Targeting anthracycline-resistant tumor cells with synthetic aloe-emodin glycosides

Elinor Breiner-Goldstein, Zoharia Evron, Michael Frenkel, Keren Cohen, Keren Nir Meiron, Dan Peer, Yael Roichman, Eliezer Flescher, Micha Fridman

Research output: Contribution to journalArticlepeer-review

8 Scopus citations


The cytotoxic activity of aloe-emodin (AE), a natural anthranoid that readily permeates anthracycline-resistant tumor cells, was improved by the attachment of an amino-sugar unit to its anthraquinone core. The new class of AE glycosides (AEGs) showed a significant improvement in cytotoxicity-up to more than 2 orders of magnitude greater than those of AE and the clinically used anthracycline doxorubicin (DOX)-against several cancer cell lines with different levels of DOX resistance. Incubation with the synthetic AEGs induced cell death in less than one cell cycle, indicating that these compounds do not directly target the cell division mechanism. Confocal microscopy provided evidence that unlike DOX, AEGs accumulated in anthracycline-resistant tumor cells in which resistance is conferred by P-glycoprotein efflux pumps. The results of this study demonstrate that AEGs may serve as a promising scaffold for the development of cytotoxic agents capable of overcoming anthracycline resistance in tumor cells.

Original languageEnglish (US)
Pages (from-to)528-531
Number of pages4
JournalACS Medicinal Chemistry Letters
Issue number7
StatePublished - Jul 14 2011


  • aloe-emodin
  • Anathracycline analogues
  • anthranoids
  • antitumor agents
  • P-glycoproteins

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry


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