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Evaluation the interaction of ABC multidrug transporter MDR1 with thymoquinone: substrate or inhibitor?

Vahideh Keyvani1, Zeinab Nasserifar2, Mohammad-Reza Saberi3

  • 1Department of Biology, Faculty of Science, Shahid Chamran University of Ahvaz, Ahvaz, Iran.

Iranian Journal of Basic Medical Sciences
|November 5, 2020
PubMed
Abstract

Insights

Thymoquinone (TQ) shows anticancer effects but does not interact with the MDR1 protein. This suggests TQ may bypass common drug resistance mechanisms in gastric cancer cells.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Cancer Research

Background:

  • Thymoquinone (TQ) exhibits promising anticancer properties.
  • Multidrug resistance (MDR) is a major challenge in cancer chemotherapy.
  • MDR1 protein plays a significant role in conferring drug resistance.

Purpose of the Study:

  • To investigate the interaction between Thymoquinone (TQ) and the MDR1 protein.
  • To determine if TQ is a substrate or inhibitor of MDR1 in gastric cancer cells.

Main Methods:

  • Cell viability assessed using MTT assay.
  • TQ influx and efflux quantified by HPLC.
  • Molecular docking simulations performed to analyze TQ-MDR1 binding.

Main Results:

  • TQ inhibited cell viability dose-dependently.
  • TQ entered drug-resistant cells but did not efflux.
  • Molecular docking indicated TQ does not bind to the MDR1 active site like known inhibitors or substrates.

Conclusions:

  • Thymoquinone (TQ) does not appear to be an inhibitor or substrate of the MDR1 transporter.
  • TQ's mechanism of action may circumvent MDR1-mediated drug resistance in gastric cancer.
Keywords:
Drug transportersMDR1Multi drug resistanceNigella sativaThymoquinone

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