%0 Journal Article %1 RN236 %A Parra, T. %A Benites, J. %A Ruiz, L.M. %A Sepulveda, B. %A Simirgiotis, M. %A Areche, C. %D 2015 %I 2015 Elsevier Ltd. %J Bioorganic & Medicinal Chemistry Letters %K baccharis defense, derivatives, diterpenoids, dqcauchile ent-beyerene, gastric injury mucosal natural-products, semisynthetic tola, ulcer, %N 14 %P 2813-2817 %R 10.1016/j.bmcl.2015.04.095 %T Gastroprotective Activity of Ent-Beyerene Derivatives in Mice: Effects on Gastric Secretion, Endogenous Prostaglandins and Non-Protein Sulfhydryls %U /brokenurl#<Go to ISI>://WOS:000355663100017 %V 25 %X 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.

@article{RN236, 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. }, added-at = {2019-12-04T03:57:35.000+0100}, author = {Parra, T. and Benites, J. and Ruiz, L.M. and Sepulveda, B. and Simirgiotis, M. and Areche, C.}, biburl = {https://www.bibsonomy.org/bibtex/28295d64946ca22c44b307e4f782b7a0a/dqcauchile}, doi = {10.1016/j.bmcl.2015.04.095}, interhash = {2cd5cdd1440442579bcf60db9a48a4de}, intrahash = {8295d64946ca22c44b307e4f782b7a0a}, issn = {0960-894x}, journal = {Bioorganic & Medicinal Chemistry Letters}, keywords = {baccharis defense, derivatives, diterpenoids, dqcauchile ent-beyerene, gastric injury mucosal natural-products, semisynthetic tola, ulcer,}, number = 14, pages = {2813-2817}, publisher = {2015 Elsevier Ltd.}, timestamp = {2019-12-04T03:58:17.000+0100}, title = {Gastroprotective Activity of Ent-Beyerene Derivatives in Mice: Effects on Gastric Secretion, Endogenous Prostaglandins and Non-Protein Sulfhydryls}, type = {Journal Article}, url = {/brokenurl#<Go to ISI>://WOS:000355663100017}, volume = 25, year = 2015 }