Pharmacology in Health Food: Metabolism of Quercetin In Vivo and Its Protective Effect Against Arteriosclerosis

Keisuke Ishizawa; Masanori Yoshizumi; Yoshichika Kawai; Junji Terao; Yoshitaka Kihira; Yasumasa Ikeda; Shuhei Tomita; Kazuo Minakuchi; Koichiro Tsuchiya; Toshiaki Tamaki

doi:10.1254/jphs.10R38FM

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Pharmacology in Health Food:
Metabolism of Quercetin In Vivo and Its Protective Effect Against Arteriosclerosis

Keisuke Ishizawa, Masanori Yoshizumi, Yoshichika Kawai, Junji Terao, Yoshitaka Kihira, Yasumasa Ikeda, Shuhei Tomita, Kazuo Minakuchi, Koichiro Tsuchiya, Toshiaki Tamaki

Author information

Keisuke Ishizawa
Department of Medical Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School, Japan
Masanori Yoshizumi
Department of Pharmacology, Nara Medical University School of Medicine, Japan
Yoshichika Kawai
Department of Food Science, Institute of Health Bioscience, The University of Tokushima Graduate School, Japan
Junji Terao
Department of Food Science, Institute of Health Bioscience, The University of Tokushima Graduate School, Japan
Yoshitaka Kihira
Department of Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School, Japan
Yasumasa Ikeda
Department of Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School, Japan
Shuhei Tomita
Department of Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School, Japan
Kazuo Minakuchi
Department of Clinical Pharmacy, Institute of Health Bioscience, The University of Tokushima Graduate School, Japan
Koichiro Tsuchiya
Department of Medical Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School, Japan
Toshiaki Tamaki
Department of Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School, Japan

Keywords: quercetin glucuronide, cardiovascular disease, vascular smooth muscle cell, health food

JOURNAL FREE ACCESS

2011 Volume 115 Issue 4 Pages 466-470

DOI https://doi.org/10.1254/jphs.10R38FM

View "Advance Publication" version (March 24, 2011).

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Abstract

Quercetin, a member of the bioflavonoids family, has been proposed to have anti-atherogenic, anti-inflammatory, and anti-hypertensive properties leading to the beneficial effects against cardiovascular diseases. It was recently demonstrated that quercetin 3-O-β-D-glucuronide (Q3GA) is one of the major quercetin conjugates in human plasma, in which the aglycone could not be detected. Although most of the in vitro pharmacological studies have been carried out using only the quercetin aglycone form, experiments using Q3GA would be important to discover the preventive mechanisms of cardiovascular diseases by quercetin in vivo. Therefore we examined the effects of the chemically synthesized Q3GA, as an in vivo form, on vascular smooth muscle cell (VSMC) disorders related to the progression of arteriosclerosis. Platelet-derived growth factor–induced cell migration and proliferation were inhibited by Q3GA in VSMCs. Q3GA attenuated angiotensin II–induced VSMC hypertrophy via its inhibitory effect on JNK and the AP-1 signaling pathway. Q3GA scavenged 1,1-diphenyl-2-picrylhydrazyl radical measured by the electron paramagnetic resonance method. In addition, immunohistochemical studies with monoclonal antibody 14A2 targeting the Q3GA demonstrated that the positive staining specifically accumulates in human atherosclerotic lesions, but not in the normal aorta. These findings suggest Q3GA would be an active metabolite of quercetin in plasma and may have preventative effects on arteriosclerosis relevant to VSMC disorders.

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