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首页> 外文期刊>Journal of Functional Foods >Inhibitory activity of sesaminol and sesaminol triglycoside on cytochrome P450 enzymes and their pharmacokinetics in rats. (Special Section: Bioavailability and metabolism of functional food bioactives.)
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Inhibitory activity of sesaminol and sesaminol triglycoside on cytochrome P450 enzymes and their pharmacokinetics in rats. (Special Section: Bioavailability and metabolism of functional food bioactives.)

机译：芝麻素和芝麻素三糖苷对大鼠细胞色素P450酶的抑制活性及其药代动力学（特别部分：功能性食品生物活性物质的生物利用度和代谢。）

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摘要

Sesame lignans have been shown to possess several health benefits. Lignans with a methylenedioxyphenyl group such as sesaminol, sesaminol triglycoside, sesamin or sesamolin are major constituents of sesame. Bioavailability of plant lignans is affected by phytochemical structure and metabolized enzyme (cytochrome P450, CYP). This investigation studied the interference of CYPs on bioavailability of sesaminol and sesaminol triglycoside. Biological fluids were sampled following orally fed sesaminol (120 mg/kg) and sesaminol triglycoside (100 mg/kg), and intravenously injected sesaminol (30 mg/kg) and sesaminol triglycoside (100 mg/kg) through the femoral vein. Results show that maximum concentrations were 0.2+or-0.1 and 0.7+or-0.2 micro g/mL, and the area under the concentration-time curve were 17.2+or-2.8 and 17.6+or-7.6 min micro g/mL after a single oral ingestion of sesaminol triglycoside and sesaminol, respectively. The clearances were 16.4+or-6.57 and 396+or-53.6 mL/min kg, and half-lives were 50.0+or-13.3 and 74.0+or-28.4 min via intravenous injection of sesaminol triglycoside and sesaminol, respectively. Our results show that the oral bioavailability of sesaminol and sesaminol triglycoside was 21.0+or-8.6% and 0.3+or-0.1%, respectively. This study also demonstrates that sesaminol has a more potent inhibitory activity of CYPs, compared to sesaminol triglycoside. The IC50 values of CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 for sesaminol were determined as 0.88, 0.94, 0.78, 4.04 and 0.68 micro M, respectively.
机译：芝麻木脂素已显示具有多种健康益处。具有亚甲基二氧苯基的木质素例如芝麻素，芝麻素三糖苷，芝麻素或芝麻素是芝麻的主要成分。植物木脂素的生物利用度受植物化学结构和代谢酶（细胞色素P450，CYP）的影响。这项研究研究了CYPs对芝麻素和芝麻素三糖苷生物利用度的干扰。口服饲喂芝麻胺（120 mg / kg）和芝麻糖三糖苷（100 mg / kg），并通过股静脉静脉注射芝麻糖胺（30 mg / kg）和芝麻糖三糖苷（100 mg / kg），对生物体液进行采样。结果显示最大浓度分别为0.2+或-0.1和0.7+或-0.2 micro g / mL，浓缩-时间曲线下的面积分别为17.2+或-2.8和17.6+或-7.6 min micro / g / mL。一次单独口服芝麻糖三糖苷和芝麻糖胺。通过静脉注射芝麻素三糖苷和芝麻素半衰期，清除率为16.4+或-6.57和396+或-53.6 mL / min kg，半衰期分别为50.0+或-13.3和74.0+或-28.4 min。我们的结果表明，芝麻素和芝麻素三糖苷的口服生物利用度分别为21.0+或-8.6％和0.3+或-0.1％。这项研究还表明，与芝麻素三糖苷相比，芝麻素具有更强的CYP抑制活性。 CYP1A2，CYP2C9，CYP2C19，CYP2D6和CYP3A4对芝麻素的IC50值分别确定为0.88、0.94、0.78、4.04和0.68 micro M.

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