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

College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou 450046, China
Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment & Chinese Medicine Development of Henan Province, Zhengzhou 450046, China
Zhengzhou Key Laboratory of Chinese Medicine Quality Control and Evaluation, Zhengzhou 450046, China
College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, China
Authors to whom correspondence should be addressed.
Academic Editor: Lothar Brecker
Molecules 2019, 24(10), 1898;
Received: 7 April 2019 / Revised: 6 May 2019 / Accepted: 14 May 2019 / Published: 17 May 2019
(This article belongs to the Special Issue Investigation of the Molecular Interactions of Natural Products)
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(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. View Full-Text
Keywords: anthraquinones; pharmacodynamics; pharmacodynamics; pharmacokinetics; interaction anthraquinones; pharmacodynamics; pharmacodynamics; pharmacokinetics; interaction

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Li, R.-R.; Liu, X.-F.; Feng, S.-X.; Shu, S.-N.; Wang, P.-Y.; Zhang, N.; Li, J.-S.; Qu, L.-B. Pharmacodynamics of Five Anthraquinones (Aloe-emodin, Emodin, Rhein, Chysophanol, and Physcion) and Reciprocal Pharmacokinetic Interaction in Rats with Cerebral Ischemia. Molecules 2019, 24, 1898.

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