Onkologie. 2013:7(5):248-252

The use of biological activity of quercetin in cancer therapy

Barbora Novotná1, Lenka Borská2, Zdeněk Fiala1, Jan Krejsek3
1 Ústav hygieny a preventivního lékařství, Univerzita Karlova v Praze, Lékařská fakulta v Hradci Králové
2 Ústav patologické fyziologie, Univerzita Karlova v Praze, Lékařská fakulta v Hradci Králové
3 Ústav klinické imunologie a alergologie, Univerzita Karlova v Praze, Lékařská fakulta v Hradci Králové

This review deals with biological activity of quercetin with the use of newer data from PubMed database. Quercetin is a flavonoid of

natural origin possessing antiinflamatory and antioxidative properties. Studies of quercetin effects on normal and tumor cells are resulting

in a new information about posibilities of quercetin use in cancer therapy. These studies on quercetin cellular effects in cancer

cells elucidated the fact that quercetin application leads in these cells to significant increase of apoptotic processes when these cells

produce protein p53. Increased production of protein p53 is accompanied by an activation of AMPK (AMP-activated protein kinase). It

was clearly demonstrated that a manganese-containing superoxid dismutase and BCL2 genes represent main targets in a molecular

mechanism that activates quercetin-containing chemotherapy and which also induces apoptosis through a direct activation of caspase

cascade in mitochondrias of cancer cells. Quercetin administration decreases cellular concentrations of Her-2/neu protein that indicates

unfavorable prognosis for patients with breast cancer. Quercetin also significantly increases TRAIL-induced apoptosis. This is accompanied

by an increase in death receptor 5 expression and by an inhibition of survivine expresion and also by numerous other effects that are

discused according to the type of cancer cells, in which they were investigated. Data regarding the ability of quercetin to increas effectivity

of therapies in combinations with doxorubicine, tamoxifen, vinkristin, cisplatin, 5-fluorouracil and temozolomide are of direct clinical

relevance. In many cases, quercetin increases cell sensitivity to the therapy or makes chemotherapy less toxic. However, therapeutic use

of quercetin may be limited because of its various other effects in cells and potentially in a whole organism.

Keywords: Quercetin, biological activity, tumor diseases, mechanism of action, sensitivity to therapy

Published: November 1, 2013  Show citation

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Novotná B, Borská L, Fiala Z, Krejsek J. The use of biological activity of quercetin in cancer therapy. Onkologie. 2013;7(5):248-252.
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References

  1. Middleton E, Kandaswami C. The impact of plant flavonoids on mammalian biology: Implications for immunity, inflammation, and cancer. In: Harborne JB, ed. The Flavonoids, Advances in Research Since 1986. London: Chapman&Hall, 1994: 619-652. Go to original source...
  2. Shoskes DA, Zeitlin SI, Shahed A, Rajfer J. Quercetin in men with category III chronic prostatitis: A preliminary prospective, double-blind, placebo-controlled trial. Urol 1999; 54: 960-963. Go to original source... Go to PubMed...
  3. Lean ME, Noroozi M, Kelly I. Dietary flavonols protect diabetic human lymphocytes against oxidative damage to DNA. Diabetes 1999; 48: 176-181. Go to original source... Go to PubMed...
  4. Harwood M, Danielewska-Nikiel B, Borzelleca JF, Flamm GW, Williams GM, Lines TC. A critical review of the data related to the safety of quercetin and lack of evidence of in vivo toxicity, including lack of genotoxic / carcinogenic properties. Food. Chem. Toxicol. 2007; 45: 2179-2205. Go to original source... Go to PubMed...
  5. Quercetin. Alt Med Rev 1998;3:140-143.
  6. Nieman DC, Henson DA, Davis JM et al. Quercetin's influence on exercise-induced changes in plasma cytokines and muscle and leukocyte cytokine mRNA J Appl Physiol 2007; 103: 1728-1735. Go to original source... Go to PubMed...
  7. de Pascual-Teresa S, Johnston KL, DuPont MS et al. Quercetin metabolites downregulate cyclooxygenase-2 transcription in human lymphocytes ex vivo but not in vivo. J. Nutr. 2004; 134: 552-557. Go to original source... Go to PubMed...
  8. Priego S, Feddi F, Ferrer P, et al. Natural polyphenols facilitate elimination of HT-29 colorectal cancer xenografts by chemoradiotherapy: a Bcl-2- and superoxide dismutase 2-dependent mechanism. Mol Cancer Ther 2008; 7: 3330-3342. Go to original source... Go to PubMed...
  9. Bhushan S, McLeod H, Walko CM. Role of pharmacogenetics as predictive biomarkers of response and/or toxicity in the treatment of colorectal cancer. Clin Colorectal Cancer 2009; 8: 15-21. Go to original source... Go to PubMed...
  10. Ribic CM, Sargent DJ, Moore MJ et al. Tumor microsatellite-instability status as a predictor of benefit from fluorouracil-based adjuvant chemotherapy for colon cancer. N Engl J Med2003;349:247-257. Go to original source... Go to PubMed...
  11. Xavier CP, Lima CF, Rohde M, Pereira-Wilson C. Quercetin enhances induced apoptosis in MSI colorectal cancer cells through p53 modulation. Cancer Chemother Pharmacol 2011 Apr 11. (Epub ahead of print). Go to original source... Go to PubMed...
  12. Kim HJ, Kim SK, Kim BS, et al. Apoptotic effect of quercetin on HT-29 colon cancer cells via the AMPK signaling pathway. J Agric Food Chem 2010; 58: 8643-8650. Go to original source... Go to PubMed...
  13. Chou CC, Yang JS, Lu HF, et al. Quercetin-mediated cell cycle arrest and apoptosis involving activation of a caspase cascade through the mitochondrial pathway in human breast cancer MCF-7 cells. Arch Pharm Res 2010; 33: 1181-1191. Go to original source... Go to PubMed...
  14. Moon YJ, Shin BS, An G, Morris ME. Biochanin A inhibits breast cancer tumor growth in a murine xenograft model. Pharm Res 2008; 25: 2158-2163. Go to original source... Go to PubMed...
  15. Lee YK, Park OJ. Regulation of mutual inhibitory activities between AMPK and Akt with quercetin in MCF-7 breast cancer cells. Oncol Rep 2010; 24: 1493-1497. Go to original source... Go to PubMed...
  16. Jeong JH, An JY, Kwon YT, Li LY, Lee YJ. Quercetin-induced ubiquitination and down-regulation of Her-2/neu. J Cell Biochem 2008; 105: 585-595. Go to original source... Go to PubMed...
  17. Du G, Lin H, Yang Y, et al. Dietary quercetin combining intratumoral doxorubicin injection synergistically induces rejection of established breast cancer in mice. Int Immunopharmacol 2010; 10: 819-826. Go to original source... Go to PubMed...
  18. Lee SJ, Jung YS, Lee SH, Chung HY, Park BJ. Isolation of a chemical inhibitor against K-Ras-induced p53 suppression through natural compound screening. Int. J. Oncol. 2009; 34: 1637-1643. Go to original source...
  19. Phromnoi K, Yodkeeree S, Anuchapreeda S, Limtrakul P. Inhibition of MMP-3 activity and invasion of the MDA-MB-231 human invasive breast carcinoma cell line by bioflavonoids. Acta Pharmacol Sin 2009; 30: 1169-1176. Go to original source... Go to PubMed...
  20. Oh SJ, Kim O, Lee JS et al. Inhibition of angiogenesis by quercetin in tamoxifen-resistant breast cancer cells. Food Chem Toxicol 2010; 48: 3227-3234. Go to original source... Go to PubMed...
  21. Wong MY, Chiu GN. Simultaneous liposomal delivery of quercetin and vincristine for enhanced estrogen-receptor-negative breast cancer treatment. Anticancer Drugs 2010; 21: 401-410. Go to original source... Go to PubMed...
  22. Chen W, Wang X, Zhuang J, Zhang L, Lin Y. Induction of death receptor 5 and suppression of survivin contribute to sensitization of TRAIL-induced cytotoxicity by quercetin in non-small cell lung cancer cells. Carcinogenesis. 2007; 28: 2114-2121. Go to original source... Go to PubMed...
  23. Hofmann J, Fiebig HH, Winterhalter BR, Berger DP, Grunicke H. Enhancement of the antiproliferative activity of cis-diamminedichloroplatinum(II) by quercetin. Int. J. Cancer. 1990; 45: 536-539. Go to original source... Go to PubMed...
  24. Kuhar M, Sen S, Singh N. Role of mitochondria in quercetin-enhanced chemotherapeutic response in human non-small cell lung carcinoma H-520 cells. Anticancer Res 2006; 26: 1297-1303. Go to PubMed...
  25. American Cancer Society. Cancer Facts and Figures 2010. Atlanta, Ga: American Cancer Society, 2010. http://www.cancer.org/acs/groups/content/@nho/documents/document/acspc-024113.pdf.
  26. Thompson IM, Goodman PJ, Tangen CM et al. The influence of finasteride on the development of prostate cancer. N Engl J Med 2003; 349: 215-224. Go to original source... Go to PubMed...
  27. Senthilkumar K, Elumalai P, Arunkumar R et al. Quercetin regulates insulin like growth factor signaling and induces intrinsic and extrinsic pathway mediated apoptosis in androgen independent prostate cancer cells (PC-3). Mol Cell Biochem 2010; 344: 173-184. Go to original source... Go to PubMed...
  28. Sahin E, Sahin M, Sanlio?lu AD, Gümüslü S. KNK437, a benzylidene lactam compound, sensitises prostate cancer cells to the apoptotic effect of hyperthermia. Int. J. Hyperthermia. 2011;27:63-73. Go to original source... Go to PubMed...
  29. Aalinkeel R, Bindukumar B, Reynolds JL et al. The dietary bioflavonoid, quercetin, selectively induces apoptosis of prostate cancer cells by down-regulating the expression of heat shock protein 90. Prostate 2008;68:1773-1789. Go to original source... Go to PubMed...
  30. Jung YH, Heo J, Lee YJ, Kwon TK, Kim YH. Quercetin enhances TRAIL-induced apoptosis in prostate cancer cells via increased protein stability of death receptor 5. Life Sci 2010; 86: 351-357. Go to original source... Go to PubMed...
  31. Lee DH, Lee YJ. Quercetin suppresses hypoxia-induced accumulation of hypoxia-inducible factor-1alpha (HIF-1alpha) through inhibiting protein synthesis. J Cell Biochem 2008; 105: 546-553. Go to original source... Go to PubMed...
  32. Zamin LL, Filippi-Chiela EC, Dillenburg-Pilla P, Horn F, Salbego C, Lenz G. Resveratrol and quercetin cooperate to induce senescence-like growth arrest in C6 rat glioma cells. Cancer Sci 2009; 100: 1655-1662. Go to original source... Go to PubMed...
  33. Jakubowicz-Gil J, Langner E, Wertel I, Piersiak T, Rzeski W. Temozolomide, quercetin and cell death in the MOGGCCM astrocytoma cell line. Chem Biol Interact 2010; 188: 190-203. Go to original source... Go to PubMed...
  34. Thangasamy T, Sittadjody S, Mitchell GC et al. Quercetin abrogates chemoresistance in melanoma cells by modulating deltaNp73. BMC Cancer 2010; 10: 282. Go to original source... Go to PubMed...




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