基于柑橘内源组分提高多甲氧基黄酮生物利用度的作用机制研究

Polymethoxyflavones (PMFs), which possess various health-promoting functions, such as anticancer, anti-inflammatory, antioxidant, neuroprotective, antibacterial and anti-lipogenic activities, exist exclusively in citrus genus especially in the citrus peels. Poor hydrophilic solubility and bioavailability have been technological puzzles restricting the application of PMFs in food industry. Previous studies show that emulsions based on citrus autogenous components have potential advantages in improving the oral bioavailability of PMFs. But the mechanism is still unclear. Therefore, the promotion mechanism of citrus autogenous components on PMFs bioavailability will be studied in this project, regarding the relationship among PMFs emulsion, digestion and absorption in vitro, as well as absorption, transport, distribution and metabolism in vivo as the main thread. Firstly, PMFs-loaded oil in water emulsions will be fabricated using citrus pectin as emulsifier and citrus oil as oil phase. The stability mechanism will be investigated by analyzing the physicochemical characteristics of the emulsion and the interaction between different components. Secondly, we will study the effect of citrus components on digestion and absorption of PMFs in delivery system by using in vitro digestion model combined with Caco-2 cell monolayer model. Finally, the regulation mechanism of citrus components on PMFs bioavailability in vivo will be illustrated by using Sprague-Dawley rat model. The research results will lay foundations for fully displaying the efficacy of PMFs in vivo and have great implications for the future application of PMFs in the food industry.

多甲氧基黄酮（PMFs）是一类柑橘属特有的具有抗癌、抗氧化、抗炎、抑制脂肪生成等多种生物活性的黄酮，但水溶性差、生物利用度低极大限制了其在食品中的应用。团队前期研究表明基于柑橘内源组分构建的乳液体系具有提升PMFs生物利用度的巨大潜力，但机制不明。因此本项目拟从分子互作入手以“PMFs乳液体系-体外消化吸收-体内吸收转运代谢”为主线研究柑橘内源组分对PMFs生物利用度的提升机理。以柑橘内源组分果胶为乳化剂、柑橘油和三酰甘油混合油为油相，构建PMFs乳液体系，利用乳液理化性质、组分互作研究柑橘内源组分稳定PMFs乳液体系的机制；以体外消化模型和Caco-2单层细胞模型研究柑橘内源组分对PMFs的体外消化规律和肠内吸收机制；以SD大鼠模型研究柑橘内源组分对PMFs体内吸收转运代谢分布的调控机制，本研究将为提高PMFs在体内功效的发挥提供理论依据，为PMFs在食品领域的高效利用奠定理论基础。

多甲氧基黄酮（PMFs）是一类柑橘属特有的具有抗癌、抗氧化、抗炎、抑制脂肪生成等多种生物活性的黄酮，但水溶性差、生物利用度低极大限制了其在食品中的应用。团队前期研究表明基于柑橘内源组分构建的乳液体系具有提升PMFs生物利用度的巨大潜力，但机制不明。因此，本项目以“柑橘内源性组分制备-PMFs乳液体系-消化吸收机理”为主线研究了柑橘内源组分对PMFs生物利用度的提升机理。首先，以乳化性能和发酵特性为导向研究了化学法（酸碱提取）、物理法（超高压）和生物法（酶法）及联合技术对柑橘果胶、不溶性纤维等内源性组分提取率、结构及乳化特征的影响；其次，构建了柑橘果胶-黄酮-精油等内源性组分运载体系并对其稳定机理进行了研究；然后，探讨了柑橘内源性组分乳液体系的消化机理及生物利用度的提升机制；最后，研究了柑橘多甲氧基黄酮-柚皮苷缓解ApoE−/−小鼠动脉粥样硬化的作用机理。本研究将为提高PMFs在体内功效的发挥提供理论依据，为PMFs在食品领域的高效利用奠定理论基础。