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首页> 外文期刊>Life sciences >EFFECTS OF FLAVONOLS ON P-GLYCOPROTEIN ACTIVITY IN CULTURED RAT HEPATOCYTES
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EFFECTS OF FLAVONOLS ON P-GLYCOPROTEIN ACTIVITY IN CULTURED RAT HEPATOCYTES

机译：黄酮醇对培养大鼠肝细胞中P-糖蛋白活性的影响

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The effects of flavonols on P-glycoprotein (Pgp) activity were studied in cultured rat hepatocytes by assessing the transmembrane transport of Rhodamine-123 (R-123) and doxorubicin (DOX). In freshly-plated hepatocytes, containing a low amount of Pgp, flavonols did not affect the cellular retention of DOX, but strongly inhibited the Pgp-mediated efflux of R-123. In 72h-cultured hepatocytes, spontaneously overexpressing functional Pgp, flavonols inhibited R-123 efflux in a dose-dependent manner, but significantly reduced DOX retention while increasing its efflux. A similar effect was found in hepatocytes obtained from rats in which Pqp was induced in vivo by 2-acetamino-fluorene (AAF) or alpha-naphthyl-isothiocyanate (ANIT) treatments. These findings indicate that flavonols, dietary compounds reported to strongly upregulate the apparent activity of Pgp in cancer cell lines, may also modulate differently the transport of putative Pgp substrates in normal rat hepatocytes. The ability to affect the drug-extruding activity at the hepatocite canalicular membrane could be of relevance to the chemopreventive action of these compounds towards liver carcinogens. [References: 34]
机译：通过评估罗丹明-123（R-123）和阿霉素（DOX）的跨膜转运，在培养的大鼠肝细胞中研究了黄酮醇对P-糖蛋白（Pgp）活性的影响。在含有少量Pgp的新鲜铺板的肝细胞中，黄酮醇不会影响DOX的细胞滞留，但会强烈抑制Rg-123的Pgp介导的流出。在自发地过表达功能性Pgp的72h培养的肝细胞中，黄酮醇以剂量依赖的方式抑制R-123流出，但是在增加其流出的同时显着降低了DOX保留。在从大鼠体内获得的肝细胞中也发现了类似的效果，其中2-乙酰氨基芴（AAF）或α-萘基异硫氰酸酯（ANIT）处理在体内诱导了Pqp。这些发现表明，黄酮醇（据报道能在饮食中强烈上调Pgp在癌细胞系中的表观活性的饮食化合物）也可能不同地调节正常大鼠肝细胞中假定的Pgp底物的转运。影响在肝球囊小管膜上的药物挤出活性的能力可能与这些化合物对肝致癌物的化学预防作用有关。 [参考：34]

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