TY - JOUR
T1 - Quercetin and its metabolites improve vessel function by inducing eNOS activity via phosphorylation of AMPK
AU - Shen, Y.
AU - Croft, Kevin
AU - Hodgson, Jonathan
AU - Kyle, Reece
AU - Lee, I.-L.E.
AU - Wang, Y.
AU - Stocker, R.
AU - Ward, Natalie
PY - 2012/10
Y1 - 2012/10
N2 - [Truncated abstract] Quercetin is a major flavonoid in a wide range of fruits and vegetables. Consumption of quercetin may contribute to a reduction in risk of cardiovascular disease (CVD). Following ingestion, flavonoids are metabolized rapidly by methylation or glucuronidation, which can alter their biological activity. Certain dietary flavonoids have been shown to upregulate the expression of adenosine monophosphate-activated protein kinase (AMPK). AMPK is a conserved key enzyme in cellular energy homeostasis that affects fatty acid oxidation. The aim of the present study was to investigate the effects of supraphysiological concentrations of quercetin and its methyl and glucuronide metabolites (3′-O-methyl-quercetin and quercetin-3-O-glucuronide) on activation of AMPK and eNOS in human aortic endothelial cells (HAECs) and endothelial function in isolated aortic rings from C57BL mice. We found that 5 and 10 μM quercetin and its metabolites, and pretreatment of arteries with quercetin and its metabolites can protect vessels against hypochlorous acid-induced endothelial dysfunction in isolated arteries (P <0.05). Inhibition of AMPK blocked these protective effects....
AB - [Truncated abstract] Quercetin is a major flavonoid in a wide range of fruits and vegetables. Consumption of quercetin may contribute to a reduction in risk of cardiovascular disease (CVD). Following ingestion, flavonoids are metabolized rapidly by methylation or glucuronidation, which can alter their biological activity. Certain dietary flavonoids have been shown to upregulate the expression of adenosine monophosphate-activated protein kinase (AMPK). AMPK is a conserved key enzyme in cellular energy homeostasis that affects fatty acid oxidation. The aim of the present study was to investigate the effects of supraphysiological concentrations of quercetin and its methyl and glucuronide metabolites (3′-O-methyl-quercetin and quercetin-3-O-glucuronide) on activation of AMPK and eNOS in human aortic endothelial cells (HAECs) and endothelial function in isolated aortic rings from C57BL mice. We found that 5 and 10 μM quercetin and its metabolites, and pretreatment of arteries with quercetin and its metabolites can protect vessels against hypochlorous acid-induced endothelial dysfunction in isolated arteries (P <0.05). Inhibition of AMPK blocked these protective effects....
U2 - 10.1016/j.bcp.2012.07.016
DO - 10.1016/j.bcp.2012.07.016
M3 - Article
SN - 0006-2952
VL - 84
SP - 1036
EP - 1044
JO - Biochemical Pharmacology
JF - Biochemical Pharmacology
IS - 8
ER -
