Xiao Jianbo, Högger Petra
Institut fur Pharmazie und Lebensmittelchemie, Universitat Wurzburg, Am Hubland, 97074 Wurzburg, Germany.
Curr Drug Metab. 2014 Jan;15(1):23-9. doi: 10.2174/1389200214666131210142614.
The development of food fortified with polyphenols and polyphenol-rich foods represents a novel approach to prevent or attenuate type 2 diabetes. It has been reported that type 2 diabetes may affect the pharmacokinetics of various drugs in several animal models. There is powerful evidence linking dietary polyphenols consumption with the risk factors defining type 2 diabetes, even if some opposite results occurred. This mini-review summarizes important advances on diabetes-associated changes in pharmacokinetics of natural polyphenols. The pharmacokinetic behavior between drugs and dietary polyphenols probably may be different due to (i) Ingested dose/amount per day. The dietary polyphenol intake per day is much higher than that of clinical drugs; (ii) Complexity of the components. Clinical drugs are well-characterized and typically small molecules. However, the polyphenols in diet are unimaginably complex; (iii) Interaction with food proteins. Although the effects of food proteins on the bioavailability of polyphenols are still not examined in much detail, direct binding interactions of polyphenols to proteins always occur; (iv) The most common polyphenols in the human diet have a low intrinsic activity and are poorly absorbed from the intestine, highly metabolized, or rapidly eliminated. Although there is very limited information available so far, it is proposed that type 2 diabetes influences the pharmacokinetic behavior of dietary polyphenols including: i) competition of glucose with polyphenols regarding binding to plasma proteins; ii) weakened non-covalent interaction affinities of plasma proteins for natural polyphenols due to protein glycation in type II diabetes; iii) the enhanced clearance of polyphenols in type 2 diabetes. An understanding of diabetes-associated changes in absorption, distribution, metabolism, elimination and bioactivities of natural polyphenols as well as the mechanism of the variability should lead to the improvement of the benefits of these polyphenols and clinical outcomes for diabetics.
用多酚强化食品以及富含多酚的食品的开发是预防或减轻2型糖尿病的一种新方法。据报道，在几种动物模型中，2型糖尿病可能会影响各种药物的药代动力学。有强有力的证据表明，即使出现了一些相反的结果，食用膳食多酚与定义2型糖尿病的危险因素之间也存在关联。本综述总结了天然多酚药代动力学中与糖尿病相关变化的重要进展。药物和膳食多酚之间的药代动力学行为可能不同，原因如下：（i）每天的摄入量/数量。膳食多酚的每日摄入量远高于临床药物；（ii）成分的复杂性。临床药物特征明确，通常是小分子。然而，饮食中的多酚极其复杂；（iii）与食物蛋白的相互作用。尽管食物蛋白对多酚生物利用度的影响仍未得到详细研究，但多酚与蛋白之间的直接结合相互作用总是会发生；（iv）人类饮食中最常见的多酚内在活性低，肠道吸收差，代谢快或迅速消除。尽管目前可用的信息非常有限，但有人提出2型糖尿病会影响膳食多酚的药代动力学行为，包括：i）葡萄糖与多酚在与血浆蛋白结合方面的竞争；ii）由于II型糖尿病中的蛋白糖基化，血浆蛋白对天然多酚的非共价相互作用亲和力减弱；iii）2型糖尿病中多酚清除率的提高。了解天然多酚在吸收、分布、代谢、消除和生物活性方面与糖尿病相关的变化以及变异性机制，应能提高这些多酚对糖尿病患者的益处和临床疗效。
