Multidrug resistance modulation and apoptosis induction of cancer cells by terpenic compounds isolated from Euphorbia species

Noélia Duarte, Cátia Ramalhete, Andras Varga, J. Molnár, Maria José U Ferreira

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

Background: One of the most promising strategies to overcome multidrug resistance (MDR) is to use compounds that can modulate P-glycoprotein and restore the cytotoxicity of anticancer drugs. Furthermore, the search for compounds that regulate and overcome apoptosis deficiency of cancer cells is also of great therapeutic importance. Materials and Methods: Seven known pentacyclic triterpenes and one steroid were isolated from Euphorbia lagascae methanolic extracts and identified by physical and spectroscopic methods. These compounds, together with eleven terpenoids previously isolated from Euphorbia lagascae and E. tuckeyana were tested for their MDR-reversing and/or apoptosis induction activities by flow cytometry on L5178 human MDRl gene-transfected mouse lymphoma cells. Results: Four taraxastane-type triterpenes: 21α-hydroxytaraxasterol, 21α-hydroxytaraxasterol acetate, 3β,30-dihydroxy-20(21)-taraxastene and 3β-hydroxy-20-taraxasten-30-al, and two steroids: stigmastane-3,6-dione and ergosterol peroxide exhibited a significant MDR-Pgp modulation activity. Some aspects of structure-activity relationships are discussed. Regarding apoptosis induction, the most significant results were obtained for the poly cyclic diterpenes ent-16α,17- dihydroxykauran-3-one and ent-16α,17-dihydroxyatisan-3-one.

Original languageEnglish
Pages (from-to)4467-4472
Number of pages6
JournalAnticancer Research
Volume29
Issue number11
Publication statusPublished - Nov 2009

Fingerprint

Euphorbia
Multiple Drug Resistance
Apoptosis
Pentacyclic Triterpenes
Steroids
Neoplasms
Triterpenes
Diterpenes
Terpenes
P-Glycoprotein
Structure-Activity Relationship
Lymphoma
Flow Cytometry
Acetates
Pharmaceutical Preparations
Genes
Therapeutics

Keywords

  • Apoptosis
  • Euphorbia
  • Euphorbiaceae
  • Multidrug resistance
  • P-glycoprotein
  • Steroids
  • Triterpenes

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

Multidrug resistance modulation and apoptosis induction of cancer cells by terpenic compounds isolated from Euphorbia species. / Duarte, Noélia; Ramalhete, Cátia; Varga, Andras; Molnár, J.; Ferreira, Maria José U.

In: Anticancer Research, Vol. 29, No. 11, 11.2009, p. 4467-4472.

Research output: Contribution to journalArticle

Duarte, Noélia ; Ramalhete, Cátia ; Varga, Andras ; Molnár, J. ; Ferreira, Maria José U. / Multidrug resistance modulation and apoptosis induction of cancer cells by terpenic compounds isolated from Euphorbia species. In: Anticancer Research. 2009 ; Vol. 29, No. 11. pp. 4467-4472.
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