Flavonoids from Sophora alopecuroides L. improve palmitate-induced insulin resistance by inhibiting PTP1B activity in vitro

Bioorg Med Chem Lett. 2021 Mar 1:35:127775. doi: 10.1016/j.bmcl.2021.127775. Epub 2021 Jan 5.

Abstract

Seventeen flavonoids (1-17) were isolated from Sophora alopecuroides L.. Compounds 1 and 2 were new compounds, and compounds 5, 8, 11, 12, and 17 were isolated from S. alopecuroides for the first time. The sources of compounds 1 and 2 were determined from the seeds of S. alopecuroides by UPLC-QE-Orbitrap-MS, and compounds 1, 2, 7, 13, 14, 15, 16, and 17 were proven to improve the insulin resistance of C2C12 myotubes and significantly increase glucose consumption levels. Among them, compounds 1, 2, 13, 14, 16, and 17 could bind to protein tyrosine phosphatase 1B (PTP1B), thereby significantly inhibiting the enzyme activity of PTP1B. Compound 2 had the strongest inhibitory effect, with an inhibition rate of 95.22% at 0.1 μg mL-1.

Keywords: Flavonoids; Insulin resistance; Leguminosae; PTP1B; Sophora alopecuroides L..

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Differentiation / drug effects
  • Cell Line
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology*
  • Flavonoids / chemistry
  • Flavonoids / isolation & purification
  • Flavonoids / pharmacology*
  • Insulin Resistance
  • Mice
  • Molecular Structure
  • Palmitates / chemistry
  • Palmitates / pharmacology*
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / metabolism
  • Sophora / chemistry*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Flavonoids
  • Palmitates
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1
  • Ptpn1 protein, mouse