Farnesyl-O-acetylhydroquinone and geranyl-O-acetylhydroquinone suppress the proliferation of murine B16 melanoma cells, human prostate and colon adenocarcinoma cells, human lung carcinoma cells, and human leukemia cells.

Farnesyl-O-acetylhydroquinone (IC(50)=2.5 microM/l) suppressed the proliferation of murine B16F10 melanoma cells with a potency much greater than those of farnesol (IC(50)=45 microM/l) and farnesyl anthranilate (IC(50)=46 microM/l), its alcohol, and ester counterparts with proven anti-tumor activities in vivo. Geranyl-O-acetylhydroquinone (IC(50)=5.1 microM/l) also had a much-improved activity compared to geraniol (IC(50)=160 microM/l) and geranyl anthranilate (IC(50)=30 microM/l). The suppression by farnesyl-O-acetylhydroquinone was concentration- and time-dependent and was accompanied by arrest of cell cycle at G1 and G2/M phases as shown by flow cytometry. Farnesyl-O-acetylhydroquinone and lovastatin had additive impact on B16 cell proliferation. Farnesyl-O-acetylhydroquinone also suppressed the proliferations of human cancer cells HL-60, DU145, PC-3, LNCaP, Caco-2, and A549. Our results suggested that farnesyl derivatives, suppressors of tumor 3-hydroxy-3-methylglutaryl coenzyme A reductase activities, have potential as chemopreventive or chemotherapeutic agents.
AuthorsJennifer A McAnally, Manfred Jung, Huanbiao Mo
JournalCancer letters (Cancer Lett) Vol. 202 Issue 2 Pg. 181-92 (Dec 30 2003) ISSN: 0304-3835 [Print] Ireland
PMID14643448 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Antineoplastic Agents
  • Hydroquinones
  • Terpenes
  • farnesyl-O-acetylhydroquinone
  • geranyl-O-acetylhydroquinone
  • Farnesol
  • Lovastatin
  • Animals
  • Antineoplastic Agents
  • Antineoplastic Combined Chemotherapy Protocols
  • Caco-2 Cells
  • Cell Cycle (drug effects)
  • Cell Division (drug effects)
  • Dose-Response Relationship, Drug
  • Farnesol (analogs & derivatives, pharmacology)
  • HL-60 Cells
  • Humans
  • Hydroquinones (pharmacology)
  • In Vitro Techniques
  • Lovastatin (pharmacology)
  • Mice
  • Terpenes (chemistry, pharmacology)
  • Time Factors

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