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- Title
Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone.
- Authors
Dantas, Elen Diana; de Souza, Fabia Julliana Jorge; Litaiff Nogueira, William Nascimento; Silva, Cláudia Cândida; de Azevedo, Pedro Henrique Antunes; Aragão, Cícero Flávio Soares; de Almeida, Patricia Danielle Oliveira; do Carmo Cardoso, Mariana Filomena; de Carvalho da Silva, Fernando; de Azevedo, Eduardo Pereira; Barbosa, Euzébio Guimarães; Lima, Emerson Silva; Ferreira, Vitor Francisco; de Lima, Ádley Antonini Neves
- Abstract
Chagas disease is an endemic parasitic infection that occurs in 21 Latin American countries. New therapies for this disease are urgently needed, as the only two drugs available (nifurtimox and benznidazol) have high toxicity and variable efficacy in the disease's chronic phase. Recently, a new chemical entity (NCE) named Pyranaphthoquinone (IVS320) was synthesized from lawsone. We report herein, a detailed study of the physicochemical properties and in vitro trypanocidal activity of IVS320. A series of assays were performed for characterization, where thermal, diffractometric, and morphological analysis were performed. In addition, the solubility, permeability, and hygroscopicity of IVS320 were determined. The results show that its poor solubility and low permeability may be due to its high degree of crystallinity (99.19%), which might require the use of proper techniques to increase the IVS320's aqueous solubility and permeability. The trypanocidal activity study demonstrated that IVS320 is more potent than the reference drug benznidazole, with IC50/24 h of 1.49 ±0.1 μM, which indicates that IVS320 has potential as a new drug candidate for the treatment of Chagas disease.
- Subjects
CHAGAS' disease treatment; TRYPANOSOMIASIS treatment; PARASITIC disease treatment; IMMUNOLOGICAL blood tests; INTERFERON gamma release tests
- Publication
Molecules, 2017, Vol 22, Issue 10, p1631
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules22101631