title: Gastroprotective activity of ent-beyerene derivatives in mice: Effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls.
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, N(G)-nitro-L-arginine methyl ester or ruthenium red, which suggests that prostaglandins are involved in the mode of gastroprotective action of 6.
authors.affiliation: Departamento de Química, Facultad de Ciencias, Universidad de Chile, Santiago, Chile.
authors.forename: Teresa
authors.initials: T
authors.lastname: Parra
authors.affiliation: Facultad de Ciencias de la Salud, Universidad Arturo Prat., Iquique, Chile.
authors.forename: Julio
authors.initials: J
authors.lastname: Benites
authors.affiliation: Facultad de Ciencias de la Salud, Universidad Autónoma de Chile, Santiago, Chile.
authors.forename: Lina M
authors.initials: LM
authors.lastname: Ruiz
authors.affiliation: Departamento de Ciencias Químicas, Facultad de Ciencias Exactas, Universidad Andres Bello, Quillota 980, Viña del Mar, Chile.
authors.forename: Beatriz
authors.initials: B
authors.lastname: Sepulveda
authors.affiliation: Laboratorio de Productos Naturales, Departamento de Química, Facultad de Ciencias Básicas, Universidad de Antofagasta, Antofagasta, Chile.
authors.forename: Mario
authors.initials: M
authors.lastname: Simirgiotis
authors.affiliation: Departamento de Química, Facultad de Ciencias, Universidad de Chile, Santiago, Chile. Electronic address: areche@uchile.cl.
authors.forename: Carlos
authors.initials: C
authors.lastname: Areche
mesh_terms: D045784:Abietanes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D000897:Anti-Ulcer Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D031175:Baccharis / Q000737:chemistry / Q000378:metabolism; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D005750:Gastric Juice / Q000378:metabolism*; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D007213:Indomethacin / Q000494:pharmacology; D051379:Mice; D035261:Plant Components, Aerial / Q000737:chemistry / Q000378:metabolism; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D011453:Prostaglandins / Q000494:pharmacology*; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy; D013438:Sulfhydryl Compounds / Q000494:pharmacology*
chemical_list: D045784:Abietanes; D000897:Anti-Ulcer Agents; D010936:Plant Extracts; D011453:Prostaglandins; D013438:Sulfhydryl Compounds; D007213:Indomethacin
keywords: Baccharis tola; Diterpenoids; Gastric ulcer; Semisynthetic derivatives; ent-Beyerene