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Danggui Buxue Decoction and its components dilate coronary artery through activating the inward rectification K+
Wenqiao An1, Qianqian Tian2, Pengmei Guo3
1Innovative Institute of Chinese Medicine and Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611100, China; School of Basic Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, 611100, China.
Insights
Danggui Buxue Decoction (DBD) and its active components, including quercetin, relax coronary arteries by activating inward rectification potassium (KIR) channels. This action increases coronary blood flow (CBF), offering potential therapeutic benefits for cardiovascular conditions.
Area of Science:
- Cardiovascular Pharmacology
- Traditional Chinese Medicine
- Molecular Biology
Background:
- Danggui Buxue Decoction (DBD) is a traditional Chinese medicine used for cardiovascular diseases like coronary heart disease.
- Abnormal coronary artery function is a key factor in cardiovascular disease, but DBD's mechanism for vasodilation is not fully understood.
Purpose of the Study:
- To investigate the vasodilatory effects of DBD and its key components on pre-constricted coronary arteries.
- To elucidate the molecular mechanisms underlying DBD's action on coronary arteries, focusing on ion channel interactions.
Main Methods:
- Isolated rat coronary artery rings were pre-constricted and treated with DBD and its components.
- In vivo studies assessed the impact on coronary blood flow (CBF).
- Molecular techniques including molecular docking, SPR, CETSA, and patch-clamp electrophysiology were employed to identify the mechanism.
Main Results:
- DBD and its active components (butylidenephthalide, ligustilide, calycosin, quercetin) demonstrated significant coronary artery dilation.
- These components were found to increase coronary blood flow (CBF).
- Mechanistic studies revealed that these compounds activate inward rectification potassium (KIR) channels, with quercetin shown to increase KIR current, an effect inhibited by BaCl2.
Conclusions:
- Active components of DBD, specifically butylidenephthalide, ligustilide, calycosin, and quercetin, activate KIR channels.
- This activation leads to coronary artery relaxation and increased CBF, clarifying a key mechanism of DBD in cardiovascular health.
Ethnopharmacological Relevance:
Danggui Buxue Decoction (DBD), a classic representative prescription of invigorating Qi and producing blood, is used to treat coronary heart disease angina pectoris and vascular injury diseases. Abnormal coronary artery is an important cause of cardiovascular disease. However, the mechanism of DBD dilates coronary arteries is still unclear.
Aim Of The Study:
This study aimed to elucidate the impacts and distinctions among DBD, Astragalus, Angelica sinensis, and identified active components on pre-constricted coronary arteries, as well as to delve deeper into their respective mechanisms.
Materials And Methods:
After the preconstriction of a rat isolated coronary artery ring with either 30 mM KCl or 200 nM U46619, the vascular tension was observed following the addition of DBD, and other components. Subsequently, the impact of these active components on coronary blood flow (CBF) was confirmed through in vivo testing. Further investigation into the underlying mechanism was carried out using a combination of blockers, molecular docking, surface plasmon resonance (SPR), cell heat transfer analysis (CETSA), and patch-clamp techniques.
Results:
In vitro experiments showed that DBD and its components butylidenephthalide, ligustilide, calycosin, and quercetin could dilate coronary artery preconstricted with either 30 mM KCl or 200 nM U46619. In addition, the active ingredient was found to significantly increase CBF. Mechanistically, BaCl2 was found to reduce the relaxation effect of the drug by adding a blocker. Molecular docking, SPR and CETSA results showed that the active ingredients had a strong binding potential with inward rectification K+ channels (KIR) channel protein. Patch clamp studies demonstrate that quercetin can increase KIR current, and BaCl2 can significantly reduce its current.
Conclusions:
The active components of DBD, butylidenephthalide, ligustilide, calycosin, and quercetin, activate KIR channels to relax coronary artery and increase CBF.
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