Anthelmintic activity of a nanoformulation based on thiophenes identified in Tagetes patula L. (Asteraceae) against the small ruminant nematode Haemonchus contortus

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Autor(es): dc.contributorUniversidade Estadual Paulista (Unesp)-
Autor(es): dc.contributorUniversidade de São Paulo (USP)-
Autor(es): dc.contributorUniversidade Estadual de Campinas (UNICAMP)-
Autor(es): dc.contributorFederal University of Ceará (UFC)-
Autor(es): dc.contributorEmpresa Brasileira de Pesquisa Agropecuária (EMBRAPA)-
Autor(es): dc.creatorPoliti, Flávio Augusto Sanches [UNESP]-
Autor(es): dc.creatorBueno, Renata Vieira-
Autor(es): dc.creatorZeoly, Lucas André-
Autor(es): dc.creatorFantatto, Rafaela Regina [UNESP]-
Autor(es): dc.creatorEloy, Josimar de Oliveira-
Autor(es): dc.creatorChorilli, Marlus [UNESP]-
Autor(es): dc.creatorCoelho, Fernando-
Autor(es): dc.creatorGuido, Rafael Victório Carvalho-
Autor(es): dc.creatorChagas, Ana Carolina de Souza-
Autor(es): dc.creatorFurlan, Maysa [UNESP]-
Data de aceite: dc.date.accessioned2022-02-22T00:53:53Z-
Data de disponibilização: dc.date.available2022-02-22T00:53:53Z-
Data de envio: dc.date.issued2021-06-25-
Data de envio: dc.date.issued2021-06-25-
Data de envio: dc.date.issued2021-07-01-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1016/j.actatropica.2021.105920-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/208606-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/208606-
Descrição: dc.descriptionThe synthesis of thiophenic compounds, previously identified in Tagetes patula, revealed that 4-(5′-(hydroxymethyl)-[2,2′-bithiophene]-5-yl)but-3-yn-1-ol), or simply Thio1, has a pronounced in vitro anthelmintic effect against Haemonchus contortus, showing 100% efficacy in the egg hatch and larval development tests presenting EC50 = 0.1731 mg.mL−1 and EC50 = 0.3243 mg.mL−1, respectively. So, this compound was selected to preparation of a nanostructured formulation to be orally administered to Santa Inês sheep. In general, from the fecal egg count reduction test (FECRT), it was observed that the product kept the parasitic load in the digestive tract of the hosts stable, with eggs per gram of faeces (EPG) counts having a mean value < 3,000 (EPGmean = 2167.1, efficacy = 36,45%), thus protecting the animals from health risks caused by a massive nematode infestation. To better understand the mode of action of this thiophene derivative, in silico molecular modeling studies were carried out with the glutamate-activated chloride channel (GluCl), a well-known molecular target of anthelmintic compounds. Based on the affinity score (GlideScore = -5.7 kcal.mol−1) and the proposed binding mode, Thio1 could be classified as a potential GluCl ligand, justifying the promising results observed in the anthelmintic assays.-
Descrição: dc.descriptionSchool of Pharmaceutical Sciences São Paulo State University (UNESP)-
Descrição: dc.descriptionUniversity of São Paulo (USP) Physics Institute of São Carlos (IFSC)-
Descrição: dc.descriptionUniversity of Campinas (UNICAMP) Chemistry Institute-
Descrição: dc.descriptionCollege of Pharmacy Dentistry and Nursing Federal University of Ceará (UFC)-
Descrição: dc.descriptionBrazilian Agricultural Research Corporation (EMBRAPA) Southeast Livestock-
Descrição: dc.descriptionChemistry Institute São Paulo State University (UNESP)-
Descrição: dc.descriptionSchool of Pharmaceutical Sciences São Paulo State University (UNESP)-
Descrição: dc.descriptionChemistry Institute São Paulo State University (UNESP)-
Idioma: dc.languageen-
Relação: dc.relationActa Tropica-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectDocking-
Palavras-chave: dc.subjectFrench marigold-
Palavras-chave: dc.subjectGastrointestinal nematode-
Palavras-chave: dc.subjectin vitro-
Palavras-chave: dc.subjectin vivo-
Palavras-chave: dc.subjectUNC-49 receptor-
Título: dc.titleAnthelmintic activity of a nanoformulation based on thiophenes identified in Tagetes patula L. (Asteraceae) against the small ruminant nematode Haemonchus contortus-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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