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Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor. Butein potently inhibits the tyrosine kinase activity of the EGF receptor (IC50 = 65 μM) and p60c-src (IC50 = 65 μM). The inhibition is competitive with respect to ATP and non-competitive with respect to the substrate. Butein is also a potent antioxidant and antiinflammatory agent which has been shown to inhibit glutathione reductase and rat liver GST (glutathione-S-transferase (IC50 = 9 μM)). Butein has been reported to activate sirtuins and promote the survival of eukaryotic cells. The Sirtuins, SIRT1-4 and SIRT7 are deacetylases relevant to histone modification. Butein directly inhibits IKK and suggested to also display inhibition towards PDE (c-AMP dependent PDE-IV). Also a potential CYP19 (Aromatase) inhibitor.
1. Zhang, K., et al., 1994. Inhibitory effects of plant polyphenols on rat liver glutathione S-transferases. Biochemical pharmacology. 47(11): 2063-8. PMID: 8010991
2. Zhang, K., et al., 1997. Inhibition of glutathione reductase by plant polyphenols. Biochemical pharmacology. 54(9): 1047-53. PMID: 9374426
3. Chan, S C., et al., 1998. Three new flavonoids and antiallergic, anti-inflammatory constituents from the heartwood of Dalbergia odorifera. Planta medica. 64(2): 153-8. PMID: 9525107
4. Yang, E B., et al., 1998. Butein, a specific protein tyrosine kinase inhibitor. Biochemical and biophysical research communications. 245(2): 435-8. PMID: 9571170
5. Howitz, Konrad T., et al., 2003. Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan. Nature. 425(6954): 191-6. PMID: 12939617
See how others have used Butein. Click on the entry to view the PubMed entry .
PMID: # 26676515 Woo, SM. et al. 2016. Mol Med Rep. 13: 1091-6.
PMID: # 25962638 Bai, X. et al. 2015. Oncology reports. 33: 3085-92.
PMID: # 24722292 Cioce, M. et al. 2014. Cell Death Dis. 5: e1167.
PMID: # 24919544 Cho, SG. et al. 2014. J. Exp. Clin. Cancer Res. 33: 51.
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