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Anti-diabetic xanthones from the bark of Garcinia xanthochymus
Authors:Chi N Nguyen  Binh TD Trinh  Toan B Tran  Le-Thu T Nguyen  Anna K Jäger  Lien-Hoa D Nguyen
Institution:1. Natural Product and Medicinal Chemistry Lab, Faculty of Chemistry, VNUHCM–University of Science, 227 Nguyen Van Cu, Ho Chi Minh City, Viet Nam;2. Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark
Abstract:An ethyl acetate extract the bark of Garcinia xanthochymus exhibited strong inhibition towards α-glucosidase and PTP1B with IC50 values of 0.3 ± 0.1 μg/mL and 2.3 ± 0.4 μg/mL, respectively. Chemical constituents of the extract were therefore examined, and two new compounds, xanthochymusxanthones A (1) and B (2), along with ten known xanthones (312), were isolated. Their structures were determined using spectroscopic methods, mainly 1D and 2D NMR. Inhibitory activity of the isolated compounds was then tested, and subelliptenone F (12) showed significant effect towards α-glucosidase with IC50 value of 4.1 ± 0.3 μM (compared with acarbose, IC50 = 900.0 ± 3.0 μM) whilst xanthochymusxanthone B (2) exhibited remarkable activity towards PTP1B with IC50 value of 8.0 ± 0.6 μM (compared with RK682, IC50 = 4.4 ± 0.3 μM).
Keywords:Garcinia xanthochymus  Structure determination  Xanthones  Anti-diabetic activity  α-Glucosidase  PTP1B inhibition
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