Mesía-Vela Sonia, Bielavsky Monica, Torres Luce Maria Brandão, Freire Sonia Maria, Lima-Landman Maria Teresa R, Souccar Caden, Lapa Antonio José
Natural Products Section, Department of Pharmacology, Escola Paulista de Medicina, Universidade Federal de São Paulo, 04044-020 Rua 03 de Maio 100, São Paulo, SP, Brazil.
J Ethnopharmacol. 2007 May 4;111(2):403-8. doi: 10.1016/j.jep.2006.12.009. Epub 2006 Dec 15.
The freeze-dried aqueous extract (AE) from the aerial parts of Scoparia dulcis was tested for its effects on experimental gastric hypersecretion and ulcer in rodents. Administration of AE to animals with 4h pylorus ligature potently reduced the gastric secretion with ED(50)s of 195 mg/kg (rats) and 306 mg/kg (mice). The AE also inhibited the histamine- or bethanechol-stimulated gastric secretion in pylorus-ligated mice with similar potency suggesting inhibition of the proton pump. Bio-guided purification of the AE yielded a flavonoid-rich fraction (BuF), with a specific activity 4-8 times higher than the AE in the pylorus ligature model. BuF also inhibited the hydrolysis of ATP by H(+),K(+)-ATPase with an IC(50) of 500 microg/ml, indicating that the inhibition of gastric acid secretion of Scoparia dulcis is related to the inhibition of the proton pump. Furthermore, the AE inhibited the establishment of acute gastric lesions induced in rats by indomethacin (ED(50)=313 mg/kg, p.o.) and ethanol (ED(50)=490 mg/kg, p.o.). No influence of the AE on gastrointestinal transit allowed discarding a possible CNS or a cholinergic interaction in the inhibition of gastric secretion by the AE. Collectively, the present data pharmacologically validates the popular use of Scoparia dulcis in gastric disturbances.
对甜地锦地上部分的冻干水提取物（AE）进行了研究，以考察其对啮齿动物实验性胃酸分泌过多和溃疡的影响。给幽门结扎4小时的动物施用AE可有效减少胃酸分泌，大鼠和小鼠的半数有效剂量（ED50）分别为195mg/kg和306mg/kg。AE还以相似的效力抑制幽门结扎小鼠中组胺或氨甲酰甲胆碱刺激的胃酸分泌，提示其对质子泵有抑制作用。对AE进行生物导向纯化得到富含黄酮类化合物的组分（BuF），在幽门结扎模型中其比活性比AE高4至8倍。BuF还抑制H(+)，K(+)-ATP酶对ATP的水解，半数抑制浓度（IC50）为500μg/ml，表明甜地锦对胃酸分泌的抑制作用与对质子泵的抑制有关。此外，AE抑制吲哚美辛（口服ED50 = 313mg/kg）和乙醇（口服ED50 = 490mg/kg）诱导的大鼠急性胃损伤的形成。AE对胃肠转运没有影响，这排除了AE在抑制胃酸分泌过程中可能存在的中枢神经系统或胆碱能相互作用。总体而言，目前的数据从药理学角度证实了甜地锦在胃部疾病中的广泛应用。
