Butein benefits
updated on April 7, 2009              
What is butein?
Butein (3,4,2',4'-tetrahydroxychalone), a plant polyphenol, is a major
biologically active component of the stems of Rhus verniciflua Stokes. It
has long been used as a food additive and as an herbal medicine
throughout Asia. Butein is known to exhibit anti-inflammatory, anticancer
and antifibrogenic activities. [8]

What are the potential health benefits of butein?
Recent studies have demonstrated its potential health benefits on various
conditions.

Butein is a strong antioxidant
Butein inhibited iron-induced lipid peroxidation in rat brain homogenate in a
concentration-dependent manner with an IC50, 3.3+/-0.4 microM. It was as
potent as alpha-tocopherol in reducing the stable free radical
diphenyl-2-picrylhydrazyl (DPPH) with an IC0.200, 9.2+/-1.8 microM. Butein
was also found to inhibite copper-catalyzed oxidation of human low-density
lipoprotein (LDL). Spectral analysis revealed that butein was a chelator of
ferrous and copper ions. [8]

Breast Cancer
Estrogen has long been associated with the initiation and promotion of
breast cancer. Inhibiting estrogen synthesis can be effective in the
prevention and treatment of the disease. Some studies have shown the
potential benefits of butin on cancer prevention. Researchers from Hong
Kong found butin as a strong inhibitor among for aromastse with K(i) value
of 0.32 microM. In a cell proliferation study, the cell number increased by
treatment of 10 nM-testosterone was significantly reduced by 5 microM
butein. [1]

Lee SH from Wonkwang University, Korea, demonstrated the benefits of
butein on liver fibrosis induced by carbon tetrachloride (CCl4) in rats. The
results suggest the potential use of butein to serve as an antifibrogenic
agent by inhibition of collagen accumulation and lipid peroxidation, and by
down-regulation of the expression of both alpha1(I) collagen and TIMP-1
mRNA. [4]

Fibroblasts are believed to play an important role in promoting the growth
of breast cancer cells. Researchers from UC Irvine demonstrated that
butein was able to inhibit the clonogenic growth of small numbers of
UACC-812 breast cancer cells co-cultured with fibroblasts in vitro. [2]

Colon Cancer
Butein also exhibited degrees of inhibition on the cell proliferation of human
colon adenocarcinoma cell line 220.1. Butein (the most potent chalcone) at
2 microM concentration inhibited the incorporation of 14C-labelled
thymidine, uridine and leucine into the colon cancer cells whilst
5-fluorouracil (5-FU, a chemotherapeutic drug) at 50 microM concentration
could significantly inhibit only the uridine incorporation. [3]

Blood Pressure Lowering Effects
Butein, isolated from Dalbergia odorifera T. Chen, is found to be a
cAMP-specific phosphodiesterase inhibitor. It caused
endothelium-dependent relaxation of rat aorta precontracted with
phenylephrine. Its vasorelaxant effect depended on the endothelium and
was mediated by endothelium-derived relaxing factor (EDRF). [6]
Intravenous injection of butein was found to lower the arterial blood
pressure of anesthetized rats in a dose-dependent manner. Introduction of
butein into the rats significantly inhibited the plasma ACE activities in a
dose-dependent manner. Prior exposure of endothelium-intact aortic rings
to butein was also found to attenuate angiotensin I-induced contraction. [5]

Liver Protection
Hepatic stellate cells play a key role in the pathogenesis of hepatic fibrosis.
An in vitro study demonstrated the inhibitory effect of butein on the
activation and proliferation of rat primary cultured hepatic stellate cells.  
Butein is a potent inhibitor of rat stellate cell transformation. [7]

What are the side effects of butein?
Its side effects have not been reported in scientific journal, as of April 20,
3009.

REFERENCE [1] Wang Y, et al, The plant polyphenol butein inhibits testosterone-induced
proliferation in breast cancer cells expressing aromatase. Life Sci. 2005 May 20;77(1):39-51. [2]
Samoszuk M, Tan J, Chorn G. The chalcone butein from Rhus verniciflua Stokes inhibits clonogenic
growth of human breast cancer cells co-cultured with fibroblasts. BMC Complement Altern Med.
2005 Mar 9;5:5. [3] Yit CC, Das NP. Cytotoxic effect of butein on human colon adenocarcinoma cell
proliferation. Cancer Lett. 1994 Jul 15;82(1):65-72. [4] Lee SH, The chalcone butein from Rhus
verniciflua shows antifibrogenic activity. Planta Med. 2003 Nov;69(11):990-4 [5] Kang DG, et al,
Hypotensive effect of butein via the inhibition of angiotensin converting enzyme. Biol Pharm Bull.
2003 Sep;26(9):1345-7. [6] Yu SM, et al, Endothelium-dependent relaxation of rat aorta by butein, a
novel cyclic AMP-specific phosphodiesterase inhibitor. Eur J Pharmacol. 1995 Jun 23;280(1):69-77.
[7] Woo SW, et al, Butein suppresses myofibroblastic differentiation of rat hepatic stellate cells in
primary culture. J Pharm Pharmacol. 2003 Mar;55(3):347-52. [8] Cheng ZJ, et al,  Antioxidant
properties of butein isolated from Dalbergia odorifera. Biochim Biophys Acta. 1998 Jun
15;1392(2-3):291-9. [8] Manoj K. Pandey, Santosh K. Sandur, Bokyung Sung, Gautam Sethi,
Ajaikumar B. Kunnumakkara,  and Bharat B. Aggarwal Butein, a tetrahydroxychalcone, inhibits
nuclear factor (NF)-kappa B and NF-kB-regulated gene expression through direct inhibition of IkB
kinase beta  on cysteine-179 residue J. Biol. Chem, 10.1074/jbc.M700890200
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