Anti-Trichomonas vaginalis activity of betulinic acid derivatives

被引：24

作者：

Gomes Hubner, Dariana Pimentel ^{[1
]}

Vieira, Patricia de Brum ^{[1
]}

Frasson, Amanda Piccoli ^{[1
]}

Menezes, Camila Braz ^{[1
]}

Senger, Franciane Rios ^{[1
]}

Santos da Silva, Gloria Narjara ^{[2
]}

Baggio Gnoatto, Simone Cristina ^{[2
]}

Tasca, Tiana ^{[1
]}

机构：

[1] Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, Lab Pesquisa Parasitol, Av Ipiranga 2752, BR-90610000 Porto Alegre, RS, Brazil

[2] Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, Lab Fitoquim & Sintese Organ, Av Ipiranga 2752, BR-90610000 Porto Alegre, RS, Brazil

来源：

BIOMEDICINE & PHARMACOTHERAPY | 2016年 / 84卷

关键词：

Triterpenes; Betulinic acid; Semisynthetic derivatives; Trichomoniasis; Cytotoxicity; UNITED-STATES; CYTOTOXICITY; INFECTIONS; APOPTOSIS; DIAGNOSIS; SAPONINS; EXTRACT; AGENTS; RISK;

D O I：

10.1016/j.biopha.2016.09.064

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Caused by Trichomonas vaginalis, trichomoniasis is the most common non-viral STD worldwide. Currently, metronidazole and tinidazole are the only drugs approved for treatment of the condition. However, problems such as metronidazole-resistant T. vaginalis isolates and allergic reactions have been reported. Based on data previously published by our group, structural changes in betulinic acid (1) were performed, generating three new compounds that were tested for in vitro anti-T. vaginalis activity in this study. Whereas derivative 2 did not demonstrate anti-T. vaginalis activity, derivatives 3 and 4 reduced trophozoite viability by 100%, with MIC values of 50 mM. The structural difference of two compounds was performed only on the C-28 position. Derivative 3 showed low cytotoxicity against Vero cells in 24 h; however, derivative 4 was highly cytotoxic, but efficient when associated with metronidazole in the synergism assay. ROS production by neutrophils was reduced, and derivative 3 showed anti-inflammatory effect. Collectively, the results of this study provide in vitro evidence that betulinic acid derivatives 3 and 4 are potential compounds with anti-T. vaginalis activity. (C) 2016 Elsevier Masson SAS. All rights reserved.

引用

页码：476 / 484

页数：9

共 54 条

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