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Improving the oral bioavailability of beneficial polyphenols through designed synergies

机译：通过设计的协同作用提高有益多酚的口服生物利用度

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A substantial and growing consumer demand exists for plant-based functional foods that improve general health and wellbeing. Amongst consumed phytochemicals, the polyphenolic compounds tend to be the most bioactive. Many commonly consumed polyphenols have been shown to have specific and potent health-promoting activities when assessed by high-throughput in vitro assays and when administered to experimental animals by injection. However, very few have been shown to have any beneficial effects in animals or man when orally consumed, because of the poor bioavailability exhibited by most polyphenols following the ingestion. Consumed polyphenols, like most pharmaceuticals, are regarded as xenobiotics by the body and must overcome many barriers, including extensive enzymatic and chemical modification during digestion and absorption, to reach their site(s) of action. This is especially true for polyphenols targeting the brain, which is protected by the tightly regulated blood–brain barrier. Interestingly, many polyphenols are also known to specifically modify some of the metabolic and transport processes that govern bioavailability. Therefore, the opportunity exists to increase the bioactivity of beneficial polyphenols by designing specific synergistic interactions with polyphenols that improve their oral bioavailability. This hypothesis and review paper will discuss some of the endogenous systems that limit the bioavailability of ingested polyphenols to the body and the brain, and the means by which bioavailability may be improved by specifically designing synergies between orally consumed polyphenols.
机译：消费者对改善整体健康和福祉的植物性功能食品的需求不断增长。在消耗的植物化学物质中，多酚化合物往往是最具生物活性的。当通过高通量体外试验评估并通过注射给药于实验动物时，许多常用的多酚已被证明具有特定而有效的健康促进作用。然而，由于大多数多酚在摄入后表现出较差的生物利用度，因此很少有人口服摄入对动物或人有任何有益作用。像大多数药物一样，食用多酚被人体视为异生物质，必须克服许多障碍，包括在消化和吸收过程中进行广泛的酶和化学修饰，才能达到其作用部位。对于靶向大脑的多酚来说尤其如此，它受到严格调节的血脑屏障的保护。有趣的是，还已知许多多酚会特异性地改变某些控制生物利用度的代谢和转运过程。因此，存在通过设计与多酚的特定的协同相互作用来提高有益多酚的生物活性的机会，从而改善它们的口服生物利用度。该假设和评论文章将讨论限制摄入的多酚对人体和大脑的生物利用度的某些内源性系统，以及通过专门设计口服消耗的多酚之间的协同作用来改善生物利用度的方法。

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