Absorption, tissue distribution, tissue metabolism and safety of α-mangostin in mangosteen extract using mouse models.
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.
College of Pharmacy and BK21 PLUS R-FIND Team, Dongguk University-Seoul, 32 Dongguk-lo, Ilsandong-gu, Goyang, Gyeonggi-do 410-820, South Korea. Electronic address: choiyh@dongguk.edu.
Young Hee
YH
Choi
College of Pharmacy and BK21 PLUS R-FIND Team, Dongguk University-Seoul, 32 Dongguk-lo, Ilsandong-gu, Goyang, Gyeonggi-do 410-820, South Korea.
Seung Yon
SY
Han
College of Pharmacy and BK21 PLUS R-FIND Team, Dongguk University-Seoul, 32 Dongguk-lo, Ilsandong-gu, Goyang, Gyeonggi-do 410-820, South Korea.
You-Jin
YJ
Kim
College of Pharmacy and BK21 PLUS R-FIND Team, Dongguk University-Seoul, 32 Dongguk-lo, Ilsandong-gu, Goyang, Gyeonggi-do 410-820, South Korea.
Young-Mi
YM
Kim
College of Pharmacy and BK21 PLUS R-FIND Team, Dongguk University-Seoul, 32 Dongguk-lo, Ilsandong-gu, Goyang, Gyeonggi-do 410-820, South Korea. Electronic address: f2744@dongguk.edu.
Young-Won
YW
Chin
D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D029762:Garcinia mangostana / Q000737:chemistry*; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D023421:Models, Animal; D010936:Plant Extracts / Q000009:adverse effects / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D044004:Xanthones / Q000009:adverse effects / Q000493:pharmacokinetics*
D001798:Blood Proteins; D010936:Plant Extracts; D044004:Xanthones; C021053:mangostin
Absorption; Mangosteen extract; Mouse; Pharmacokinetics; Safety; α-Mangostin