Pyrrolidinedithiocarbamate ammonium, ranging from 3 to 1000 μM, when used as a pretreatment, dose-dependently reduces IL-8 production in cells[1]. Pyrrolidinedithiocarbamate ammonium functions by inhibiting the activation of NF-κB, effectively diminishing both NF-κB DNA binding and its dependent transcriptional activity. Consequently, the inhibition of NF-κB with pyrrolidinedithiocarbamate ammonium results in decreased IL-8 production by intestinal epithelial cells, underscoring its mechanism of action[1].
体内研究
In experimental models of colitis, specifically in groups treated with DSS (dextran sulfate sodium) and pyrrolidinedithiocarbamate ammonium, there was observed suppression in the shortening of intestinal length and a reduction in the DAI (Disease Activity Index) score. Moreover, levels of activated NF-κB, IL-1β, and TNF-α were significantly lower in the DSS+pyrrolidinedithiocarbamate ammonium-treated group, suggesting that inhibiting NF-κB activity with this compound can delay the healing of mucosal tissue defects, such as erosions or ulcers, caused by inflammation. However, it can significantly suppress the expression of inflammatory cytokines (IL-1β and TNF-α), thus considerably alleviating symptoms of colitis. These properties highlight the potential of pyrrolidinedithiocarbamate ammonium in treating ulcerative colitis[2].
体外研究
Pyrrolidinedithiocarbamate ammonium, ranging from 3 to 1000 μM, when used as a pretreatment, dose-dependently reduces IL-8 production in cells[1].
Pyrrolidinedithiocarbamate ammonium functions by inhibiting the activation of NF-κB, effectively diminishing both NF-κB DNA binding and its dependent transcriptional activity. Consequently, the inhibition of NF-κB with pyrrolidinedithiocarbamate ammonium results in decreased IL-8 production by intestinal epithelial cells, underscoring its mechanism of action[1].
PDTC was used to block p-p65 activity to reduce ROS production and cell apoptosis.
Burns Trauma. 2022 Mar 14;10:tkac001.
AGS cells
20 or 40 μM
4 h
PDTC significantly reduced DCF fluorescence in H. pylori-infected or hydrogen peroxide-treated cells, indicating that PDTC inhibited STAMBPL1 degradation.
Cell Mol Life Sci. 2022 Jan 23;79(2):86.
A549 cells
10, 50, 100, 300, 500 μM
4 h
To investigate the role of PDTC on the NF-κB signaling pathway in A549 cells, results showed that PDTC pretreatment significantly increased the frequency of CD4+T cells and decreased the frequencies of Tregs and CD45RA+Tregs.
J Transl Med. 2014 Nov 11;12:304.
peripheral blood leukocytes (PBLs)
0.5 μM
6 h
to investigate the inhibitory effect of PDTC on the mRNA expressions of IL-1β and CXCL11 induced by rPf_IL-17A/F1, 2, and 3 proteins
Front Immunol. 2021 Jun 29;12:626895.
mouse primary astrocytes
200 nM
6 h
To investigate the effect of PDTC on tau PFF-induced inflammatory response in astrocytes, results showed that PDTC significantly inhibited tau PFF-induced NFκB signaling activation.
Cell Biosci. 2023 Sep 27;13(1):179.
Caco-2 cells
50 μM
4 h
To verify whether the elevation of AANAT expression resulting from gut microbiota alterations depends on NF-κB signaling
Gut Microbes. 2024 Jan-Dec;16(1):2313769.
Bone marrow-derived macrophages (BMDMs)
5 µg/ml
24 h
To investigate the inhibitory effect of PDTC on NF-ĸB p65 phosphorylation. The results showed that PDTC could inhibit N-protein-induced NF-ĸB p65 phosphorylation, thereby alleviating the inflammatory response.
Front Immunol. 2021 Dec 7;12:791753.
RAW264.7 cells
100 μM
1 h
PDTC, as a positive control, significantly suppressed TNF-α and IL-6 production in LPS-stimulated RAW264.7 cells, with inhibition rates of 90% and 55%, respectively.
PDTC enhanced the activity of 5-FU in a colorectal cancer xenograft model and reduced gastrointestinal toxicity associated with 5-FU therapy in the large bowel but not in the small bowel.
Br J Cancer. 2006 Jul 3;95(1):35-41
Mice
Myd88ΔIEC mice
Drinking water
1 g/L
Two weeks
To investigate how gut microbiota regulates host melatonin production through MyD88 signaling
Gut Microbes. 2024 Jan-Dec;16(1):2313769.
Mice
Acute lung injury model
Intraperitoneal injection
50 mg/kg
Single injection, lasting 24 hours
To investigate the inhibitory effect of PDTC on N-protein-induced acute lung injury. The results showed that PDTC could alleviate N-protein-induced lung injury, reducing total protein concentration, total cell count, and neutrophil infiltration in the bronchoalveolar lavage fluid.
Front Immunol. 2021 Dec 7;12:791753.
BALB/c mice
LPS-induced acute inflammation model
Intraperitoneal injection
50 mg/kg
Once, 1 hour before LPS challenge
The PDTC group significantly reduced serum levels of TNF-α, IL-6, and IL-1β at 9 hours after LPS challenge and significantly increased the survival rate.
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