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Celastrol in cancer therapy: Recent developments, challenges and prospects
Hannah Ying Lim1, Pei Shi Ong2, Lingzhi Wang3
1Department of Pharmacy, National University of Singapore, 117559, Singapore; Cancer Science Institute of Singapore, National University of Singapore, 117599, Singapore.
Abstract:
Cancer is one of the world's biggest healthcare burdens and despite the current advancements made in treatment plans, the outcomes for oncology patients have yet to reach their full potential. Hence, there is a pressing need to develop novel anti-cancer drugs. A popular drug class for research are natural compounds, due to their multi-targeting potential and enhanced safety profile. One such promising natural bioactive compound derived from a vine, Tripterygium wilfordii is celastrol. Pre-clinical studies revolving around the use of celastrol have revealed positive pharmacological activities in various types of cancers, thus suggesting the chemical's potential anti-cancerous effects. However, despite the numerous preclinical studies carried out over the past few decades, celastrol has not reached human trials for cancer. In this review, we summarize the mechanisms and therapeutic potentials of celastrol in treatment for different types of cancer. Subsequently, we also explore the possible reasons hindering its development for human use as cancer therapy, like its narrow therapeutic window and poor pharmacokinetic properties. Additionally, after critically analysing both in vitro and in vivo evidence, we discuss about the key pathways effected by celastrol and the suitable types of cancer that can be targeted by the natural drug, thus giving insight into future directions that can be taken, such as in-depth analysis and research of the druggability of celastrol derivatives, to aid the clinical translation of this promising anti-cancer lead compound.
Insights
Celastrol, a natural compound from Tripterygium wilfordii, shows anti-cancer potential in preclinical studies. Further research into its derivatives is needed to overcome development hurdles for human cancer therapy.
Area of Science:
- Natural Product Chemistry
- Pharmacology
- Oncology
Background:
- Cancer remains a significant global health challenge, necessitating novel therapeutic strategies.
- Natural compounds offer multi-targeting potential and improved safety profiles for drug development.
- Celastrol, derived from Tripterygium wilfordii, is a promising natural compound with demonstrated anti-cancer activities in preclinical research.
Purpose of the Study:
- To review the mechanisms and therapeutic potential of celastrol in various cancers.
- To explore challenges hindering celastrol's clinical translation, including its narrow therapeutic window and poor pharmacokinetics.
- To discuss key pathways affected by celastrol and identify suitable cancer targets for future research.
Main Methods:
- Comprehensive literature review of in vitro and in vivo studies on celastrol's anti-cancer effects.
- Analysis of celastrol's pharmacological activities and mechanisms of action.
- Critical evaluation of factors limiting clinical development and potential solutions.
Main Results:
- Celastrol exhibits significant pharmacological activities against diverse cancer types in preclinical models.
- Key pathways modulated by celastrol have been identified, suggesting specific therapeutic applications.
- Developmental challenges such as poor pharmacokinetic properties and a narrow therapeutic window were highlighted.
Conclusions:
- Celastrol is a promising natural anti-cancer lead compound with significant therapeutic potential.
- Addressing its pharmacokinetic limitations and therapeutic window is crucial for clinical advancement.
- Further research into celastrol derivatives and their druggability is essential for successful clinical translation.
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