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Barbigerone reverses multidrug resistance in breast MCF-7/ADR cells

Xiuxia Li1, Li Wan2, Fang Wang1

  • 1Department of pharmacy, East Branch of Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital, Chengdu, Sichuan, China.

Phytotherapy Research : PTR
|January 26, 2018
PubMed

Insights

Barbigerone (BA) effectively reverses multidrug resistance (MDR) in cancer by inhibiting P-glycoprotein (P-gp) ATPase activity, enhancing adriamycin

Area of Science:

  • Biochemistry
  • Pharmacology
  • Oncology

Background:

  • Multidrug resistance (MDR) is a major challenge in cancer chemotherapy.
  • P-glycoprotein (P-gp) is a key factor contributing to MDR.
  • Barbigerone (BA), a natural isoflavone, has potential anticancer properties.

Purpose of the Study:

  • To investigate the potential of barbigerone (BA) to reverse P-glycoprotein (P-gp) mediated multidrug resistance (MDR).
  • To evaluate the effects of BA on adriamycin (ADR) resistant breast cancer cells (MCF-7/ADR).

Main Methods:

  • Cell-based assays using MCF-7/ADR cells to assess cytotoxicity and drug accumulation.
  • In vivo studies using a xenograft mouse model.
  • Analysis of P-gp ATPase activity.

Main Results:

  • BA (0.5 μM) significantly enhanced adriamycin (ADR) cytotoxicity in MCF-7/ADR cells.
  • BA increased intracellular ADR accumulation and reduced its efflux in a time- and dose-dependent manner.
  • BA inhibited P-gp ATPase activity, not P-gp expression, and improved ADR efficacy in vivo.

Conclusions:

  • Barbigerone (BA) effectively reverses P-gp mediated multidrug resistance (MDR).
  • BA's mechanism involves the inhibition of P-gp ATPase activity.
  • BA shows promise as a novel therapeutic agent to enhance cancer chemotherapy.
Keywords:
MCF-7/ADRP-glycoprotein (P-gp)barbigerone (BA)multidrug resistance (MDR)

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