Related Experiment Video
Updated: Apr 15, 2026

Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis
Published on: July 3, 2015
Ganoderic acid B's influence towards the therapeutic window of trifluoperazine (TFP)
Jun Guo1, Chenming Ni2, Xiaoyang Liu3
1Department of Neurology, Tangdu Hospital, the Fourth Military Medical University, Xi'an 710038, P.R. China.
Background:
Ganoderic acid B is an important bioactive ingredient isolated from Ganoderma lucidum, and exhibits various pharmacological activities.
Aims:
To investigate the influence of Ganoderic acid B towards the therapeutic window of trifluoperazine (TFP).
Methods:
In vitro human liver microsomes (HLMs) incubation system was used to determine the inhibition of Ganoderic acid B towards the glucuronidation of trifluoperazine (TFP).
Results:
Ganoderic acid B exerted concentration-dependent inhibition towards the glucuronidation of TFP. Furthermore, Dixon plot was used to determine the inhibition type. The intersection point was located in the second quadrant in Dixon plot, indicating the competitive inhibition of Ganoderic acid B towards TFP glucuronidation. Through fitting the data using competitive nonlinear fitting equation, the inhibition kinetic parameter was calculated to be 56.7 uM.
Conclusion:
All this data indicated the potential influence of Ganoderic acid B-containing herbs towards therapeutic window of TFP. Given that the glucuronidation reaction of TFP is the probe reaction of UGT1A4, the data obtained from the present study also indicated the potential influence of Ganoderic acid-containing herbs towards the therapeutic window of drugs mainly undergoing UGT1A4-mediated metabolism.
More Related Videos
Related Concept Videos
Therapeutic Drug Monitoring: Affecting Factors
Combined Effects of Drugs: Antagonism
The most common type is receptor antagonism, where one drug acts as an antagonist to block the effects of another drug by...
Pharmacodynamics in Geriatric Patients: Effects of Age
Drug Dosing: Geriatric Patients
Antipsychotic Drugs: Therapeutic Uses and Side Effects
Despite these side effects, antipsychotics are used therapeutically for various purposes, including managing schizophrenia, preventing nausea and vomiting, curbing...
Drug Toxicity: Dose-Dependent Reactions

