Uptake of Vitamins D(2), D(3), D(4), D(5), D(6), and D(7) Solubilized in Mixed Micelles by Human Intestinal Cells, Caco-2, an Enhancing Effect of Lysophosphatidylcholine on the Cellular Uptake, and Estimation of Vitamins D' Biological Activities

人肠道细胞 Caco-2 对混合胶束中溶解的维生素 D(2)、D(3)、D(4)、D(5)、D(6) 和 D(7) 的吸收,溶血磷脂酰胆碱对细胞吸收的增强作用,以及维生素 D 生物活性的评估

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Abstract

Vitamins D have various biological activities, as well as intestinal calcium absorption. There has been recent concern about insufficient vitamin D intake. In addition to vitamins D(2) and D(3), there are lesser-known vitamins D(4)-D(7). We synthesized vitamins D(5)-D(7), which are not commercially available, and then evaluated and compared the mixed micelles-solubilized vitamins D uptake by Caco-2 cells. Except for vitamin D(5), the uptake amounts of vitamins D(4)-D(7) by differentiated Caco-2 cells were similar to those of vitamins D(2) and D(3). The facilitative diffusion rate in the ezetimibe inhibited pathway was approximately 20% for each vitamin D type, suggesting that they would pass through the pathway at a similar rate. Lysophosphatidylcholine enhanced each vitamin D uptake by approximately 2.5-fold. Lysophosphatidylcholine showed an enhancing effect on vitamin D uptake by reducing the intercellular barrier formation of Caco-2 cells by reducing cellular cholesterol, suggesting that increasing the uptakes of vitamins D and/or co-ingesting them with lysophosphatidylcholine, would improve vitamin D insufficiency. The various biological activities in the activated form of vitamins D(4)-D(7) were estimated by Prediction of Activity Spectra for Substances (PASS) online simulation. These may have some biological activities, supporting the potential as nutritional components.

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