Anti-inflammatory properties and inhibition of leukotriene C4 biosynthesis in vitro by flavonoid baicalein from Scutellaria baicalensis georgy roots.
Anti-inflammatory activity of baicalein (5,6,7-trioxyflavone-7-O-beta-D-glucuronide) was greater in the chronic inflammation model (rat adjuvant arthritis, ED50 = 120.6 mg/kg) than observed in the rat carrageenan-induced paw edema, ED50 > or = 200.0 mg/kg. A comparative study of the 5-lipoxygenase (5-LO) inhibitory activity of baicalein, BW 755 C, and hydroxamic acid arachidonate on leukotriene C4 (LTC4) biosynthesis by rat resident peritoneal macrophages stimulated with calcium ionophore (A 23186) showed that these drugs significantly inhibited LTC4 production, IC50: 9.5, 41.8, and 2.8 microM, respectively. This finding suggests that inhibition of the 5-LO pathway of arachidonic acid metabolism may be one of the mechanisms of baicalein's anti-inflammatory activity.
Butenko
I G
IG
State Scientific Center of Drugs, Kharkov, Ukraine.
Gladtchenko
S V
SV
Galushko
S V
SV
D015772:4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D001095:Arachidonic Acids / Q000494:pharmacology; D001169:Arthritis, Experimental / Q000188:drug therapy*; D002351:Carrageenan / Q000633:toxicity; D004008:Diclofenac / Q000494:pharmacology; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D044950:Flavanones; D005419:Flavonoids / Q000494:pharmacology* / Q000627:therapeutic use; D006877:Hydroxamic Acids / Q000494:pharmacology; D007249:Inflammation / Q000188:drug therapy*; D017997:Leukotriene C4 / Q000037:antagonists & inhibitors*; D016859:Lipoxygenase Inhibitors; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051381:Rats; D017208:Rats, Wistar
D001095:Arachidonic Acids; D044950:Flavanones; D005419:Flavonoids; D006877:Hydroxamic Acids; D016859:Lipoxygenase Inhibitors; D004008:Diclofenac; D017997:Leukotriene C4; C006680:baicalein; D015772:4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine; C060260:arachidonate hydroxamic acid; D002351:Carrageenan