A medicinal extract of Scutellaria baicalensis and Acacia catechu acts as a dual inhibitor of cyclooxygenase and 5-lipoxygenase to reduce inflammation.
A mixed extract containing two naturally occurring flavonoids, baicalin from Scutellaria baicalensis and catechin from Acacia catechu, was tested for cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibition via enzyme, cellular, and in vivo models. The 50% inhibitory concentration for inhibition of both ovine COX-1 and COX-2 peroxidase enzyme activities was 15 microg/mL, while the mixed extract showed a value for potato 5-LOX enzyme activity of 25 microg/mL. Prostaglandin E2 generation was inhibited by the mixed extract in human osteosarcoma cells expressing COX-2, while leukotriene production was inhibited in both human cell lines, immortalized THP-1 monocyte and HT-29 colorectal adenocarcinoma. In an arachidonic acid-induced mouse ear swelling model, the extract decreased edema in a dose-dependent manner. When arachidonic acid was injected directly into the intra-articular space of mouse ankle joints, the mixed extract abated the swelling and restored function in a rotary drum walking model. These results suggest that this natural, flavonoid mixture acts via "dual inhibition" of COX and LOX enzymes to reduce production of pro-inflammatory eicosanoids and attenuate edema in an in vivo model of inflammation.
Burnett
B P
BP
Primus Pharmaceuticals, Inc, Scottsdale, AZ 85251, USA.
Jia
Q
Q
Zhao
Y
Y
Levy
R M
RM
D000045:Acacia / Q000737:chemistry*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage; D002392:Catechin / Q000008:administration & dosage; D002461:Cell Line, Transformed; D045744:Cell Line, Tumor; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D016861:Cyclooxygenase Inhibitors / Q000008:administration & dosage*; D015232:Dinoprostone / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000008:administration & dosage; D005419:Flavonoids / Q000008:administration & dosage; D019073:HT29 Cells; D006801:Humans; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy*; D016859:Lipoxygenase Inhibitors; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009000:Monocytes; D012516:Osteosarcoma; D010936:Plant Extracts / Q000008:administration & dosage*; D031364:Scutellaria baicalensis / Q000737:chemistry*; D012756:Sheep
D000893:Anti-Inflammatory Agents; D016861:Cyclooxygenase Inhibitors; D004791:Enzyme Inhibitors; D005419:Flavonoids; D016859:Lipoxygenase Inhibitors; D010936:Plant Extracts; C038044:baicalin; D002392:Catechin; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D015232:Dinoprostone