Gastroprotective activity of synthetic coumarins: Role of endogenous prostaglandins, nitric oxide, non-protein sulfhydryls and vanilloid receptors

Beatriz Sepulveda, Cristina Quispe, Mario Simirgiotis, Alfredo Torres-Benítez, Johanna Reyes-Ortíz, Carlos Areche, Olimpo García-Beltrán

Resultado de la investigación: Article

4 Citas (Scopus)

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.

Idioma originalEnglish
Páginas (desde-hasta)5732-5735
Número de páginas4
PublicaciónBioorganic and Medicinal Chemistry Letters
Volumen26
N.º23
DOI
EstadoPublished - 2016
Publicado de forma externa

Huella dactilar

TRPV Cation Channels
Coumarins
Prostaglandins
Nitric Oxide
Stomach
Lansoprazole
Ethylmaleimide
Sulfhydryl Compounds
Indomethacin
Animals
Ethanol
Animal Models
Experiments

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Citar esto

Sepulveda, Beatriz ; Quispe, Cristina ; Simirgiotis, Mario ; Torres-Benítez, Alfredo ; Reyes-Ortíz, Johanna ; Areche, Carlos ; García-Beltrán, Olimpo. / Gastroprotective activity of synthetic coumarins : Role of endogenous prostaglandins, nitric oxide, non-protein sulfhydryls and vanilloid receptors. En: Bioorganic and Medicinal Chemistry Letters. 2016 ; Vol. 26, N.º 23. pp. 5732-5735.
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abstract = "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.",
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Sepulveda, B, Quispe, C, Simirgiotis, M, Torres-Benítez, A, Reyes-Ortíz, J, Areche, C & García-Beltrán, O 2016, 'Gastroprotective activity of synthetic coumarins: Role of endogenous prostaglandins, nitric oxide, non-protein sulfhydryls and vanilloid receptors', Bioorganic and Medicinal Chemistry Letters, vol. 26, n.º 23, pp. 5732-5735. https://doi.org/10.1016/j.bmcl.2016.10.056

Gastroprotective activity of synthetic coumarins : Role of endogenous prostaglandins, nitric oxide, non-protein sulfhydryls and vanilloid receptors. / Sepulveda, Beatriz; Quispe, Cristina; Simirgiotis, Mario; Torres-Benítez, Alfredo; Reyes-Ortíz, Johanna; Areche, Carlos; García-Beltrán, Olimpo.

En: Bioorganic and Medicinal Chemistry Letters, Vol. 26, N.º 23, 2016, p. 5732-5735.

Resultado de la investigación: Article

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AU - Quispe, Cristina

AU - Simirgiotis, Mario

AU - Torres-Benítez, Alfredo

AU - Reyes-Ortíz, Johanna

AU - Areche, Carlos

AU - García-Beltrán, Olimpo

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N2 - 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.

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