EGFR
16 μM (IC 50 , in HepG2 cells)
PDE4
10.4 μM (IC 50 )
Butein potently inhibits cAMP-specific phosphodiesterase (type IV) activity with an IC 50 of 10.4±0.4 μM. In contrast, phosphodiesterase I, III and V activities were inhibited by Butein above 100 μM. Butein, a plant polyphenol, is a specific protein tyrosine kinase inhibitor. Butein inhibits not only the EGF-stimulated auto-phosphotyrosine level of EGFR in HepG2 cells but also tyrosine-specific protein kinase activities of EGFR (IC 50 =16 μM) and p60 c-src (IC 50 =65 μM) in vitro. Butein (10, 20, and 40 μM; 24, 48, and 72 hours) inhibits cell growth in a dose- and time-dependent manner. Butein exhibits anticancer activity through the inhibition of the activation of PKB/AKT and MAPK pathways, which are two pathways known to be involved in resistance to cisplatin. Butein (20 µM) decreases phosphorylation of AKT, ERK and p38 following 24 h of co-treatment with Cisplatin (20 µM).
Cell Viability Assay
Western Blot Analysis
Butein (2 mg/kg every 2 days) in combination with Cisplatin (2 mg/kg every 2 days) for 3 weeks suppresses tumor growth in vivo.
Butrin, isobutrin, and butein from medicinal plant Butea monosperma selectively inhibit nuclear factor-κB in activated human mast cells: suppression of tumor necrosis factor-α, interleukin (IL)-6, and IL-8. Anti-inflammatory agent