ArticlePloS one2016
Up-Regulation of CYP2C19 Expression by BuChang NaoXinTong via PXR Activation in HepG2 Cells.
Article in PloS one, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 12 citations in OpenAlex.
- Integrative analysis of thiamethoxam induced hepatocellular carcinoma toxicity mechanisms.Scientific reports · 2025Article
- Naoxintong capsule for treating cardiovascular and cerebrovascular diseases: from bench to bedside.Frontiers in pharmacology · 2024Review
- Article
- Integrative Medicine on Optimizing Clopidogrel and Aspirin Therapy.Chinese journal of integrative medicine · 2019Review
- A Metabonomics Investigation into the Therapeutic Effects of BuChang NaoXinTong Capsules on Reversing the Amino Acid-Protein Interaction Network of Cerebral Ischemia.Oxidative medicine and cellular longevity · 2019Article
- Chinese Experts Consensus on Clinical Application of Naoxintong Capsule ().Chinese journal of integrative medicine · 2018Article
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
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Abstract
backgroundCytochrome P450 2C19 (CYP2C19) is an important drug-metabolizing enzyme (DME), which is responsible for the biotransformation of several kinds of drugs such as proton pump inhibitors, platelet aggregation inhibitors and antidepressants. Previous studies showed that Buchang NaoXinTong capsules (NXT) increased the CYP2C19 metabolic activity in vitro and enhanced the antiplatelet effect of clopidogrel in vivo. However, the underlying molecular mechanism remained unclear. In the present study, we examined whether Pregnane X receptor (PXR) plays a role in NXT-mediated regulation of CYP2C19 expression.
methodsWe applied luciferase assays, real-time quantitative PCR (qPCR), Western blotting and cell-based analysis of metabolic activity experiments to investigate the NXT regulatory effects on the CYP2C19 promoter activity, the mRNA/ protein expression and the metabolic activity.
resultsOur results demonstrated that NXT significantly increased the CYP2C19 promoter activity when co-transfected with PXR in HepG2 cells. Mutations in PXR responsive element abolished the NXT inductive effects on the CYP2C19 promoter transcription. Additionally, NXT incubation (150 and 250μg/mL) also markedly up-regulated endogenous CYP2C19 mRNA and protein levels in PXR-transfected HepG2 cells. Correspondingly, NXT leaded to a significant enhancement of the CYP2C19 catalytic activity in PXR-transfected HepG2 cells.
conclusionIn summary, this is the first study to suggest that NXT could induce CYP2C19 expression via PXR activation.
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