Absorption, tissue distribution, tissue metabolism and safety of α-mangostin in mangosteen extract using mouse models

- The LD50 of α-mangostin (α-MG) is smaller than mangosteen extract (ME) in mice.
- The absorption of α-MG in ME is greater than pure α-MG in mice.
- The hepatic metabolism of α-MG in ME is slower than pure α-MG in mice.
- The intestinal metabolism of α-MG in ME is comparable to pure α-MG in mice.
- The tissue distribution of α-MG is affected by constituents in ME.

The commercially available herbal products as the form of extract were usually mixtures containing various compounds. In spite of the purported efficacy in each active constituent, the coexisting constituents in the herbal extract might interfere with the efficacy and safety and affect the pharmacokinetic properties of active constituents. To compare for the pharmacokinetic properties of α-mangostin, a major bioactive compound, in mangosteen extract and pure α-mangostin, the pharmacokinetics as well as tissue distribution, in vitro metabolism, plasma protein binding and safety evaluation were conducted in mice because a mouse model is required a small amount of compounds and useful to develop disease models. The absorption of α-mangostin was increased and hepatic metabolism of α-mangostin was decreased in mice treated with mangosteen extract. However, the intestinal metabolism α-mangostin is comparable and still extensive in mice treated with α-mangostin and mangosteen extract. Intraperitorial LC50 of α-mangostin and mangosteen extract was 150 and 231 mg/kg, respectively. These findings may be valuable to explain the different pharmacokinetics and safety of α-mangostin and mangosteen extract. Furthermore, these findings are useful to design the efficacy and safety investigation of α-mangostin or mangosteen extract in mice with disease models or combination therapies to extrapolate into the clinical levels.