Inhibition of gastric H+,K+-ATPase and acid secretion by cassigarol A (cas 106387-02-4), a polyphenol from Cassia garrettiana Craib

Add time:07/25/2019    Source:sciencedirect.com

The effects of cassigarol A, a naturally occurring polyphenol, on gastric H+,K+-ATPase and gastric acid secretion were studied. Cassigarol A inhibited H+,K+-ATPase and K-stimulated p-nitrophenyl phosphatase from hog gastric mucosa with 50% inhibition of 1.2 × 10−6 and 6.3 × 10−6 M, respectively. The kinetic study showed that the inhibition of H+,K+-ATPase by cassigarol A was competitive with respect to ATP and non-competitive with respect to K+. Cassigarol A inhibited both H+,K+-ATPase-mediated proton transport and 2-deoxy-d-glucose-induced acid secretion. On the other hand, cassigarol A acetate, in which phenolic hydroxy groups are acetylated, was not effective in the inhibition of enzyme activity and acid secretion. These results indicate that cassigarol A is a potent inhibitor of gastric H+,K+-ATPase, that the anti-secretory activity of cassigarol A is related to the inhibition of H+,K+-ATPase and that an important moiety of cassigarol A in the interaction with the enzyme is the phenolic hydroxy groups.

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