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Tenulin and isotenulin inhibit P-glycoprotein function and overcome multidrug resistance in cancer cells

Ying-Tzu Chang1, Charles C N Wang2, Jiun-Yi Wang3

  • 1Department of Pharmacy, College of Pharmacy, China Medical University, 91 Hsueh-Shih Road, Taichung 40402, Taiwan, ROC.

Phytomedicine : International Journal of Phytotherapy and Phytopharmacology
|January 23, 2019
PubMed
Abstract

Insights

Natural compounds tenulin and isotenulin inhibit P-glycoprotein (P-gp) efflux, a key mechanism in multidrug resistance (MDR) cancer. These P-gp inhibitors resensitize MDR cancer cells to chemotherapy, offering potential for synergistic cancer treatment.

Area of Science:

  • Pharmacology
  • Biochemistry
  • Oncology

Background:

  • Multidrug resistance (MDR) in cancer is a major challenge in chemotherapy.
  • P-glycoprotein (P-gp) mediated drug efflux is a primary cause of MDR.
  • Natural products offer a promising avenue for developing novel P-gp inhibitors.

Purpose of the Study:

  • To investigate the effects of tenulin and isotenulin on human P-gp.
  • To explore the kinetic mechanisms of tenulin and isotenulin interactions with P-gp.

Main Methods:

  • Established human P-gp expressing cells using the Flp-In™ system.
  • Assessed cell viability, transporter inhibition, P-gp efflux kinetics, and ATPase activity.
  • Utilized SRB assays, calcein-AM uptake, rhodamine123 and doxorubicin efflux assays, and Pgp-Glo™ Assay System.

Main Results:

  • Tenulin and isotenulin significantly inhibited P-gp efflux by stimulating ATPase activity.
  • Tenulin and isotenulin exhibited competitive and noncompetitive inhibition, respectively.
  • Combinations of tenulin/isotenulin with chemotherapy resensitized MDR cancer cells.

Conclusions:

  • Tenulin and isotenulin demonstrate potential as P-gp inhibitors.
  • These compounds could be developed for synergistic treatment strategies in MDR cancers.
Keywords:
IsotenulinKinetic mechanismMultidrug resistanceP-glycoproteinSesquiterpene lactoneTenulin

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