Cardiothoracic and Vascular Department, University of Pisa, Pisa, Italy.
Eur J Pharm Biopharm. 2012 Jan;80(1):176-84. doi: 10.1016/j.ejpb.2011.09.002. Epub 2011 Sep 24.
To evaluate the ability of grape skin and seeds to protect endothelial progenitor cells (EPC) from oxidative stress induced by hyperglycemia (HG) compared to red wine (RW) and prepare innovative pharmaceutical systems for the oral administration of red grape extract allowing the overcoming of its poor intestinal absorption.
Human EPC were characterized by expression of cell surface markers. Cells were incubated with different concentrations of total polyphenols from grape components or RW in the presence or absence of HG. Cell viability, migration, adhesion, and reactive oxygen species (ROS) production were assayed. Intestinal permeation of polyphenols was studied in the absence or presence of a quaternary ammonium-chitosan conjugate (N⁺(60)-Ch). Grape components and RW increased EPC viability, adhesion and migration, and prevented the HG effect (P < 0.01). ROS production induced by HG was significantly reduced only by grape seed extract and RW (P < 0.01). N⁺(60)-Ch acted as an effective enhancer of polyphenol permeability across the excised rat intestine.
Red grape components are a source of antioxidant compounds that ameliorate EPC viability and function, while preventing endothelial dysfunction. The use of polycationic chitosan derivatives can promote the absorption of polyphenols across intestinal epithelium, thus increasing their bioavailability and potential therapeutic value in atherosclerosis.
评估葡萄皮和籽在保护内皮祖细胞(EPC)免受高血糖(HG)诱导的氧化应激方面的能力,与红葡萄酒(RW)相比,并制备用于口服红葡萄提取物的创新药物系统,以克服其肠道吸收不良的问题。
通过细胞表面标志物的表达来鉴定人 EPC。将细胞与来自葡萄成分的总多酚或 RW 的不同浓度在存在或不存在 HG 的情况下孵育。测定细胞活力、迁移、粘附和活性氧(ROS)的产生。在不存在或存在季铵化壳聚糖缀合物(N⁺(60)-Ch)的情况下研究多酚的肠渗透。葡萄成分和 RW 增加了 EPC 的活力、粘附和迁移,并防止了 HG 的作用(P < 0.01)。仅葡萄籽油和 RW 显著降低了 HG 诱导的 ROS 产生(P < 0.01)。N⁺(60)-Ch 作为一种有效的多酚跨肠上皮通透性增强剂。
红葡萄成分是抗氧化化合物的来源,可改善 EPC 的活力和功能,同时预防内皮功能障碍。使用聚阳离子壳聚糖衍生物可以促进多酚在肠道上皮细胞中的吸收,从而提高其生物利用度和在动脉粥样硬化中的潜在治疗价值。