoma cruzi, the causative agent of Chagas disease. In order to investigate the venom-derived components responsible for such antitrypanosomal activity, four dinoponeratoxins (DnTxs) were identified, namely M-PONTX-Dq3a, -Dq3b, -Dq3c and -Dq4e, that are diverse in size, net charge, hydrophobicity and propensity to interact with eukaryote cell membranes. These peptides were tested against epimastigote, trypomastigote and amastigote forms of benznidazole (Bz)-resistant Y strain of T. cruzi and in mammalian host cells. The M-PONTX-Dq3a and -Dq4e inhibited all developmental forms of T. cruzi, including amastigotes, the responsible form for the maintenance of infection on chronic phase of the disease. The M-PONTX-Dq3a showed the highest selectivity index (SI) (80) and caused morphological alterations in T. cruzi, as observed by scanning electron microscopy (SEM), and induced cell death through necrosis, as seen by multiparametric flow cytometry analysis with specific biochemical markers. Altogether, the D. quadriceps venom appears as a source for the prospection of trypanocidal peptides and the M-PONTX-Dq3a arises as a candidate among the dinoponeratoxin-related peptides in the development of compounds against Chagas disease.
巨型蚂蚁四节大头蚁(Dinoponera quadriceps)的粗毒液是一种由多肽和有机化合物组成的混合物,对恰加斯病的病原体克氏锥虫(Trypanosoma cruzi)具有抗寄生虫作用。为了研究毒液中导致这种抗锥虫活性的成分,鉴定出了四种大头蚁毒素(DnTxs),即M-PONTX-Dq3a、-Dq3b、-Dq3c和-Dq4e,它们在大小、净电荷、疏水性以及与真核细胞膜相互作用的倾向方面存在差异。这些肽针对克氏锥虫苯并硝唑(Bz)耐药Y株的前鞭毛体、 trypomastigote和无鞭毛体形式以及哺乳动物宿主细胞进行了测试。M-PONTX-Dq3a和-Dq4e抑制了克氏锥虫的所有发育形式,包括无鞭毛体,而无鞭毛体是疾病慢性期维持感染的致病形式。M-PONTX-Dq3a表现出最高的选择性指数(SI)(80),通过扫描电子显微镜(SEM)观察,它会导致克氏锥虫出现形态改变,并且通过使用特定生化标记的多参数流式细胞术分析可以看出,它会通过坏死诱导细胞死亡。总的来说,四节大头蚁毒液似乎是筛选杀锥虫肽的一个来源,而M-PONTX-Dq3a在开发抗恰加斯病化合物方面作为与大头蚁毒素相关的肽中的一个候选者脱颖而出。