Clioquinol is an antiseptic drug and is effective against multidrug-resistant Candida. Clioquinol prevented more than 90 % of biofilm formation, which can be attributed to blockade of hyphal development. Clioquinol also reduced the metabolic activity of sessile Candida but the susceptibility was lower compared to planktonic cells (0.031 - 0.5 µg/ml required to inhibit 50 % planktonic cells and 4 - 16 µg/ml to inhibit 50% preformed biofilms)[3]. Clioquinol fully protected D. melanogaster from the infection. Effective concentration found in modelling indicated that clioquinol was highly effective against C. albicans (0.306 μg/mL) in easily achievable serum levels; clioquinol rapidly achieved kill rate reaching the maximum effect after 13 hours[4]. The antimicrobial strength of 3% clioquinol cream depended on the species but it can act on most of the species. It could inhibit the growth of most fungal species with different strength, but the antibacterial activity was weak. For Candida tropicalis, Candida guilliermondii, Aspergillus terreus, Fusarium solani and Trichoderma harzianum, the inhibition zone was biggest among all the tested drugs. The antifungal activity for Dermatophytes and Candida albicans was moderate[5].
CQ treatment increased total H3K4me3, H3K9me3, and H3K27me3
iScience. 2022 Jun 3;25(7):104517.
Human adipocyte-derived stem cells (hADSCs)
25 µM and 50 µM
16 hours
CQ treatment increased total H3K4me3, H3K9me3, and H3K27me3
iScience. 2022 Jun 3;25(7):104517.
Yeast cells
0.6 µM
16 hours
Clioquinol significantly reduced the accumulation of Aβ, and this effect was dependent on metal binding.
Proc Natl Acad Sci U S A. 2014 Mar 18;111(11):4013-8.
DRG neurons
3 µM
20 seconds
To investigate the effect of CQ in DRG neurons, results showed that CQ activated Ca2+ influx via TRPA1.
Proc Natl Acad Sci U S A. 2009 May 19;106(20):8374-9.
MCF10A
20 µM
24 hours
To test the proteasome inhibition and apoptosis induction effects of Clioquinol mixed with copper on normal and malignant breast cells. Results showed that Clioquinol mixed with copper had significant inhibitory effects on malignant cells but no effect on normal cells.
Breast Cancer Res. 2005;7(6):R897-908.
MDA-MB-231
20 µM
24 hours
To test the proteasome inhibition and apoptosis induction effects of Clioquinol mixed with copper on breast cancer cells. Results showed that Clioquinol mixed with copper significantly inhibited proteasome activity and induced apoptosis.
To evaluate the effect of CQ on tau protein levels. Results showed that 5 µM CQ significantly reduced tau protein levels detected by non-phospho dependent Tau5
Int J Mol Sci. 2021 Nov 8;22(21):12063.
M1C cells
1 µM
24 hours
To evaluate the effect of CQ on intracellular Cu+ levels. Results showed that 1 µM CQ significantly reduced intracellular Cu+ levels
Int J Mol Sci. 2021 Nov 8;22(21):12063.
M1C cells
0.1 to 10 µM
24 hours
To evaluate the effect of CQ on cell viability. Morphological analysis and ATP assay showed that CQ up to 10 µM had no effect on cell viability, but 100 µM CQ was cytotoxic
Int J Mol Sci. 2021 Nov 8;22(21):12063.
HL-1 cardiomyocytes
80 μg/ml
24 hours
Evaluate the inhibitory effect of Clioquinol on ISO-induced ferroptosis in HL-1 cardiomyocytes. Results showed that Clioquinol significantly inhibited ISO-induced ferroptosis in HL-1 cardiomyocytes.
Front Pharmacol. 2022 Jul 22;13:918292.
HL-1 cardiomyocytes
0, 10, 20, 40, 60, 80, 100 μg/ml
24 hours
Evaluate the cytotoxicity of Clioquinol on HL-1 cardiomyocytes. Results showed that when the concentration of Clioquinol was 60–100 μg/ml, HL-1 cells exhibited significant cytotoxicity.
Front Pharmacol. 2022 Jul 22;13:918292.
HEK293 cells
0, 1, 5, 6, 8, 10 µM
24 hours
To evaluate the effect of CQ on lipid peroxidation. CQ increased lipid peroxidation in HEK293 cells, while the antioxidants NAC and Trolox significantly reduced CQ-induced lipid peroxidation.
Front Pharmacol. 2022 Oct 4;13:1000278.
HepG2 cells
0, 1, 2, 3, 4, 5, 10 µM
24 hours
To evaluate the effect of CQ on ATP levels. Only at the highest concentrations, a small but significant reduction of ATP was detected in both media.
Front Pharmacol. 2022 Oct 4;13:1000278.
SK-N-SH cells
5 µM
24 hours
Clioquinol at low dose increased cell viability and reversed cell death caused by MPP+ or H2O2, reducing apoptosis and ROS levels.
Aging (Albany NY). 2020 May 18;12(10):9515-9533.
HEK293 cells
0.5–8 µM
30 minutes
Reduced mutant protein expression and cell death
Proc Natl Acad Sci U S A. 2005 Aug 16;102(33):11840-5.
PC12 cells
4 µM
48 hours
Reduced mutant protein accumulation and cell death
Proc Natl Acad Sci U S A. 2005 Aug 16;102(33):11840-5.
HDMECs
10 µM
48 hours
Assessed cell viability, showing selective and significant reduction
Angiogenesis. 2025 Feb 3;28(2):13.
HUVECs
10 µM
48 hours
Assessed cell viability, showing selective and significant reduction
Angiogenesis. 2025 Feb 3;28(2):13.
CNE-2s cells
1 µM
6 hours
Enhanced radiosensitivity of CNE-2s cells through autophagy inhibition, activation of the caspase system and impairment of DNA damage repair
Int J Biol Sci. 2020 Jan 14;16(5):777-789.
Yeast cells
0.8 µM
7 hours
Clioquinol promotes Aβ degradation through a metal-dependent mechanism, reducing Aβ levels and restoring functional vesicle trafficking
ACS Chem Neurosci. 2017 Sep 20;8(9):2039-2055.
A2780 cells
13.00±2.1 µM (IC50)
72 hours
Compare the cytotoxicity of clioquinol and its analogues, IC50 value was 13.00±2.1 μM
Cancer Lett. 2011 Dec 15;312(1):11-7.
Panc-1 cells
5.89±0.28 µM (IC50)
72 hours
Compare the cytotoxicity of clioquinol and its analogues, IC50 value was 5.89±0.28 μM
Cancer Lett. 2011 Dec 15;312(1):11-7.
DHL-4 cells
2.71±0.18 µM (IC50)
72 hours
Compare the cytotoxicity of clioquinol and its analogues, IC50 value was 2.71±0.18 μM
Cancer Lett. 2011 Dec 15;312(1):11-7.
HL-60 cells
12.90±0.16 µM (IC50)
72 hours
Compare the cytotoxicity of clioquinol and its analogues, IC50 value was 12.90±0.16 μM
Cancer Lett. 2011 Dec 15;312(1):11-7.
Raji cells
5.09±0.20 µM (IC50)
72 hours
Compare the cytotoxicity of clioquinol and its analogues, IC50 value was 5.09±0.20 μM
Cancer Lett. 2011 Dec 15;312(1):11-7.
CHO cells
10 µM
To investigate whether CQ directly activates TRPA1, results showed that CQ evoked currents in CHO cells via TRPA1 activation.
Proc Natl Acad Sci U S A. 2009 May 19;106(20):8374-9.
Human glioblastoma (U87)
50 µM
CQ treatment increased total H3K4me3, H3K9me3, and H3K27me3
iScience. 2022 Jun 3;25(7):104517.
Clioquinol/氯碘羟喹 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Caenorhabditis elegans
Glutamatergic neuron-specific Aβ expression model
Soaking administration
0.125-0.25 μM
24-hour treatment followed by 4-day observation
Clioquinol synergizes with DHPM-thiones to significantly protect Aβ-expressing glutamatergic neurons from toxicity
ACS Chem Neurosci. 2017 Sep 20;8(9):2039-2055.
Caenorhabditis elegans
Glutamatergic neuron model expressing Aβ
Acute administration
0.5 μM, 1 μM, 2 μM
Single dose, transferred to normal media after 24 hours
Clioquinol significantly reduced Aβ-induced neuronal loss and improved the survival rate of the worms.
Proc Natl Acad Sci U S A. 2014 Mar 18;111(11):4013-8.
BALB/c mice
Matrigel plug assay
Subcutaneous injection
10 µM
7 days
Assessed blood vessel formation, showing a 43% reduction in microvessel density
Angiogenesis. 2025 Feb 3;28(2):13.
BALB/C nu/nu mice
CNE-2s cell xenograft model
Intraperitoneal injection
10 mg/kg
Once every other day for one week
CQ combined with zinc significantly enhanced the radiosensitivity of CNE-2s cells and inhibited tumor growth
Int J Biol Sci. 2020 Jan 14;16(5):777-789.
Rhesus monkeys (Macaca mulatta lasiotis)
MPTP-induced Parkinson’s disease model
Oral
10 mg/kg
Twice daily for four weeks
Clioquinol significantly improved motor and non-motor deficits induced by MPTP, reduced iron content and ROS levels in the SN, improved pathology, and activated the AKT/mTOR pathway.
Aging (Albany NY). 2020 May 18;12(10):9515-9533.
Mice
Wild-type and TRPA1-deficient mice
Intraplantar injection
2.5 nmoles
Single injection, observed for 4 hours
To investigate the acute nociceptive effects of CQ in mice, results showed that CQ caused mechanical hyperalgesia and cold hypersensitivity via TRPA1.
Proc Natl Acad Sci U S A. 2009 May 19;106(20):8374-9.
C57BL/6 mice
Diabetic wound model
Local injection
4 μg/wound
Dressing changed on postoperative days 3 and 6
To evaluate the efficacy of EXOsiFDX1-PDA@CQ in diabetic wound models. Results showed that EXOsiFDX1-PDA@CQ significantly promoted wound healing, reduced Cu content, and inhibited FDX1 expression.
Adv Sci (Weinh). 2025 Jan;12(4):e2413408
C57BL/6 mice
MSU-induced acute peritonitis
Intraperitoneal injection
5 mg/kg or 10 mg/kg
Every 12 hours for 24 hours
To evaluate the therapeutic effect of CQ on MSU-induced acute peritonitis, results showed that CQ significantly reduced the frequency and number of white blood cells, neutrophils, and monocytes, and decreased the release of IL-1β, IL-6, and TNF-α.
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