Niclosamide (BAY2353) is an orally active antihelminthic agent primarily employed in research related to parasitic infections[1]. Niclosamide also functions as a potent STAT3 inhibitor, demonstrating an IC50 of 0.25 μM in HeLa cells[4]. Additionally, Niclosamide exhibits anticancer properties and can inhibit DNA replication in Vero E6 cells[2].[3].[5]. Niclosamide, produced under Good Manufacturing Practice (GMP) guidelines as Niclosamide, is used in parasitic infection research and also serves as an auxiliary reagent for cell therapy manufacturing[1]. This formulation maintains its potency as a STAT3 inhibitor with an IC50 of 0.25 µM in HeLa cells[4]. Niclosamide shows anti-cancer activities, including the inhibition of DNA replication in Vero E6 cells[2].[3].[5].
体内研究
In vivo, Niclosamide administered via oral gavage at doses of 100 mg/kg and 200 mg/kg once a week over eight weeks, significantly reduces tumor growth in models of adrenocortical carcinoma[3].
The same dosage and administration schedule for Niclosamide (100 mg/kg, 200 mg/kg; oral gavage; once a week; 8 weeks) is used to inhibit tumor growth in adrenocortical carcinoma in vivo, confirming its therapeutic potential across different formulations and applications[3].
体外研究
In studies focusing on adrenocortical carcinoma, Niclosamide treatment ranging from 0.6 nM to 46 μM significantly curbs cell proliferation in BD140A, SW-13, and NCI-H295R cell lines[3].
When administered at concentrations between 0.05 to 5 μM for 24 hours, Niclosamide effectively suppresses STAT3-mediated luciferase reporter activity in HeLa cells[4].
At a concentration of 10 μM, it also impedes virus replication in Vero E6 cells[5].
Moreover, Niclosamide at concentrations ranging from 0.6 nM to 46 µM curtails adrenocortical carcinoma cell proliferation in cell lines BD140A, SW-13, and NCI-H295R[3].
Niclosamide also decreases STAT3-mediated luciferase reporter activity in HeLa cells at 0.05-5 µM over 24 hours[4].
Niclosamide (GMP) up to 2 µM for 24 hours shows effectiveness against Zika virus infection in SNB-19 cells[6].
Furthermore, at 1.5 µM over five days, it impedes nuclear factor‐κB ligand (RANKL)-induced transformation of macrophages into osteoclast precursors, especially during the initial phase of osteoclastogenesis[7].
Niclosamide/氯硝柳胺 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Escherichia coli Δ7NR tolC
0.016 μg/ml
16-48 hours
Study the antibacterial activity of niclosamide against E. coli strains lacking TolC and nitroreductases, showing a significant reduction in MIC
mBio. 2020 Sep 15;11(5):e02068-20
Niclosamide/氯硝柳胺 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Murine abscess model
Subcutaneous injection
10 mg/kg
Single dose, 1 hour post-infection
Validate the in vivo synergistic efficacy of niclosamide combined with colistin against MDR Gram-negative pathogens, showing significant reduction in bacterial load
mBio. 2020 Sep 15;11(5):e02068-20
C57BL/6 mice
Bleomycin (BLM)-induced pulmonary fibrosis model
Intravenous injection
2.5 mg/kg
Administered once every other day for 14 days
To evaluate the reversal effect of Ncl-NPs on established pulmonary fibrosis, results showed that Ncl-NPs significantly reduced hydroxyproline content and collagen expression in lung tissues, and reduced lung morphological changes and collagen deposition.
J Adv Res. 2023 Sep;51:109-120.
Mice
ZIKV infection model
Intraperitoneal injection
20 mg/kg
From 5 dpi till euthanasia or death
Test the effect of S100A4 inhibitor niclosamide on ZIKV-induced testicular damage, results showed niclosamide effectively reduces S100A4+ monocyte/macrophage infiltration, inhibits complement activation, alleviates testicular damage, and rescues the fertility of male mice
Nat Commun. 2023 Apr 29;14(1):2476
Mice
SOD1-G93A and FUS transgenic mouse models
Intraperitoneal injection
20 mg/kg and 50 mg/kg
Daily administration, starting from symptom onset until the end stage of the disease
Niclosamide slowed disease progression, increased survival rates, and improved tissue pathology, characterized by reduced gliosis, motor neuron loss, muscle atrophy, and inflammatory pathways.
Neurotherapeutics. 2024 Apr;21(3):e00346
NSG mice
MDS/AML xenograft model
Intraperitoneal (AZA), Oral (NCL)
AZA 2.5 mg/kg/day, NCL 100 mg/kg/day
AZA for 7 consecutive days, NCL for 14 consecutive days
To evaluate the in vivo efficacy of AZA combined with NCL against TP53-mutated MDS/AML cells. Results showed the combination significantly reduced leukemic cell infiltration in all tissues and decreased the proportion of TP53-mutated cells.
Cytoprotective activity against anthrax fusion toxin FP59-induced cell death in CHO cells assessed as cell viability by MTT reduction assay
19540764
HEK293 cells
Function assay
8 h
Inhibition of Wnt/beta-catenin in HEK293 cells assessed as inhibition of Wnt3A-stimulated TOPFlash activity after 8 hrs, IC50=0.34 μM
26272032
HEK293 cells
Function assay
8 h
Inhibition of Wnt3A/beta-casein signaling in HEK293 cells after 8 hrs by TOPflash reporter assay, IC50=0.4 μM
23453073
human A431 cells
Proliferation assay
72 h
Antiproliferative activity against human A431 cells after 72 hrs by MTT assay, IC50=8.8 μM
24900231
human A549 cells
Proliferation assay
120 h
Antiproliferative activity against human A549 cells after 120 hrs by MTT assay, IC50=0.4 μM
16680159
human A549 cells
Proliferation assay
72 h
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=3 μM
24900231
human AsPC1 cells
Cytotoxic assay
72 h
Cytotoxicity against human AsPC1 cells after 72 hrs by MTS assay, IC50=1.47 μM
23459613
human Ava5 cells
Cytotoxic assay
3 days
Cytotoxicity against human Ava5 cells after 3 days by neutral red dye assay, CC50=10 μM
22059983
human blood cancer cells
Cytotoxic assay
72 h
Cytotoxicity against human blood cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM
26272032
human breast cancer cells
Cytotoxic assay
72 h
Cytotoxicity against human breast cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM
26272032
human colon cancer cells
Cytotoxic assay
72 h
Cytotoxicity against human colon cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM
26272032
human DU145 cells
Proliferation assay
72 h
Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay, IC50=0.7 μM
24900231
human HCT116 cells
Cytotoxic assay
72 h
Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=0.45 μM
26272032
human HeLa cells
Growth inhibition assay
24 h
Inhibition of STAT3 in human HeLa cells after 24 hrs by luciferase reporter gene assay, IC50=0.25 μM
24900231
human HeLa cells
Proliferation assay
72 h
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=1.4 μM
24900231
human HeLa cells
5 μM
Function assay
24 h
Inhibition of STAT3 in human HeLa cells at 5 uM after 24 hrs by luciferase reporter gene assay
24900231
human HT-29 cells
Proliferation assay
72 h
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=7.2 μM
24900231
human LoVo cells
Proliferation assay
120 h
Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay, IC50=0.7 μM
16680159
human lung cancer cells
Cytotoxic assay
72 h
Cytotoxicity against human lung cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM
26272032
human MCF7 cells
Cytotoxic assay
Cytotoxicity against ER-positive human MCF7 cells by MTS assay, IC50 =1.06 μM
23416191
human MIAPaCa2 cells
Proliferation assay
120 h
Antiproliferative activity against human MIAPaCa2 cells after 120 hrs by MTT assay, IC50=1.1 μM
16680159
human ovarian cancer cells
Cytotoxic assay
72 h
Cytotoxicity against human ovarian cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM
26272032
human PANC1 cells
Cytotoxic assay
72 h
Cytotoxicity against human PANC1 cells after 72 hrs by MTS assay, IC50=1.73 μM
23459613
human pancreatic cancer cells
Cytotoxic assay
72 h
Cytotoxicity against human pancreatic cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM
26272032
human PC3 cells
Proliferation assay
120 h
Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay, IC50=0.4 μM
16680159
human PC3 cells
Proliferation assay
72 h
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50=11.7 μM
24900231
human prostate cancer cells
Cytotoxic assay
72 h
Cytotoxicity against human prostate cancer cells assessed as growth inhibition after 72 hrs by Cell Titer Glo Assay, IC50=0.13 μM
26272032
human U2OS cells
12.5 μM
Function assay
6 h
Induction of internalization of Frizzled1-GFP (unknown origin) expressed in human U2OS cells at 12.5 uM after 6 hrs by confocal microscopy
23453073
human U87MG cells
Proliferation assay
120 h
Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay, IC50=0.4 μM
16680159
MDA-MB-231 cells
Cytotoxic assay
72 h
Cytotoxicity against human ER negative MDA-MB-231 cells after 72 hrs by MTS assay, IC50=0.79 μM
23459613
mouse RAW264.7 cells
10 μM
Function assay
Cytoprotective activity against anthrax toxin lethal factor/protective antigen-induced cell death in mouse RAW264.7 cells assessed as cell viability at 10 uM by MTT reduction assay
19540764
Vero E6 cells
Function assay
Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA, EC50=0.1 μM
Metastatic Prostate Carcinoma
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Stage IV Prostate Cancer 收起 <<
Phase 2
Recruiting
December 2020
United States, California
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University of California Davis Comprehensive Cancer Center
Recruiting
Sacramento, California, United States, 95817
Contact: Chong-Xian Pan 916-734-3771 cxpan@ucdavis.edu
Principal Investigator: Chong-Xian Pan 收起 <<
Metastatic Prostate Carcinoma
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Recurrent Prostate Carcinoma
Stage IV Prostate Cancer 收起 <<
Phase 1
Recruiting
January 2021
United States, California
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University of California Davis Comprehensive Cancer Center
Recruiting
Sacramento, California, United States, 95817
Contact: Chong-Xian Pan 916-734-3771 cxpan@ucdavis.edu
Principal Investigator: Chong-Xian Pan 收起 <<
United States, North Carolina
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Duke University
Recruiting
Durham, North Carolina, United States, 27710
Contact: Michael Morse, MD 919-684-5705 michael.morse@duke.edu 收起 <<
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