Overcoming multidrug resistance in human cancer cells by natural compounds

Toxins (Basel). 2010 Jun;2(6):1207-24. doi: 10.3390/toxins2061207. Epub 2010 May 28.


Multidrug resistance is a phenomenon whereby tumors become resistant to structurally unrelated anticancer drugs. P-glycoprotein belongs to the large ATP-binding cassette (ABC) transporter superfamily of membrane transport proteins. P-glycoprotein mediates resistance to various classes of anticancer drugs including vinblastine, daunorubicin, and paclitaxel, by actively extruding the drugs from the cells. The quest for inhibitors of anticancer drug efflux transporters has uncovered natural compounds, including (-)-epigallocatechin gallate, curcumin, capsaicin, and guggulsterone, as promising candidates. In this review, studies on the effects of natural compounds on P-glycoprotein and anticancer drug efflux transporters are summarized.

Keywords: ABC transporter; P-glycoprotein; anticancer drug; cancer chemoprevention; multidrug resistance; phytochemical.

Publication types

  • Review

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Biological Products / pharmacology*
  • Drug Resistance, Multiple* / drug effects
  • Drug Resistance, Neoplasm* / drug effects
  • Humans
  • Multidrug Resistance-Associated Proteins / metabolism
  • Neoplasms / drug therapy


  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Antineoplastic Agents
  • Biological Products
  • Multidrug Resistance-Associated Proteins