Related Experiment Video
Updated: Oct 28, 2025

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
The Intracellular Mechanism of Berberine-Induced Inhibition of CYP3A4 Activity
Pan-Feng Feng1, Long-Xun Zhu1, Jing Jie2
1Department of Pharmacy, Affiliated Hospital 2 of Nantong University, and First People's Hospital of Nantong City, Jiangsu Province, 226001, China.
Background:
Berberine (BBR) is an isoquinoline alkaloid extracted from the Chinese medicine, exerting a variety of pharmacological effects. BBR is partially metabolized by cytochrome 3A4 (CYP3A4) in vivo. Some reports indicated that BBR could inhibit the activity of CYP3A4. However, the underlying mechanisms are not completely understood. CYP3A4 is reported to be transcriptionally regulated by two nuclear receptors, nuclear transcription X receptor (PXR) and constitutive androstane receptor (CAR), and degraded via the ubiquitin-proteasome system. Hence, we tried to explore the mechanisms of CYP3A4 inhibition on both transcriptive and protein levels.
Methods:
Western Blot, RT-PCR and Co-immunoprecipitation were used to perform the experiments.
Results:
Our results showed that BBR inhibited the transcription of CYP3A4 gene by downregulating PXR. In addition, BBR accelerated the degradation of CYP3A4 protein via polyubiquitination pathway.
Conclusion:
These findings may lead to the determination of novel drug-drug interactions with BBR, and contribute to future clinical application of BBR.
More Related Videos
13:35Structural Biology and Analytical Chemistry Approaches for Characterizing C-Glycoside Metabolic Enzymes in Human Gut Microbiota
Published on: May 23, 2025
08:03Unveiling Xenobiotic Transport and Effects in Isolated Mitochondria: Insights from Respirometric and Enzymatic Assays
Published on: March 7, 2025
Related Concept Videos
Pharmacokinetics: Drug–Drug Interactions
Inhibition of Cdk Activity
Enzyme Inhibition
Pharmacokinetics: Drug–Food and Drug–Viral Interactions
Drug Elimination by Renal Route: Tubular Secretion
The Electron Transport Chain
Inhibitors of the electron transport chain
Rotenone, a widely used pesticide, prevents electron transfer from Fe-S cluster to ubiquinone or Q...