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Updated: May 22, 2026

Extraction and Purification of Polyphenols from Freeze-dried Berry Powder for the Treatment of Vascular Smooth Muscle Cells In Vitro
Published on: July 5, 2017
Polyphenols counteract tumor cell chemoresistance conferred by multidrug resistance proteins
Krystyna Michalak1, Olga Wesolowska
1Wrocław Medical University, Department of Biophysics, ul. Chałubińskiego 10, 50-368 Wrocław, Poland. michalak@biofiz.am.wroc.pl
Abstract:
One of the main reasons of cancer resistance to chemotherapeutic treatment is the presence of different ABC multidrug transporters in plasma membranes. The transporters extrude wide spectrum of anticancer agents out of cancer cells at the expense of energy derived from ATP-hydrolysis. Plant-origin polyphenolic compounds, mainly flavonoids and stilbenes or their synthetic derivatives, can modulate the main ABC transporters responsible for cancer drug resistance, including P-glycoprotein, MRP1 and BCRP. The recent studies on different resistant cancer cell lines enabled the discovery of a number of polyphenolic compounds able to reverse drug resistance in vitro and these compounds could be promising candidates for further clinical trials. The review summarizes the recent advances in the field of polyphenols interaction with ATP-binding cassette multidrug transporters. The mechanism of flavonoids interactions with the multidrug transporters and the structure-activity relationship are also discussed.
Insights
Plant-derived polyphenols can reverse cancer drug resistance by modulating ATP-binding cassette (ABC) multidrug transporters. These compounds show promise for overcoming chemotherapy resistance in clinical trials.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Cancer multidrug resistance is often mediated by ATP-binding cassette (ABC) transporters.
- These transporters efflux anticancer drugs from cancer cells, reducing treatment efficacy.
- Polyphenolic compounds from plants, such as flavonoids and stilbenes, are being investigated for their potential to overcome this resistance.
Purpose of the Study:
- To review recent advances in understanding polyphenol interactions with ABC multidrug transporters.
- To discuss the mechanisms by which flavonoids modulate these transporters.
- To explore the structure-activity relationships of polyphenols in reversing multidrug resistance.
Main Methods:
- Literature review of recent studies on polyphenol-ABC transporter interactions.
- Analysis of in vitro data from resistant cancer cell lines.
- Discussion of mechanistic insights and structure-activity relationships.
Main Results:
- Numerous plant-derived polyphenols and their synthetic derivatives demonstrate the ability to reverse drug resistance in vitro.
- Specific polyphenols modulate key ABC transporters like P-glycoprotein, MRP1, and BCRP.
- Understanding the interaction mechanisms and structure-activity relationships is crucial for developing new therapies.
Conclusions:
- Polyphenols represent a promising class of compounds for overcoming cancer multidrug resistance.
- Further clinical trials are warranted to evaluate the therapeutic potential of identified polyphenolic compounds.
- Targeting ABC transporters with polyphenols offers a viable strategy to enhance chemotherapy effectiveness.
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