Effects of methyl gallate on arachidonic acid metabolizing enzymes: Cyclooxygenase-2 and 5-lipoxygenase in mouse bone marrow-derived mast cells

• Published in: Archives of pharmacal research Vol. 29; no. 10; pp. 874 - 878
• Main Authors: Kim, Se Jong, Jin, Meihua, Lee, Eunkyung, Moon, Tae Chul, Quan, Zhejiu, Yang, Ju Hye, Son, Kun Ho, Kim, Kil-Ung, Son, Jong Kun, Chang, Hyeun Wook
• Format: Journal Article
• Language: English
• Published: Korea (South) Pharmaceutical Society of Korea 01.10.2006; 대한약학회
• Subjects: Animals; anti-inflammatory agents; Arachidonate 5-Lipoxygenase - metabolism; arachidonic acid; Arachidonic Acid - metabolism; bone marrow; Bone Marrow Cells - drug effects; Bone Marrow Cells - enzymology; Cell Line, Tumor; Cyclooxygenase 2 - metabolism; Cyclooxygenase Inhibitors - isolation & purification; Cyclooxygenase Inhibitors - pharmacology; dose response; Dose-Response Relationship, Drug; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - isolation & purification; Enzyme Inhibitors - pharmacology; gallates; Gallic Acid - analogs & derivatives; Gallic Acid - chemistry; Gallic Acid - isolation & purification; Gallic Acid - pharmacology; inhibitory concentration 50; Interleukin-10 - pharmacology; Leukotriene C4 - antagonists & inhibitors; Leukotriene C4 - biosynthesis; leukotrienes; Lipopolysaccharides - pharmacology; lipoxygenase; Male; mast cells; Mast Cells - drug effects; Mast Cells - enzymology; Mice; Mice, Inbred BALB C; Molecular Structure; Paeonia - chemistry; Plant Extracts - chemistry; Plant Extracts - isolation & purification; Plant Extracts - pharmacology; Plant Leaves - chemistry; Plant Stems - chemistry; Prostaglandin D2 - antagonists & inhibitors; Prostaglandin D2 - biosynthesis; prostaglandin synthase; prostaglandins; protein synthesis; Stem Cell Factor - pharmacology; 약학
• ISSN: 0253-6269; 1976-3786
• DOI: 10.1007/BF02973908

Methyl gallate (MG) is a medicinal herbal product that is isolated fromPaeonia 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 μM. 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 μM, using a COX enzyme assay kit. However, at concentrations up to 80 μM, 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 μM. These results demonstrate that MG has a dual cyclooxygenase-2/5-lipoxygenase inhibitory activity, which provide the basis for novel anti-inflammatory drugs.