Butein benefits
     
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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