PTP1B inhibitory effect of alkyl p-coumarates from Calystegia soldanella

Nat Prod Commun. 2014 Nov;9(11):1585-8.

Abstract

In this report, the PTP1B inhibitory effect of Calystegia soldanella was investigated. Bioassay-guided fractionation of the crude extracts revealed that the n-hexane fraction had the strongest PTP1B inhibitory effect. Nine known alkyl p-coumarates were isolated from the n-hexane fraction, and each compound was evaluated for its effect on PTP1B. All compounds effectively inhibited PTP1B activity. The IC50 values of the compounds were 3 (10.8 μg/mL) > 2 (15.5 μg/mL) > 7 (26.6 μg/mL) > 1 (37.0 μg/mL) > 8 (41.2 μg/mL) > 9 (43.4 μg/mL) > 5 (44.7 μg/mL) > 4 (> 50 μg/mL) > 6 (> 50 μg/mL).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calystegia / chemistry*
  • Coumaric Acids / chemistry*
  • Coumaric Acids / pharmacology*
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Hexanes / chemistry
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / metabolism*

Substances

  • Coumaric Acids
  • Enzyme Inhibitors
  • Hexanes
  • n-hexane
  • PTPN1 protein, human
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1