IngentaConnect Inhibition of H+/K+ ATPase in the gastroprotective effect of Bacc...

Authors: Freitas, Cristina S.¹; Baggio, Cristiane H.¹; Finau, Jaqueline¹; Anginoni, Margano¹; Pizzolatti, Moacir G.²; Santos, Adair R.S.³; Marques, Maria C.A.⁴

Source: Journal of Pharmacy and Pharmacology, Volume 60, Number 8, August 2008 , pp. 1105-1110(6)

Publisher: Pharmaceutical Press

Abstract:

Baccharis illinita DC (Compositae) is used in folk medicine to treat gastric disturbances. Preliminary studies with other extracts of B. Illinita showed gastric protection against ethanol-, indometacin- and stress-induced ulcers and the inhibition of gastric secretion. Based on these data, the aim of this study was to verify the pathways involved in the inhibition of gastric secretion. The chloroform extract (CE) of flowers from B. illinita (3, 10, 30 and 100 mg kg^-1 i.p.) tested on rats with pylorus ligature reduced the volume and the total acidity of gastric content by approximately 50% (ED50 = 69 mg kg^-1). Treatment with CE (100 mg kg^-1 i.p.) reduced the gastric total acidity stimulated by histamine, bethanechol and pentagastrin to 42%, 27% and 57% of that in the stimulated control group, respectively. The CE (10, 30 and 100 μM) inhibited H⁺/K⁺ ATPase activity in-vitro, with an IC50 of 37 μM. The isolated flavonoid luteolin (1, 3, 10 and 30 μM) also inhibited H⁺/K⁺ ATPase activity by 50%, at a dose of 30 μM. Our results suggest that the reduction in gastric secretion occurs through inhibition of H⁺/K⁺ ATPase, which is the final step in acid secretion and therefore one of the most important steps.

Document Type: Short communication

DOI: 10.1211/jpp.60.8.0017

Affiliations: 1: Department of Pharmacology, Sector of Biological Sciences, Universidade Federal do Paraná, Curitiba, 81531-990, PR, Brazil 2: Department of Chemistry, Universidade Federal de Santa Catarina, Florianópolis, SC, 88040-900, Brazil 3: Department of Physiological Sciences, Centre of Biological Sciences, Universidade Federal de Santa Catarina, Florianópolis, SC, 88040-900, Brazil 4: Department of Pharmacology, Sector of Biological Sciences, Universidade Federal do Paraná, Curitiba, 81531-990, PR, Brazil., Email: mconsu@ufpr.br

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Inhibition of H+/K+ ATPase in the gastroprotective effect of Baccharis illinita DC

Inhibition of H⁺/K⁺ ATPase in the gastroprotective effect of Baccharis illinita DC