Archives of Pharmacal Research

, Volume 30, Issue 11, pp 1435–1439 | Cite as

Inhibition of topoisomerase I activity and efflux drug transporters’ expression by xanthohumol from hops

  • Sung Ho Lee
  • Hyun Jung Kim
  • Jung Sun Lee
  • Ik-Soo Lee
  • Bok Yun KangEmail author
Article Drug efficacy and safety


Xanthohumol (XN) and its related compounds were evaluated for their cytotoxicity against four different human cancer cell lines, A549 (lung), SK-OV-3 (ovarian), SK-MEL-2 (melanoma), and HCT-15 (colon) using a sulforhodamine B assay. XN showed the most active cytotoxicity against the human cancer cell lines. Isoxanthohumol, 8-prenylnaringenin, and xanthohumol 4’-O-β-D-glucopyranoside showed comparable cytotoxicity and (2S)-5-methoxy-8-prenylnaringe-nin 7-O-β-D-glucopyranoside was the least cytotoxic compound. The anticancer properties of XN, the most active cytotoxic compound, were further investigated. XN showed an inhibitory effect on the activity of DNA topoisomerase I (topo I), which was measured from the relaxation of supercoiled DNA. The inhibition of topo I by XN might explain the cytotoxicity against the human cancer cell lines. Moreover, the expression of the drug efflux genes was investigated to predict the drug resistance. XN clearly decreased the mRNA levels of ABCB1 (MDR1), ABCC1 (MRP1), ABCC2 (MRP2), and ABCC3 (MRP3). These results suggest that XN has anticancer properties by inhibiting the topo I activity and it might be used in conjunction with other anticancer chemotherapeutic agents to reduce the drug resistance inhibiting the efflux drug transporters.

Key words

Xanthohumol Cytotoxicity Topoisomerase I Efflux drug transporter Cancer 


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Copyright information

© The Pharmaceutical Society of Korea 2007

Authors and Affiliations

  • Sung Ho Lee
    • 1
  • Hyun Jung Kim
    • 1
  • Jung Sun Lee
    • 1
  • Ik-Soo Lee
    • 1
  • Bok Yun Kang
    • 1
    Email author
  1. 1.College of Pharmacy and Research Institute of Drug DevelopmentChonnam National UniversityGwangjuKorea

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