2. Academic Validation
  3. High-Resolution PTP1B Inhibition Profiling Combined with HPLC-HRMS-SPE-NMR for Identification of PTP1B Inhibitors from Miconia albicans

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

  • Molecules. 2018 Jul 17;23(7):1755. doi: 10.3390/molecules23071755.
Rita de Cássia Lemos Lima 1,  Kenneth T Kongstad 2,  Lucília Kato 3,  Marcos José das Silva 4,  Henrik Franzyk 5,  Dan Staerk 6
Affiliations

Affiliations

  • 1 Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark. ritalemosrm@gmail.com.
  • 2 Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark. kenneth.kongstad@sund.ku.dk.
  • 3 Instituto de Química, Universidade Federal de Goiás, Goiânia 70040-010, Brazil. luciliakato@gmail.com.
  • 4 Instituto de Ciências Biológicas, Universidade Federal de Goiás, Goiânia 70040-010, Brazil. marcos_agrorural@hotmail.com.
  • 5 Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark. henrik.franzyk@sund.ku.dk.
  • 6 Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark. ds@sund.ku.dk.
PMID: 30018269 DOI: 10.3390/molecules23071755
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

HPLC-HRMS-SPE-NMR; Miconia albicans; PTP1B; type 2 diabetes.

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