Yagi T, Yamauchi K, Kuwano S
Faculty of Pharmaceutical Sciences, Mukogawa Women's University, Hyogo, Japan.
J Pharm Pharmacol. 1997 Jan;49(1):22-5. doi: 10.1111/j.2042-7158.1997.tb06745.x.
This study aimed to explore the mechanism involved in the synergistic purgative action of aloe-emodin anthrone and rhein anthrone, the active metabolites of sennoside C. Aloe-emodin anthrone and rhein anthrone, and their equimolar mixture, induced excretion of an approximately equal number of faeces by intracaecal administration at a dose of 23.2 mumol kg-1 in mice (= 1.0 standard dose). The number of wet faeces induced by aloe-emodin anthrone was less than those of rhein anthrone and the mixture. At the same dose, rhein anthrone and the mixture significantly stimulated large intestinal propulsion, though aloe-emodin anthrone had little stimulatory effect. Aloe-emodin anthrone and rhein anthrone decreased net water absorption but could not reverse it to the net secretion at 1/2 dose. The mixture significantly decreased net water absorption and reversed it to the net secretion at this dose. These anthrones did not stimulate mucus secretion in the colon at 1/2 dose. We concluded that the synergistic purgative effect of aloe-emodin anthrone and rhein anthrone in mice results from synergistic stimulation of large intestinal transit and large intestinal water secretion.
本研究旨在探讨番泻苷C的活性代谢产物芦荟大黄素蒽酮和大黄酸蒽酮协同致泻作用的机制。芦荟大黄素蒽酮和大黄酸蒽酮及其等摩尔混合物,以23.2 μmol kg-1的剂量经盲肠内给药(相当于1.0标准剂量),在小鼠中诱导排出数量大致相等的粪便。芦荟大黄素蒽酮诱导的湿粪数量少于大黄酸蒽酮及其混合物。在相同剂量下,大黄酸蒽酮及其混合物显著刺激大肠推进运动,而芦荟大黄素蒽酮几乎没有刺激作用。芦荟大黄素蒽酮和大黄酸蒽酮可降低净吸水量,但在1/2剂量时不能将其逆转为净分泌量。该混合物在该剂量下显著降低净吸水量并将其逆转为净分泌量。这些蒽酮在1/2剂量时不刺激结肠黏液分泌。我们得出结论,芦荟大黄素蒽酮和大黄酸蒽酮在小鼠中的协同致泻作用源于对大肠转运和大肠水分泌的协同刺激。