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Absorption,tissue distribution,tissue metabolism and safety of α-mangostin in mangosteen extract using mouse models
Institution:1. Department of Food and Nutrition, Sunchon National University, Suncheon 540-950, Republic of Korea;2. Department of Bioscience and Biotechnology, Kyushu University, Fukuoka 812-8581, Japan;3. School of Food Science and Biotechnology, Kyungpook National University, Daegu 702-701, Republic of Korea;4. Jeonnam Institute of National Resources Research, Jangheung 529-851, Republic of Korea;5. Division of Applied Life Science, IALS, Graduate School of Gyeongsang National University, Jinju 660-701, Republic of Korea;1. Department of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, Taibah University, Al Madinah Al Munawwarah, Saudi Arabia;2. Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt;3. Department of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia;4. Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt;5. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia;6. Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assuit, Egypt;7. Cardiology Unit, College of Medicine, Taibah University, Al Madinah Al Munawwarah, Saudi Arabia;8. Department of Medicine, Faculty of Medicine, King Abdulaziz University, Jeddah, Saudi Arabia;1. Department of Pharmacy, Yijishan Hospital, Wannan Medical College, Wuhu, China;2. Anhui Provincial Engineering Technology Research Center of Polysaccharides Drug, Wuhu, China;1. Institute of Biotechnology, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet Road, Hanoi, Viet Nam;2. Graduate University of Science and Technology, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet Road, Hanoi, Viet Nam;3. Institute of Chemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet Road, Hanoi, Viet Nam;4. Center of Excellence for Innovation in Chemistry and Department of Chemistry, Faculty of Science, Mahidol University, Rama 6 Road, Bangkok 10400, Thailand;5. Department of Pharmacy and Pharmacology, University of Bath, Claverton Down Bath, BA2 7AY, Bath, UK
Abstract: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.
Keywords:α-Mangostin  Mangosteen extract  Pharmacokinetics  Mouse  Absorption  Safety
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