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Review ArticleSpecial Section on Natural Products: Experimental Approaches to Elucidate Disposition Mechanisms and Predict Pharmacokinetic Drug Interactions — Minireview

The Effects of Traditional Chinese Medicine on P-Glycoprotein–Mediated Multidrug Resistance and Approaches for Studying the Herb–P-Glycoprotein Interactions

Yuhong Cao, Yiwei Shi, Ying Cai, Zhanying Hong and Yifeng Chai
Drug Metabolism and Disposition October 2020, 48 (10) 972-979; DOI: https://doi.org/10.1124/dmd.120.000050
Yuhong Cao
School of Pharmacy, Second Military Medical University, Shanghai Key Laboratory for Pharmaceutical (Chinese Materia Medica) Metabolites Research, Shanghai, China (Yu.C., Y.S., Yi.C., Z.H., Y.Ch.) and School of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, China (Yi.C.)
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Yiwei Shi
School of Pharmacy, Second Military Medical University, Shanghai Key Laboratory for Pharmaceutical (Chinese Materia Medica) Metabolites Research, Shanghai, China (Yu.C., Y.S., Yi.C., Z.H., Y.Ch.) and School of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, China (Yi.C.)
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Ying Cai
School of Pharmacy, Second Military Medical University, Shanghai Key Laboratory for Pharmaceutical (Chinese Materia Medica) Metabolites Research, Shanghai, China (Yu.C., Y.S., Yi.C., Z.H., Y.Ch.) and School of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, China (Yi.C.)
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Zhanying Hong
School of Pharmacy, Second Military Medical University, Shanghai Key Laboratory for Pharmaceutical (Chinese Materia Medica) Metabolites Research, Shanghai, China (Yu.C., Y.S., Yi.C., Z.H., Y.Ch.) and School of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, China (Yi.C.)
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Yifeng Chai
School of Pharmacy, Second Military Medical University, Shanghai Key Laboratory for Pharmaceutical (Chinese Materia Medica) Metabolites Research, Shanghai, China (Yu.C., Y.S., Yi.C., Z.H., Y.Ch.) and School of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, China (Yi.C.)
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Abstract

As a member of the ATP-dependent membrane transport proteins, P-Glycoprotein (P-gp) is known to pump substrates out of cells using an ATP-dependent mechanism. The overexpression of P-gp in tumor cells reduces the intracellular drug concentrations, which decreases the efficacy of extensive antitumor drugs and leads to multidrug resistance (MDR) clinically. The combination of anticancer drugs with P-gp inhibitor has been an attractive and promising strategy to reverse MDR in cancer treatment. However, nonspecific or nonselective distribution of P-gp inhibitors to nontarget organs is one of the most fatal shortcomings in clinical application. Thus, there is an urgent need for effective and nontoxic MDR reversal agents, particularly in P-gp–mediated MDR. Traditional Chinese medicine (TCM) natural products may prove less toxic for use in P-gp inhibition to promote MDR reversal. P-gp modulatory effects have been previously demonstrated using selected TCM, including the flavonoid, alkaloid, terpenoid, coumarin, and quinonoid compounds, and some Chinese medicine extracts. Moreover, the approaches for screening active components from TCM are necessary, and these approaches face challenges. At present, the approaches to study the interaction between TCM and P-gp are divided into in vitro, in vivo, and in silico methods. This review will provide an overview and update on the role of TCM in overcoming P-gp–mediated MDR and the approaches to study the interaction between TCM and P-gp.

SIGNIFICANCE STATEMENT This review summarized some traditional Chinese medicines identified to have a modulatory effect on P-gp, including flavonoids, alkaloids, terpenoids, coumarins, quinonoid compounds, and some Chinese medicine extracts, and it introduced possible mechanisms. The approaches to study the interaction between TCM and P-gp are divided into in vitro, in vivo, and in silico methods.

Footnotes

    • Received March 30, 2020.
    • Accepted July 20, 2020.
  • This work was financially supported by the National Natural Science Foundation of China [NO. 81673386, NO. 81872829].

  • All authors were supported by their own institutions during the preparation of this manuscript and had no conflict of interest.

  • https://doi.org/10.1124/dmd.120.000050.

  • Copyright © 2020 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 48 (10)
Drug Metabolism and Disposition
Vol. 48, Issue 10
1 Oct 2020
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Review ArticleSpecial Section on Natural Products: Experimental Approaches to Elucidate Disposition Mechanisms and Predict Pharmacokinetic Drug Interactions — Minireview

TCM Natural Products as P-gp–Mediated MDR Reversal Agents

Yuhong Cao, Yiwei Shi, Ying Cai, Zhanying Hong and Yifeng Chai
Drug Metabolism and Disposition October 1, 2020, 48 (10) 972-979; DOI: https://doi.org/10.1124/dmd.120.000050

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Review ArticleSpecial Section on Natural Products: Experimental Approaches to Elucidate Disposition Mechanisms and Predict Pharmacokinetic Drug Interactions — Minireview

TCM Natural Products as P-gp–Mediated MDR Reversal Agents

Yuhong Cao, Yiwei Shi, Ying Cai, Zhanying Hong and Yifeng Chai
Drug Metabolism and Disposition October 1, 2020, 48 (10) 972-979; DOI: https://doi.org/10.1124/dmd.120.000050
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