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

• Published in: Molecules (Basel, Switzerland) Switzerland), 2018-07, Vol.23 (7), p.1755
• Main Authors: de Cássia Lemos Lima, Rita, T Kongstad, Kenneth, Kato, Lucília, José das Silva, Marcos, Franzyk, Henrik, Staerk, Dan
• Format: Article
• Language: English
• Subjects: Acetic acid; Acids; Antidiabetics; Diabetes mellitus; Diabetes mellitus (non-insulin dependent); Ethyl acetate; High resolution; High-performance liquid chromatography; HPLC-HRMS-SPE-NMR; Inhibition; Inhibitors; Insulin; Insulin resistance; Kaempferol; L-Rhamnopyranoside; Liquid chromatography; Miconia; Miconia albicans; NMR; Nuclear magnetic resonance; Oleanolic acid; Protein-tyrosine-phosphatase; Proteins; PTP1B; Quercetin; Signal transduction; Triterpenoids; type 2 diabetes; Tyrosine; Ursolic acid
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules23071755

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 (IC = 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- -( )-caffeoyl-4,6-di- -galloyl-β-d-glucopyranose ( ), myricetin 3- -α-l-rhamnopyranoside ( ), quercetin 3- -(2″-galloyl)-α-l-rhamnopyranoside ( ), mearnsetin 3- -α-l-rhamnopyranoside ( ), and kaempferol 3- -α-l-arabinopyranoside ( ) as well as eight triterpenoids: maslinic acid ( ), 3- -sumaresinolic acid ( ), sumaresinolic acid ( ), 3- - - -coumaroyl maslinic acid ( ), 3- - - -coumaroyl maslinic acid ( ), 3- - - -coumaroyl 2α-hydroxydulcioic acid ( ), oleanolic acid ( ), and ursolic acid ( ). These results support the use of as a traditional medicine with antidiabetic properties and its potential as a source of PTP1B inhibitors.