Lim Jung-Sun, Jeong Sun-Young, Hwang Ji-Yoon, Park Han-Jin, Kim Yong-Bum, Rana Suresh V S, Yoon Seokjoo
Toxicogenomics Team, Korea Institute of Toxicology, Yuseong, Daejeon, Republic of Korea.
Int J Toxicol. 2007 May-Jun;26(3):213-20. doi: 10.1080/10915810701352697.
An attempt has been made to identify molecular markers of intrahepatic cholestasis in mice employing phalloidin as a cholestatic agent. Phalloidin was administered to BALB/c mice at three predetermined dose: 250 microg/kg, 500 microg/kg, and 1 mg/kg for 1, 3, and 7 days. Liver function was estimated to confirm cholestasis. Histopathological observations on liver were also made to confirm liver injury. Phalloidin at 1 mg/kg for 7 days was found to induce cholestasis. Therefore gene expression studies were confined to this group only. A total of 88 genes were found to be affected by phalloidin. These were the genes associated with cytoskeleton regulation as well as tight junction, focal adhesion, and ATP-binding cassette transporters. Such proteins obstruct the removal of bile components from hepatocytes to the bile canaliculus or blood. Phalloidin treatment did not affect the proteins responsible for cell maintenance or death. The authors show that phalloidin-induced intrahepatic cholestasis is manifested by disturbing the cytoskeleton. The set of genes up-regulated by phalloidin can be considered as molecular markers of intrahepatic cholestasis. The observations are further expected to be helpful in the management of cholestatic pharmaceuticals and associated problems of liver diseases in humans.
研究人员尝试利用鬼笔环肽作为致胆汁淤积剂来鉴定小鼠肝内胆汁淤积的分子标志物。将鬼笔环肽以250微克/千克、500微克/千克和1毫克/千克这三种预定剂量给予BALB/c小鼠,给药1天、3天和7天。评估肝功能以确认胆汁淤积。还对肝脏进行组织病理学观察以确认肝损伤。发现1毫克/千克的鬼笔环肽给药7天可诱导胆汁淤积。因此,基因表达研究仅局限于该组。总共发现88个基因受鬼笔环肽影响。这些基因与细胞骨架调节以及紧密连接、粘着斑和ATP结合盒转运蛋白相关。此类蛋白质阻碍胆汁成分从肝细胞向胆小管或血液的转运。鬼笔环肽处理不影响负责细胞维持或死亡的蛋白质。作者表明,鬼笔环肽诱导的肝内胆汁淤积表现为细胞骨架紊乱。鬼笔环肽上调的一组基因可被视为肝内胆汁淤积的分子标志物。这些观察结果有望进一步有助于人类胆汁淤积性药物的管理及相关肝脏疾病问题的解决。