Objective: To investigate the influence of isoliensinine (IL) on CYP3A enzyme activity.
Methods: A mixture metabolic system of liver microsome enzymes in vitro was developed. A HPLC method to test the metabolic activity of CYP3A was established with testosterone as a probe. The activities of CYP3A enzymes were measured with different IL concentrations and incubation time with testosterone.
Results: In mixture metabolic system of liver microsome enzymes, the best incubation concentration of testosterone was 200 μmol/L, the best incubation time was 210 min, in this condition the IC₅₀ of IL for CYP3A inhibition was >1 000 μmol/L.
Conclusion: No significant interaction between IL and CYP3A is detected, which indicates that IL might be used with CYP 3A enzyme substrates.