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Article

High-Resolution PTP1B Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of PTP1B Inhibitors from Miconia albicans

by
Rita De Cássia Lemos Lima
1,
Kenneth T. Kongstad
1,
Lucília Kato
2,
Marcos José das Silva
3,
Henrik Franzyk
1 and
Dan Staerk
1,*
1
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark
2
Instituto de Química, Universidade Federal de Goiás, Goiânia 70040-010, Brazil
3
Instituto de Ciências Biológicas, Universidade Federal de Goiás, Goiânia 70040-010, Brazil
*
Author to whom correspondence should be addressed.
Molecules 2018, 23(7), 1755; https://doi.org/10.3390/molecules23071755
Submission received: 14 June 2018 / Revised: 9 July 2018 / Accepted: 12 July 2018 / Published: 17 July 2018
(This article belongs to the Section Natural Products Chemistry)
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Abstract

Protein tyrosine phosphatase 1B (PTP1B) is an intracellular enzyme responsible for deactivation of the insulin receptor, and consequently acts as a negative regulator of insulin signal transduction. In recent years, PTP1B has become an important target for controlling insulin resistance and type 2 diabetes. In the present study, the ethyl acetate extract of leaves of Miconia albicans (IC50 = 4.92 µg/mL) was assessed by high-resolution PTP1B inhibition profiling combined with HPLC-HRMS-SPE-NMR for identification of antidiabetic compounds. This disclosed eleven PTP1B inhibitors, including five polyphenolics: 1-O-(E)-caffeoyl-4,6-di-O-galloyl-β-d-glucopyranose (2), myricetin 3-O-α-l-rhamnopyranoside (3), quercetin 3-O-(2″-galloyl)-α-l-rhamnopyranoside (5), mearnsetin 3-O-α-l-rhamnopyranoside (6), and kaempferol 3-O-α-l-arabinopyranoside (8) as well as eight triterpenoids: maslinic acid (13), 3-epi-sumaresinolic acid (14), sumaresinolic acid (15), 3-O-cis-p-coumaroyl maslinic acid (16), 3-O-trans-p-coumaroyl maslinic acid (17), 3-O-trans-p-coumaroyl 2α-hydroxydulcioic acid (18), oleanolic acid (19), and ursolic acid (20). These results support the use of M. albicans as a traditional medicine with antidiabetic properties and its potential as a source of PTP1B inhibitors.
Keywords: Miconia albicans; type 2 diabetes; PTP1B; HPLC-HRMS-SPE-NMR Miconia albicans; type 2 diabetes; PTP1B; HPLC-HRMS-SPE-NMR
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MDPI and ACS Style

De Cássia Lemos Lima, R.; T. Kongstad, K.; Kato, L.; José das Silva, M.; Franzyk, H.; Staerk, D. High-Resolution PTP1B Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of PTP1B Inhibitors from Miconia albicans. Molecules 2018, 23, 1755. https://doi.org/10.3390/molecules23071755

AMA Style

De Cássia Lemos Lima R, T. Kongstad K, Kato L, José das Silva M, Franzyk H, Staerk D. High-Resolution PTP1B Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of PTP1B Inhibitors from Miconia albicans. Molecules. 2018; 23(7):1755. https://doi.org/10.3390/molecules23071755

Chicago/Turabian Style

De Cássia Lemos Lima, Rita, Kenneth T. Kongstad, Lucília Kato, Marcos José das Silva, Henrik Franzyk, and Dan Staerk. 2018. "High-Resolution PTP1B Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of PTP1B Inhibitors from Miconia albicans" Molecules 23, no. 7: 1755. https://doi.org/10.3390/molecules23071755

APA Style

De Cássia Lemos Lima, R., T. Kongstad, K., Kato, L., José das Silva, M., Franzyk, H., & Staerk, D. (2018). High-Resolution PTP1B Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of PTP1B Inhibitors from Miconia albicans. Molecules, 23(7), 1755. https://doi.org/10.3390/molecules23071755

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