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. 2020 May 6;35:101735. doi: 10.1016/j.tmaid.2020.101735

Table 3.

In vitro antiviral activity of CQ and its derivatives on non-CoVs.

Drug Virus Cells EC50 (μM) SI Main findings Year Ref
CQ HIV-1 HL3Tl – – ↑ viral replicationp 1988 [126]
CQ HIV-1 H-9 – low toxicity ↓ viral replication 1990 [118]
CQa HIV-1 H-9 – No toxicity ↓ viral replication 1998 [119]
CQa HIV-1 U-937 – No toxicity ↓ viral replication 1998 [119]
CQb HIV-1 H-9 0.9 No toxicity ↓ viral replication 1999 [120]
CQb HIV-1 U-937 0.4 No toxicity ↓ viral replication 1999 [120]
CQb HIV-1 T cellsk 0.9 No toxicity ↓ viral replication 1999 [120]
CQb HIV-1 Monocytesk 0.2 No toxicity ↓ viral replication 1999 [120]
CQb HIV-1 U-1l 0.1 No toxicity ↓ viral replication 1999 [120]
CQb HIV-1 ACH-2m 1 No toxicity ↓ viral replication 1999 [120]
CQc HIV-1 U-937 0.4 No toxicity ↓ viral replication 2001 [121]
CQc HIV-1 H-9 0.9 No toxicity ↓ viral replication 2001 [121]
CQc HIV-1 T cellsk 0.9 No toxicity ↓ viral replication 2001 [121]
CQc HIV-1 MΦk 0.2 No toxicity ↓ viral replication 2001 [121]
CQc HIV-1 U-1l 0.1 No toxicity ↓ viral replication 2001 [121]
CQc HIV-1 ACH-2m 1 No toxicity ↓ viral replication 2001 [121]
CQd HIV-1 H-9 1–10 No toxicity ↓ viral replication 2004 [122]
CQ HIV-1 MT-4 8.86 ± 1.18 6 ↓ viral replication 2006 [106] r
HCQ HIV-1 U-937 1 low toxicity ↓ viral replication 1993 [123]
HCQ HIV-1 CEM 10 low toxicity ↓ viral replication 1993 [123]
HCQ HIV-1 63 0.01 No toxicity ↓ viral replication 1996 [124]
HCQ HIV-1 SP 0.1 No toxicity ↓ viral replication 1996 [124]
HCQ HIV-1 63HIV – – ↓ viral replication 1996 [124]
HCQ HIV-1 SPH – – ↓ viral replication 1996 [124]
HCQ HIV-1 MT-4 >12 – Ineffective 2006 [106] r
FQ HIV-1 MT-4 >2.4 – Ineffective 2006 [106] r
HFQ HIV-1 MT-4 2.9 ± 1.1 3 ↓ viral replication 2006 [106]
CQd HIV-2 MT-4 1–10 No toxicity ↓ viral replication 2004 [122]
CQ IAV H1N1 MDCK – – ↓ viral replication 1981 [127]
CQ IAV H1N1 MDCK 3.60 – ↓ viral replication 2006 [128]
CQ IAV H1N1 A549 – – ↓ viral replication 2007 [129]
CQ IAV H1N1 MDCK 1.26 – ↓ viral replication 2007 [130]
CQ IAV H3N2 MDCK 0.84 – ↓ viral replication 2006 [128]
CQ IAV H3N2 MDCK 1.53 – ↓ viral replication 2007 [130]
CQ IAV H3N2 A549 – – ↓ viral replication 2007 [129]
CQ IAV H5N1 A549 – – ↓ viral replication 2013 [29]
CQ IAV H5N9 MDCK 14.38 – ↓ viral replication 2007 [130]
CQ IAV H7N3fh MDCK >20 – Ineffective 2007 [130]
CQ IAV H7N3gh MDCK 14.39 – ↓ viral replication 2007 [130]
CQ Flu B MDCK – – ↓ viral replication 1983 [131]
CQ DENV-2 BHK – – ↓ viral replicationq 1990 [43]
CQ DENV-2 Vero – No toxicity ↓ viral replication 2013 [141]
CQ DENV-2 C6/36 – No toxicity Ineffective 2013 [141]
CQ DENV-2 U-937 – No toxicity ↓ viral replication 2014 [140]
CQ ZIKV Vero 9.82 No toxicity ↓ viral replication 2016 [135]
CQ ZIKV hBMECs 14.20 No toxicity ↓ viral replication 2016 [135]
CQ ZIKV NSCs 12.36 No toxicity ↓ viral replication 2016 [135]
CQ ZIKV NSs – – ↓ viral replication 2016 [135]
CQ ZIKV Vero 4.15 – ↓ viral replication 2017 [134]
CQ ZIKV Huh7 1.72–2.72 – ↓ viral replication 2017 [134]
CQ ZIKV NSs 10 – ↓ viral replication 2017 [136]
AMD ZIKV Vero – – ↓ viral replication 2017 [134]
CQ CHIKV HeLa – – ↓ viral replication 2007 [132]
CQ pre CHIKV Vero 7.0 ± 1.5 37.14 ↓ viral replication 2010 [41]
CQ post CHIKV Vero 17.2 ± 2.1 15.29 ↓ viral replication 2010 [41]
CQ con CHIKV Vero 10.0 ± 1.2 26 ↓ viral replication 2010 [41]
CQ CHIKV MDMn – low toxicity ↓ viral replication 2018 [133]
CQ CHIKV Fibroblastsn – high toxicity ↓ viral replication 2018 [133]
CQ EBOVi HEK 293T 4.7 – ↓ viral replication 2013 [139]
CQ EBOVj Vero 76 16 – ↓ viral replication 2013 [139]
HCQ EBOVi HEK 293T 9.5 – ↓ viral replication 2013 [139]
HCQ EBOVj Vero 76 22 – ↓ viral replication 2013 [139]
AMD EBOVi HEK 293T 2.6 – ↓ viral replication 2013 [139]
AMD EBOVj Vero 76 8.4 – ↓ viral replication 2013 [139]
AQ EBOVi HEK 293T 4.3 – ↓ viral replication 2013 [139]
AQ EBOVj Vero 76 21 – ↓ viral replication 2013 [139]
CQ EBOV MRC-5 – low toxicity ↓ viral replication 2015 [137]
CQ EBOV Vero E6 1.77o – ↓ viral replication 2015 [138]
CQ SINV BHK-21 – – ↓ viral replication 1981 [142]
CQ VSV BHK-21 – – ↓ viral replication 1981 [142]
CQ VSV B104 – – ↓ viral replication 2010 [149]
CQ Rabies NS-20 – – ↓ viral replication 1984 [143]
CQ PICV BHK-21 ↓ viral replication 1989 [147]
CQ Poliovirus HeLa – – Ineffective 1991 [151]
CQ SLE BHK – – ↓ viral replicationq 1990 [43]
CQ POW BHK – – ↓ viral replicationq 1990 [43]
CQ NiV Vero – – ↓ viral replication 2009 [150]
CQ NiV HeLa 0.62 – ↓ viral replication 2010 [148]
CQ HeV Vero – – ↓ viral replication 2009 [150]
CQ HeV HeLa 0.71 – ↓ viral replication 2010 [148]
CQ EBV HH514-16 – – ↑ viral replication 2017 [125]
CQe HCV Huh-7 0.22 – ↓ viral replication 2010 [144]
CQ DHBV PDH – – ↓ viral replication 1990 [145]
CQ DHBV PDH – No toxicity ↓ viral replication 1991 [146]
CQ JEV B104 – – ↓ viral replication 2010 [149]
CQ MARVi HEK 293T 5.5 – ↓ viral replication 2013 [139]
CQ MARVj Vero 76 15 – ↓ viral replication 2013 [139]
HCQ MARVi HEK 293T 9.8 – ↓ viral replication 2013 [139]
HCQ MARVj Vero 76 18 – ↓ viral replication 2013 [139]
AMD MARVi HEK 293T 2.3 – ↓ viral replication 2013 [139]
AMD MARVj Vero 76 8.3 – ↓ viral replication 2013 [139]
AQ MARVi HEK 293T 4.3 – ↓ viral replication 2013 [139]
AQ MARVj Vero 76 42 – ↓ viral replication 2013 [139]
CQ CCHFV Vero E6 – – ↓ viral replication 2015 [150]
CQ CCHFV Huh7 – 21.3 ↓ viral replication 2015 [150]

CQ: Chloroquine; HCQ: Hydroxychloroquine; FQ: Ferroquine; HFQ: Hydroxy ferroquine; AMD: Amodiaquine; Pre: pre-treatment; Post: post-treatment; Con: concurrent; AQ: Aminoquinoline; HIV: Human immunodeficiency viruses; IAV: Influenza A virus; Flu B: Influenza B virus DENV-2: Dengue virus 2; ZIKV: Zika virus; CHIKV: Chikungunya virus; EBOV: Ebola virus; SINV: Sindbis virus; VSV: Vesicular stomatitis virus; PICV: Pichinde virus; SLE: St. Louis encephalitis virus; POW: Powassan virus; NiV: Nipah virus; HeV: Hendra virus; EBV: Epstein-Barr virus; HCV: Hepatitis C virus; DHBV: Duck hepatitis B virus; JEV: Japanese encephalitis virus; MARV: Marburg virus; CCHFV: Crimean-Congo hemorrhagic virus; HL3Tl: HeLa derivative cells; H-9: Human T lymphocytic cells; U-937: Human promonocytic cells; U-1: Human promonocytic cells; ACH-2: Human T lymphocytic cells; MΦ: macrophages; MT-4 cells: HTLV-I-transformed T-cell line; CEM: Human T lymphoblast cells; 63: Human macrophage hybridoma; SP: T-cell line derived from the pleural fluid of an HIV- 1-infected individual; 63HIV: 63 cells infected by HIV; SPH: SP cells infected by HIV; MDCK: Madin Darby canine kidney; A549 cells: Human adenocarcinomic alveolar basal epithelial cells; BHK/BHK-21 cells: Syrian golden Syrian golden fibroblast cells; Vero cells: African green monkey kidney epithelial cells; C6/36: Aedes albopictus cell line; hBMEC: Human brain microvascular endothelial cells; NSCs: Neural stem cells; NS: Neurospheres; Huh7 cells: Human hepatocyte-derived carcinoma cells; HeLa: Human epithelial cell line; MDM: Monocyte-derived macrophages; HEK 293T: Human embryonic kidney cells; MRC-5: Human normal lung fibroblasts; MRC-5: Medical Research Council cell strain 5; B104: Rat neuroblastoma cell; NS-20: Murine neuroblastoma; HH514–16: Burkitt lymphoma cell line; PDH: Primary duck hepatocytes; EC50: 50% Effective concentration; SI: selectivity index defined as the ratio of drug efficacy to cytotoxicity (when no SI value was reported, level of toxicity was indicated if available).

a

Either alone or combined with hydroxyurea (HU1) + didanosine (ddI).

b

In combination with hydroxyurea (HU1) + didanosine (ddI).

c

In combination with hydroxyurea (HU1) + didanosine (ddI) or with hydroxyurea (HU1) + zidovudine (ZDV).

d

Enhanced inhibition against HIV-1 and HIV-2 in combination with HCQ in H9 and MT-4 cells; and against HIV-1 in combination with indinavir (IDV), saquinavir (SQV) or ritonavir (RTV) in MT-4 cells or peripheral blood mononuclear cells (PBMCs).

e

Synergistic inhibitory effect of CQ with IFN-α.

f

A/Mallard/It/43/01 (H7N3).

g

A/Ty/It/220158/02 (H7N3).

h

The haemagglutinins (HAs) of the two avian H7N3 strains differ in two amino acid residues (261 in the HA1 subunit and 161 in HA2 subunit) and display different pH requirements.

i

Viral entry (viral pseudotype assay).

j

Viral replication.

k

Primary cells.

l

Cells stimulated with LPS.

m

Cells stimulated with PMA.

n

Primary non-human primates derived cells.

o

EC50 in μg/mL.

p

Suggested enhanced replication and protection of tat from proteolytic degradation with CQ.

q

Suggested inhibition of virus replication based on increased prM protein in progeny virions rather than M protein due to inhibition of proteolytic process.

r

CQ, HCQ and FQ showed no significant activity against parainfluenza-3 virus, reovirus-1, Sindbis virus, Coxsackie virus, Punta Toro virus, respiratory syncytial virus (RSV), herpes simplex virus-1 (HSV-1), herpes simplex virus-2 (HSV-2), vaccinia virus, vesicular stomatitis virus (VSV), and influenza A virus (H3N2).