Inhibition of phospholipase cgamma1 and cancer cell proliferation by triterpene esters from Uncaria rhynchophylla

J Nat Prod. 2000 Jun;63(6):753-6. doi: 10.1021/np990478k.

Abstract

Investigation of the hooks of Uncaria rhynchophylla resulted in isolation of six phospholipase Cgamma1 (PLCgamma1) inhibitors (1-6). The structures of these compounds were elucidated as pentacyclic triterpene esters by spectroscopic and chemical analysis. Three of them, namely uncarinic acids C (1), D (2), and E (3), are newly reported as natural products. All the compounds showed dose-dependent inhibitory activities against PLCgamma1 in vitro with IC(50) values of 9.5-44.6 microM and inhibited the proliferation of human cancer cells with IC(50) values of 0.5-6.5 microg/mL.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3T3 Cells
  • Animals
  • Cell Division / drug effects
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / isolation & purification*
  • Enzyme Inhibitors / pharmacology
  • Esters / isolation & purification*
  • Esters / pharmacology*
  • Humans
  • Isoenzymes / antagonists & inhibitors*
  • Mice
  • Neoplasms / enzymology
  • Neoplasms / pathology*
  • Phospholipase C gamma
  • Plants, Medicinal / chemistry*
  • Rubiaceae / chemistry*
  • Structure-Activity Relationship
  • Triterpenes / isolation & purification*
  • Triterpenes / pharmacology*
  • Tumor Cells, Cultured
  • Type C Phospholipases / antagonists & inhibitors*

Substances

  • Enzyme Inhibitors
  • Esters
  • Isoenzymes
  • Triterpenes
  • uncarinic acid-C
  • uncarinic acid-D
  • uncarinic acid-E
  • Type C Phospholipases
  • Phospholipase C gamma