Parthenolide: from plant shoots to cancer roots

Drug Discov Today. 2013 Sep;18(17-18):894-905. doi: 10.1016/j.drudis.2013.05.005. Epub 2013 May 17.


Parthenolide (PTL), a sesquiterpene lactone (SL) originally purified from the shoots of feverfew (Tanacetum parthenium), has shown potent anticancer and anti-inflammatory activities. It is currently being tested in cancer clinical trials. Structure-activity relationship (SAR) studies of parthenolide revealed key chemical properties required for biological activities and epigenetic mechanisms, and led to the derivatization of an orally bioavailable analog, dimethylamino-parthenolide (DMAPT). Parthenolide is the first small molecule found to be selective against cancer stem cells (CSC), which it achieves by targeting specific signaling pathways and killing cancer from its roots. In this review, we highlight the exciting journey of parthenolide, from plant shoots to cancer roots.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / isolation & purification
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Antineoplastic Agents, Phytogenic / therapeutic use
  • Humans
  • Molecular Structure
  • Neoplastic Stem Cells / drug effects*
  • Neoplastic Stem Cells / pathology
  • Phytotherapy
  • Plant Shoots
  • Plants, Medicinal
  • Sesquiterpenes / chemistry
  • Sesquiterpenes / isolation & purification
  • Sesquiterpenes / pharmacology*
  • Sesquiterpenes / therapeutic use
  • Structure-Activity Relationship
  • Tanacetum parthenium* / chemistry


  • Antineoplastic Agents, Phytogenic
  • LC-1 compound
  • Sesquiterpenes
  • parthenolide