Abstract |
In the present study, an offline analytical method combining β1-adrenergic receptor/cell membrane chromatography (β1-AR/CMC) with ultra-performance liquid chromatography/mass spectrometry (UPLC/MS) was used for direct recognition, separation, and identification of β1-AR inhibitors from Evodia rutaecarpa (Juss) Benth, by which rutaecarpine and evodiamine were screened and identified as potential β1-AR antagonists and the β1-AR inhibition activity of them was confirmed by downregulation of cAMP and PKA in vitro test. In addition, the results of in vivo pharmacological trials revealed that rutaecarpine (1.1mg/ml) and evodiamine (1.1mg/ml) attenuated myocardial infarct size injured by myocardial ischemia/reperfusion, improved metabolism disorders between fatty acid and glucose, increased the content of ATP, Ca(2+)- ATPase activity and reduced the content of peroxisome proliferator-activated receptor α (PPARα) protein level. Thus, the β1-AR/CMC-offline-UPLC/MS method developed in this study could be used as an effective alternative for screening β1-AR binding bioactive components in traditional Chinese medicines and the bioactive components could be used to remedy cardiac diseases via energy modulation.
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Authors | Hui Xue, Yongjie Cheng, Xin Wang, Yuan Yue, Weifang Zhang, Xiaoni Li |
Journal | Journal of pharmaceutical and biomedical analysis
(J Pharm Biomed Anal)
Vol. 115
Pg. 307-14
(Nov 10 2015)
ISSN: 1873-264X [Electronic] England |
PMID | 26263059
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2015 Elsevier B.V. All rights reserved. |
Chemical References |
- Adrenergic beta-1 Receptor Antagonists
- Indole Alkaloids
- Quinazolines
- Receptors, Adrenergic, beta-1
- rutecarpine
- evodiamine
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Topics |
- Adrenergic beta-1 Receptor Antagonists
(isolation & purification, pharmacology, therapeutic use)
- Animals
- CHO Cells
- Cell Membrane
(drug effects, metabolism)
- Cell Survival
(drug effects)
- Chromatography, High Pressure Liquid
(methods)
- Cricetulus
- Energy Metabolism
(drug effects)
- Evodia
(chemistry)
- Indole Alkaloids
(isolation & purification, pharmacology, therapeutic use)
- Male
- Mass Spectrometry
(methods)
- Myocardial Reperfusion Injury
(metabolism, prevention & control)
- Quinazolines
(isolation & purification, pharmacology, therapeutic use)
- Rats, Wistar
- Receptors, Adrenergic, beta-1
(metabolism)
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