Food Industry Research and Development Institute, Hsinchu, Taiwan.
J Agric Food Chem. 2012 Sep 5;60(35):8616-23. doi: 10.1021/jf302699f. Epub 2012 Aug 23.
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 IC(50) 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.
芝麻木脂素如芝麻素、芝麻素醇和芝麻林素是芝麻油的主要成分，都具有亚甲二氧基苯基和多种体内功能。以前的研究报告表明，芝麻素醇，一种四氢呋喃型木质素，被代谢为哺乳动物木质素。本研究检测了芝麻素醇在 Sprague-Dawley（SD）大鼠中的组织分布。在 SD 大鼠管饲（po 220mg/kg）后 24 小时内，测定了芝麻素醇及其代谢物（芝麻素醇葡萄糖醛酸/硫酸盐、羟甲基芝麻素-四氢呋喃、肠内酯和肠二醇）在组织中的浓度变化。在器官（肝、心、脑和肾）中，肠二醇和肠内酯的浓度明显高于芝麻素醇及其四氢呋喃代谢物。这项研究表明，与四氢呋喃代谢物相比，芝麻素醇对细胞色素 P450（CYPs）具有更强的抑制作用。芝麻素醇对 CYP1A2、CYP2C9、CYP2C19、CYP2D6 和 CYP3A4 的 IC（50）值分别为 3.57、3.93、0.69、1.33 和 0.86μM。此外，羟甲基芝麻素-四氢呋喃和肠二醇分别是 CYP2C9 和 CYP1A2 的弱抑制剂。
