Departamento de Farmacologia, Setor de Ciências Biológicas, Universidade Federal do Paraná, Curitiba, PR, Brazil.
Programa de Pós-Graduação em Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade do Vale do Itajaí, Itajaí, SC, Brazil.
Inflammopharmacology. 2018 Apr;26(2):521-530. doi: 10.1007/s10787-017-0378-4. Epub 2017 Jul 28.
Arctium lappa L., popularly known as burdock, is a medicinal plant used worldwide. The antiulcer and gastric-acid antisecretory effects of ethanolic extract from roots of Arctium lappa (EET) were already demonstrated. However, the mechanism by which the extract reduces the gastric acid secretion remains unclear. Therefore, this study was designed to evaluate the antisecretory mode of action of EET.
The effects of EET on H, K-ATPase activity were verified in vitro, whereas the effects of the extract on cholinergic-, histaminergic- or gastrinergic-acid gastric stimulation were assessed in vivo on stimulated pylorus ligated rats. Moreover, ex vivo contractility studies on gastric muscle strips from rats were also employed.
The incubation with EET (1000 µg/ml) partially inhibited H, K-ATPase activity, and the intraduodenal administration of EET (10 mg/kg) decreased the volume and acidity of gastric secretion stimulated by bethanechol, histamine, and pentagastrin. EET (100-1000 µg/ml) did not alter the gastric relaxation induced by histamine but decreased acetylcholine-induced contraction in gastric fundus strips. Interestingly, EET also reduced the increase in the gastric muscle tone induced by 40 mM KCl depolarizing solution, as well as the maximum contractile responses evoked by CaCl in Ca-free depolarizing solution, without impairing the effect of acetylcholine on fundus strips maintained in Ca -free nutritive solution.
Our results reinforce the gastric antisecretory properties of preparations obtained from Arctium lappa, and indicate that the mechanisms involved in EET antisecretory effects include a moderate reduction of the H, K-ATPase activity associated with inhibitory effects on calcium influx and of cholinergic pathways in the stomach muscle.
牛蒡，俗称牛蒡，是一种在世界各地使用的药用植物。已证明牛蒡根的乙醇提取物（EET）具有抗溃疡和胃酸分泌抑制作用。然而，提取物减少胃酸分泌的机制尚不清楚。因此，本研究旨在评估 EET 的抗分泌作用模式。
在体外验证 EET 对 H、K-ATP 酶活性的影响，而在刺激幽门结扎大鼠体内评估提取物对胆碱能、组胺能或胃泌素能胃酸刺激的影响。此外，还采用大鼠胃肌条的离体收缩性研究。
EET（1000μg/ml）孵育部分抑制 H、K-ATP 酶活性，EET（10mg/kg）十二指肠内给药可减少胆堿、组胺和五肽胃泌素刺激引起的胃酸分泌量和酸度。EET（100-1000μg/ml）不改变组胺诱导的胃松弛，但降低胃底带乙酰胆碱诱导的收缩。有趣的是，EET 还降低了 40mM KCl 去极化溶液引起的胃平滑肌张力增加，以及 Ca 2+ -free 去极化溶液中 CaCl 2 引起的最大收缩反应，而不损害乙酰胆碱对 Ca 2+ -free 营养液中维持的胃底带的作用。
我们的结果加强了牛蒡制剂的胃抗分泌特性，并表明 EET 抗分泌作用的机制包括对胃平滑肌中 H、K-ATP 酶活性的适度降低，以及对钙内流和胆碱能途径的抑制作用。
