Gastroprotective activity of ent-beyerene derivatives in mice: Effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls

Teresa Parra, Julio Benites, Lina M. Ruiz, Beatriz Sepulveda, Mario Simirgiotis, Carlos Areche

Resultado de la investigación: Contribución a una revistaArtículo

6 Citas (Scopus)

Resumen

Seventeen compounds (2-18) synthetized from the diterpenoid ent-beyer-15-en-18-ol (1) isolated from aerial part of Baccharis tola were tested for their gastroprotective activity on the model of HCl/EtOH-induced gastric lesions in mice. Furthermore cytotoxicity test toward fibroblasts and AGS cells were performed. The results showed that compound 1 (ED50 = 50 mg/kg), 2, 6 and 13 were the most active regarding gastroprotective activity. Compounds 8-10 and 17-18 showed the lowest cytotoxicity toward fibroblasts and AGS cells. Regarding to mode of gastroprotective action, the effect elicited by 6 (50 mg/kg) was reversed by Indomethacin but not by N-ethylmaleimide, NG-nitro-l-arginine methyl ester or ruthenium red, which suggests that prostaglandins are involved in the mode of gastroprotective action of 6.

Idioma originalInglés
Páginas (desde-hasta)2813-2817
Número de páginas5
PublicaciónBioorganic and Medicinal Chemistry Letters
Volumen25
N.º14
DOI
EstadoPublicada - 4 jun 2015
Publicado de forma externa

Áreas temáticas de ASJC Scopus

  • Bioquímica
  • Medicina molecular
  • Biología molecular
  • Ciencias farmacéuticas
  • Descubrimiento de medicamentos
  • Bioquímica clínica
  • Química orgánica

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