2015 |
Parra, T; Benites, J; Ruiz, L M; Sepulveda, B; Simirgiotis, M; Areche, C Gastroprotective Activity of Ent-Beyerene Derivatives in Mice: Effects on Gastric Secretion, Endogenous Prostaglandins and Non-Protein Sulfhydryls Artículo de revista Bioorganic & Medicinal Chemistry Letters, 25 (14), pp. 2813-2817, 2015, ISSN: 0960-894x. Resumen | Enlaces | BibTeX | Etiquetas: baccharis defense, derivatives, diterpenoids, ent-beyerene, gastric injury mucosal natural-products, semisynthetic tola, ulcer @article{RN236, title = {Gastroprotective Activity of Ent-Beyerene Derivatives in Mice: Effects on Gastric Secretion, Endogenous Prostaglandins and Non-Protein Sulfhydryls}, author = { T. Parra and J. Benites and L.M. Ruiz and B. Sepulveda and M. Simirgiotis and C. Areche}, url = {/brokenurl#<Go to ISI>://WOS:000355663100017}, doi = {10.1016/j.bmcl.2015.04.095}, issn = {0960-894x}, year = {2015}, date = {2015-01-01}, journal = {Bioorganic & Medicinal Chemistry Letters}, volume = {25}, number = {14}, pages = {2813-2817}, publisher = {2015 Elsevier Ltd.}, 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.}, keywords = {baccharis defense, derivatives, diterpenoids, ent-beyerene, gastric injury mucosal natural-products, semisynthetic tola, ulcer}, pubstate = {published}, tppubtype = {article} } 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. |
2015 |
Gastroprotective Activity of Ent-Beyerene Derivatives in Mice: Effects on Gastric Secretion, Endogenous Prostaglandins and Non-Protein Sulfhydryls Artículo de revista Bioorganic & Medicinal Chemistry Letters, 25 (14), pp. 2813-2817, 2015, ISSN: 0960-894x. |