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Sear~h for Inhibitors of Cytchronxe P450 3A4 froiyi foods

Research Project

Project/Area Number 14571999
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Chemical pharmacy
Research InstitutionKanazawa University

Principal Investigator

TSUKAMOTO Sachiko  Kanazawa University, Faculty of Pharmaceutical Sciences, Associate Professor, 薬学部, 助教授 (40192190)

Project Period (FY) 2002 – 2003
Project Status Completed (Fiscal Year 2003)
Budget Amount *help
¥3,400,000 (Direct Cost: ¥3,400,000)
Fiscal Year 2003: ¥1,800,000 (Direct Cost: ¥1,800,000)
Fiscal Year 2002: ¥1,600,000 (Direct Cost: ¥1,600,000)
Keywordscytochrome P450 / drug metabolism / food / grapefruit juice / white pepper / strawberry
Research Abstract

Cytochrome P450(CYP)enzymes are home-containing monooxygenases and constitute three families, CYP1, CYP2, and CYP3.These enzymes have been mainly expressed in liver microsomes, and are recognized to be responsible for drug metabolism, carcinogenesis, and degradation of xenobiotics. CYPs are also responsible for the biosynthesis of lipids, steroids, and other secondary metabolites.CYP3A4 is the most abundant enzyme in human liver microsomes ; approximately 30% of the total CYP was suggested to be CYP3A4.Recent investigations have shown that more than 50% of clinically used drugs are oxidized by CYP3A4.It is reported that concomitant oral administration of several foods and herbs affect drug metabolism in humans by inhibiting CYP3A4 activity and that grapefruit juice alters the pharmacokinetics of various drugs, including cyclosporine, midazolam, dihydropyridine-type calcium channel blockers, and triazolam.In the course of our study of.CYP inhibitors, we have reported the isolation and structure elucidation of furanocoumarins, paradisins A, B, and C, from grapefruit juice, bisalkaloids, dipiperamides A-E, from the white pepper Piper nigrum, and three glycosides from the strawberry Fragaria ananassa Duch.cv.Tochiotome.

Report

(3 results)
  • 2003 Annual Research Report   Final Research Report Summary
  • 2002 Annual Research Report
  • Research Products

    (20 results)

All Other

All Publications (20 results)

  • [Publications] Sachiko Tsukamoto: "Dipiperamides A, B, and C : bisalkaloids from the white pepper Piper nigrum inhibiting CYP3A4 activity"Tetrahedron. 58. 1667-1671 (2002)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Sachiko Tsukamoto: "CYP3A4 Inhibitory Activity of New Bisalkaloids Dipiperamides D and E and Cognate Alkaloids from the White Pepper"Bioorg.Med.Chem.. 10. 2981-2985 (2002)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Tomihisa Ohta: "Paradisin C : a new CYP3A4 inhibitor from grapefruit juice"Tetrahedron. 58. 6631-6635 (2002)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Tomihisa Ohta: "Localization and contents of paradisins, the most potent CYP3A4 inhibitors, in a grapefruit Citrus paradisii and grapefruit juice"Nat.Med.. 56. 264-267 (2002)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Tomihisa Ohta: "Dihydroxybergamottin Caproate as a Potent and Stable CYP3A4 Inhibitor."Bioorg.Med.Chem.. 10. 969-973 (2002)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Sachiko Tsukamoto: "Dipiperamides A, B, and C : bisalkaloids from the white pepper Piper nigrum inhibiting CYP3A4 activity"Tetrahedron. 58. 1667-1671 (2002)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Sachiko Tsukamoto: "CYP3A4 Inhibitory Activity of New Bisalkaloids Dipiperamides D and E and Cognate Alkaloids from the White Pepper"Bioorg.Med.Chem.. 10. 2981-2985 (2002)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Tomihisa Ohta: "Paradisin C : a new CYP3A4 inhibitor from grapefruit juice"Tetrahedron. 58. 6631-6635 (2002)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Tomihisa Ohta: "Localization and contents of paradisins, the most potent CYP3A4 inhibitors, in a grapefruit Citrus paradisii and grapefruit juice"Nat.Med.. 56. 264-267 (2002)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Tomihisa Ohta: "Dihydroxybergamottin Caproate as a Potent and Stable CYP3A4 Inhibitor."Bioorg.Med.Chem.. 10. 969-973 (2002)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      2003 Final Research Report Summary
  • [Publications] Sachiko Tsukamoto: "Dipiperamides A, B, and C : bisalkaloids from the white pepper Piper nigrum inhibiting CYP3A4 activity"Tetrahedron. 58(9). 1667-1671 (2002)

    • Related Report
      2003 Annual Research Report
  • [Publications] Sachiko Tsukamoto: "CYP3A4 Inhibitory Activity of New Bisalkaloids Dipiperamides D and E and Cognate Alkaloids from the White Pepper"Bioorg.Med.Chem.. 10(9). 2981-2985 (2002)

    • Related Report
      2003 Annual Research Report
  • [Publications] Tomihisa Ohta: "Paradisin C : a new CYP3A4 inhibitor from grapefruit juice"Tetrahedron. 58(33). 6631-6635 (2002)

    • Related Report
      2003 Annual Research Report
  • [Publications] Tomihisa Ohta: "Localization and contents of paradisins, the most potent CYP3A4 inhibitors, in a grapefruit Citrus paradisii and grapefruit juice"Nat.Med.. 56(6). 264-267 (2002)

    • Related Report
      2003 Annual Research Report
  • [Publications] Tomihisa Ohta: "Dihydroxybergamottin Caproate as a Potent and Stable CYP3A4 Inhibitor"Bioorg.Med.Chem.. 10(4). 969-973 (2002)

    • Related Report
      2003 Annual Research Report
  • [Publications] Sachiko Tsukamoto: "Dipiperamides A, B, and C : bisalkaloids from the white pepper Piper nigrum inhibiting CYP3A4 activity"Tetrahedron. 58(9). 1667-1671 (2002)

    • Related Report
      2002 Annual Research Report
  • [Publications] Tomihisa Ohta: "Dihydroxybergamottin Caproate as a Potent and Stable CYP3A4 Inhibitor"Bioorg. Med. Chem.. 10(4). 969-973 (2002)

    • Related Report
      2002 Annual Research Report
  • [Publications] Sachiko Tsukamoto: "CYP3A4 Inhibitory Activity of New Bisalkaloids Dipiperamides D and E and Cognate Alkaloids from the White Pepper"Bioorg. Med. Chem.. 10(9). 2981-2985 (2002)

    • Related Report
      2002 Annual Research Report
  • [Publications] Tomihisa Ohta: "Paradisin C : a new CYP3A4 inhibitor from grapefruit juice"Tetrahedron. 58(33). 6631-6635 (2002)

    • Related Report
      2002 Annual Research Report
  • [Publications] Tomihisa Ohta: "Localization and contents of paradisins, the most potent CYP3A4 inhibitors, in a grapefruit Citrus paradisii and grapefruit juice"Nat. Med. 56(6). 264-267 (2002)

    • Related Report
      2002 Annual Research Report

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Published: 2002-04-01   Modified: 2019-04-12  

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