Inhibition of lipoxygenases and cyclooxygenase-2 enzymes by extracts isolated from Bacopa monniera (L.) Wettst.
OBJECTIVE
Bacopa monniera Linn is described in the Ayurvedic Materia Medica, as a therapeutically useful herb for the treatment of inflammation. In the current study, we investigated the anti-inflammatory activity of methanolic extract of Bacopa monniera (BME). For some experiments EtOAc and bacoside fractions were prepared from BME. The effect of these extracts in modulating key mediators of inflammation was evaluated.


METHODS
Carrageenan-induced rat paw edema, rat mononuclear cells and human whole blood assay were employed as in vivo and in vitro models.


RESULTS
In carrageenan-induced rat paw edema, BME brought about 82% edema inhibition at a dose of 100mg/kg i.p. when compared to indomethacin (INDO) (3mg/kg) that showed 70% edema inhibition. BME also significantly inhibited 5-lipoxygenase (5-LOX), 15-LOX and cyclooxygenase-2 (COX-2) activities in rat monocytes in vivo. Among the fractions tested in vitro, EtOAc fraction possessed significant 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity with IC(50) value of 30 microg/ml compared to butylated hydroxyl toluene (IC(50) = 13 microg/ml). This fraction also exerted significant hydroxyl radical scavenging activity with IC(50) value of 25 microg/ml in comparison with quercetin (IC(50) = 5 microg/ml). Inhibitory effects of EtOAc and bacoside fractions on LOX and COX activities in Ca-A23187 stimulated rat mononuclear cells were also assessed. 5-LOX IC(50) values were 25 microg/ml for EtOAc, 68 microg/ml for bacosides and 2 microg/ml for nordihydroguaiaretic acid (NDGA) where as COX-2 IC(50) values were 1.32 microg/ml for EtOAc, 1.19 microg/ml for bacoside fraction and 0.23 microg/ml for indomethacin. EtOAc and bacoside fractions also brought about significant decrease in TNF-alpha release ex vivo.


CONCLUSIONS
Bacopa monniera possesses anti-inflammatory activity through inhibition of COX and LOX and downregulation of TNF-alpha.
Department of Biochemistry, University of Kerala, Kariavattom, Thiruvananthapuram, Kerala 695 581, India.
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D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D034681:Bacopa / Q000737:chemistry*; D051546:Cyclooxygenase 2 / Q000187:drug effects / Q000378:metabolism; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D015536:Down-Regulation / Q000187:drug effects; D004487:Edema / Q000188:drug therapy; D006801:Humans; D007194:India; D007213:Indomethacin / Q000494:pharmacology; D007249:Inflammation / Q000188:drug therapy* / Q000503:physiopathology; D020128:Inhibitory Concentration 50; D008084:Lipoxygenase / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008515:Medicine, Ayurvedic; D009000:Monocytes / Q000187:drug effects / Q000378:metabolism; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D014409:Tumor Necrosis Factor-alpha / Q000187:drug effects / Q000378:metabolism
D000893:Anti-Inflammatory Agents; D010936:Plant Extracts; D014409:Tumor Necrosis Factor-alpha; D008084:Lipoxygenase; D051546:Cyclooxygenase 2; D007213:Indomethacin