Metabolism and tissue distribution of sulforaphane in Nrf2 knockout and wild-type mice

John D. Clarke, Anna Hsu, David E. Williams, Roderick H. Dashwood, Jan F. Stevens, Masayuki Yamamoto, Emily Ho

Research output: Contribution to journalArticlepeer-review

126 Citations (Scopus)


Purpose: To determine the metabolism and tissue distribution of the dietary chemoprotective agent sulforaphane following oral administration to wild-type and Nrf2 knockout (Nrf2 -/-) mice. Methods: Male and female wild-type and Nrf2 -/- mice were given sulforaphane (5 or 20 μmoles) by oral gavage; plasma, liver, kidney, small intestine, colon, lung, brain and prostate were collected at 2, 6 and 24 h (h). The five major metabolites of sulforaphane were measured in tissues by high performance liquid chromatography coupled with tandem mass spectrometry. Results: Sulforaphane metabolites were detected in all tissues at 2 and 6 h post gavage, with the highest concentrations in the small intestine, prostate, kidney and lung. A dose-dependent increase in sulforaphane concentrations was observed in all tissues except prostate. At 5 μmole, Nrf2 -/- genotype had no effect on sulforaphane metabolism. Only Nrf2 -/- females given 20 μmoles sulforaphane for 6 h exhibited a marked increase in tissue sulforaphane metabolite concentrations. The relative abundance of each metabolite was not strikingly different between genders and genotypes. Conclusions: Sulforaphane is metabolized and reaches target tissues in wild-type and Nrf2 -/- mice. These data provide further evidence that sulforaphane is bioavailable and may be an effective dietary chemoprevention agent for several tissue sites.

Original languageEnglish
Pages (from-to)3171-3179
Number of pages9
JournalPharmaceutical research
Issue number12
Publication statusPublished - 2011 Dec


  • Nrf2
  • broccoli
  • metabolism
  • sulforaphane
  • tissue distribution

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)


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