Tissue distribution and elimination of sesaminol triglucoside and its metabolites in rat.

Sesame exhibits many beneficial physiological effects, which are mostly related to its lignan compounds, such as sesaminol glucosides. This investigation studies the distribution and elimination of sesaminol triglucoside from sesame in Sprague Dawley (SD) rats. In order to investigate the distribution of sesaminol triglucoside (p.o. 500 mg/kg) in SD rats, the changes in concentration of sesaminol triglucoside and its metabolites were determined in tissues and plasma within 24 h period after tube-feeding to SD rats. Results showed that sesaminol triglucoside may be deglycosylated to form sesaminol first by intestinal microflora and then incorporated via lymphatic absorption into the cardiovascular system, transported to other tissues. The concentrations of sesaminol triglucoside and its metabolites in rectum, caecum, colon, and small intestines are higher than those in liver, lung, kidney, and heart. Its concentration in brain is low but detectable. Glucuronidation and sulfation was the main metabolic pathway for sesaminol in urine, and fecal elimination was a major route of elimination. From LC/MS/MS analysis of rat organs, sesaminol triglucoside can be converted to mammalian lignans, enterodiol (END), and enterolactone (ENL), by rat intestinal microflora. In the plasma, concentrations of END and ENL were 5.9 +/- 0.2 and 5.5 +/- 0.2 micromol/mL, respectively.