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. 2019 May 7;10:496. doi: 10.3389/fphar.2019.00496

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Copyright © 2019 Qin, Zhang, Yang, Li, Xu, Yao, Zhang, Gonzalez and Yao.

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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UGT1A9-mediated propofol-O-glucuronidation, excretion of propofol-O-glucuronide in HeLa1A9 cells, and expression of UGT1A9 and efflux transporters in HeLa1A9 cells. (A) Kinetic profiles for the glucuronidation of propofol (5–400 μM) by UGT1A9. (B) kinetic profiles for the glucuronidation of propofol (5–400 μM) by the HeLa1A9 cell lysate. In each panel, the inset shows the corresponding Eadie–Hofstee plot. (C) Excreted propofol-O-glucuronide in the extracellular solution at two concentrations of propofol (40 and 80 μM). (D) excretion rates of propofol-O-glucuronide at different concentrations (40 and 80 μM). (E) protein expression of transporters UGT1A9, BCRP, and four transporters of the MRP family in HeLa and HeLa1A9 cells. Data are presented as mean ± SD. ^∗p < 0.05, ^∗∗p < 0.01, or ^∗∗∗p < 0.001 as compared with propofol (40 μM).