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.
%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
}