Description
Baicalein (491-67-8) is an inhibitor of protein tyrosine kinase in leukemia (CEM) cells. Induces cell cycle arrest and apoptosis.1?Originally reported as a selective inhibitor of 12-lipoxygenase, baicalein has since been shown to inhibit both 12-LO and 15-LO (IC50=0.64 μM for 12-LO and 1.6 μM for 15-LO).2 Baicalein displays anti-inflammatory activity and inhibits adjuvant-induced arthritis. Also inhibits prolyl oligopeptidase (IC50=36 μM).3
Chemical Properties
Yellow Crystalline Solid
Uses
An inhibitor of Ca2+ uptake, 5-LO, and 12-LO
Uses
inhibitor of lipoxidase and leukotriene biosynthesis
Uses
Baicalein is a flavonoid originally isolated from the roots of Scutellaria baicalensis Georgi. Several different functions of baicalein have been reported. Platelet 12-lipoxygenase is inhibited by baicalein with an ID50 value of 0.12 μM, with minimal inhibition of platelet cyclooxygenase-1 (IC50 = 0.83 mM). Baicalein inhibits lipid peroxidation, as assessed by production of TBARS, with an IC50 value of 5 μM. In addition to these effects, baicalein may play a role in apoptosis, as the compound inhibits cell growth of three human hepatocellular carcinoma cell lines with IC50 values ranging from 17-70 μg/ml.
Uses
An inhibitor of 12-lipoxygenase, leukotriene biosynthesis and release of lysosomal enzymes. It also inhibits cellular Ca2+ uptake and mobilization and adjuvant-induced arthritis. Baicalein is the fl
avonoid component of Nepalese and Sino-Japanese crude drugs.
Definition
ChEBI: A trihydroxyflavone with the hydroxy groups at positions C-5, -6 and -7.
General Description
Baicalein, a flavonoid, is a xanthine oxidase inhibitor. Anti-inflammatory effects of baicalein in peripheral human leukocytes has been studied.
Biological Activity
Inhibitor of 5- and platelet 12-lipoxygenases (IC 50 values are 9.5 and 0.12 mM respectively). Also inhibits Raf-mediated MEK-1 phosphorylation in C6 rat glioma cells and induces G1 and G2 cell cycle arrest by decreasing cdk1, cdk2, cyclin D2 and cyclin A expression. Anti-inflammatory in vivo .
Biochem/physiol Actions
The flavonoid component of Nepalese and Sino-Japanese crude drugs. Baicalein, a major flavone of Scutellariae baicalensis, inhibits the 12-lipoxygenase (12-LOX) pathway of arachidonic acid metabolism, which inhibits cancer cell proliferation and induces apoptosis.
References
1) Lee?et al. (2005),?Baicalein induced cell cycle arrest and apoptosis in human lung squamous carcinoma CH27 cells; Anticancer Res.,?25?959
2) Deschamps?et al. (2006),?Baicalein is a potent in vitro inhibitor against both reticulocyte 15-human and platelet 12-human lipoxygenases; Bioorg. Med. Chem.,?14?4295
3) Tarrago?et al. (2008),?Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor; Bioorg. Med. Chem.,?16?7516
