Gastroprotective activity of ent-beyerene derivatives in mice: Effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls
作者:Teresa Parra、Julio Benites、Lina M. Ruiz、Beatriz Sepulveda、Mario Simirgiotis、Carlos Areche
DOI:10.1016/j.bmcl.2015.04.095
日期:2015.7
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
十七化合物(2 - 18)从所述二萜synthetized ENT -beyer-15-SC-18醇(1)从地上部分分离Baccharis托拉对盐酸/模型的胃保护活性进行了测试EtOH中诱导的胃损伤在老鼠。此外,对成纤维细胞和AGS细胞进行了细胞毒性测试。结果表明,化合物1(ED 50 = 50毫克/千克),2,6和13是最活跃关于胃保护活性。化合物8 – 10和17 – 18对成纤维细胞和AGS细胞显示出最低的细胞毒性。关于到胃保护作用方式,其效果由诱发6(50毫克/千克)经吲哚美辛逆转,但不是由Ñ乙基马来,Ñ ģ硝基-升-精氨酸甲基酯或钌红,这表明前列腺素参与6的胃保护作用模式。