Measurement of Cytochrome P450 Enzyme Induction and Inhibition in human cells

Scope of the method

The Method relates to
  • Human health
The Method is situated in
  • Basic Research
Type of method
  • In vitro - Ex vivo
This method makes use of
  • Human derived cells / tissues / organs
Specify the type of cells/tissues/organs
parenchymal liver cells, stem cell-derived hepatocyte-like cells
Animal and human derived cells


Method keywords
  • in vitro
  • hepatic cell line
  • luminescence
  • liver enzyme
  • viability test
Scientific area keywords
  • Toxicology
  • Drug metabolism
  • drug screening
  • in vitro cell culture
Method description

By the use of monolayer cultures as an in vitro system, the effects of drugs on CYP3A activity can be evaluated. It relies on the use of a luminogenic CYP3A substrate, namely luciferin-6′-pentafluorobenzylether (luciferin- PFBE). Upon biotransformation by CYP3A, luciferin-PFBE is converted into luciferin, which generates light when combined with a luciferin detection reagent. The normalization of the data relies on the cell number and cell viability and is evaluated by another bioluminescence reaction in which the levels of adenosine- 5′-triphosphate (ATP), the basic energy source of living cells, is measured.

Lab equipment
  • Biosafety cabinet;
  • Luminescence plate reader;
  • White opaque;
  • 96-well plates.
Method status
  • History of use

Pros, cons & Future potential


Quick and easy to use.

References, associated documents and other information

Contact person

Steven Branson


Vrije Universiteit Brussel (VUB)
Pharmaceutical and Pharmacological Sciences
In Vitro Toxicology and Dermato-Cosmetology
Brussels Region