Abstract
Methyl gallate (MG) is a medicinal herbal product that is isolated from Paeonia lactiflora that inhibits cyclooxygenase-2 (COX-2) dependent phases of prostaglandin D2 (PGD2) generation in bone marrow-derived mast cells (BMMC) in a concentration-dependent manner with an IC50 values of 17.0 microM. This compound also found inhibited the COX-2-dependent conversion of the exogenous arachidonic acid to PGD2 in a dose-dependent manner with an IC50 values of 19.0 microM, using a COX enzyme assay kit. However, at concentrations up to 80 microM, MG did not inhibit COX-2 protein expression in BMMC, indicating that MG inhibits COX-2 activity directly. Furthermore, MG consistently inhibited the production of leukotriene C4 (LTC4) in a dose dependent manner, with an IC50 value of 5.3 microM. These results demonstrate that MG has a dual cyclooxygenase-2/5-lipoxygenase inhibitory activity, which might provide the basis for novel anti-inflammatory drugs.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Arachidonate 5-Lipoxygenase / metabolism*
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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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Cell Line, Tumor
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Cyclooxygenase 2 / metabolism*
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Cyclooxygenase Inhibitors / isolation & purification
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Cyclooxygenase Inhibitors / pharmacology
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / isolation & purification
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Enzyme Inhibitors / pharmacology
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Gallic Acid / analogs & derivatives*
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Gallic Acid / chemistry
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Gallic Acid / isolation & purification
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Gallic Acid / pharmacology
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Interleukin-10 / pharmacology
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Leukotriene C4 / antagonists & inhibitors
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Leukotriene C4 / biosynthesis
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Lipopolysaccharides / pharmacology
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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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Molecular Structure
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Paeonia / chemistry
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology
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Plant Leaves / chemistry
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Plant Stems / chemistry
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Prostaglandin D2 / antagonists & inhibitors
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Prostaglandin D2 / biosynthesis
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Stem Cell Factor / pharmacology
Substances
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Cyclooxygenase Inhibitors
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Enzyme Inhibitors
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Lipopolysaccharides
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Plant Extracts
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Stem Cell Factor
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Interleukin-10
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Arachidonic Acid
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Leukotriene C4
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methyl gallate
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Gallic Acid
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Arachidonate 5-Lipoxygenase
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Cyclooxygenase 2
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Prostaglandin D2