Guo Yi, Bruno Richard S
Human Nutrition Program, Department of Human Sciences, The Ohio State University, Columbus, OH 43210, USA.
Human Nutrition Program, Department of Human Sciences, The Ohio State University, Columbus, OH 43210, USA.
J Nutr Biochem. 2015 Mar;26(3):201-10. doi: 10.1016/j.jnutbio.2014.10.008. Epub 2014 Nov 12.
Quercetin is a dietary flavonol that has poor and highly variable bioavailability. Epidemiological studies suggest that higher dietary intakes of quercetin decease cardiovascular disease (CVD) risk. However, experimental findings examining its cardioprotective activities are inconsistent, thereby precluding a full understanding of its health benefits. Bioavailability of dietary constituents is a critical mediator of their health benefits. Thus, a better understanding of the factors regulating quercetin bioavailability is expected to support its potential role in managing CVD risk. This review provides an update on the evidence describing endogenous and exogenous factors responsible for the limited and highly variable bioavailability of quercetin. It focuses on pharmacokinetics studies in clinical and animal models, while also describing strategies aimed at improving quercetin bioavailability to better realize its cardioprotective activities in vivo that are routinely observed in vitro. Although significant advances have been made in understanding determinants of quercetin bioavailability, additional research in controlled trials is needed to more comprehensively examine dose-response effects, whether its cardioprotective activities improve in response to its greater bioavailability, and if the putative health benefits of quercetin are mediated directly or indirectly from one or more of its metabolites generated during xenobiotic metabolism.
槲皮素是一种膳食黄酮醇，其生物利用度较低且变化很大。流行病学研究表明，较高的膳食槲皮素摄入量可降低心血管疾病（CVD）风险。然而，研究其心脏保护活性的实验结果并不一致，因此无法全面了解其健康益处。膳食成分的生物利用度是其健康益处的关键调节因素。因此，更好地了解调节槲皮素生物利用度的因素有望支持其在管理CVD风险中的潜在作用。本综述提供了有关描述槲皮素生物利用度有限且变化很大的内源性和外源性因素的证据的最新情况。它侧重于临床和动物模型中的药代动力学研究，同时还描述了旨在提高槲皮素生物利用度以更好地在体内实现其体外常规观察到的心脏保护活性的策略。尽管在了解槲皮素生物利用度的决定因素方面取得了重大进展，但仍需要在对照试验中进行更多研究，以更全面地检查剂量反应效应、其心脏保护活性是否会随着生物利用度的提高而改善，以及槲皮素假定的健康益处是否直接或间接由其在异生物质代谢过程中产生的一种或多种代谢物介导。
