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New Eugenol Derivatives with Enhanced Insecticidal Activity.
Fernandes, Maria José G; Pereira, Renato B; Pereira, David M; Fortes, A Gil; Castanheira, Elisabete M S; Gonçalves, M Sameiro T.
Afiliación
  • Fernandes MJG; Centre of Chemistry, Department of Chemistry, Campus of Gualtar, University of Minho, 4710-057 Braga, Portugal.
  • Pereira RB; REQUIMTE/LAQV, Laboratory of Pharmacognosy, Department of Chemistry, Faculty of Pharmacy, University of Porto, R. Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
  • Pereira DM; REQUIMTE/LAQV, Laboratory of Pharmacognosy, Department of Chemistry, Faculty of Pharmacy, University of Porto, R. Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
  • Fortes AG; Centre of Chemistry, Department of Chemistry, Campus of Gualtar, University of Minho, 4710-057 Braga, Portugal.
  • Castanheira EMS; Centre of Physics, Department of Physics, Campus of Gualtar, University of Minho, 4710-057 Braga, Portugal.
  • Gonçalves MST; Centre of Chemistry, Department of Chemistry, Campus of Gualtar, University of Minho, 4710-057 Braga, Portugal.
Int J Mol Sci ; 21(23)2020 Dec 04.
Article en En | MEDLINE | ID: mdl-33291666
Eugenol, the generic name of 4-allyl-2-methoxyphenol, is the major component of clove essential oil, and has demonstrated relevant biological potential with well-known antimicrobial and antioxidant actions. New O-alkylated eugenol derivatives, bearing a propyl chain with terminals like hydrogen, hydroxyl, ester, chlorine, and carboxylic acid, were synthesized in the present work. These compounds were later subjected to epoxidation conditions to give the corresponding oxiranes. All derivatives were evaluated against their effect upon the viability of insect cell line Sf9 (Spodoptera frugiperda), demonstrating that structural changes elicit marked effects in terms of potency. In addition, the most promising molecules were evaluated for their impact in cell morphology, caspase-like activity, and potential toxicity towards human cells. Some molecules stood out in terms of toxicity towards insect cells, with morphological assessment of treated cells showing chromatin condensation and fragmentation, which are compatible with the occurrence of programmed cell death, later confirmed by evaluation of caspase-like activity. These findings point out the potential use of eugenol derivatives as semisynthetic insecticides from plant natural products.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Eugenol / Insecticidas Límite: Animals / Humans Idioma: En Revista: Int J Mol Sci Año: 2020 Tipo del documento: Article País de afiliación: Portugal Pais de publicación: Suiza

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Eugenol / Insecticidas Límite: Animals / Humans Idioma: En Revista: Int J Mol Sci Año: 2020 Tipo del documento: Article País de afiliación: Portugal Pais de publicación: Suiza