Down-regulation of 20-HETE synthesis and signaling inhibits renal adenocarcinoma cell proliferation and tumor growth

Anticancer Res. 2009 Oct;29(10):3819-24.

Abstract

Background: We examined the ability of inhibitors of the synthesis or actions of 20-HETE, metabolite of arachidonic acid, to inhibit proliferation of human renal carcinoma cell lines.

Materials and methods: 786-O and 769-P cells were exposed to either 10 microM HET0016 (selective inhibitor of 20-HETE synthesis), 10 microM WIT002 (20-HETE antagonist), or vehicle. Subsequently, we assessed the effect of WIT002 on tumor growth in vivo using an ectopic mouse model of clear-cell renal carcinoma.

Results: Addition of HET0016 and WIT002 inhibited the proliferation of 786-O and 769-P human renal cell carcinoma lines. HET0016 and WIT002 had little effect on the proliferation of primary cultures of normal human proximal tubule epithelial cells. WIT002 (10 mg/kg, s.c.) administered daily to athymic nude mice implanted subcutaneously with 786-O cells reduced the growth of the tumors by 84 % compared to vehicle (p<0.001).

Conclusion: 20-HETE is required for proliferation of human renal epithelial cancer.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amidines / pharmacology*
  • Animals
  • Arachidonic Acid / metabolism
  • Carcinoma, Renal Cell / drug therapy*
  • Carcinoma, Renal Cell / metabolism*
  • Carcinoma, Renal Cell / pathology
  • Cell Growth Processes / drug effects
  • Cell Growth Processes / physiology
  • Cytochrome P-450 Enzyme System / biosynthesis
  • Cytochrome P-450 Enzyme System / genetics
  • Cytochrome P450 Family 4
  • Down-Regulation / drug effects
  • Humans
  • Hydroxyeicosatetraenoic Acids / antagonists & inhibitors*
  • Hydroxyeicosatetraenoic Acids / biosynthesis
  • Hydroxyeicosatetraenoic Acids / pharmacology
  • Kidney Neoplasms / drug therapy*
  • Kidney Neoplasms / metabolism*
  • Kidney Neoplasms / pathology
  • Mice
  • Mice, Nude
  • RNA, Messenger / biosynthesis
  • RNA, Messenger / genetics
  • TNF-Related Apoptosis-Inducing Ligand / pharmacology
  • Xenograft Model Antitumor Assays

Substances

  • Amidines
  • HET0016
  • Hydroxyeicosatetraenoic Acids
  • RNA, Messenger
  • TNF-Related Apoptosis-Inducing Ligand
  • Arachidonic Acid
  • 20-hydroxy-5,8,11,14-eicosatetraenoic acid
  • Cytochrome P-450 Enzyme System
  • Cytochrome P450 Family 4
  • CYP4F2 protein, human
  • CYP4F3 protein, human