Bitencourt Fernanda Gobbi, de Brum Vieira Patrícia, Meirelles Lucia Collares, Rigo Graziela Vargas, da Silva Elenilson Figueiredo, Gnoatto Simone Cristina Baggio, Tasca Tiana
Laboratório de Pesquisa em Parasitologia, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752, Porto Alegre, RS, 90610-000, Brazil.
Laboratório de Fitoquímica e Síntese Orgânica, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752, Porto Alegre, RS, 90610-000, Brazil.
Parasitol Res. 2018 May;117(5):1573-1580. doi: 10.1007/s00436-018-5839-1. Epub 2018 Mar 23.
Trichomonas vaginalis is an extracellular parasite that binds to the epithelium of the human urogenital tract and causes the sexually transmitted infection, trichomoniasis. In view of increased resistance to drugs belonging to the 5-nitroimidazole class, new treatment alternatives are urgently needed. In this study, eight semisynthetized triterpene derivatives were evaluated for in vitro anti-T. vaginalis activity. Ursolic acid and its derivative, 3-oxime-urs-12-en-28-oic-ursolic acid (9), presented the best anti-T. vaginalis activity when compared to other derivatives, with minimum inhibitory concentration (MIC) at 25 μM. Moreover, 9 was active against several T. vaginalis fresh clinical isolates. Hemolysis assay demonstrated that 9 presented a low hemolytic effect. Importantly, 25 μM 9 was not cytotoxic against the Vero cell lineage. Finally, we demonstrated that compound 9 acts synergistically with metronidazole against a T. vaginalis metronidazole-resistant isolate. This report reveals the high potential of the triterpenoid derivative 9 as trichomonicidal agent.
阴道毛滴虫是一种细胞外寄生虫，它附着于人类泌尿生殖道上皮并引起性传播感染——滴虫病。鉴于对5-硝基咪唑类药物的耐药性增加，迫切需要新的治疗选择。在本研究中，评估了八种半合成三萜衍生物对阴道毛滴虫的体外活性。与其他衍生物相比，熊果酸及其衍生物3-肟基-乌苏-12-烯-28-乌苏酸（9）表现出最佳的抗阴道毛滴虫活性，最低抑菌浓度（MIC）为25μM。此外，9对几种阴道毛滴虫新鲜临床分离株具有活性。溶血试验表明9具有较低的溶血作用。重要的是，25μM的9对Vero细胞系无细胞毒性。最后，我们证明化合物9与甲硝唑对一株甲硝唑耐药的阴道毛滴虫分离株具有协同作用。本报告揭示了三萜类衍生物9作为抗滴虫剂的巨大潜力。
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