科研之友
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摘要
The metabolism behavior and metabolism-mediated drug-drug interaction might change in the patients with diseases. The present study aims to determine the influence of liver cancers on the metabolism and metabolism-mediated drug-drug interaction of arbidol. Tumor and surrounding tissues were taken to prepare liver tumor liver microsomes and normal liver microsomes. Compared with human liver microsomes (HLMs) from the surrounding tissues, in HLMs from tumor tissues, the metabolism rate decreased at various concentrations of arbidol. The Km value was calculated to be 65 mu M and 6.6 mu M for normal liver microsomes and tumor liver microsomes, respectively. The Vmax value was calculated to be 1.8 and 1.25 nmol/min/mg protein for the normal liver microsomes and tumor liver microsomes. The inhibition difference of arbidol towards the activity of UGT1A9 and UGT2B7 was also investigated, and the results showed that the weaker inhibition of arbidol towards these two UGT isoforms in the tumor liver microsomes was observed. In conclusion, liver cancers affect the metabolism behavior and metabolism mediated drug-drug interaction for arbidol.
- 出版日期2016
- 单位汕头大学
