Department of Food Science, Rutgers University, 65 Dudley Road, New Brunswick 08901, New Jersey, USA.
Food Funct. 2021 Apr 21;12(8):3307-3323. doi: 10.1039/d0fo03403g. Epub 2021 Mar 18.
Citrus fruits are among the most popularly consumed fruits worldwide, including oranges, grapefruits, pomelos and lemons. Citrus flavonoids such as hesperidin, naringin and nobiletin have shown an array of health benefits in cell, animal and clinical studies, including antioxidative, anti-inflammatory, neuroprotective, anticancer, and anti-obesity activities. Citrus flavonoids have limited bioavailability after oral administration, leaving the major part unabsorbed and persisted in the colon. Recent studies have highlighted the important role of the gut microbiota and in vivo biotransformation on the bioactivity of citrus flavonoids. This article discusses the biological fate of citrus flavonoids from the viewpoint of their absorption, distribution, metabolism and excretion in vivo. Many delivery systems have been designed to enhance the oral bioavailability of citrus flavonoids, such as emulsions, self-emulsifying systems, nanoparticles and solid dispersions. The ultimate goal of these delivery systems is to enhance the bioefficacy of citrus flavonoids. Several studies have found that the increased bioavailability leads to enhanced bioefficacy of citrus flavonoids in specific animal models. Regarding the complex dynamics of citrus flavonoids and gut microbiota, the bioavailability-bioactivity relationship is an interesting but under-discussed area. Comprehensively understanding the biological fate and bioefficacy of citrus flavonoids would be helpful to develop functional foods with better health benefits.
柑橘类水果是全球最受欢迎的水果之一，包括橙子、葡萄柚、柚子和柠檬。在细胞、动物和临床研究中，柑橘类黄酮，如橙皮苷、柚皮苷和诺米林，表现出了一系列的健康益处，包括抗氧化、抗炎、神经保护、抗癌和抗肥胖活性。柑橘类黄酮经口服给药后生物利用度有限，大部分未被吸收并在结肠中持续存在。最近的研究强调了肠道微生物群和体内生物转化对柑橘类黄酮生物活性的重要作用。本文从柑橘类黄酮在体内的吸收、分布、代谢和排泄的角度讨论了其生物学命运。已经设计了许多输送系统来提高柑橘类黄酮的口服生物利用度，如乳液、自乳化系统、纳米粒子和固体分散体。这些输送系统的最终目标是提高柑橘类黄酮的生物功效。一些研究发现，生物利用度的增加导致柑橘类黄酮在特定动物模型中的生物功效增强。考虑到柑橘类黄酮和肠道微生物群的复杂动态，生物利用度-生物功效关系是一个有趣但讨论较少的领域。全面了解柑橘类黄酮的生物学命运和生物功效将有助于开发具有更好健康益处的功能性食品。
