Yeditepe University, Faculty of Pharmacy, Department of Pharmacognosy, Kayişdaği 34755, Istanbul, Turkey.
J Ethnopharmacol. 2010 Aug 19;131(1):17-21. doi: 10.1016/j.jep.2010.05.011. Epub 2010 May 19.
The aerial parts of Equisetum palustre L. are used to treat peptic ulcer disease in Turkey. In a previous study, a flavonol diglucoside i.e., kaempferol 3-O-1''-beta-D-glucopyranosyl-3-O-1'''-beta-D-glucopyranoside (KGG) was isolated as the major antiulcerogenic constituent from the plant.
The present study was undertaken to evaluate the antiulcer activity profile of KGG using various in vivo experimental ulcer models as well as by assessing gastric biochemical parameters.
KGG was obtained from the ethanol extract of the aerial parts of the plant by successive chromatographical methods. The activity profile of the compound was investigated using several ulcerogenesis models such as indomethacin-, indomethacin plus HCl/EtOH-, cysteamine-, serotonin-, N(G)-nitro-L-arginine methyl ester plus EtOH-, diethyldithiocarbamate-, N-ethylmaleimide plus EtOH-, water immersion and restraint stress-, pyloric ligation-induced ulcers. In addition, effects of KGG on the biochemical parameters of gastric juice; i.e., inhibition of titratable gastric acidity, acid output, gastric pH, gastric secretion volume and peptic activity were studied.
KGG exerted statistically significant gastroprotective activity against indomethacin-, indomethacin plus HCl/EtOH- and N-ethylmaleimide plus EtOH-induced ulcerogenesis. Moreover, KGG demonstrated weak activity against N(G)-nitro-L-arginine methyl ester plus EtOH, water immersion and immobilization-induced stress, pyloric ligation-induced and diethyldithiocarbamate-induced gastric ulcer models, and also it was ineffective in the prevention of ulcers induced by serotonin and cysteamine. On the other hand, among the gastric biochemical parameters studied, KGG was only found to increase the gastric acid pH from 2.03 to 3.35.
Results of this investigation have clearly demonstrated that KGG was found to improve the cytoprotective mechanisms of the gastric mucosa. On the other hand, a weak activity profile was observed on the parameters affecting the gastric acidity (water immersion and restraint-induced-, pyloric ligation-induced-ulcerogenesis and titratable acidity).
在土耳其,木贼的地上部分被用于治疗消化性溃疡疾病。在之前的研究中,一种黄酮醇双葡萄糖苷,即山柰酚 3-O-1''-β-D-吡喃葡萄糖基-3-O-1'''-β-D-吡喃葡萄糖苷(KGG)被分离为该植物的主要抗溃疡成分。
本研究旨在通过评估 KGG 对各种体内实验性溃疡模型的抗溃疡活性谱以及通过评估胃生化参数,来评估 KGG 的抗溃疡活性谱。
KGG 是通过连续的色谱方法从植物地上部分的乙醇提取物中获得的。该化合物的活性谱通过使用几种溃疡发生模型来研究,例如吲哚美辛、吲哚美辛加盐酸/乙醇、半胱氨酸、血清素、N(G)-硝基-L-精氨酸甲酯加乙醇、二乙基二硫代氨基甲酸盐、N-乙基马来酰亚胺加乙醇、水浸和束缚应激、幽门结扎诱导的溃疡。此外,还研究了 KGG 对胃液生化参数的影响,即抑制可滴定胃酸、酸分泌、胃 pH 值、胃分泌量和消化活性。
KGG 对吲哚美辛、吲哚美辛加盐酸/乙醇和 N-乙基马来酰亚胺加乙醇诱导的溃疡发生具有统计学显著的胃保护活性。此外,KGG 对 N(G)-硝基-L-精氨酸甲酯加乙醇、水浸和束缚应激诱导、幽门结扎诱导和二乙基二硫代氨基甲酸盐诱导的胃溃疡模型表现出较弱的活性,并且对血清素和半胱氨酸诱导的溃疡也无效。另一方面,在所研究的胃生化参数中,仅发现 KGG 能使胃酸 pH 值从 2.03 升高到 3.35。
本研究结果清楚地表明,KGG 被发现能改善胃黏膜的细胞保护机制。另一方面,在影响胃酸的参数(水浸和束缚诱导、幽门结扎诱导和可滴定酸度)上观察到较弱的活性谱。