Inhibition of protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase by xanthones from Cratoxylum cochinchinense, and their kinetic characterization

Bioorganic & Medicinal Chemistry
Zuopeng LiKi Hun Park

Abstract

Cratoxylum cochinchinense displayed significant inhibition against protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase, both of which are key target enzymes to attenuate diabetes and obesity. The compounds responsible for both enzymes inhibition were identified as twelve xanthones (1-12) among which compounds 1 and 2 were found to be new ones. All of them simultaneously inhibited PTP1B with IC50s of (2.4-52.5 µM), and α-glucosidase with IC50values of (1.7-72.7 µM), respectively. Cratoxanthone A (3) and γ-mangostin (7) were estimated to be most active inhibitors against both PTP1B (IC50 = 2.4 µM for 3, 2.8 µM for 7) and α-glucosidase (IC50 = 4.8 µM for 3, 1.7 µM for 7). In kinetic studies, all isolated xanthones emerged to be mixed inhibitors of α-glucosidase, whereas they behaved as competitive inhibitors of PTP1B. In time dependent experiments, compound 3 showed isomerization inhibitory behavior with following kinetic parameters: Kiapp = 2.4 µM; k5 = 0.05001 µM-1 S-1and k6 = 0.02076 µM-1 S-1.

Citations

Sep 5, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·Janar JenisKi Hun Park
Dec 11, 2019·Journal of Natural Medicines·Peeravat NatrsangaSanti Tip-Pyang
Jan 3, 2021·Fitoterapia·Vu Thi Kim OanhThanh Nguyen Le
Oct 20, 2020·International Journal of Biological Macromolecules·Abdul Bari ShahKi Hun Park
Aug 14, 2021·Journal of Receptor and Signal Transduction Research·Shahin AhmadiAli Almasirad
Aug 28, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Massimo GenovesePaolo Paoli

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