A safety study of oral tangeretin and xanthohumol administration to laboratory mice.
BACKGROUND
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.


METHODS
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. Blood samples were collected for the analysis of a variety of haematological and biochemical parameters.


RESULTS
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.


CONCLUSIONS
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.
Vanhoecke
Barbara W
BW
Department of Gynaecological Oncology, De Pintelaan 185, University Hospital Ghent, B-9000 Ghent, Belgium. barbara_vanhoecke@hotmail.com
Delporte
Femke
F
Van Braeckel
Eva
E
Heyerick
Arne
A
Depypere
Herman T
HT
Nuytinck
Margareta
M
De Keukeleire
Denis
D
Bracke
Marc E
ME
D000284:Administration, Oral; D000818:Animals; D000830:Animals, Laboratory; D001835:Body Weight; D004353:Drug Evaluation, Preclinical / Q000009:adverse effects*; D005260:Female; D047309:Flavones / Q000008:administration & dosage / Q000009:adverse effects* / Q000494:pharmacology; D005419:Flavonoids; D051379:Mice; D008809:Mice, Inbred C3H; D008819:Mice, Nude; D009929:Organ Size; D010936:Plant Extracts / Q000008:administration & dosage / Q000009:adverse effects* / Q000494:pharmacology; D011427:Propiophenones / Q000008:administration & dosage / Q000009:adverse effects* / Q000494:pharmacology
D047309:Flavones; D005419:Flavonoids; D010936:Plant Extracts; D011427:Propiophenones; C059006:tangeretin; C104536:xanthohumol