title: Inhibition of gastric H+, K(+)-ATPase activity by compounds from medicinal plants.
abstract: H+, K(+)-ATPase enzyme is a therapeutic target for the treatment of gastric disturbances. Several medicinal plants and isolated compounds inhibit the acid gastric secretion through interaction with the proton pump. In order to add new properties to some natural constituents, five compounds, a benzylated derivative of vincoside, a diterpene (abietic acid) and three alkaloids (cephaeline, vinblastine and vindoline), were tested for their activities on gastric H+, K(+)-ATPase isolated from rabbit stomach. All the compounds inhibited H+, K(+)-ATPase activity with varied potency. The IC50 value for benzylvincoside was 121 (50-293) microM, and for abietic acid 177 (148-211) microM. The alkaloids cephaeline, vinblastine and vindoline inhibited the H+, K(+)-ATPase activity with IC50 values of 194, 761 and 846 microM, respectively. The results suggest that benzylvincoside, abietic acid and cephaeline can be important sources for the development of anti-secretor agents.
authors.affiliation: Department of Pharmacology, Sector of Biological Sciences, Universidade Federal do Paraná, Centro Politécnico, CP 19031, CEP 81531-990, Curitiba, PR, Brazil.
authors.forename: Cristina Setim
authors.initials: CS
authors.lastname: Freitas
authors.forename: Cristiane Hatsuko
authors.initials: CH
authors.lastname: Baggio
authors.forename: Bárbara
authors.initials: B
authors.lastname: Mayer
authors.forename: Ana Cristina
authors.initials: AC
authors.lastname: dos Santos
authors.forename: André
authors.initials: A
authors.lastname: Twardowschy
authors.forename: Cid Aimbiré de Moraes
authors.initials: CA
authors.lastname: Santos
authors.forename: Maria Consuelo Andrade
authors.initials: MC
authors.lastname: Marques
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D017506:H(+)-K(+)-Exchanging ATPase / Q000378:metabolism; D008297:Male; D010946:Plants, Medicinal / Q000737:chemistry*; D054328:Proton Pump Inhibitors; D011817:Rabbits
chemical_list: D004791:Enzyme Inhibitors; D054328:Proton Pump Inhibitors; D017506:H(+)-K(+)-Exchanging ATPase