天然 P-糖蛋白抑制剂 EGCG 可提高 Caco-2 细胞单层中叶苷的吸收，并增加大鼠中叶苷的口服生物利用度。
Natural P-gp inhibitor EGCG improves the acteoside absorption in Caco-2 cell monolayers and increases the oral bioavailability of acteoside in rats.
机构信息
College of Biosystems Engineering and Food Science, Fuli Institute of Food Science, National-Local Joint Engineering Laboratory of Intelligent Food Technology and Equipment, Key Laboratory for Agro-Products Nutritional Evaluation of Ministry of Agriculture and Rural Affairs, Key Laboratory of Agro-Products Postharvest Handling of Ministry of Agriculture and Rural Affairs, Zhejiang Key Laboratory for Agro-Food Processing, Zhejiang International Scientific and Technological Cooperation Base of Health Food Manufacturing and Quality Control, Zhejiang University, Hangzhou, 310058, China; College of Standardization, China Jiliang University, Hangzhou, 310018, China.
Department of Applied Technology, Zhejiang Economic and Trade Polytechnic, Hangzhou, 310018, China.
出版信息
Food Chem Toxicol. 2020 Dec;146:111827. doi: 10.1016/j.fct.2020.111827. Epub 2020 Oct 24.
Acteoside is one of the most widespread phenylethanoid glycosides with pharmacological activities, including antioxidant, neuroprotective property, etc. However, its bioavailability is poor due to the low absorption and P-gp efflux. This study aimed to select food derived P-gp inhibitors for promoting the acteoside absorption and investigate whether the inhibitors could increase the bioavailability and stability of acteoside. Results showed that EGCG and quercetin significantly decreased the BL-to-AP efflux and promoted the AP-to-BL influx of acteoside across Caco-2 monolayers with optimum concentrations of 320 μM EGCG or 240 μM quercetin adding to 320 μM acteoside. EGCG increased the bioavailability of acteoside to 1.43-fold, but quercetin had no such effect. Further study showed that EGCG and quercetin had no effects on the storage and digestion stability of acteoside. This work revealed that EGCG could improve the acteoside absorption across the Caco-2 monolayers and enhance the bioavailability of acteoside in rats.
毛蕊花糖苷是具有抗氧化、神经保护等多种药理活性的苯乙醇苷类化合物之一。但其生物利用度较差，这主要是由于其吸收和 P-糖蛋白外排率低所致。本研究旨在筛选促进毛蕊花糖苷吸收的食物来源 P-糖蛋白抑制剂，并探讨抑制剂是否能增加毛蕊花糖苷的生物利用度和稳定性。结果表明，EGCG 和槲皮素分别以 320μM EGCG 或 240μM 槲皮素添加到 320μM 毛蕊花糖苷时，可显著降低 BL-to-AP 的外排，并促进毛蕊花糖苷在 Caco-2 单层细胞中的 AP-to-BL 内流，最佳浓度分别为 320μM EGCG 或 240μM 槲皮素。EGCG 使毛蕊花糖苷的生物利用度提高到 1.43 倍，但槲皮素没有这种作用。进一步的研究表明，EGCG 和槲皮素对毛蕊花糖苷的储存和消化稳定性没有影响。本研究揭示了 EGCG 可提高毛蕊花糖苷在 Caco-2 单层细胞中的吸收，并增强毛蕊花糖苷在大鼠体内的生物利用度。
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