A new P-glycoprotein inhibitor from the caper spurge (Euphorbia lathyris)

J Nat Prod. 2003 Jan;66(1):140-2. doi: 10.1021/np0203537.

Abstract

The macrocyclic lathyrane polyester Euphorbia factor L10 (1a) has been obtained from the seeds of the caper spurge (E. lathyris). The interaction of L10 (1a) and its acetyl derivative (1b) with P-glycoprotein, a multidrug transporter overexpressed in cancer cells and responsible for resistance to chemotherapy, was investigated. The results established lathyrane diterpenoids as a novel chemotype for P-glycoprotein inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
  • Diterpenes / chemistry
  • Diterpenes / isolation & purification*
  • Diterpenes / pharmacology
  • Drug Resistance, Multiple
  • Drug Resistance, Neoplasm
  • Drug Screening Assays, Antitumor
  • Euphorbia / chemistry*
  • Germany
  • Humans
  • K562 Cells / drug effects
  • Leukemia
  • Molecular Structure
  • Plants, Medicinal / chemistry*
  • Seeds / chemistry
  • Tumor Cells, Cultured / drug effects

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Diterpenes
  • Euphorbia factor L10
  • Euphorbia factor L10, acetyl derivative