Inhibition of gastric H+, K(+)-ATPase activity by compounds from medicinal plants

Autor: Cristina Setim, Freitas, Cristiane Hatsuko, Baggio, Bárbara, Mayer, Ana Cristina, dos Santos, André, Twardowschy, Cid Aimbiré de Moraes, Santos, Maria Consuelo Andrade, Marques
Rok vydání: 2011
Předmět:
Zdroj: Natural product communications. 6(9)
ISSN: 1934-578X
Popis: 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.
Databáze: OpenAIRE