INHIBITION OF GASTRIC H+,K+-ATPASE AND ACID-SECRETION BY CASSIGAROL-A, A POLYPHENOL FROM CASSIA-GARRETTIANA CRAIB

被引：25

作者：

MURAKAMI, S ^{[1
]}

ARAI, I ^{[1
]}

MURAMATSU, M ^{[1
]}

OTOMO, S ^{[1
]}

BABA, K ^{[1
]}

KIDO, T ^{[1
]}

KOZAWA, M ^{[1
]}

机构：

[1] OSAKA UNIV PHARMACEUT SCI,MATSUBARA,OSAKA 580,JAPAN

来源：

BIOCHEMICAL PHARMACOLOGY | 1992年 / 44卷 / 01期

关键词：

D O I：

10.1016/0006-2952(92)90034-G

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 x 10(-6) and 6.3 x 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.

引用

页码：33 / 37

页数：5

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