C29 acts as an inhibitor of TLR2. It effectively inhibits signaling through human TLR1/2 and TLR2/6 with IC50 values of 19.7μM and 37.6μM, respectively. C29, at concentrations of 10 or 50 μM for 1 hour, dose-dependently obstructs the induction of IL-8 mRNA by P3C and P2C in HEK-TLR2 stable transfectants. Additionally, C29, in the range of 50 to 200 μM for 1 hour, significantly suppresses the expression of the IL-1β gene triggered by P3C and P2C at both 1 hour and 4 hours post-stimulation in THP-1 cells. When treated with C29 at 25 or 50 μM for one hour, there is a significant reduction in TNF-α mRNA and IL-12 p40 protein levels in response to P3C, but not to P2C, in primary murine macrophages. C29, at a concentration of 50 μM for a duration of one hour, inhibits the expression of proinflammatory genes in HEK-TLR2 cells and murine macrophages, which is induced by TLR2 bacterial agonists[1].
C29 细胞实验
Cell Line
Concentration
Treated Time
Description
References
786-O cells
2.5 µM
24 h
To evaluate the stability of C29 in cells, results showed that C29 is highly stable in cells
Theranostics. 2019 Jul 9;9(18):5332-5346.
HuVEC cells
2.5 µM
1 h
To evaluate the effect of C29 on CXCR1 or CXCR2 levels at the plasma membrane of HuVEC cells stimulated with CXCL7 or CXCL8, results showed that C29 prevented CXCL7/8-dependent internalization of their receptors
Theranostics. 2019 Jul 9;9(18):5332-5346.
HepG2 cells
different doses
To evaluate the effect of C29 on the mRNA levels of ESRRα, ApoB, MTTP, and PLA2G12B in HepG2 cells, results showed that C29 dose-dependently suppressed the expression of these genes.
Theranostics. 2020 Aug 29;10(24):10874-10891.
BV-2 microglial cells
100 µM
60 min
C29, as a TLR2 inhibitor, was used to study the effects of P. gingivalis-LPS and E. coli-LPS on the immuno-inflammatory response in BV-2 microglial cells. The results showed that C29 could reverse the LPS-induced upregulation of TLR2 and inflammatory factors.
Front Cell Infect Microbiol. 2021 Mar 18;11:606986.
RAW 264.7 murine macrophages
100 μM
1 h
Inhibited the TLR2/MyD88/NF-κB signaling pathway, reducing M1 macrophage polarization and cytokine production
EBioMedicine. 2024 Oct;108:105340.
LS174T cells
50 µM
6 h
C29 significantly abolished the induction of TFF3 by EcN EVs and prevented the downregulation of miR7-5p
C29 significantly blocked the upregulation of COX-2 protein levels caused by LTA treatment.
J Cell Mol Med. 2024 Dec;28(23):e70247.
C29 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
RCC xenograft model
Oral gavage
50 mg/kg
Five times a week for four weeks
To evaluate the effect of C29 on RCC tumor growth, results showed that C29 significantly reduced tumor volume and weight
Theranostics. 2019 Jul 9;9(18):5332-5346.
C57BL/6 mice
LPS-induced cognitive impairment model
Oral
1 × 10^9 CFU/mouse
Once daily for 5 days
C29 significantly alleviated LPS-induced cognitive impairment, increased spontaneous alternation in the Y-maze task and exploration in the NOR task, suppressed NF-κB activation and inflammatory cytokine expression in the hippocampus, and increased BDNF expression.
Nutrients. 2021 Sep 19;13(9):3273
Mice
HFD-induced NAFLD model
Intragastric administration
30 mg/kg
Once a day for 3 weeks
To evaluate the effect of C29 on HFD-induced NAFLD model, results showed that C29 exacerbated hepatic steatosis and reduced plasma TG and ApoB levels as well as hepatic VLDL-TG secretion rate.
搜索
