Article
Gastroprotective activity of synthetic coumarins: Role of endogenous prostaglandins, nitric oxide, non-protein sulfhydryls and vanilloid receptors
Registro en:
Sepulveda, B., Quispe, C., Simirgiotis, M., Torres-Ben?tez, A., Reyes-Ort?z, J., Areche, C., & Garc?a-Beltr?n, O. (2016). Gastroprotective activity of synthetic coumarins: Role of endogenous prostaglandins, nitric oxide, non-protein sulfhydryls and vanilloid receptors. Bioorganic & Medicinal Chemistry Letters, 26(23), 5732?5735.
0960-894X
Autor
Sep?lveda, Beatriz
Quispe, Cristina
Simirgiotis, Mario
Torres-Ben?tez, Alfredo
Reyes-Ort?z, Johanna
Areche, Carlos
Garc?a-Beltr?n, Olimpo
Institución
Resumen
Natural or synthetic coumarins showed gastroprotective and antiulcer activity in animal models. In this study, we have synthetized twenty coumarins using classic methods to evaluate their gastroprotective effects on the ethanol/HCl-induced gastric lesion model in mice at 20 mg/kg. Among the coumarins synthetized, compounds 6 and 10 showed the greatest gastroprotective activity being as active as lansoprazole at 20 mg/kg and reducing gastric lesions by 75 and 76%, respectively. Then, in a second experiment, compounds 6 and 10 were re-evaluated in order to understand the possible mode of gastroprotective activity. Regarding coumarin 6, the protective effect was reduced by pre-treatment of the mice with N-ethylmaleimide and l-NAME suggesting that sulfhydryl compounds and endogenous nitric oxide are involved in its gastroprotective activity. While for coumarin 10 the effect was reduced by pre-treatment with indomethacin suggesting that prostaglandins are positively involved in its gastroprotective activity.