The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cells.

The transport mechanism of monocarboxylate transporter on spinosin in Caco-2 cells.
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Caco-2细胞中斯皮诺素单羧酸转运蛋白的转运机制

DOI:
10.1016/j.jsps.2016.04.021
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发表时间:
2016-05
期刊:
Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society
影响因子:
--
通讯作者:
Ying Huang H
Ying Huang H
中科院分区:
其他
文献类型:
--
作者:
Meng XL;Guo YL;Ying Huang H

文献摘要

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目的:本研究旨在探讨Caco-2细胞中单羧酸转运蛋白(MCT)对多杀菌素(SPI)的摄取机制。研究方法:用不同的一元羧酸预处理Caco-2细胞,用高效液相色谱法(HPLC)测定Caco-2细胞摄取棘球蛋白的量。主要发现:不同单羧酸的预加载均能促进Caco-2细胞对SPI的摄取,尤其是MCT的底物水杨酸对SPI的摄取增加了23.4倍,表明单羧酸转运蛋白对SPI的摄取具有外排作用,水杨酸对SPI外排有较强的抑制作用。同时,Caco-2细胞对SPI的吸收具有Na+和温度依赖性,不加Na+预处理可显著提高SPI的吸收量1.85倍,在低温(4 °C)下培养,SPI的吸收量比37 °C下提高20%。大豆分离蛋白主要通过载体介导的方式转运[Vmax = 5.364 μg/mg protein,Km = 657.0 μg/mL]。结论:Caco-2细胞摄取Spinosin(SPI)主要受单羧酸转运蛋白的调控,其中水杨酸的摄取受单羧酸转运蛋白沿着。
Objectives: The aim of this study was to determine the uptake mechanism of spinosin (SPI) by the monocarboxylic acid transporters (MCTs) in Caco-2 cells. Methods: The Caco-2 cells were pretreated with various monocarboxylic acids, and the uptake of spinosin from Caco-2 cells was measured by High Performance Liquid Chromatography (HPLC). Key findings: Preloading of various monocarboxylic acids enhanced the uptake of SPI, especially salicylic acid (a substrate of MCTs) had a 23.4 times increase in SPI uptake, indicating that the monocarboxylic acid transporters had an efflux effect on SPI uptake and salicylic acid had a strong inhibition on SPI efflux in Caco-2 cells. At the same time, the uptake of SPI through Caco-2 cells was Na+- and temperature-dependent, pretreatment without Na+ significantly increased the uptake of SPI by 1.85 times and incubated at low temperature (4 °C) SPI uptake increased 20% than that of 37 °C. Furthermore, SPI was transported mainly via a carrier-mediated transport: [Vmax = 5.364 μg/mg protein, Km = 657.0 μg/mL]. Conclusion: The uptake of spinosin (SPI) in Caco-2 cells was mainly regulated by the monocarboxylic acid transporters along with Salicylic acid.