Pharmacokinetics of α-mangostin in rats after intravenous and oral application

✍ Scribed by Li Li; Isabelle Brunner; Ah-Reum Han; Matthias Hamburger; Alan Douglas Kinghorn; Reginald Frye; Veronika Butterweck

• Publisher: John Wiley and Sons
• Year: 2011
• Tongue: English
• Weight: 171 KB
• Volume: 55
• Category: Article
• ISSN: 1613-4125
• DOI: 10.1002/mnfr.201000511

✦ Synopsis

Abstract

Scope: 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.

Methods and 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.

Conclusion: 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.