The anti‐Trichomonas vaginalis phloroglucinol derivative isoaustrobrasilol B modulates extracellular nucleotide hydrolysis

作者: Camila Braz Menezes , Graziela Vargas Rigo , Henrique Bridi , Danielle da Silva Trentin , Alexandre José Macedo

DOI: 10.1111/CBDD.13002

关键词:

摘要: Trichomonas vaginalis causes trichomoniasis, a neglected sexually transmitted disease. Due to severe health consequences and treatment failure, new therapeutic alternatives are crucial. Phloroglucinols from southern Brazilian Hypericum species demonstrated anti-T. vaginalis anti-Leishmania amazonensis activities. The modulation of biochemical pathways involved in the control inflammatory response by ectonucleotidases, NTPDase, ecto-5′-nucleotidase represents targets for combating protozoa. This study investigated activity phloroglucinol derivatives Brazil against T. vaginalis as well its ability on modulating parasite ectonucleotidases and, consequently, immune parameters through ATP adenosine effects. Phloroglucinol screening revealed isoaustrobrasilol B (IC50 38 μm) with no hemolytic activity. Although most active compound induced cytotoxicity mammalian cell lineage, vivo model evidenced absence toxicity. Isoaustrobrasilol significantly inhibited NTPDase activities, attributed extracellular nucleotide accumulation was evaluated. production ROS IL-6 T. vaginalis-stimulated neutrophils not affected treatment. Conversely, IL-8 levels were enhanced. associative mechanism trophozoites death may increase susceptibility host innate like contributing clearance.

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