Gastroprotective activity of ent-beyerene derivatives in mice: Effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls. Issue 14 (15th July 2015)

• Record Type: Journal Article
• Authors: Parra, Teresa; Benites, Julio; Ruiz, Lina M.; Sepulveda, Beatriz; Simirgiotis, Mario; Areche, Carlos
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 14(2015)
• Page Start: 2813
• Page End: 2817
• Publication Date: 2015-07-15
• Subjects: Baccharis tola -- Diterpenoids -- ent-Beyerene -- Gastric ulcer -- Semisynthetic derivatives; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.04.095
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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 compound1 (ED50 = 50 mg/kg), 2, 6 and13 were the most active regarding gastroprotective activity. Compounds8 –10 and17 –18 showed the lowest cytotoxicity toward fibroblasts and AGS cells. Regarding to mode of gastroprotective action, the effect elicited by6 (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 of6 .