Eucommicin A, a β-truxinate lignan from Eucommia ulmoides, is a selective inhibitor of cancer stem cells

Phytochemistry. 2016 Feb:122:139-145. doi: 10.1016/j.phytochem.2015.11.017. Epub 2015 Dec 8.

Abstract

Cancer stem cells (CSCs) constitute a small population of undifferentiated cells within a tumor that have the ability to self-renew and drive tumor formation, thus behaving as cancer-initiating cancer cells. Therapeutic interventions that eliminate CSCs are necessary to completely cure patients, since CSCs are a crucial source of tumor recurrence and metastasis. An induced CSC-like (iCSCL) model was recently established using induced pluripotent stem cells (iPSCs). In this study, a natural product-eucommicin A-was identified from Eucommia ulmoides leaves by screening for anti-CSC activity using the iCSCL model. Its structure was elucidated by spectroscopic methods as a quinic acid diester of 3,4,3',4'-tetrahydroxy-β-truxinic acid. Eucommicin A exhibited selective anti-CSC activity and inhibited tumor sphere formation by iCSCL cells. The results of this study suggest that eucommicin A could serve as a lead compound in the development of drugs to abrogate the stemness and self-renewal ability of CSCs.

Keywords: Cancer stem cell; Eucommia ulmoides; Eucommiaceae; Lignan; β-Truxinate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / isolation & purification*
  • Antineoplastic Agents / pharmacology*
  • Drug Resistance, Neoplasm
  • Eucommiaceae / chemistry*
  • Humans
  • Lignans / chemistry
  • Lignans / isolation & purification*
  • Lignans / pharmacology*
  • Molecular Structure
  • Neoplastic Stem Cells / drug effects*

Substances

  • Antineoplastic Agents
  • Lignans
  • eucommicin A