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The Pharmaceutical Society of Korea (대한약학회)
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Inhibitory Constituents against Cyclooxygenases from Aralia cordata Thunb

  • Dang Nguyen Hai (College of Pharmacy, Chungnam National University) ;
  • Zhang XinFeng (College of Pharmacy, Chungnam National University) ;
  • Zheng MingShan (College of Pharmacy, Chungnam National University) ;
  • Son Kun Ho (Department of Food and Nutrition, Andong National University) ;
  • Chang Hyeun Wook (College of Pharmacy, Yeungnam University) ;
  • Kim Hyun Pyo (College of Pharmacy, Kangwon National University) ;
  • Bae KiHwan (College of Pharmacy, Chungnam National University) ;
  • Kang Sam Sik (Natural Products Research Institute and College of Pharmacy, Seoul National University)
  • Published : 2005.01.01
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Abstract

Seven diterpenes, four polyacetylenes, a lipid glycerol, and two sterols were isolated from the methylene chloride fraction of the root of Aralia 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), $7{\alpha}$-hydroxy-(-)-pimara-8(14), 15-dien-19-oic acid (10), $16\alpha$, 17 -dihydroxy-(-)-kauran-19-oic acid (11), 16-hydroxy-17-isovaleroyloxy-ent-kauran-19­oic 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 compounds 2, 4, 5, 6, 7, 8, and 10 inhibited COX-1 dependent conversion of the exogenous arachidonic acid to $PGE_2$ in a dose-dependent manner with $IC_{50}$ values of $134.2{\mu}M$, $121.6{\mu}M$, $170{\mu}M$, $50.4{\mu}M$, $11.7{\mu}M$, $99.6{\mu}M$, and $69.6{\mu}M$, respectively. But, most of these compounds weakly inhibited COX-2 dependent $PGE_2$ generation. Among them, only compound 4 showed relatively significant inhibitory activity $(IC_{50}\;:\;127.6{\mu}M)$.

Keywords

References

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