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KMID : 0043320080310020210
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Archives of Pharmacal Research
2008 Volume.31 No. 2 p.210 ~ p.215
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The Effects of Isoimperatorin Isolated from Angelicae dahuricae on Cyclooxygenase-2 and 5-Lipoxygenase in Mouse Bone Marrow-derived Mast Cells
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Moon Tae-Chul
Jin Mei-Hua
Son Jong-Keun
Chang Hyun-Wook
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Abstract
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isoimperatorin (4-[(3-Methyl-2-butenyl)oxy]-7H-furo[3,2-g][1]benzopyran-7-one) is a medicinal herbal product that is isolated from the dried roots of Angelicae dahuricae. Isoimperatorin inhibits the cyclooxygenase-2 (COX-2) and COX-1-dependent phases of prostaglandin D2(PGD2) generation in bone marrow-derived mast cells (BMMC) in a concentration-dependent manner, with IC50 values of 10.7 μM and 24 μM, respectively. However, this compound was not able to inhibit COX-1 and 2 protein expression in BMMC that were treated with concentrations of up to 50 μM, which indicates that isoimperatorin directly inhibits COX-2 activity. Furthermore, this compound consistently inhibited the production of leukotriene C4(LTC4), as well as the degranulation reaction in BMMC, with an value of 5.7 μM and 9 μM, respectively, and these effects occurred in a dose dependent fashion. These results demonstrate that isoimperatorin has a dual cyclooxygenase-2 selective/5-lipoxygenase inhibitory activity, and therefore may provide the basis for novel anti-inflammatory drugs.
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KEYWORD
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Angelicae dahuricae, Isoimperatorin, Cyclooxygenase-1, 2, 5-Lipoxygenase, Bone marrow-derived mast cells
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