High-Resolution Ptp1b Inhibition Profiling Combined With Hplc-Hrms-Spe-Nmr For Identification Of Ptp1b Inhibitors From Miconia Albicans
MOLECULES(2018)
摘要
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 mu g/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--d-glucopyranose (2), myricetin 3-O--l-rhamnopyranoside (3), quercetin 3-O-(2-galloyl)--l-rhamnopyranoside (5), mearnsetin 3-O--l-rhamnopyranoside (6), and kaempferol 3-O--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 2-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.
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关键词
Miconia albicans, type 2 diabetes, PTP1B, HPLC-HRMS-SPE-NMR
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