关键词: Caco-2 cell assay anti-proliferative activity bioaccessibility epigallocatechin gallate molecular docking polyphenol

Mesh : Catechin / analogs & derivatives chemistry Humans Whey Proteins / chemistry Caseins / chemistry Caco-2 Cells Biological Availability Emulsions / chemistry Molecular Docking Simulation Reactive Oxygen Species / metabolism Oxidative Stress / drug effects Drug Carriers / chemistry Antioxidants / pharmacology chemistry pharmacokinetics Intestinal Absorption / drug effects

来  源:   DOI:10.3390/molecules29112588   PDF(Pubmed)

Abstract:
Epigallocatechin gallate (EGCG), the principal catechin in green tea, exhibits diverse therapeutic properties. However, its clinical efficacy is hindered by poor stability and low bioavailability. This study investigated solid particle-in-oil-in-water (S/O/W) emulsions stabilized by whey protein isolate (WPI) and sodium caseinate (NaCas) as carriers to enhance the bioavailability and intestinal absorption of EGCG. Molecular docking revealed binding interactions between EGCG and these macromolecules. The WPI- and NaCas-stabilized emulsions exhibited high encapsulation efficiencies (>80%) and significantly enhanced the bioaccessibility of EGCG by 64% compared to free EGCG after simulated gastrointestinal digestion. Notably, the NaCas emulsion facilitated higher intestinal permeability of EGCG across Caco-2 monolayers, attributed to the strong intermolecular interactions between caseins and EGCG. Furthermore, the emulsions protected Caco-2 cells against oxidative stress by suppressing intracellular reactive oxygen species generation. These findings demonstrate the potential of WPI- and NaCas-stabilized emulsions as effective delivery systems to improve the bioavailability, stability, and bioactivity of polyphenols like EGCG, enabling their applications in functional foods and nutraceuticals.
摘要:
表没食子儿茶素没食子酸酯(EGCG),绿茶中的主要儿茶素,表现出不同的治疗特性。然而,其临床疗效受到稳定性差和生物利用度低的阻碍。这项研究研究了以乳清分离蛋白(WPI)和酪蛋白酸钠(NaCas)为载体稳定的固体颗粒水包油(S/O/W)乳液,以提高EGCG的生物利用度和肠道吸收。分子对接揭示了EGCG与这些大分子之间的结合相互作用。WPI和NaCas稳定的乳液表现出高包封效率(>80%),并且在模拟胃肠消化后与游离EGCG相比,EGCG的生物可及性显著提高64%。值得注意的是,NaCas乳液促进了EGCG跨Caco-2单层的更高的肠道通透性,归因于酪蛋白和EGCG之间强烈的分子间相互作用。此外,乳液通过抑制细胞内活性氧的产生来保护Caco-2细胞免受氧化应激。这些发现证明了WPI和NaCas稳定的乳液作为有效的递送系统来提高生物利用度的潜力。稳定性,和EGCG等多酚的生物活性,使其在功能性食品和营养食品中的应用成为可能。
公众号