Tangeretin is one of the Citrus bioflavonoids. Tangeretin may play a role, like many flavonoids, in reducing the risk for certain cancers. Tangeretin has also shown promise in protecting nerve cells.
Tangeritin and cancer
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. Morley KL, Ferguson PJ,
Koropatnick J. Cancer Research Laboratory Program, London Regional Cancer
Program, Lawson Health Research Institute, London Health Sciences Centre,
London, Ont., Canada.
Tangeretin and nobiletin are citrus
flavonoids that are among the most effective at inhibiting cancer cell
growth in vitro and in vivo. The antiproliferative activity of tangeretin
and nobiletin was investigated in human breast cancer cell lines
MDA-MB-435 and MCF-7 and human colon cancer line HT-29. Both flavonoids
inhibited proliferation in a dose- and time-dependent manner, and blocked
cell cycle progression at G1 in all three cell lines. Conclusion:
Thus, tangeretin and nobiletin could be effective cytostatic anticancer
agents. Inhibition of proliferation of human cancers without inducing cell
death may be advantageous in treating tumors as it would restrict
proliferation in a manner less likely to induce cytotoxicity and death in
normal, non-tumor tissues.
Tangeretin Research Update
A safety study of oral tangeretin and
xanthohumol administration to
laboratory mice.
In Vivo. 2005 Jan-Feb;19(1):103-7.
The detection of molecular targets for flavonoids in cell
signalling has opened new perspectives for their application in medicine. Both
tangeretin, a citrus methoxyflavone, and xanthohumol, the main prenylated
chalcone present in hops (Humulus lupulus L.), act on the mitogen-activated
protein kinase pathway and await further investigation for administration in
vivo. A safety study was designed in laboratory mice
orally administered concentrates of purified tangeretin (1 x 10(-4) M) or
xanthohumol (5 x 10(-4) M) at libitum for 4 weeks. A reduction of the circulating lymphocyte number was noticed for tangeretin, while all other parameters were unaffected by treatment with either
tangeretin or xanthohumol. The parameters encompassed an integrity check of the
following tissues and organs: bone marrow, liver, exocrine pancreas, kidneys,
muscles, thyroid, ovaries and surrenal cortex. Furthermore, no differences were
noted in the metabolism of proteins, lipids,
carbohydrates and uric acid, as
well as in ion concentrations. All data indicate that oral
administration of tangeretin or xanthohumol to laboratory mice does not affect
major organ functions and opens the gate for further safety studies in humans.
Tangeretin inhibits extracellular-signal-regulated kinase (ERK)
phosphorylation.
FEBS Lett. 2005 Mar 14;579(7):1665-9.
Tangeretin is a methoxyflavone from citrus fruits, which inhibits growth of
human mammary cancer cells and cytolysis by natural killer cells. Attempting to
unravel the flavonoid's action mechanism, we found that it inhibited
extracellular-signal-regulated kinases 1/2 (ERK1/2) phosphorylation in a dose-
and time-dependent way. In human T47D mammary cancer cells this inhibition was
optimally observed after priming with estradiol. The spectrum of the
intracellular signalling kinase inhibition was narrow and comparison of
structural congeners showed that inhibition of ERK phosphorylation was not
unique for tangeretin. Our data add tangeretin to the list of small kinase
inhibitors with a restricted intracellular inhibition profile.
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.
Neuroprotective effects of a natural antioxidant tangeretin, a citrus flavonoid,
were elucidated in the 6-hydroxydopamine (6-OHDA) lesion rat model of
Parkinson's disease (PD), after bioavailability studies. Following the chronic
oral administration (10 mg/kg/day for 28 days), significant levels of tangeretin
were detected in the hypothalamus, striatum and hippocampus (3.88, 2.36 and 2.00
ng/mg, respectively). The levels in the liver and plasma were 0.59 ng/mg and
0.11 ng/ml respectively. Unilateral infusion of the dopaminergic neurotoxin,
6-hydroxydopamine (6-OHDA; 8 microg), onto medial forebrain bundle significantly
reduced the number of tyrosine hydroxylase positive (TH+) cells in the
substantia nigra and decreased striatal dopamine content in the vehicle treated
rats. Sub-chronic treatment of the rats with high doses of tangeretin (20
mg/kg/day for 4 days; p.o.) before 6-OHDA lesioning markedly reduced the loss of
both TH+ cells and striatal dopamine content. These studies, for the first time,
give evidence that tangeretin crosses the blood-brain barrier. The significant
protection of striato-nigral integrity and functionality by tangeretin suggests
its potential use as a neuroprotective agent.