Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226001, U.P., India.
Phytomedicine. 2013 Oct 15;20(13):1180-5. doi: 10.1016/j.phymed.2013.06.017. Epub 2013 Jul 20.
Gastroprotective mechanism of peganine hydrochloride isolated from Peganum harmala seeds was investigated. Peganine hydrochloride was evaluated against cold restraint (CRU), aspirin (AS), alcohol (AL) and pyloric ligation (PL) induced gastric ulcer models in rats. Potential anti-ulcer activity of peganine was observed against CRU (50.0%), AS (58.5%), AL (89.41%) and PL (62.50%) induced ulcer models. The reference drug omeprazole (10mg/kg, p.o.) showed 77.45% protection against CRU, 49.97% against AS and 69.42% against PL model. Sucralfate, another reference drug (500mg/kg, p.o.) showed 62.50% protection in AL induced ulcer model. Peganine significantly reduced free acidity (33.38%), total acidity (38.09%) and upregulated mucin secretion by 67.91%, respectively. Further, peagnine significantly inhibited H(+) K(+)-ATPase activity in vitro with IC50 of 73.47μg/ml as compared to the IC50 value of omeprazole (30.24μg/ml) confirming its anti-secretory activity.
从骆驼蓬种子中分离得到的盐酸猪毛菜碱的胃保护机制。盐酸猪毛菜碱用于评价大鼠冷束缚（CRU）、阿司匹林（AS）、酒精（AL）和幽门结扎（PL）诱导的胃溃疡模型。盐酸猪毛菜碱对 CRU（50.0%）、AS（58.5%）、AL（89.41%）和 PL（62.50%）诱导的溃疡模型具有潜在的抗溃疡活性。参考药物奥美拉唑（10mg/kg，po）对 CRU 模型的保护率为 77.45%，对 AS 模型的保护率为 49.97%，对 PL 模型的保护率为 69.42%。另一种参考药物硫糖铝（500mg/kg，po）对 AL 诱导的溃疡模型的保护率为 62.50%。盐酸猪毛菜碱显著降低游离酸度（33.38%）、总酸度（38.09%），并分别使粘蛋白分泌增加 67.91%。此外，盐酸猪毛菜碱在体外显著抑制 H(+) K(+)-ATP 酶活性，IC50 为 73.47μg/ml，与奥美拉唑（IC50 为 30.24μg/ml）的 IC50 值相比，证实其具有抗分泌活性。
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