ArticleBMC complementary and alternative medicine2017
Triptolide Induces hepatotoxicity via inhibition of CYP450s in Rat liver microsomes.
Article in BMC complementary and alternative medicine, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 60 citations in OpenAlex.
- Triptolide: A Narrative Review of Its Traditional Use, Derivatives, Pharmacology, Antitumor Effect, and Clinical Applications.Cancers · 2026Review
- Drug Delivery Systems Based on Dendritic-Cell-Derived Exosomes.Pharmaceutics · 2025Review
- The value of fibroblast growth factor 21 (FGF21) promoter methylation in the repair and regeneration during the course of chronic hepatitis B.Frontiers in cell and developmental biology · 2025Article
- A comprehensive review ofFrontiers in pharmacology · 2023Review
- The molecular pathogenesis of triptolide-induced hepatotoxicity.Frontiers in pharmacology · 2022Review
- A review of herb-induced liver injury in mainland china.Frontiers in pharmacology · 2022Review
- Inflammation aggravated the hepatotoxicity of triptolide by oxidative stress, lipid metabolism disorder, autophagy, and apoptosis in zebrafish.Frontiers in pharmacology · 2022Article
- Therapeutic potential of triptolide in autoimmune diseases and strategies to reduce its toxicity.Chinese medicine · 2021Review
- Zuotai (β-HgS)-containing 70 Wei Zhen-Zhu-Wan differs from mercury chloride and methylmercury on hepatic cytochrome P450 in mice.F1000Research · 2021Article
- Triptolide: pharmacological spectrum, biosynthesis, chemical synthesis and derivatives.Theranostics · 2021Review
- Comprehensive analysis of transcriptomics and metabolomics to understand triptolide-induced liver injury in mice.Toxicology letters · 2020Article
- Integrative analysis of proteomic and metabonomics data for identification of pathways related to Rhizoma Paridis-induced hepatotoxicity.Scientific reports · 2020Article
- Metabolic alterations in triptolide-induced acute hepatotoxicity.Biomedical chromatography : BMC · 2018Article
- The Effect of Triptolide in Rheumatoid Arthritis: From Basic Research towards Clinical Translation.International journal of molecular sciences · 2018Review
- Triptolide Induces Apoptosis Through Fas Death and Mitochondrial Pathways in HepaRG Cell Line.Frontiers in pharmacology · 2018Article
- A Mechanistic Overview of Triptolide and Celastrol, Natural Products fromFrontiers in pharmacology · 2018Review
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundTriptolide (TP), an active constituent of Tripterygium wilfordii, possesses numerous pharmacological activities. However, its effects on cytochrome P450 enzymes (CYP450s) in rats remain unexplored.
methodsIn this study, the effects of triptolide on the six main CYP450 isoforms (1A2, 2C9, 2C19, 2D6, 2E1, and 3A) were investigated both in vivo and in vitro. We monitored the body weight, survival proportions, liver index, changes in pathology, and biochemical index upon TP administration, in vivo. Using a cocktail probe of CYP450 isoform-specific substrates and their metabolites, we then carried out in vitro enzymatic studies in liver microsomal incubation systems via ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). Finally, we verified our results at the messenger ribonucleic acid (mRNA) and protein level through quantitative real-time polymerase chain reaction (RT-qPCR), western blotting, and immunohistochemical detection.
resultsThe in vivo toxicity study confirmed that Sprague-Dawley (SD) rats exhibited dose-dependent hepatotoxicity after intragastric administration of TP [200, 400, and 600 μg/(kg.day)] for 28 days. In case of the CYP450 isoforms 3A, 2C9, 2C19, and 2E1, the in vitro metabolic study demonstrated a decrease in the substrate metabolic rate, metabolite production rate, and Vmax, with an increase in the Km value, compared with that observed in the control group. Additionally, a TP dose-dependent decrease in the mRNA levels was observed in the four major isoforms of CYP3A subfamily (3A1/3A23, 3A2, 3A9, and 3A62) and CYP2C9. A similar effect was also observed with respect to the protein levels of CYP2C19 and CYP2E1.
conclusionsThis study suggests that TP can cause hepatotoxicity by reducing the substrate affinity, activity, and expression at the transcriptional and protein levels of the CYP450 isoforms 3A, 2C9, 2C19, and 2E1. TP also has the potential to cause pharmacokinetic drug interactions when co-administered with drugs metabolized by these four isoforms. However, further clinical studies are needed to evaluate the significance of this interaction.
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