Tissue distribution and cytochrome P450 inhibition of sesaminol and its tetrahydrofuranoid metabolites

Kuo Ching Jan, Yi Wei Chang, Lucy Sun Hwang, Chi Tang Ho

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


Sesame lignans such as sesamin, sesaminol, and sesamolin are major constituents of sesame oil, and all have a methylenedioxyphenyl group and multiple functions in vivo. It was previously reported that sesaminol, a tetrahydrofurofuran type lignin, was metabolized to mammalian lignans. The present study examined the tissue distribution of sesaminol in Sprague-Dawley (SD) rats. Changes in the concentration of sesaminol and its metabolites (sesaminol glucuronide/sulfate, hydroxymethylsesaminol-tetrahydrofuran, enterolactone, and enterodiol) were determined in tissues within a 24 h period after tube feeding (po 220 mg/kg) to SD rats. The concentrations of enterodiol and enterolactone were significantly higher than those of sesaminol and its tetrahydrofuranoid metabolites in the organs (liver, heart, brain, and kidney). This study demonstrates that sesaminol has potent inhibition of cytochrome P450 (CYPs), compared to tetrahydrofuranoid metabolites. The IC50 values of CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 for sesaminol were determined as 3.57, 3.93, 0.69, 1.33, and 0.86 μM, respectively. In addition, hydroxymethylsesaminol-tetrahydrofuran and enterodiol were weak inhibitors of CYP2C9 and CYP1A2, respectively.

Original languageEnglish (US)
Pages (from-to)8616-8623
Number of pages8
JournalJournal of agricultural and food chemistry
Issue number35
StatePublished - Sep 5 2012

All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Agricultural and Biological Sciences(all)


  • cytochrome P450
  • sesaminol
  • tetrahydrofuranoid lignans
  • tissue distribution


Dive into the research topics of 'Tissue distribution and cytochrome P450 inhibition of sesaminol and its tetrahydrofuranoid metabolites'. Together they form a unique fingerprint.

Cite this