Celastrol Applications in Cancer Therapy and Inflammation

Celastrol, a quinone methide triterpene derived from the traditional Chinese medicinal herb Tripterygium wilfordii, has attracted intense interest for its dual capacity to combat cancer and modulate inflammatory processes. In oncology, celastrol exerts antiproliferative effects across a spectrum of tumour types by inducing cell‐cycle arrest, promoting programmed cell death and triggering autophagy through pathways such as ROS/JNK signalling and suppression of Akt/mTOR activity. Structural optimisation and novel delivery systems seek to overcome limitations in solubility, bioavailability and therapeutic window. In parallel, celastrol’s anti‐inflammatory credentials derive from targeted inhibition of NF-κB activation, down-regulation of proinflammatory cytokines and blockade of damage-associated molecular pattern molecules, thereby attenuating tissue injury in models of colitis, diabetic nephropathy and ischaemia–reperfusion. The compound’s multi-target profile, including modulation of heat shock proteins and covalent engagement of critical redox enzymes, underpins a growing pipeline of preclinical studies exploring combination regimens and derivative design to enhance efficacy and safety.

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Celastrol Applications in Cancer Therapy and Inflammation publication trend

The graph below shows the total number of articles in celastrol applications in cancer therapy and inflammation across all publications each year (not limited to Nature Index journals).

Technical terms

PROTAC: A chimeric molecule that recruits an E3 ubiquitin ligase to a target protein, enabling its proteasomal degradation.

Quantitative proteomics: Mass spectrometry-based methods to measure relative or absolute abundances of proteins in complex samples.

Reactive oxygen species (ROS): Chemically reactive molecules derived from oxygen that can induce oxidative stress and modulate signalling pathways.

Epithelial–mesenchymal transition (EMT): A cellular programme in which epithelial cells acquire mesenchymal traits, enhancing migratory and invasive potential.

Peroxiredoxin 1 (PRDX1): A thiol-dependent peroxidase involved in reactive oxygen species detoxification and redox signalling.

High mobility group protein 1 (HMGB1): A nuclear protein that, when released extracellularly, acts as a proinflammatory alarmin by binding to pattern recognition receptors.

References

1. Celastrol mediates autophagy and apoptosis via the ROS/JNK and Akt/mTOR signaling pathways in glioma cells. Journal of Experimental & Clinical Cancer Research (2019).
2. Celastrol: A Review of Useful Strategies Overcoming its Limitation in Anticancer Application. Frontiers in Pharmacology (2020).
3. Celastrol, an NF-κB Inhibitor, Improves Insulin Resistance and Attenuates Renal Injury in db/db Mice. PLOS ONE (2013).
4. Celastrols as Inducers of the Heat Shock Response and Cytoprotection* [boxs]. Journal of Biological Chemistry (2004).
5. Celastrol suppresses colorectal cancer via covalent targeting peroxiredoxin 1. Signal Transduction and Targeted Therapy (2023).
6. Degradation‐Based Protein Profiling: A Case Study of Celastrol. Advanced Science (2024).
7. Celastrol exerts a neuroprotective effect by directly binding to HMGB1 protein in cerebral ischemia–reperfusion. Journal of Neuroinflammation (2021).