Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine (CHQ, 20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine (20 μM) enhances IL-1–induced IL-23 secretion in MoLC and subsequently increases IL-17A release by primed CD4+ T cells[1]. Chloroquine suppressed matrix metalloproteinase (MMP)-2 and MMP-9 mRNA expression and protein activity, whereas MMP-13 mRNA expression and proteolytic activity were increased. Despite enhancing TLR9 mRNA expression, chloroquine suppressed TLR9 protein expression in vitro. Daily treatment of mice with intraperitoneal (i.p.) chloroquine (80 mg/kg/day) for 22 days, did not inhibit the growth of control siRNA or TLR9 siRNA MDA-MB-231 breast cancer cells[2]. The combination of chloroquine with zinc enhanced chloroquine's cytotoxicity and induced apoptosis in A2780 cells[3]. Chloroquine (0.01-100μM; 48 hours) potently blocked virus infection (vero E6 cells infected with SARS-CoV-2) at low-micromolar concentration (EC50=1.13 μM). Chloroquine blocks virus infection by increasing endosomal pH required for virus/cell fusion, as well as interfering with the glycosylation of cellular receptors of SARS-CoV[4].
Chloroquine/氯喹 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Werner syndrome-specific mesenchymal stem cells (WS hMSCs)
0.2 μM to 100 μM
Low concentrations of CQ (0.2-5 μM) promoted cell self-renewal, while higher concentrations (20 μM or above) inhibited cell proliferation. Treatment with 1 μM CQ decreased the percentage of SA-β-gal-positive cells and increased the number of Ki67-positive cells, while also reducing IL-6 secretion.
Inhibited autophagy, decreased transcriptional activity and disrupted the localization of p53-R273H
Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
A549
2.5 ~ 60 µM
Blocked the PI3K/AKT signaling pathway, mediated mitochondrial apoptosis and inhibited autophagy
Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
MCF-7
20 μM
Inhibition of autophagy/mitophagy, induced apoptosis
Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
BT549
20 μM
Inhibition of autophagy/mitophagy, induced apoptosis
Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
MDA-MB-231
20 μM
Inhibition of autophagy/mitophagy, induced apoptosis
Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
MiaPaca-2
100 μM
72 h
Assess the cytotoxicity of CQ-HES, results showed similar cytotoxicity between CQ-HES and HCQ
Biomacromolecules. 2017 Aug 14;18(8):2247-2257.
MiaPaca-1
100 μM
72 h
Assess the cytotoxicity of CQ-HES, results showed similar cytotoxicity between CQ-HES and HCQ
Biomacromolecules. 2017 Aug 14;18(8):2247-2257.
AsPC-1
100 μM
72 h
Assess the cytotoxicity of CQ-HES, results showed similar cytotoxicity between CQ-HES and HCQ
Biomacromolecules. 2017 Aug 14;18(8):2247-2257.
Calu-3 cells
64.7 μM (CQ), 119 μM (HCQ)
To study the inhibitory effect of CQ and HCQ on SARS-CoV-2 infection, results showed that the effective dose in Calu-3 cells was significantly higher than in Vero E6 cells.
J Mol Cell Biol. 2021 Jul 6;13(3):175-184.
Vero E6 cells
6.5 μM
To study the inhibitory effect of CQ and HCQ on SARS-CoV-2 infection, results showed that CQ and HCQ effectively inhibited viral invasion in Vero E6 cells.
J Mol Cell Biol. 2021 Jul 6;13(3):175-184.
Chloroquine/氯喹 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
HCT116 human colon carcinoma xenografts
Intraperitoneal injection
20 mg/kg
Every second day for 16 days
Evaluate the inhibitory effect of CQ on tumor growth, results showed CQ as a single-agent treatment had no significant effect on tumor growth
Autophagy. 2014 Apr;10(4):562-71
C57BL/6J mice
Nilotinib-induced nephrotoxicity model
Intragastric administration
30 mg/kg
Daily for 30 days
To investigate the intervention effect of chloroquine on nilotinib-induced nephrotoxicity. The results showed that chloroquine significantly ameliorated nilotinib-induced renal injury, reduced blood urea nitrogen and serum creatinine levels, and decreased renal fibrosis.
Adv Sci (Weinh). 2023 Sep;10(26):e2302002.
Sprague Dawley (SD) rats
24-month-old rats
Oral
0.1 mg/kg
Twice a week for 5 months
Low-dose CQ treatment extended the lifespan of rats, repressed systemic inflammation, and inhibited fibrosis across multiple tissues. CQ treatment also reduced serum TNF-α levels and the numbers of circulating white blood cells and neutrophils, indicating attenuated chronic inflammation.
Protein Cell. 2022 Jun;13(6):454-461.
Mice
C57Bl/6j mice
Intraperitoneal injection
50 mg/kg
Once daily for 10 days
Detected eIF2α phosphorylation levels, indicating that HCQ can induce eIF2α phosphorylation in vivo
Cell Death Dis. 2021 Jan 6;12(1):6.
Mouse
Breast cancer model
Intraperitoneal injection
40 mg/kg
Once every two days
Inhibition of autophagy/mitophagy, induced apoptosis
Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
Mice
HCoV-OC43 infection model
15 mg/kg
To study the preventive effect of CQ on HCoV-OC43 infection, results showed that 15 mg/kg of CQ effectively prevented infection in mice.
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