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: Article

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

Huella dactilar

Fibroblasts
Cytotoxicity
Prostaglandins
Stomach
Baccharis
Derivatives
Ruthenium Red
Ethylmaleimide
Diterpenes
Indomethacin
Antennas
arginine methyl ester
methyl red
compound 18

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Citar esto

Parra, Teresa ; Benites, Julio ; Ruiz, Lina M. ; Sepulveda, Beatriz ; Simirgiotis, Mario ; Areche, Carlos. / Gastroprotective activity of ent-beyerene derivatives in mice : Effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls. En: Bioorganic and Medicinal Chemistry Letters. 2015 ; Vol. 25, N.º 14. pp. 2813-2817.
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abstract = "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.",
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Gastroprotective activity of ent-beyerene derivatives in mice : Effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls. / Parra, Teresa; Benites, Julio; Ruiz, Lina M.; Sepulveda, Beatriz; Simirgiotis, Mario; Areche, Carlos.

En: Bioorganic and Medicinal Chemistry Letters, Vol. 25, N.º 14, 04.06.2015, p. 2813-2817.

Resultado de la investigación: Article

TY - JOUR

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T2 - Effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls

AU - Parra, Teresa

AU - Benites, Julio

AU - Ruiz, Lina M.

AU - Sepulveda, Beatriz

AU - Simirgiotis, Mario

AU - Areche, Carlos

PY - 2015/6/4

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