Artemisinins as Anticancer Drugs: Novel Therapeutic Approaches, Molecular Mechanisms, and Clinical Trials

Artemisinin and its derivatives have shown broad-spectrum antitumor activities in vitro and in vivo. Furthermore, outcomes from a limited number of clinical trials provide encouraging evidence for their excellent antitumor activities. However, some problems such as poor solubility, toxicity and cont...

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Main Authors: Cangcang Xu, Huihui Zhang, Lingli Mu, Xiaoping Yang
Format: Article
Language:English
Published: Frontiers Media S.A. 2020-10-01
Series:Frontiers in Pharmacology
Subjects:
Online Access:https://www.frontiersin.org/article/10.3389/fphar.2020.529881/full
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author Cangcang Xu
Huihui Zhang
Lingli Mu
Xiaoping Yang
author_facet Cangcang Xu
Huihui Zhang
Lingli Mu
Xiaoping Yang
author_sort Cangcang Xu
collection DOAJ
description Artemisinin and its derivatives have shown broad-spectrum antitumor activities in vitro and in vivo. Furthermore, outcomes from a limited number of clinical trials provide encouraging evidence for their excellent antitumor activities. However, some problems such as poor solubility, toxicity and controversial mechanisms of action hamper their use as effective antitumor agents in the clinic. In order to accelerate the use of ARTs in the clinic, researchers have recently developed novel therapeutic approaches including developing novel derivatives, manufacturing novel nano-formulations, and combining ARTs with other drugs for cancer therapy. The related mechanisms of action were explored. This review describes ARTs used to induce non-apoptotic cell death containing oncosis, autophagy, and ferroptosis. Moreover, it highlights the ARTs-caused effects on cancer metabolism, immunosuppression and cancer stem cells and discusses clinical trials of ARTs used to treat cancer. The review provides additional insight into the molecular mechanism of action of ARTs and their considerable clinical potential.
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spelling doaj.art-ea799e7c97124c179920fcb3f8d0e5632022-12-21T19:27:34ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122020-10-011110.3389/fphar.2020.529881529881Artemisinins as Anticancer Drugs: Novel Therapeutic Approaches, Molecular Mechanisms, and Clinical TrialsCangcang XuHuihui ZhangLingli MuXiaoping YangArtemisinin and its derivatives have shown broad-spectrum antitumor activities in vitro and in vivo. Furthermore, outcomes from a limited number of clinical trials provide encouraging evidence for their excellent antitumor activities. However, some problems such as poor solubility, toxicity and controversial mechanisms of action hamper their use as effective antitumor agents in the clinic. In order to accelerate the use of ARTs in the clinic, researchers have recently developed novel therapeutic approaches including developing novel derivatives, manufacturing novel nano-formulations, and combining ARTs with other drugs for cancer therapy. The related mechanisms of action were explored. This review describes ARTs used to induce non-apoptotic cell death containing oncosis, autophagy, and ferroptosis. Moreover, it highlights the ARTs-caused effects on cancer metabolism, immunosuppression and cancer stem cells and discusses clinical trials of ARTs used to treat cancer. The review provides additional insight into the molecular mechanism of action of ARTs and their considerable clinical potential.https://www.frontiersin.org/article/10.3389/fphar.2020.529881/fullartemisininsantitumormechanism of actionclinical trialstherapeutic approach
spellingShingle Cangcang Xu
Huihui Zhang
Lingli Mu
Xiaoping Yang
Artemisinins as Anticancer Drugs: Novel Therapeutic Approaches, Molecular Mechanisms, and Clinical Trials
Frontiers in Pharmacology
artemisinins
antitumor
mechanism of action
clinical trials
therapeutic approach
title Artemisinins as Anticancer Drugs: Novel Therapeutic Approaches, Molecular Mechanisms, and Clinical Trials
title_full Artemisinins as Anticancer Drugs: Novel Therapeutic Approaches, Molecular Mechanisms, and Clinical Trials
title_fullStr Artemisinins as Anticancer Drugs: Novel Therapeutic Approaches, Molecular Mechanisms, and Clinical Trials
title_full_unstemmed Artemisinins as Anticancer Drugs: Novel Therapeutic Approaches, Molecular Mechanisms, and Clinical Trials
title_short Artemisinins as Anticancer Drugs: Novel Therapeutic Approaches, Molecular Mechanisms, and Clinical Trials
title_sort artemisinins as anticancer drugs novel therapeutic approaches molecular mechanisms and clinical trials
topic artemisinins
antitumor
mechanism of action
clinical trials
therapeutic approach
url https://www.frontiersin.org/article/10.3389/fphar.2020.529881/full
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