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Repurposing Artemisinin and its Derivatives as Anticancer Drugs: A Chance or Challenge?
Zhaowu Ma1, Clariis Yi-Ning Woon2, Chen-Guang Liu1
1School of Basic Medicine, Health Science Center, Yangtze University, Jingzhou, China.
Abstract:
Cancer has become a global health problem, accounting for one out of six deaths. Despite the recent advances in cancer therapy, there is still an ever-growing need for readily accessible new therapies. The process of drug discovery and development is arduous and takes many years, and while it is ongoing, the time for the current lead compounds to reach clinical trial phase is very long. Drug repurposing has recently gained significant attention as it expedites the process of discovering new entities for anticancer therapy. One such potential candidate is the antimalarial drug, artemisinin that has shown anticancer activities in vitro and in vivo. In this review, major molecular and cellular mechanisms underlying the anticancer effect of artemisinin and its derivatives are summarised. Furthermore, major mechanisms of action and some key signaling pathways of this group of compounds have been reviewed to explore potential targets that contribute to the proliferation and metastasis of tumor cells. Despite its established profile in malaria treatment, pharmacokinetic properties, anticancer potency, and current formulations that hinder the clinical translation of artemisinin as an anticancer agent, have been discussed. Finally, potential solutions or new strategies are identified to overcome the bottlenecks in repurposing artemisinin-type compounds as anticancer drugs.
Insights
Artemisinin, an antimalarial drug, shows promise as an anticancer therapy by targeting tumor cell proliferation and metastasis. This review explores its mechanisms, potential, and challenges for clinical use.
Area of Science:
- Oncology
- Pharmacology
- Drug Discovery
Background:
- Cancer is a leading global cause of death, necessitating novel therapeutic strategies.
- Traditional drug discovery is lengthy; drug repurposing offers a faster alternative for identifying new anticancer agents.
- Artemisinin, an established antimalarial, exhibits promising anticancer activities in preclinical studies.
Purpose of the Study:
- To review the molecular and cellular mechanisms of artemisinin's anticancer effects.
- To explore signaling pathways targeted by artemisinin and its derivatives in cancer.
- To identify challenges and potential solutions for repurposing artemisinin as an anticancer drug.
Main Methods:
- Literature review of studies on artemisinin's anticancer properties.
- Analysis of molecular and cellular mechanisms of action.
- Evaluation of pharmacokinetic properties and formulation challenges.
Main Results:
- Artemisinin derivatives exhibit anticancer effects through various molecular and cellular pathways.
- Key signaling pathways involved in tumor proliferation and metastasis are modulated by artemisinin.
- Pharmacokinetic limitations and formulation issues currently hinder clinical translation.
Conclusions:
- Artemisinin holds significant potential for repurposing as an anticancer agent.
- Overcoming pharmacokinetic and formulation challenges is crucial for its clinical application.
- Further research into optimized artemisinin-type compounds could lead to new cancer therapies.
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