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

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Author(s)

    • TERAO Junji
    • Department of Food Science, Institute of Health Bioscience, The University of Tokushima Graduate School
    • KIHIRA Yoshitaka
    • Department of Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School
    • IKEDA Yasumasa
    • Department of Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School
    • TOMITA Shuhei
    • Department of Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School
    • MINAKUCHI Kazuo
    • Department of Clinical Pharmacy, Institute of Health Bioscience, The University of Tokushima Graduate School
    • TSUCHIYA Koichiro
    • Department of Medical Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School
    • TAMAKI Toshiaki
    • Department of Pharmacology, Institute of Health Bioscience, The University of Tokushima Graduate School

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-<I>O</I>-<I>β</I>-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.

Journal

  • Journal of Pharmacological Sciences

    Journal of Pharmacological Sciences 115(4), 466-470, 2011-04-20

    The Japanese Pharmacological Society

References:  46

Cited by:  1

Codes

  • NII Article ID (NAID)
    10029893264
  • NII NACSIS-CAT ID (NCID)
    AA11806667
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    13478613
  • NDL Article ID
    11049217
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  CJPref  NDL  J-STAGE 
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