Flavonoid metabolites transport across a human BBB model
Flavonoid metabolites transport across a human BBB model
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DOI：
10.1016/j.foodchem.2013.10.095
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发表时间：
2014-04-15
期刊：
影响因子：
8.8
通讯作者：
Calhau, Conceicao
中科院分区：
文献类型：
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作者：
Faria, Ana;Meireles, Manuela;Calhau, Conceicao
本研究旨在评估不同黄酮类化合物（黄烷-3-醇、花青素和黄酮醇）及其代谢产物（甲基化和葡萄糖醛酸结合）跨hCMEC/D3细胞（血脑屏障（BBB）模型）的跨膜转运。进一步代谢的测试化合物进行了测定和他们的运输调制，试图阐明这一过程背后的机制。HPLC-DAD/MS法检测了1、3和18 h时黄酮类化合物及其代谢产物在hCMEC/D3细胞中的转运情况。在一般情况下，代谢产物表现出更高的运输效率比天然类黄酮。由于细胞代谢，未发现代谢物的进一步生物转化。花青素及其代谢产物以亲脂性依赖的方式穿过BBB细胞模型。槲皮素的运输受到磷酸酶调节剂的影响，表明磷酸化/去磷酸化调节机制。总的来说，这项工作表明类黄酮能够穿过BBB并到达中枢神经系统。(C)2013爱思唯尔有限公司保留所有权利。
This study aimed to evaluate the transmembrane transport of different flavonoids (flavan-3-ols, anthocyanins and flavonols) and some of their metabolites (methylated and conjugated with glucuronic acid) across hCMEC/D3 cells (a blood-brain barrier (BBB) model). Further metabolism of the tested compounds was assayed and their transport modulated in an attempt to elucidate the mechanisms behind this process. The transport across hCMEC/D3 cells was monitored in basolateral media at 1, 3 and 18 h by HPLC-DAD/MS.All the flavonoids and their metabolites were transported across hCMEC/D3 cells in a time-dependent manner. In general, the metabolites showed higher transport efficiency than the native flavonoid. No further biotransformation of the metabolites was found as consequence of cellular metabolism. Anthocyanins and their metabolites crossed this BBB cell model in a lipophilicity-dependent way. Quercetin transport was influenced by phosphatase modulators, suggesting a phosphorylation/dephosphorylation regulation mechanism. Overall, this work suggests that flavonoids are capable of crossing the BBB and reaching the central nervous system. (C) 2013 Elsevier Ltd. All rights reserved.