Synthesis, characterization and utilization of a new series of 1,2,3-triazole derivatives to neutralize some toxic activities of Bothrops jararaca snake venom
Título del documento: Synthesis, characterization and utilization of a new series of 1,2,3-triazole derivatives to neutralize some toxic activities of Bothrops jararaca snake venom
Revue: Brazilian Journal of Pharmaceutical Sciences
Base de datos: PERIÓDICA
Número de sistema: 000451849
ISSN: 1984-8250
Autores: 1
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2
4
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4
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1
Instituciones: 1Universidade Federal Fluminense, Instituto de Biologia, Niteroi, Rio de Janeiro. Brasil
2Fundacao Ezequiel Dias, Centro de Pesquisa e Desenvolvimento, Belo Horizonte, Minas Gerais. Brasil
3Universidade Federal Fluminense, Faculdade de Farmacia, Niteroi, Rio de Janeiro. Brasil
4Universidade Federal do Rio de Janeiro, Instituto de Quimica, Rio de Janeiro. Brasil
Año:
Volumen: 58
País: Brasil
Idioma: Inglés
Tipo de documento: Artículo
Enfoque: Experimental, aplicado
Resumen en inglés Snake envenomation is a public health problem, and while serum therapy prevents death, the local effects of venoms can lead to amputations or morbidities. Thus, alternative treatments deserve attention. In this study, we tested eight derivatives of 1,2,3-triazole against some toxic activities of Bothrops jararaca venom. The derivatives were synthesized, and their structures analyzed by infrared and nuclear magnetic resonance. After that, the ability of compounds to inhibit hemolysis, coagulation, proteolysis, hemorrhaging, edema, and lethal activities of B. jararaca venom was investigated. The derivatives were incubated with B. jararaca venom (incubation protocol), administered before (prevention protocol) or after (treatment protocol) injecting venom into the mice. Then, hemorrhaging assay occurred. As a result, most of the derivatives inhibited the activities, even if they were incubated, injected before or after B. jararaca venom. However, the derivatives TRI 07 and TRI 18 seemed to be the most efficient in impairing hemorrhaging. The derivatives showed a low drug score of toxicity based on an in silico technique. Therefore, the derivatives fulfilled physicochemical and biological requirements to become drugs, and they may be a brand new initiative for designing antivenom molecules to complement antivenom therapy to efficiently block tissue necrosis or any other local effects
Disciplinas: Química,
Medicina
Palabras clave: Toxicología,
Farmacología,
Veneno de víbora,
Antivenenos,
Derivados de triazol,
Síntesis orgánica,
Bothrops jararaca
Keyword: Toxicology,
Pharmacology,
Snake venom,
Antivenoms,
Triazole derivatives,
Organic synthesis,
Bothrops jararaca
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