Abstract
Meso-dihydroguaiaretic acid (MDGA) is a medicinal herbal product isolated from the aerial parts of Saururus chinensis that inhibits the cyclooxygenase-2 (COX-2)-dependent phase of prostaglandin D(2) (PGD(2)) generation in bone marrow-derived mast cells (BMMC) (IC(50) 9.8 microM). However, this compound did not inhibit COX-2 protein expression in BMMC at concentrations up to 30 microM, indicating that MDGA directly inhibits COX-2 activity. In addition, this compound consistently inhibited the production of leukotriene C(4) (IC(50) 1.3 microM). These results demonstrate that MDGA inhibits both COX-2 and 5-lipoxygenase. Furthermore, this compound strongly inhibited the degranulation reaction in BMMC (IC(50) 11.4 microM). Therefore, this compound might provide a basis for novel anti-inflammatory drug development.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / isolation & purification
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Arachidonic Acid / metabolism
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Bone Marrow Cells / drug effects*
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Bone Marrow Cells / enzymology
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Cells, Cultured
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Cyclooxygenase 2 Inhibitors / isolation & purification
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Cyclooxygenase 2 Inhibitors / pharmacology*
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Guaiacol / analogs & derivatives*
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Guaiacol / isolation & purification
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Guaiacol / pharmacology
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Lignans / isolation & purification
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Lignans / pharmacology*
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Lipoxygenase Inhibitors*
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Male
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Mast Cells / drug effects*
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Mast Cells / enzymology
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Mice
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Mice, Inbred BALB C
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Saururaceae*
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Cyclooxygenase 2 Inhibitors
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Lignans
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Lipoxygenase Inhibitors
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Arachidonic Acid
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dihydroguaiaretic acid
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Guaiacol