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

Pharm Res. 2011 Dec;28(12):3171-9. doi: 10.1007/s11095-011-0500-z. Epub 2011 Jun 17.


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.

Publication types

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

MeSH terms

  • Animals
  • Anticarcinogenic Agents / metabolism*
  • Anticarcinogenic Agents / pharmacokinetics*
  • Female
  • Isothiocyanates
  • Male
  • Mice
  • Mice, Knockout
  • NF-E2-Related Factor 2 / genetics*
  • Thiocyanates / metabolism*
  • Thiocyanates / pharmacokinetics*
  • Tissue Distribution


  • Anticarcinogenic Agents
  • Isothiocyanates
  • NF-E2-Related Factor 2
  • Thiocyanates
  • sulforafan