Pharmacokinetics of α-mangostin in rats after intravenous and oral application.
METHODS
The xanthone α-mangostin is one of the major bioactive secondary metabolites in Garcinia mangostana. Until now, in vivo studies on the absorption, bioavailability, disposition, and metabolism of α-mangostin are limited.


RESULTS
In the present study, an LC-MS/MS assay has been established for the determination of α-mangostin in rat plasma. The validated method was used successfully to support pharmacokinetic studies in rats after intravenous (i.v.) and oral administration. Both non-compartmental and compartmental analyses were performed, where the two-compartment body model had a good fit with the i.v. data. Following i.v. administration, the disposition of α-mangostin in rat plasma was biphasic, subdivided into a fast distribution and a slow elimination phase. The half-life of the distribution phase was 3 min, and that of the terminal elimination phase 3.5 h, indicating a high tissue binding. However, for oral administration, the bioavailability was so low that it was not possible to obtain a full concentration-time profile.


CONCLUSIONS
Although pure α-mangostin has shown a variety of pharmacological activities in in vitro assays at present it is uncertain if the same magnitude of effects will be achieved in vivo when its low bioavailability is considered.
Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA.
Li
L
Li
Isabelle
I
Brunner
Ah-Reum
AR
Han
Matthias
M
Hamburger
Alan Douglas
AD
Kinghorn
Reginald
R
Frye
Veronika
V
Butterweck
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002853:Chromatography, Liquid; D029762:Garcinia mangostana / Q000737:chemistry; D006207:Half-Life; D007275:Injections, Intravenous; D016014:Linear Models; D008297:Male; D010936:Plant Extracts / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D053719:Tandem Mass Spectrometry; D044004:Xanthones / Q000493:pharmacokinetics*
D010936:Plant Extracts; D044004:Xanthones; C021053:mangostin