INHIBITION OF GASTRIC H+,K+-ATPASE BY CHALCONE DERIVATIVES, XANTHOANGELOL AND 4-HYDROXYDERRICIN, FROM ANGELICA-KEISKEI KOIDZUMI

被引:46
作者
MURAKAMI, S [1 ]
KIJIMA, H [1 ]
ISOBE, Y [1 ]
MURAMATSU, M [1 ]
AIHARA, H [1 ]
OTOMO, S [1 ]
BABA, K [1 ]
KOZAWA, M [1 ]
机构
[1] OSAKA UNIV PHARMACEUT SCI,MATSUBARA,OSAKA 580,JAPAN
关键词
D O I
10.1111/j.2042-7158.1990.tb06568.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Abstract— Two chalcone derivatives, xanthoangelol (I) and 4‐hydroxyderricin (II) isolated from Angelica keiskei Koidzumi, inhibited pig gastric H+, K+ ‐ATPase with IC50 values of 1.8 and 3.3 μM, respectively. The inhibition by I or II was competitive with respect to ATP and was non‐competitive with respect to K+. I and II also inhibited K+, stimulated p‐nitrophenyl phosphatase, with IC50 values of 1.3 and 3.5 μM, respectively. Proton transport in‐vitro was inhibited by I or II, in a dose‐dependent manner. I at 100 mg kg−1, i.p. significantly inhibited acid secretion and the formation of stress‐induced gastric lesions. These results suggest that the antisecretory effect of I is due to the inhibition of gastric H+, K+‐ATPase. 1990 Royal Pharmaceutical Society of Great Britain
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页码:723 / 726
页数:4
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