The health benefits of
Tangeretin
September 2008
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Tangeretin (5,6,7,8,4'-pentamethoxyflavone) is a
polymethoxylated flavonoid concentrated in the peel of citrus
fruits. [2]

Tangeretin may have health benefits of brain protection.
Datla KP, and co-workers at Imperial College of Science,
London, demonstrated the neuro-protective effect of
tangeretin in the 6-hydroxydopamine (dopaminergic
neurotoxin) lesion rat model of Parkinson's disease.
Sub-chronic treatment of the rats with high doses of
tangeretin (20 mg/kg/day for 4 days; p.o.) before the
6-hydroxydopamine lesioning markedly reduced the loss of
both tyrosine hydroxylase positive cells and striatal
dopamine content. [4]

Tangeretin may offer health benefits of anti-cancer activities,
as it is one of the most effective at inhibiting cancer cell
growth in vitro and in vivo. Morley KL and co-workers at
London Health Sciences Centre, Ont., Canada, found it
inhibited proliferation in a dose- and time-dependent
manner, and blocked cell cycle progression at G1 in human
breast cancer cell lines MDA-MB-435 and MCF-7 and
human colon cancer line HT-29. [1] While, a Spanish
research group at University of Murcia, Spain, noticed the
antimetastatic effect of tangeretin on an experimental model
of pulmonary metastasis. [3]

Depypere HT and co-workers at University Hospital, Ghent,
Belgium, found tangeretin to be an effective tumour growth
and invasion inhibitor in vitro of human MCF 7/6 breast
cancer cells. However, when added to the drinking water of
MCF 7/6 tumor-bearing mice it neutralises the beneficial
tumour-suppressing effect of tamoxifen. Tangeretin reduces
the number of natural killer cells. [5] This group further
pointed out two effects of tangeretin on cell-cell interactions.
Firstly, tangeretin upregulates the function of the
E-cadherin/catenin complex in human MCF-7/6 breast
carcinoma cells. This leads to firm cell-cell adhesion and
inhibition of invasion in vitro. Secondly, tangeretin
down-regulates the interleukin-2 receptor on T-lymphocytes
and natural killer cells. This leads to a decrease in the
cytotoxic competence of these immunocytes against cancer
cells!

Reference [1] Morley KL, et al, Tangeretin and nobiletin induce G1 cell
cycle arrest but not apoptosis in human breast and colon cancer cells.
Cancer Lett. 2007 Jun 18;251(1):168-78. Epub 2007 Jan 2. [2] Chen KH,  et
al, Tangeretin suppresses IL-1beta-induced cyclooxygenase (COX)-2
expression through inhibition of p38 MAPK, JNK, and AKT activation in
human lung carcinoma cells. Biochem Pharmacol. 2007 Jan
15;73(2):215-27. Epub 2006 Sep 22. [3] Martínez Conesa C, et al,
Treatment of metastatic melanoma B16F10 by the flavonoids tangeretin,
rutin, and diosmin. J Agric Food Chem. 2005 Aug 24;53(17):6791-7. [4]
Datla KP, et al, Tissue distribution and neuroprotective effects of citrus
flavonoid tangeretin in a rat model of Parkinson's disease. Neuroreport.
2001 Dec 4;12(17):3871-5. [5] Depypere HT, et al, Inhibition of tamoxifen's
therapeutic benefit by tangeretin in mammary cancer. Eur J Cancer. 2000
Sep;36 Suppl 4:S73. [6] The citrus methoxyflavone tangeretin affects
human cell-cell interactions. Adv Exp Med Biol. 2002;505:135-9.

This article can not be used as medical advice. Please, consult with your
medical doctor for any question or before taking any drug products and
supplements. ALL RIGHTS RESERVED zhion 2008