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Evaluation of Absorption and Plasma Pharmacokinetics of Tyrosol Acyl Esters in Rats.
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2020-01-13 , DOI: 10.1021/acs.jafc.9b05112 Fawen Yin 1, 2 , Xinmiao Wang 1 , Yuanyuan Hu 1 , Hongkai Xie 3 , Xiaoyang Liu 1, 2 , Lei Qin 1, 2 , Jianghua Zhang 1 , Dayong Zhou 1, 2 , Fereidoon Shahidi 4
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2020-01-13 , DOI: 10.1021/acs.jafc.9b05112 Fawen Yin 1, 2 , Xinmiao Wang 1 , Yuanyuan Hu 1 , Hongkai Xie 3 , Xiaoyang Liu 1, 2 , Lei Qin 1, 2 , Jianghua Zhang 1 , Dayong Zhou 1, 2 , Fereidoon Shahidi 4
Affiliation
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Lipophenols are regarded as an emerging source of functional food ingredients. However, little is known about their in vivo digestion, absorption, and metabolism. Thus, the pharmacokinetic characteristics in rat and the gut microbial degradation of tyrosol acyl esters (TYr-Es) with fatty acids of C12:0, C18:0, and C18:2 were investigated for the first time. Major metabolites including tyrosol sulfate and tyrosol glucuronide, rather than the parent compounds, were detected in rat plasma after oral administration of TYr-Es. The increased plasma half-life (T1/2) and mean residence time demonstrated that TYr-Es display a longer duration of action in vivo than TYr, potentially leading to higher oral bioavailability. TYr-Es could be hydrolyzed by the gut microbiota to free TYr, which may result in the appearance of the second absorption peak in pharmacokinetic profiles. Therefore, TYr-Es exhibit improved bioavailability compared to that of TYr because of their prolonged duration of action.
中文翻译：
评价大鼠酪醇酰基酯的吸收和血浆药代动力学。
脂酚被认为是功能性食品成分的新兴来源。但是，关于它们的体内消化，吸收和代谢知之甚少。因此，首次研究了大鼠体内的药代动力学特征和脂肪酸C12：0，C18：0和C18：2对酪醇酰基酯（TYr-Es）的肠道微生物降解作用。口服TYr-Es后在大鼠血浆中检测到主要的代谢产物，包括硫酸酪醇和酪醇葡糖醛酸，而不是母体化合物。血浆半衰期（T1 / 2）和平均停留时间的增加表明，TYr-Es在体内的作用持续时间比TYr长，可能导致更高的口服生物利用度。TYr-Es可被肠道菌群水解成游离TYr，这可能会导致药物动力学曲线中出现第二个吸收峰。因此，由于TYr-E的作用时间延长，因此与TYr相比具有更高的生物利用度。
更新日期：2020-01-24
中文翻译：
评价大鼠酪醇酰基酯的吸收和血浆药代动力学。
脂酚被认为是功能性食品成分的新兴来源。但是，关于它们的体内消化，吸收和代谢知之甚少。因此，首次研究了大鼠体内的药代动力学特征和脂肪酸C12：0，C18：0和C18：2对酪醇酰基酯（TYr-Es）的肠道微生物降解作用。口服TYr-Es后在大鼠血浆中检测到主要的代谢产物，包括硫酸酪醇和酪醇葡糖醛酸，而不是母体化合物。血浆半衰期（T1 / 2）和平均停留时间的增加表明，TYr-Es在体内的作用持续时间比TYr长，可能导致更高的口服生物利用度。TYr-Es可被肠道菌群水解成游离TYr，这可能会导致药物动力学曲线中出现第二个吸收峰。因此，由于TYr-E的作用时间延长，因此与TYr相比具有更高的生物利用度。
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