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从葛中分离得到的米槁素和去甲米槁素对小鼠肝脏中 BSEP 和 MRP2 的抑制作用。

Suppression of BSEP and MRP2 in mouse liver by miroestrol and deoxymiroestrol isolated from Pueraria candollei.

机构信息

Academic Office for Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, Thailand.

出版信息

Phytomedicine. 2012 Nov 15;19(14):1332-5. doi: 10.1016/j.phymed.2012.06.007. Epub 2012 Sep 25.

Abstract

Miroestrol and deoxymiroestrol are highly active phytoestrogens isolated from the tuberous root of Pueraria candollei var. mirifica (Leguminosae). Modulatory effects of miroestrol and deoxymiroestrol on the mRNAs of BSEP and MRP2 genes involved in bile salt transportation, in C57BL/6 mice were investigated. In contrast to estradiol, miroestrol and deoxymiroestrol suppressed the expression of BSEP and MRP2 mRNA in both male and female mice. The results suggest for the first time that the use of miroestrol and deoxymiroestrol-containing products as alternative medicines or health supplements should be concerned according to their effects on key genes that regulate the bile salt export pump, which could result in the risk of hepatotoxicity and intrahepatic cholestasis.

摘要

米罗昔芬和脱氧米罗昔芬是从美洛昔芬藤(豆科)的块根中分离得到的高活性植物雌激素。本研究探讨了米罗昔芬和脱氧米罗昔芬对参与胆汁盐转运的 BSEP 和 MRP2 基因在 C57BL/6 小鼠中的 mRNA 的调节作用。与雌二醇不同,米罗昔芬和脱氧米罗昔芬在雌雄小鼠中均抑制 BSEP 和 MRP2 mRNA 的表达。这些结果首次表明,由于米罗昔芬和脱氧米罗昔芬会影响调节胆汁盐输出泵的关键基因,因此在将含有米罗昔芬和脱氧米罗昔芬的产品作为替代药物或保健品使用时应谨慎,这可能会导致肝毒性和肝内胆汁淤积的风险。

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