Study on the synthesis and structure-activity relationship of 1,2,3-triazoles against toxic activities of Bothrops jararaca venom
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Jenifer Frouche de Souza
Abstract
Snakebite envenoming is a health concern and has been a neglected tropical disease since 2017, according to the World Health Organization. In this study, we evaluated the ability of ten 1,2,3-triazole derivatives AM001 to AM010 to inhibit pertinent in vitro (coagulant, hemolytic, and proteolytic) and in vivo (hemorrhagic, edematogenic, and lethal) activities of Bothrops jararaca venom. The derivatives were synthesized, and had their molecular structures fully characterized by CHN element analysis, Fourier-transform infrared spectroscopy and Nuclear magnetic resonance. The derivatives were incubated with the B. jararaca venom (incubation protocol) or administered before (prevention protocol) or after (treatment protocol) the injection of B. jararaca venom into the animals. Briefly, the derivatives were able to inhibit the main toxic effects triggered by B. jararaca venom, though with varying efficacies, and they were devoid of toxicity through in vivo, in silico or in vitro analyses. However, it seemed that the derivatives AM006 or AM010 inhibited more efficiently hemorrhage or lethality, respectively. The derivatives were nontoxic. Therefore, the 1,2,3-triazole derivatives may be useful as an adjuvant to more efficiently treat the local toxic effects caused by B. jararaca envenoming.
Funding source: Coordenaçãoo de Aperfeiçoamento de Pessoal de Nivel Superior
Award Identifier / Grant number: Fellowships
Funding source: Universidade Federal Fluminense
Award Identifier / Grant number: FOPESQ-PROPPi
Funding source: Conselho Nacional de Desenvolvimento Científico e Tecnológico
Award Identifier / Grant number: 304719/2012-9
Award Identifier / Grant number: Fellowships of research members of CNPq
Funding source: Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro
Award Identifier / Grant number: 26/01.001918/2015
Award Identifier / Grant number: E−26/201.163/2014
Funding source: Fundação de Amparo à Pesquisa do Estado de Minas Gerais
Award Identifier / Grant number: APQ-01858-15
Award Identifier / Grant number: AUC-00022-16
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Author contributions: All the authors have accepted responsibility for the entire content of this submitted manuscript and approved submission.
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Research funding: The authors thank the Brazilian funding agencies: FAPERJ, FAPEMIG, CNPq, CAPES, and PROPPi-UFF.
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Conflict of interest statement: The authors declare no conflicts of interest, financial or otherwise regarding this article.
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© 2022 Walter de Gruyter GmbH, Berlin/Boston
Articles in the same Issue
- Frontmatter
- Research Articles
- Synthesis, characterization, molecular docking, dynamics simulations, and in silico absorption, distribution, metabolism, and excretion (ADME) studies of new thiazolylhydrazone derivatives as butyrylcholinesterase inhibitors
- Study on the synthesis and structure-activity relationship of 1,2,3-triazoles against toxic activities of Bothrops jararaca venom
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- Comparative study of phenolic profile, antioxidant and antimicrobial activities of aqueous extract of white and green tea
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- Antidepressant alkaloids from the rhizomes of Corydalis decumbens
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- Chemical composition and bioactivities of Magnolia candollii H.Keng essential oil
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Articles in the same Issue
- Frontmatter
- Research Articles
- Synthesis, characterization, molecular docking, dynamics simulations, and in silico absorption, distribution, metabolism, and excretion (ADME) studies of new thiazolylhydrazone derivatives as butyrylcholinesterase inhibitors
- Study on the synthesis and structure-activity relationship of 1,2,3-triazoles against toxic activities of Bothrops jararaca venom
- In-silico elucidation reveals potential phytochemicals against angiotensin-converting enzyme 2 (ACE-2) receptor to fight coronavirus disease 2019 (COVID-19)
- Comparative study of phenolic profile, antioxidant and antimicrobial activities of aqueous extract of white and green tea
- Methylglyoxal and high glucose inhibit VEGFR2 phosphorylation at specific tyrosine residues
- Antidepressant alkaloids from the rhizomes of Corydalis decumbens
- Synthesis of new derivatives containing pyridine, investigation of MAO inhibitory activities and molecular docking studies
- Rapid Communications
- Chemical composition and bioactivities of Magnolia candollii H.Keng essential oil
- Chemical composition and anticholinesterase activity of Lepisanthes rubiginosa (Roxb.) Leenh. essential oil
