In vitro and Quantitative and Structure Activity Relationship (QSAR) evaluation of the antifungal activity of terpenoid constituents of essential oils against Alternaria alternata and Fusarium oxysporum.

Introduction. Fungal genera Alternaria and Fusarium include human and plant pathogenic species. Several antifungals have been used for their control, but excessive use has contributed to resistance development in pathogens. An alternative to searching for and developing new antifungal agents is usin...

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Publicado en:Biomédica: Revista del Instituto Nacional de Salud Vol. 43; pp. 156 - 170
Autores principales: Andrade-Ochoa, Sergio, Sánchez-Aldana, Daniela, María Rodríguez-Valdez, Luz, Virginia Nevárez-Moorillón, Guadalupe
Formato: Artículo
Publicado: Instituto Nacional de Salud of Colombia 2023 Supplement
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Acceso en línea:Ver este registro en EBSCOhost
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      pub: Instituto Nacional de Salud of Colombia
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        atl: In vitro and Quantitative and Structure Activity Relationship (QSAR) evaluation of the antifungal activity of terpenoid constituents of essential oils against Alternaria alternata and Fusarium oxysporum.
      aug:
        au:
          Andrade-Ochoa, Sergio
          Sánchez-Aldana, Daniela
          María Rodríguez-Valdez, Luz
          Virginia Nevárez-Moorillón, Guadalupe
        affil:
          Facultad de Ciencias Químicas, Universidad Autónoma de Chihuahua, Chihuahua, México
          Facultad de Medicina y Ciencias Biomédicas, Universidad Autónoma de Chihuahua, Chihuahua, México
      su:
        Structure-activity relationships
        Essential oils
        Fusarium oxysporum
        Alternaria alternata
        Pharmaceutical chemistry
        Antifungal agents
      sug:
        subj:
          Structure-activity relationships
          Essential oils
          Fusarium oxysporum
          Alternaria alternata
          Pharmaceutical chemistry
          Antifungal agents
      keyword:
        aceites volátiles
        Alternaria
        Fusarium
        oils
        quantitative structureactivity relationship
        relación estructura-actividad cuantitativa
        volatile
        aceites volátiles
        relación estructura-actividad cuantitativa
      ab:
        Introduction. Fungal genera Alternaria and Fusarium include human and plant pathogenic species. Several antifungals have been used for their control, but excessive use has contributed to resistance development in pathogens. An alternative to searching for and developing new antifungal agents is using essential oils and their main components, which have biological activities of interest in medicine and food production. Objective. To evaluate in vitro and in silico the antifungal activities of terpenoids against Alternaria alternata and Fusarium oxysporum. Materials and methods. The minimum inhibitory concentration and minimum fungicidal concentration values of 27 constituents of essential oils used against Alternaria alternata and Fusarium oxysporum were evaluated in vitro. In addition, using genetic algorithms, quantitative models of the structure-activity relationship were used to identify the structural and physicochemical properties related to antifungal activity. Results. The evaluated compounds proved to be effective antifungals. Thymol was the most active with a minimum inhibitory concentration of 91.6 ± 28.8 µg/ml for A. alternata and F. oxysporum. Quantitative structure-activity relationship models revealed the octanolwater cleavage ratio as the molecular property, and the phenols as the main functional group contributing to antifungal activity. Conclusion. Terpenoids exhibit relevant antifungal activities that should be incorporated into the study of medicinal chemistry. Inclusion of in silico assays in the in vitro evaluation is a valuable tool in the search for and rational design of terpene derivatives as new potential antifungal agents.
        Introducción. Los géneros Alternaria y Fusarium contienen especies patógenas para los humanos y los cultivos. Para su control, se han utilizado diversos antifúngicos. Sin embargo, su uso desmedido ha contribuido al desarrollo de agentes patógenos resistentes. Una alternativa para buscar y desarrollar nuevos agentes antimicóticos son los aceites esenciales y sus componentes principales, los cuales poseen diversas actividades biológicas de interés para la medicina y en la preservación de alimentos. Objetivo. Evaluar in vitro e in silico las actividades antifúngicas de terpenoides contra Alternaria alternata y Fusarium oxysporum. Materiales y métodos. Se evaluaron in vitro las concentraciones inhibitorias mínimas y las concentraciones fungicidas mínimas de 27 constituyentes de aceites esenciales contra A. alternata y F. oxysporum. Además, mediante algoritmos genéticos, se crearon modelos cuantitativos de la relación estructura-actividad para determinar las propiedades estructurales y fisicoquímicas relacionadas con la actividad antifúngica. Resultados. Los compuestos evaluados mostraron ser antifúngicos activos. El timol fue el compuesto con mayor actividad, con un valor de concentración inhibitoria mínima de 91.6 ± 28.8 µg/ml, tanto para Alternaria alternata como para Fusarium oxysporum. Los modelos cuantitativos de la relación estructura-actividad incluyeron la avidez por los lípidos y los fenoles como los principales grupos funcionales que contribuyen en la actividad antifúngica. Conclusión. Los terpenoides poseen actividades antifúngicas relevantes para ser incorporados en el estudio de la química medicinal. La inclusión de pruebas in silico a la evaluación in vitro es una herramienta útil para la búsqueda y el diseño racional de derivados terpénicos como posibles agentes antifúngicos.
      pubtype: Academic Journal
      doctype: Article
      src: R
    language: English
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