Inhibition of H+/K+ ATPase in the gastroprotective effect of Baccharis illinita DC.
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 microM) inhibited H+/K+ ATPase activity in-vitro, with an IC50 of 37 microM. The isolated flavonoid luteolin (1, 3, 10 and 30 microM) also inhibited H+/K+ ATPase activity by 50%, at a dose of 30 microM. 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.
Freitas
Cristina S
CS
Department of Pharmacology, Sector of Biological Sciences, Universidade Federal do Paraná, Curitiba, 81531-990, PR, Brazil.
Baggio
Cristiane H
CH
Finau
Jaqueline
J
Anginoni
Margano
M
Pizzolatti
Moacir G
MG
Santos
Adair R S
AR
Marques
Maria C A
MC
D000818:Animals; D001285:Atropine / Q000494:pharmacology; D031175:Baccharis / Q000737:chemistry; D018723:Bethanechol / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005260:Female; D035264:Flowers; D005744:Gastric Acid / Q000378:metabolism; D005745:Gastric Acidity Determination; D017506:H(+)-K(+)-Exchanging ATPase / Q000378:metabolism; D006632:Histamine / Q000378:metabolism; D047311:Luteolin / Q000494:pharmacology; D009853:Omeprazole / Q000494:pharmacology; D010418:Pentagastrin / Q000494:pharmacology; D010936:Plant Extracts / Q000494:pharmacology; D054328:Proton Pump Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013270:Stomach / Q000187:drug effects* / Q000201:enzymology
D010936:Plant Extracts; D054328:Proton Pump Inhibitors; D018723:Bethanechol; D001285:Atropine; D006632:Histamine; D017506:H(+)-K(+)-Exchanging ATPase; D010418:Pentagastrin; D009853:Omeprazole; D047311:Luteolin