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印度黄檀冻干水提取物在大鼠、小鼠和豚鼠中的抗溃疡作用机制

Anti-ulcerogenic mechanisms of a lyophilized aqueous extract of Dalbergia monetaria L. in rats, mice and guinea-pigs.

作者信息

Cota R H, Grassi-Kassisse D M, Spadari-Bratfisch R C, Souza Brito A R

机构信息

Departamento de Fisiologia e Biofísica, Instituto de Biologia, Universidade Estadual de Campinas, São Paulo, Brazil.

出版信息

J Pharm Pharmacol. 1999 Jun;51(6):735-40. doi: 10.1211/0022357991772880.

Abstract

The decoction of Dalbergia monetaria L. is popularly used in Brazil for the treatment of gastric ulcer and the lyophilized aqueous extract (LAE) of D. monetaria has significant anti-ulcerogenic activity and inhibits gastric ulcer lesions induced by pylorus-ligature, ethanol and hypothermic-restraint stress. This work was conducted to identify the antiulcerogenic mechanisms of action of the LAE of D. monetaria. We analysed the effect of the LAE on prostaglandin E2 (PGE2) synthesis and on the characteristics (pH, volume and total acid content) of gastric juice. The antagonism between the LAE and histamine or carbachol was also analysed. The LAE increased gastric mucosal PGE2 synthesis compared with control (89.7+/-21.5 and 52.6+/-11.8 pg mg(-1), respectively) as assayed by enzyme immunoassay in the rat stomach. The LAE reduced the total acid content of gastric juice, but did not modify pH or gastric volume significantly, in Shay rats. Dose-response curves to histamine were shifted to the right in guinea-pig isolated right atria (pD2 values were 5.77+/-0.2 and 5.42+/-0.3, respectively, in the absence and presence of the LAE), with a significant reduction in maximum response (140+/-15.1 and 98+/-13.0, respectively). The same effect was observed when the agonist was isoprenaline. The LAE had no effect on the dose-response curve to carbachol in rat fundus strips. Thus, the protective effect of the LAE on induced gastric lesions might be because of synergistic effects, e.g. increased PGE2 synthesis and antagonism of H2 histamine and beta-adrenergic receptors, reducing gastric acid secretion. Increased PGE2 synthesis results in increased protection, and antagonism of H2 histamine and beta-adrenergic receptors reduces aggressive factors against the gastric mucosa.

摘要

巴西人普遍使用黑黄檀煎剂治疗胃溃疡,黑黄檀的冻干水提取物(LAE)具有显著的抗溃疡活性,可抑制幽门结扎、乙醇和低温束缚应激诱导的胃溃疡损伤。本研究旨在确定黑黄檀LAE的抗溃疡作用机制。我们分析了LAE对前列腺素E2(PGE2)合成以及胃液特性(pH值、体积和总酸含量)的影响。还分析了LAE与组胺或卡巴胆碱之间的拮抗作用。通过酶免疫测定法在大鼠胃中检测发现,与对照组相比,LAE可增加胃黏膜PGE2合成(分别为89.7±21.5和52.6±11.8 pg mg(-1))。在Shay大鼠中,LAE可降低胃液中的总酸含量,但对pH值或胃体积无显著影响。在豚鼠离体右心房中,组胺的剂量-反应曲线向右移动(分别在不存在和存在LAE的情况下,pD2值为5.77±0.2和5.42±0.3),最大反应显著降低(分别为140±15.1和98±13.0)。当激动剂为异丙肾上腺素时,观察到相同的效果。LAE对大鼠胃底条带中卡巴胆碱的剂量-反应曲线无影响。因此,LAE对诱导性胃损伤的保护作用可能是由于协同作用,例如增加PGE2合成以及对H2组胺和β-肾上腺素能受体的拮抗作用,从而减少胃酸分泌。PGE2合成增加导致保护作用增强,而对H2组胺和β-肾上腺素能受体的拮抗作用减少了对胃黏膜的侵袭因素。

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