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Jatrophane diterpenes from Euphorbia mellifera and their activity as P-glycoprotein modulators on multidrug-resistant mouse lymphoma and human colon adenocarcinoma cells.

Abstract
Three new macrocyclic jatrophane diterpenes, named euphomelliferine (1) and euphomelliferenes A (2) and B (3), and one new tetracyclic triterpene, 19(10→9)-abeo-8α,9β,10α-tirucalla-5,25-diene-3β,24-diol (6, C-24 epimers), were isolated from the methanolic extract of Euphorbia mellifera. A known ingenane (7) and two jatrophane diterpenes (4 and 5) were also isolated. Their structures were elucidated by extensive spectroscopic methods, including 1D and 2D homo- and heteronuclear NMR experiments. Jatrophane diterpenes 1-3 and 5 were evaluated for their effects on the reversion of multidrug resistance (MDR) mediated by P-glycoprotein, by using the rhodamine-123 exclusion test, on human MDR1 gene-transfected mouse lymphoma cells (L5178Y MDR) and on human colon adenocarcinoma cells (COLO 320). The apoptosis-inducing activity of these compounds was also tested on COLO 320 cells, using the annexin-V/propidium iodide assay. Diterpenes 1 and 2 displayed significant MDR reversing activity, in a dose-dependent manner, on both cancer cell models. The tested compounds did not induce apoptosis in the COLO 320 cells.
AuthorsInês Valente, Mariana Reis, Noélia Duarte, Julianna Serly, Joséph Molnár, Maria-José U Ferreira
JournalJournal of natural products (J Nat Prod) Vol. 75 Issue 11 Pg. 1915-21 (Nov 26 2012) ISSN: 1520-6025 [Electronic] United States
PMID23098168 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 19(10-9)-abeo-8alpha,9beta,10alpha-tirucalla-5,25-diene-3beta,24-diol
  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Diterpenes
  • Triterpenes
  • euphomelliferene A
  • euphomelliferene B
  • euphomelliferine
  • ingenane
  • jatrophane
Topics
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 (drug effects, pharmacology)
  • Algorithms
  • Animals
  • Apoptosis (drug effects)
  • Colonic Neoplasms (drug therapy)
  • Diterpenes (chemistry, isolation & purification, pharmacology)
  • Drug Resistance, Multiple (drug effects)
  • Drug Resistance, Neoplasm (drug effects)
  • Euphorbia (chemistry)
  • Humans
  • Mice
  • Molecular Structure
  • Portugal
  • Triterpenes (chemistry, isolation & purification, pharmacology)
  • Tumor Cells, Cultured

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