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Review
. 2020 Sep 16;25(11):2012-2022.
doi: 10.1016/j.drudis.2020.09.010. Online ahead of print.

Chloroquine against malaria, cancers and viral diseases

Wenmin Zhou  1 , Hui Wang  2 , Yuqi Yang  3 , Zhe-Sheng Chen  4 , Chang Zou  5 , Jianye Zhang  6
Affiliations
Review

Chloroquine against malaria, cancers and viral diseases

Wenmin Zhou et al. Drug Discov Today. .

Abstract

Quinoline (QN) derivatives are often used for the prophylaxis and treatment of malaria. Chloroquine (CQ), a protonated, weakly basic drug, exerts its antimalarial effect mainly by increasing pH and accumulating in the food vacuole of the parasites. Repurposing CQ is an emerging strategy for new indications. Given the inhibition of autophagy and its immunomodulatory action, CQ shows positive efficacy against cancer and viral diseases, including Coronavirus 2019 (COVID-19). Here, we review the underlying mechanisms behind the antimalarial, anticancer and antiviral effects of CQ. We also discuss the clinical evidence for the use of CQ and hydroxychloroquine (HCQ) against COVID-19.

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Figures

None
Graphical abstract
Figure 1
Figure 1
The chemical structures of antimalarial quinoline derivatives. (a) Chloroquine (CQ); (b) hydroxychloroquine (HCQ); (c) amodiaquine; (d) pyronaridine; (e) piperaquine; (f) mefloquine; (g) lumefantrine; and (h) primaquine.
Figure 2
Figure 2
The process of autophagy. The phagophore, which originated from the endoplasmic reticulum, is extended to form autophagosomes. The autophagosome can engulf damaged or dysfunctional cellular organelles and proteins. It then fuses with lysosomes to form autolysosomes, and the components are eventually degraded by acidic lysosomal hydrolases, which is inhibited by chloroquine (CQ).
Figure 3
Figure 3
Viral infection. The process of viral infection has several stages: viral entry, viral particle transport, uncoating, nucleic acid replication and transcription, post-translational processing, virus assembly, and virus release.
Figure 4
Figure 4
The roles of chloroquine (CQ) in malaria, cancer, and viral diseases.
See this image and copyright information in PMC

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