α-Glucosidase inhibition and antihyperglycemic activity of prenylated xanthones from Garcinia mangostana
Abstract
An ethanol extract of the fruit case of Garcinia mangostan, whose most abundant chemical species are xanthones, showed potent α-glucosidase inhibitory activity (IC(50)=3.2 μg/ml). A series of isolated xanthones (1-16) demonstrated modest to high inhibition of α-glucosidase with IC(50) values of 1.5-63.5 μM. In particular, one hitherto unknown xanthone 16 has a very rare 2-oxoethyl group on C-8. Kinetic enzymatic assays with a p-nitrophenyl glucopyranoside indicated that one of them, compound (9) exhibited the highest activity (K(i)=1.4 μM) and mixed inhibition. Using, a physiologically relevant substrate, maltose, as substrate, many compounds (6, 9, 14, and 15) also showed potent inhibition which ranged between 17.5 and 53.5 μM and thus compared favorably with deoxynojirimycin (IC(50)=68.8 μM). Finally, the actual pharmacological potential of the ethanol extract was demonstrated by showing that it could elicit reduction of postprandial blood glucose levels. Furthermore, the most active α-glucosidase inhibitors (6, 9, and 14) were proven to be present in high quantities in the native seedcase by a HPLC chromatogram.
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- Authors
- Ryu, H. W., Cho, J. K., Curtis-Long, M. J., Yuk, H. J., Kim, Y. S., Jung, S., Kim, Y. S., Lee, B. W., & Park, K. H.
- Affiliations
- Gyeongsang National University (KR)
- Rural Development Administration (KR)
- Corresponding author
- Park, Ki Hun
- Venue
- Phytochemistry
- Publisher
- Elsevier BV
- Published
- 2011-12
- Volume
- 72
- Issue
- 17
- Pages
- 2148-2154
- ISSN
- 0031-9422 (ISSN-L)
- OpenAlex
- W2058928007
- Cited by
- 161
- References
- 26
- Citations by year
- 2026: 3 · 2025: 8 · 2024: 4 · 2023: 8 · 2022: 14 · 2021: 14 · 2020: 9 · 2019: 19 · 2018: 13 · 2017: 16 · 2016: 17 · 2015: 12 · 2014: 8 · 2013: 10 · 2012: 6
- FWCI
- 9.22
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Phytochemistry (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Kyungpook National University
- Topics
- Life Sciences › Agricultural and Biological Sciences › Plant Science › Natural Compound Pharmacology Studies
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Natural Antidiabetic Agents Studies
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Bioactive natural compounds
- Keywords
- α-glucosidase inhibition, antidiabetic activity, prenylated xanthones, Garcinia mangostana, mixed-type inhibition, maltose, postprandial blood glucose, deoxynojirimycin, enzyme kinetics
- MeSH terms
- Animals, Blood Glucose, Disease Models, Animal, Enzyme Inhibitors, Fruit, Hyperglycemia, Hypoglycemic Agents, Male, Maltose, Phytotherapy, Plant Extracts, Seeds, Rats, Sprague-Dawley, 1-Deoxynojirimycin, Postprandial Period, Inhibitory Concentration 50, Garcinia mangostana, Xanthones, Rats, Glycoside Hydrolase Inhibitors
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