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Research ArticleArticle

INHIBITION OF LUNG CANCER CELL GROWTH BY QUERCETIN GLUCURONIDES VIA G2/M ARREST AND INDUCTION OF APOPTOSIS

Jen-Hung Yang, Te-Chun Hsia, Hsiu-Maan Kuo, Pei-Dawn Lee Chao, Chi-Chung Chou, Yau-Huei Wei and Jing-Gung Chung
Drug Metabolism and Disposition February 2006, 34 (2) 296-304; DOI: https://doi.org/10.1124/dmd.105.005280
Jen-Hung Yang
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Te-Chun Hsia
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Hsiu-Maan Kuo
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Pei-Dawn Lee Chao
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Chi-Chung Chou
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Yau-Huei Wei
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Jing-Gung Chung
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Abstract

Lung cancer is the leading cause of cancer death in many developed countries, including Taiwan. Quercetin, a widely distributed bioflavonoid, is well known to induce growth inhibition in a variety of human cancer cells. Quercetin glucuronides are the main circulating metabolites after dietary supplements with quercetin in humans. However, there is little information available as to how quercetin glucuronides affect human cancer cells. We investigated the effects of quercetin glucuronides in a human lung cancer cell line NCI-H209. We checked the cell viability, cell cycle checkpoint proteins, pro- and antiapoptotic proteins, caspase-3 activity, and gene expression by flow cytometry and Western blot. The viability of cells decreased in a dose- and time-dependent manner. Cell cycle analysis revealed a significant increase of the proportion of cells in G2/M phase and subG0/G1 phase (corresponding to apoptotic cells). Moreover, quercetin glucuronides increased the expressions of cyclin B, Cdc25c-ser-216-p, and Wee1 proteins, indicating the G2/M arrest. We also demonstrated a concurrent decrease of the mitochondrial membrane potential, release of cytochrome c, up-regulation of Bax, down-regulation of Bcl-2, and activation of caspase-3, and subsequently, cleavage of poly(ADP-ribose) polymerase. In addition, quercetin glucuronide-induced apoptosis was totally blocked by the broad-spectrum caspase inhibitor benzyloxycarbonyl-Val-Ala-Asp fluoromethylketone. Taken together, we demonstrated that quercetin glucuronides inhibited proliferation through G2/M arrest of the cell cycle and induced apoptosis via caspase-3 cascade in the human lung cancer cell line NCI-H209. Delineation of the biological effects of specific major quercetin metabolites on chemotherapeutic potential or chemoprevention of human cancers warrants further investigation.

Footnotes

  • This study was supported by Grant CMU-M-17 (2003) from the Biomedical Research Section of China Medical University, Taichung, Taiwan.

  • Article, publication date, and citation information can be found at http://dmd.aspetjournals.org.

  • doi:10.1124/dmd.105.005280.

  • ABBREVIATIONS: SCLC, small-cell lung carcinoma; DMSO, dimethyl sulfoxide; FBS, fetal bovine serum; PBS, phosphate-buffered saline; z-VAD-fmk, benzyloxycarbonyl-Val-Ala-Asp fluoromethylketone; PARP, poly(ADP-ribose) polymerase; PAGE, polyacrylamide gel electrophoresis; ROS, reactive oxygen species; CDK, cyclin-dependent kinase; IAP, inhibitor of apoptosis protein; ER, endoplasmic reticulum.

    • Received April 30, 2005.
    • Accepted November 8, 2005.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 34 (2)
Drug Metabolism and Disposition
Vol. 34, Issue 2
1 Feb 2006
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Research ArticleArticle

INHIBITION OF LUNG CANCER CELL GROWTH BY QUERCETIN GLUCURONIDES VIA G2/M ARREST AND INDUCTION OF APOPTOSIS

Jen-Hung Yang, Te-Chun Hsia, Hsiu-Maan Kuo, Pei-Dawn Lee Chao, Chi-Chung Chou, Yau-Huei Wei and Jing-Gung Chung
Drug Metabolism and Disposition February 1, 2006, 34 (2) 296-304; DOI: https://doi.org/10.1124/dmd.105.005280

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Research ArticleArticle

INHIBITION OF LUNG CANCER CELL GROWTH BY QUERCETIN GLUCURONIDES VIA G2/M ARREST AND INDUCTION OF APOPTOSIS

Jen-Hung Yang, Te-Chun Hsia, Hsiu-Maan Kuo, Pei-Dawn Lee Chao, Chi-Chung Chou, Yau-Huei Wei and Jing-Gung Chung
Drug Metabolism and Disposition February 1, 2006, 34 (2) 296-304; DOI: https://doi.org/10.1124/dmd.105.005280
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