Differential effects of calcium antagonists on ABCG2/BCRP-mediated drug resistance and transport in SN-38-resistant HeLa cells

  • Authors:
    • Kohji Takara
    • Mika Matsubara
    • Kazuhiro Yamamoto
    • Tetsuya Minegaki
    • Shigehiko Takegami
    • Minoru Takahashi
    • Teruyoshi Yokoyama
    • Katsuhiko Okumura
  • View Affiliations

  • Published online on: December 22, 2011     https://doi.org/10.3892/mmr.2011.734
  • Pages:603-609
0

Abstract

The effects of 9 calcium antagonists on ABCG2/BCRP-mediated resistance and transport were examined in HeLa and SN-38-resistant HeLa (HeLa/SN100) cells, overexpressing ABCG2/BCRP. Sensitivity to mitoxantrone, an ABCG2/BCRP substrate, in HeLa/SN100 cells was significantly reversed by the coexistence of the calcium antagonists, except for diltiazem and verapamil. The accelerated transport activity of Hoechst33342, an ABCG2/BCRP substrate, in HeLa/SN100 cells was significantly decreased by the presence of the calcium antagonists, except for diltiazem, nifedipine or verapamil, returning to the level of HeLa cells. The present study classifies the calcium antagonists into 3 categories: strong (benidipine, felodipine, nicardipine, nisoldipine and nitrendipine), moderate (amlodipine and nifedipine) and weak (diltiazem and verapamil) inhibitors of ABCG2/BCRP.

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March 2012
Volume 5 Issue 3

Print ISSN: 1791-2997
Online ISSN:1791-3004

2016 Impact Factor: 1.692
Ranked #19/128 Medicine Research and Experimental
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APA
Takara, K., Matsubara, M., Yamamoto, K., Minegaki, T., Takegami, S., Takahashi, M. ... Okumura, K. (2012). Differential effects of calcium antagonists on ABCG2/BCRP-mediated drug resistance and transport in SN-38-resistant HeLa cells. Molecular Medicine Reports, 5, 603-609. https://doi.org/10.3892/mmr.2011.734
MLA
Takara, K., Matsubara, M., Yamamoto, K., Minegaki, T., Takegami, S., Takahashi, M., Yokoyama, T., Okumura, K."Differential effects of calcium antagonists on ABCG2/BCRP-mediated drug resistance and transport in SN-38-resistant HeLa cells". Molecular Medicine Reports 5.3 (2012): 603-609.
Chicago
Takara, K., Matsubara, M., Yamamoto, K., Minegaki, T., Takegami, S., Takahashi, M., Yokoyama, T., Okumura, K."Differential effects of calcium antagonists on ABCG2/BCRP-mediated drug resistance and transport in SN-38-resistant HeLa cells". Molecular Medicine Reports 5, no. 3 (2012): 603-609. https://doi.org/10.3892/mmr.2011.734