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Inhibitory Constituents against Cyclooxygenases fromAralia cordata Thunb

  • Nguyen Hai Dang
  • XinFeng Zhang
  • MingShan Zheng
  • Kun Ho Son
  • Hyeun Wook Chang
  • Hyun Pyo Kim
  • KiHwan Bae
  • Sam Sik Kang
Article Drug design

Abstract

Seven diterpenes, four polyacetylenes, a lipid glycerol, and two sterols were isolated from the methylene chloride fraction of the root ofAralia cordata. Their chemical structures were determined as (-)-pimara-8(14),15-dien-19-oic acid (2), pimaric acid (3), (-)-kaur-16-en-19-oic acid (4), 17-hydroxy-ent-kaur-15-en-19-oic acid (9), 7α-hydroxy-(-)-pimara-8(14),15-dien-19-oic acid (10), 16α, 17-dihydroxy-(-)-kauran-19-oic acid (11), 16-hydroxy-17-isovaleroyloxy-ent-kauran-19-oic acid (12), falcarindiol (5), dehydrofalcarindiol (6), dehydrofalcarindiol-8-acetate (7), falcarindiol-8-acetate (8), alpha-mono palmitin (13), stigmasterol (1), and daucosterol (14) by the spectral evidences. These compounds were tested with COX-1 and COX-2 inhibition assays. This study found that compounds2, 4, 5, 6, 7, 8, and10 inhibited COX-1 dependent conversion of the exogenous arachidonic acid to PGE2 in a dose-dependent manner with IC50 values of 134.2 μM, 121.6 μM, 170 μM, 50.4 μM, 11.7 μM, 99.6 μM, and 69.6 μM, respectively. But, most of these compounds weakly inhibited COX-2 dependent PGE2 generation. Among them, only compound 4 showed relatively significant inhibitory activity (IC50: 127.6 μM).

Key words

Aralia cordata Diterpenoids Polyacetylenes Lipid glycerol Steroids Anti-inflammatory COX-1 COX-2 

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Copyright information

© The Pharmaceutical Society of Korea 2005

Authors and Affiliations

  • Nguyen Hai Dang
    • 5
  • XinFeng Zhang
    • 5
  • MingShan Zheng
    • 5
  • Kun Ho Son
    • 1
    • 5
  • Hyeun Wook Chang
    • 2
    • 5
  • Hyun Pyo Kim
    • 3
    • 5
  • KiHwan Bae
    • 4
    • 5
  • Sam Sik Kang
    • 4
    • 5
  1. 1.Department of Food and NutritionAndong National UniversityAndongKorea
  2. 2.College of PharmacyYeungnam UniversityGyongsanKorea
  3. 3.College of PharmacyKangwon National UniversityChuncheonKorea
  4. 4.Natural Products Research Institute and College of PharmacySeoul National UniversitySeoulKorea
  5. 5.College of PharmacyChungnam National UniversityTaejon,DaejeonKorea

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