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中链脂肪酸及其酰基甘油对青霉素V跨Caco-2细胞单层转运的影响。

Effects of medium-chain fatty acids and their acylglycerols on the transport of penicillin V across Caco-2 cell monolayers.

作者信息

Shima M, Yohdoh K, Yamaguchi M, Kimura Y, Adachi S, Matsuno R

机构信息

Department of Food Science and Technology, Faculty of Agriculture, Kyoto University, Japan.

出版信息

Biosci Biotechnol Biochem. 1997 Jul;61(7):1150-5. doi: 10.1271/bbb.61.1150.

DOI:10.1271/bbb.61.1150
PMID:9255979
Abstract

The transport-enhancing effects of medium-chain fatty acids (caproic, caprylic, and capric acids) and their acylglycerols (mono-, di-, and triacylglycerols) were investigated by using Caco-2 cell monolayers as a model of the human intestinal epithelium. Penicillin V was used as a model for a hydrophilic bioactive compound. Among the fatty acids and acylglycerols tested, 1,2-dicaproin, monocaprin, monocaprylin, and capric acid sodium salt effectively enhanced the transport rate, whereas other substances enhanced the rate only slightly or not at all. With each of these four substances, the rate of enhancement was proportional to the concentration at low concentrations, but leveled off at high concentrations. The transport-enhancing effects were well correlated with the reduction in surface tension and with a physico-chemical parameter, denoted by the surface energy-lowering coefficient, characterizing the surface activity of a substance.

摘要

以Caco-2细胞单层作为人肠上皮模型,研究了中链脂肪酸(己酸、辛酸和癸酸)及其酰基甘油(单酰基甘油、二酰基甘油和三酰基甘油)对转运的促进作用。青霉素V用作亲水性生物活性化合物的模型。在所测试的脂肪酸和酰基甘油中,1,2-二己酰甘油、单癸酰甘油、单辛酰甘油和癸酸钠盐有效提高了转运速率,而其他物质仅轻微提高或根本没有提高转运速率。对于这四种物质中的每一种,在低浓度下增强速率与浓度成正比,但在高浓度下趋于平稳。转运增强作用与表面张力的降低以及一个物理化学参数密切相关,该参数由表面能降低系数表示,表征物质的表面活性。

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