科研之友
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摘要
The present study aims to evaluate the inhibition potential of scutellarin and scutellarein towards the glucuronidation elimination of propofol which is a popular intravenous short-acting hypnotic agent for both induction/maintenance of anesthesia and sedation of mechanically ventilated adults. The in vitro incubation system using human liver microsomes (HLMs)-catalyzed propofol glucuronidation was employed. At the same concentration (100 mu M), scutellarein showed stronger inhibitory effect than scutellarin towards the glucuronidation activity of propofol. Further kinetic study using data fitting with Dixon plot and Lineweaver-Burk plot was carried out to demonstrate the noncompetitive inhibition of scutellarein towards HLMs-catalyzed propofol glucurronidation. The inhibition kinetic parameter (K-i) was calculated to be 69.4 mu M. Relatively weak in vivo inhibition magnitude was predicted using in vivo maximum plasma concentration (C-max) of scutellarein after administration of 400 mg/kg scutellarin for rat. However, complex herbal factors and pharmacokinetic factors might affect the in vitro-in vivo extrapolation (IV-IVE). All these results remind us the necessary monitoring when co-administration of scutellarin or scutellarin- containing herbs with propofol.
- 出版日期2013
- 单位郑州大学
