来自明日叶的查尔酮衍生物、黄当归醇和4-羟基德里辛对胃H⁺，K⁺-ATP酶的抑制作用。

Inhibition of gastric H+, K(+)-ATPase by chalcone derivatives, xanthoangelol and 4-hydroxyderricin, from Angelica keiskei Koidzumi.

作者信息

Murakami S, Kijima H, Isobe Y, Muramatsu M, Aihara H, Otomo S, Baba K, Kozawa M

机构信息

Research Center, Taisho Pharmaceutical Co. Ltd, Saitama, Japan.

出版信息

J Pharm Pharmacol. 1990 Oct;42(10):723-6. doi: 10.1111/j.2042-7158.1990.tb06568.x.

DOI:10.1111/j.2042-7158.1990.tb06568.x

PMID:1982146

Abstract

Two chalcone derivatives, xanthoangelol (1) and 4-hydroxyderricin (II) isolated from Angelica keiskei Koidzumi, inhibited pig gastric H+, K(+)-ATPase with IC50 values of 1.8 and 3.3 microM, 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 microM, respectively. Proton transport in-vitro was inhibited by I or II, in a dose-dependent manner, 1 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 1 is due to the inhibition of gastric H+, K(+)-ATPase.

摘要

从明日叶中分离得到的两种查尔酮衍生物，即黄当归醇（1）和4-羟基德里辛（II），对猪胃H⁺，K⁺-ATP酶具有抑制作用，IC50值分别为1.8和3.3微摩尔。I或II的抑制作用在ATP方面具有竞争性，而在K⁺方面是非竞争性的。I和II还抑制K⁺刺激的对硝基苯磷酸酶，IC50值分别为1.3和3.5微摩尔。I或II以剂量依赖性方式抑制体外质子转运，腹腔注射100毫克/千克的1可显著抑制胃酸分泌和应激诱导的胃损伤形成。这些结果表明，1的抗分泌作用是由于对胃H⁺，K⁺-ATP酶的抑制。