Resumo

RAMOS GRANJA, Rachel; ALFONSO, Yenisey; COX, Raymundo  e  MONZOTE FIDALGO, Lianet. In vitro activity of antiretroviral tipranavir against Toxoplasma gondii tachyzoites. Rev Cubana Med Trop [online]. 2018, vol.70, n.2, pp. 1-8. ISSN 1561-3054.

The introduction of highly efficient antiretroviral therapy has brought about a decrease in the frequency of neurotoxoplasmosis among people with HIV. It was demonstrated experimentally that protease inhibitor antiretrovirals may also have a direct action against the parasite, in this case Toxoplasma gondii. The purpose of the study was to evaluate the antitoxoplasma activity in vitro of tipranavir, a third-generation protease inhibitor antiretroviral. To achieve this aim, determination was made of the growth inhibition caused by tipranavir in Toxoplasma gondii intracellular tachyzoites, as well as its cytotoxicity against macrophages living in the peritoneum of OF-1 mice. Additionally, evaluation was conducted of atazanavir, sulfadiazine and pyrimethamine as reference drugs. Tipranavir displayed inhibitory activity against T. gondii tachyzoites, with a IC₅₀ of 21.2 ± 3,0 µM, similar (p> 0.05) to the one obtained with sulfadiazine (IC₅₀= 23.3 ± 3.6 µM) and higher (p< 0.05) than atazanavir (IC₅₀= 2.8 ± 0.7 µM) and pyrimethamine (IC₅₀= 1.2 ± 0.2 µM). However, its CC₅₀ value (105.9 ± 10.0 µM) was higher (p< 0.05) than that of the reference drugs atazanavir (CC₅₀= 25.0 ± 0.5 µM), sulfadiazine (CC₅₀= 25.2 ± 3.2 µM) and pyrimethamine (CC₅₀= 4.4 ± 1.2 µM). This is the first time a description is provided of the in vitro activity of tipranavir against T. gondii tachyzoites.

Palavras-chave : tipranavir; tachyzoites; Toxoplasma gondii.

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