Oral Bioavailability and Metabolism of Hydroxytyrosol from Food Supplements.
Oral Bioavailability and Metabolism of Hydroxytyrosol from Food Supplements.
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DOI：
10.3390/nu15020325
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发表时间：
2023-01-09
期刊：
影响因子：
5.9
通讯作者：
Golz C
中科院分区：
文献类型：
--
作者：
Bender C;Strassmann S;Golz C
橄榄和橄榄油是羟基酪醇（HT）的主要膳食来源，HT是一种天然抗氧化化合物，已成为预防心血管风险的潜在援助。橄榄油的生物利用度研究表明，HT的游离形式和结合形式（如橄榄苦苷及其苷元）均可生物利用。尽管如此，其低膳食摄入量，生物利用度差，以及通过胃肠道吸收后的高个体间差异阻碍了其全部益处。在一项随机、对照、盲法、交叉研究中，我们通过比较两种含有不同剂量HT（30.58和61.48 mg HT/剂量）的橄榄衍生水补充剂，研究了HT代谢和生物利用度的影响。此外，对照组使用HT强化橄榄油。为此，在12名健康志愿者中，在摄入单剂量的补充剂或强化橄榄油后，对血浆和尿液样本进行了评价。在基线和摄入后0.5、1、1.5、2、4和12 h采集血液和尿液样本。HT及其代谢产物采用UHPLC-DAD-MS/MS进行分析。药代动力学结果表明，通过食品补充剂给予的膳食HT是生物可利用的，生物利用度随给药剂量增加而增加。摄入后，高香草酸、HT-3-O-硫酸盐和3，4-二羟基苯乙酸是血浆和尿液中发现的主要代谢物。血浆中的最大浓度在摄入后30 min达到峰值。由于化合物的生物利用度是其作用的基本先决条件，这些结果预示着两种食品补充剂都有很好的潜力，可以防止氧化应激和随之而来的心血管风险。
Table olives and olive oils are the main dietary sources of hydroxytyrosol (HT), a natural antioxidant compound that has emerged as a potential aid in protection against cardiovascular risk. Bioavailability studies with olive oils showed that HT is bioavailable from its free form and from conjugated forms such as oleuropein and its aglycone. Still, its low dietary intake, poor bioavailability, and high inter-individual variability after absorption through the gastrointestinal tract hamper its full benefits. In a randomized, controlled, blinded, cross-over study, we investigated the impact of HT metabolism and bioavailability by comparing two olive-derived watery supplements containing different doses of HT (30.58 and 61.48 mg of HT/dosage). Additionally, HT-fortified olive oil was used in the control group. To this aim, plasma and urine samples were evaluated in 12 healthy volunteers following the intake of a single dose of the supplements or fortified olive oil. Blood and urine samples were collected at baseline and at 0.5, 1, 1.5, 2, 4, and 12 h after intake. HT and its metabolites were analyzed using UHPLC-DAD-MS/MS. Pharmacokinetic results showed that dietary HT administered through the food supplements is bioavailable and bioavailability increases with the administered dose. After intake, homovanillic acid, HT-3-O-sulphate, and 3,4-dihydroxyphenylacetic acid are the main metabolites found both in plasma and urine. The maximum concentrations in plasma peaked 30 min after intake. As bioavailability of a compound is a fundamental prerequisite for its effect, these results promise a good potential of both food supplements for protection against oxidative stress and the consequent cardiovascular risk.