Pharmacodynamics and Toxicology of Triptolide in Cancer Treatment
Summary
Triptolide is a highly bioactive diterpenoid epoxide derived from Tripterygium wilfordii, notable for its potent antitumour properties across a range of solid and haematological malignancies. Its pharmacodynamics are diverse, encompassing inhibition of transcriptional machinery, modulation of key survival signalling pathways and induction of multiple forms of programmed cell death, including apoptosis and, more recently, cuproptosis. By targeting transcription factors, epigenetic regulators and efflux transporters, triptolide can reverse chemotherapy resistance and suppress tumour growth in vitro and in vivo. However, its clinical translation is constrained by a narrow therapeutic window and cumulative organ toxicity. Preclinical toxicology studies have implicated oxidative stress, disruption of bile acid homeostasis and inhibition of cytochrome P450 enzymes in hepatotoxicity, prompting the development of structural analogues, targeted delivery systems and combination regimens to improve safety and efficacy.
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Pharmacodynamics and Toxicology of Triptolide in Cancer Treatment publication trend
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Technical terms
Pharmacodynamics: Study of how a drug affects biological systems at molecular and cellular levels.
Toxicology: Assessment of adverse effects of chemical substances on living organisms and their mechanisms.
Cuproptosis: Copper-dependent programmed cell death mediated by accumulation of intracellular copper and mitochondrial protein aggregation.
SHH signalling pathway: Cellular communication cascade initiated by Sonic Hedgehog ligand, involved in cell proliferation and survival.
ABCB1: ATP-binding cassette transporter that mediates drug efflux and contributes to chemotherapy resistance.
Cytochrome P450 enzymes: Family of liver enzymes responsible for metabolism of xenobiotics and endogenous compounds.
Hepatotoxicity: Toxic damage to the liver characterized by impaired metabolic function and cellular injury.
References
- Triptolide: pharmacological spectrum, biosynthesis, chemical synthesis and derivatives. Theranostics (2021).
- Triptolide (TPL) Inhibits Global Transcription by Inducing Proteasome-Dependent Degradation of RNA Polymerase II (Pol II). PLOS ONE (2011).
- Triptolide-induced cuproptosis is a novel antitumor strategy for the treatment of cervical cancer. Cellular & Molecular Biology Letters (2024).
- Targeted inhibition of the HNF1A/SHH axis by triptolide overcomes paclitaxel resistance in non-small cell lung cancer. Acta Pharmacologica Sinica (2024).
- Activation of Nrf2 Protects against Triptolide-Induced Hepatotoxicity. PLOS ONE (2014).
- Triptolide Induces hepatotoxicity via inhibition of CYP450s in Rat liver microsomes. BMC Complementary Medicine and Therapies (2017).
- Activation of Sirt1/FXR Signaling Pathway Attenuates Triptolide-Induced Hepatotoxicity in Rats. Frontiers in Pharmacology (2017).
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