Elaeodendron orientale as a source of cytotoxic cardenolides.

In the present study, we report six cardiac glycosides (1-6) along with four known ones (7-10) isolated from the leaves and fruits of Elaeodendron orientale. Their stereostructures were elucidated on the basis of spectroscopic analysis, including 1D and 2D NMR, and the absolute configuration of 1 was determined by X-ray diffraction analysis. The compounds were evaluated for growth inhibitory activity against a panel of human cancer cell lines, HeLa, A-549, MCF-7 and HL-60, and normal Vero cells. Four compounds from this series (5 and 7-9, IC50 values ranging from 0.01 to 0.07μM) exhibited cytotoxicity against three of the cancer cell lines assayed that was similar to or higher than the well-known therapies digoxin and digitoxigenin. Taking into account the narrow safety range of cardiac glycosides used in clinic, this series shows a selectivity index higher than 3 for three of the cancer cell lines assayed, increasing their interest for further study.
AuthorsAlex A Osorio, Manuel R López, Ignacio A Jiménez, Laila M Moujir, Matías L Rodríguez, Isabel L Bazzocchi
JournalPhytochemistry (Phytochemistry) Vol. 105 Pg. 60-7 (Sep 2014) ISSN: 1873-3700 [Electronic] England
PMID25014657 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2014 Elsevier Ltd. All rights reserved.
Chemical References
  • Antineoplastic Agents, Phytogenic
  • Cardenolides
  • Digoxin
  • Animals
  • Antineoplastic Agents, Phytogenic (chemistry, isolation & purification, pharmacology)
  • Cardenolides (chemistry, isolation & purification, pharmacology)
  • Celastraceae (chemistry)
  • Cercopithecus aethiops
  • Digoxin (pharmacology)
  • HL-60 Cells
  • HeLa Cells
  • Humans
  • Molecular Structure
  • Nuclear Magnetic Resonance, Biomolecular
  • Plant Leaves (chemistry)
  • Vero Cells
  • X-Ray Diffraction

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