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Flavonoids inhibit breast cancer resistance protein-mediated drug resistance: transporter specificity and

Kazuhiro Katayama1, Kazuto Masuyama, Sho Yoshioka

  • 1Department of Chemotherapy, Kyoritsu University of Pharmacy, Tokyo, 105-8512, Japan.

Cancer Chemotherapy and Pharmacology
|March 9, 2007
PubMed
Abstract

Insights

Many flavonoids can reverse drug resistance mediated by breast cancer resistance protein (BCRP), but not P-glycoprotein (P-gp) or multidrug resistance-related protein 1 (MRP1). 3

Area of Science:

  • Pharmacology
  • Biochemistry
  • Cancer Research

Background:

  • ATP-binding cassette (ABC) transporters, including P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and multidrug resistance-related protein 1 (MRP1), are crucial in conferring resistance to anticancer drugs.
  • Previous research indicated that certain flavonoids possess BCRP-inhibitory activity.

Purpose of the Study:

  • To investigate the reversal effects of a broad range of flavonoids on drug resistance mediated by BCRP, P-gp, and MRP1.
  • To identify specific flavonoids that can overcome ABC transporter-mediated drug resistance.

Main Methods:

  • Drug resistance reversal was assessed using cell growth inhibition assays in engineered human leukemia (K562) and epidermoid carcinoma (KB-3-1) cell lines expressing BCRP, MDR1, or MRP1.
  • Inhibitory concentrations (IC50) and reversal index (RI50) values were determined.
  • BCRP activity reversal was further evaluated by measuring intracellular topotecan fluorescence.

Main Results:

  • Out of 32 screened flavonoids, 20 exhibited BCRP-inhibitory activity.
  • 3',4',7-trimethoxyflavone demonstrated potent BCRP inhibition, with RI50 values of 0.012 µM for SN-38 and 0.044 µM for mitoxantrone.
  • Limited anti-P-gp activity was observed for 3',4',7-trimethoxyflavone and acacetin; no tested flavonoids inhibited MRP1.

Conclusions:

  • The study highlights that numerous flavonoids selectively inhibit BCRP, offering potential strategies to overcome BCRP-mediated drug resistance.
  • The findings provide insights into the structure-activity relationship concerning BCRP inhibition by flavonoids.

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