Butein potently inhibits cAMP-specific phosphodiesterase (type IV) activity with an IC50 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 (IC50=16 μM) and p60 (IC50=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
| Cell Line: |
HeLa cells |
| Concentration: |
10, 20, and 40 μM |
| Incubation Time: |
24, 48, and 72 hours |
| Result: |
Inhibited cell growth in a dose- and time-dependent manner. |
Western Blot Analysis
| Cell Line: |
HeLa cells |
| Concentration: |
20 µM |
| Incubation Time: |
24 hours |
| Result: |
Decreased phosphorylation of AKT, ERK and p38 co-treatment with Cisplatin (20 µM). |