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Pharmacodynamics of Five Anthraquinones (Aloe-emodin Emodin Rhein Chysophanol and Physcion) and Reciprocal Pharmacokinetic Interaction in Rats with Cerebral Ischemia

机译:五种蒽醌(芦荟大黄素大黄素大黄酸大麦酚和物理杀伤剂)在大鼠脑缺血中的药效动力学和相互的药代动力学相互作用

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摘要

(1) Background: Rhubarb anthraquinones—a class of components with neuroprotective function—can be used to alleviate cerebral ischemia reperfusion injury. (2) Methods: The three pharmacodynamic indicators are neurological function score, brain water content, and cerebral infarction area; UPLC-MS/MS was used in pharmacokinetic studies to detect plasma concentrations at different time points, and DAS software was used to calculate pharmacokinetic parameters in a noncompartmental model. (3) Results: The results showed that the pharmacodynamics and pharmacokinetics of one of the five anthraquinone aglycones could be modified by the other four anthraquinones, and the degree of interaction between different anthraquinones was different. The chrysophanol group showed the greatest reduction in pharmacodynamic indicators comparing with other four groups where the rats were administered one of the five anthraquinones, and there was no significant difference between the nimodipine group. While the Aloe-emodin + Physcion group showed the most obvious anti-ischemic effect among the groups where the subjects were administered two of the five anthraquinones simultaneously. Emodin, rhein, chrysophanol, and physcion all increase plasma exposure levels of aloe-emodin, while aloe-emodin lower their plasma exposure levels. (4) Conclusions: This experiment provides a certain preclinical basis for the study of anthraquinone aglycones against cerebral ischemia and a theoretical basis for the study of the mechanism of interaction between anthraquinones.
机译:(1)背景:大黄蒽醌是一种具有神经保护功能的成分,可用于减轻脑缺血再灌注损伤。 (2)方法:三个药效学指标为神经功能评分,脑含水量和脑梗死面积。 UPLC-MS / MS用于药代动力学研究,以检测不同时间点的血浆浓度,DAS软件用于计算非房室模型中的药代动力学参数。 (3)结果:结果表明,五个蒽醌苷元之一可以被另外四个蒽醌修饰,而不同蒽醌之间的相互作用程度是不同的。与其他四组(分别给大鼠施用五种蒽醌之一)相比,中苯三酚组的药效学指标下降幅度最大,尼莫地平组之间无显着差异。芦荟大黄素+ Physcion组在受试者同时给予五个蒽醌中的两个中显示出最明显的抗缺血作用。大黄素,大黄酸,大黄酚和physcion均可增加芦荟大黄素的血浆暴露水平,而芦荟大黄素可降低其血浆暴露水平。 (4)结论:该实验为蒽醌苷元抗脑缺血的研究提供了一定的临床前基础,为研究蒽醌之间的相互作用机理提供了理论基础。

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