Related Experiment Video
Updated: Oct 3, 2026

Isolation of Cerebral Capillaries from Fresh Human Brain Tissue
Published on: September 12, 2018
Subcellular expression of UGT1A6 and CYP1A1 responsible for propofol metabolism in human brain
1Department of Anesthesiology, Union Hospital, Huazhong University of Science & Technology, Wuhan 430022, China. zhangshv@public.wh.hb.cn
Aim:
To observe the subcellular expression of UDP-glucuronosyltransferase 1A6 (UGT1A6) and cytochrome P-450 1A1 (CYP1A1) mRNA in the human brain and investigate the effect of brain on extrahepatic metabolism of propofol.
Methods:
Fifteen patients scheduled for craniotomy under propofol anesthesia were selected. Brain tis sue was taken and blood samples from the radial artery and the internal jugular vein were drawn simultaneously. PCR technique was used to detect UGT1A6 and CYP1A1 mRNA in the microsomes and mitochondria. Enzymatic activities were assayed. Blood propofol and propofol-glucuronide concentrations were measured with HPLC and GC, respectively.
Results:
UGT1A6 mRNA was located mainly in the microsomes, and CYP1A1 mRNA was mainly in the mitochondria. The higher blood concentration of propofol and lower blood concentration of propofol-glucuronide were observed from the radial artery than from the internal jugular vein, respectively. The Km of UGT1A6 and CYP1A1 was (0.74 +/- 0.21) mmol and (548 +/- 50) mmol, respectively. The Vmax was (536 +/- 98) nmol . h-1 . mg-1 and (37 +/- 5) nmol . h-1 . mg-1, respectively.
Conclusion:
The human brain is an important organ for extrahepatic metabolism of propofol. The metabolism occurs within microsomes and mitochondria in brain.
More Related Videos
Related Concept Videos
Pharmacogenetics of Phase I Enzymes: Cytochrome P450 Isozymes
Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters
Pharmacokinetics in Pediatric Patients: Drug Metabolism
Pharmacogenetics of Drug Metabolism: Overview
Drug Metabolism: Phase II Reactions

