Ferulic Acid, a kind of phenolic compound isolated from Tetragonia tetragonioides, has many biological activities. In vitro studies, ferulic acid has whitening effect on the B16F10 mouse melanoma cell line and anti-wrinkle activity on the CCD-986sk human dermal fibroblast cell line, while shows no cytotoxicity at concentrations up to 20 μM[1]. Besides this, it was found that ferulic acid could effectively inhibit the epidermal growth factor receptor (EGFR) in human breast cancer cells, through down-regulating the Tyr 1068 autophosphorylation[2]. In vivo studies, ferulic acid has the ability of ameliorating the diabetes-induced cognition lesions in rat via the regulation of protein tyrosine phosphatase 1B (PTP1B) and insulin signaling pathway[3]. In addition, ferulic acid could contribute to the reversal of inflammatory response induced by chronic unpredictable mild stress (CUMS) in mice[4].
Ferulic Acid/阿魏酸 细胞实验
Cell Line
Concentration
Treated Time
Description
References
J774A.1 cells
12.5-100 µg/ml
2 h
To investigate the inhibitory effect of ferulic acid on NLRP3 inflammasome-mediated canonical pyroptosis, results showed that ferulic acid significantly inhibited the release of LDH and IL-1β
MedComm (2020). 2023 Apr 20;4(3):e255.
RAW264.7 cells
50 µg/ml
2 h
To investigate the inhibitory effect of ferulic acid on caspase-11 inflammasome-mediated non-canonical pyroptosis, results showed that ferulic acid significantly reduced LDH release and PI uptake
MedComm (2020). 2023 Apr 20;4(3):e255.
BMDMs
50 µg/ml
2 h
To investigate the inhibitory effect of ferulic acid on caspase-11 inflammasome-mediated non-canonical pyroptosis, results showed that ferulic acid significantly reduced LDH release and IL-1β secretion
MedComm (2020). 2023 Apr 20;4(3):e255.
Caco-2 cells
0-500 µM
24 h
To assess the dose-dependent toxicity of FA in vitro, cell viabilities were determined on Caco-2 using a WST assay. Up to 500 µM FA, cell survival was 100% for 24 h, while 1250 µM FA significantly reduced cell viability.
Antioxidants (Basel). 2022 Jul 26;11(8):1448.
Hippocampal Neurons
5 and 10 µM
2 h
FA preincubation prevented the Aβ-induced loss of synaptic proteins, including GluN2B, PSD-95, and synapsin1
Neurotherapeutics. 2023 Jul;20(4):1081-1108.
BV2 microglial cells
0.5 mg/ml
18 h
To evaluate the regulatory effect of Ferulic Acid on BV2 microglial cell polarization under hypoxia, the results showed that Ferulic Acid significantly reduced the number of iNOS+ cells and increased the number of Arg1+ cells, indicating that Ferulic Acid can shift microglial polarization from M1 to M2 phenotype.
Front Immunol. 2022 Sep 2;13:976729.
Human retinal endothelial cells (HRECs)
0.5 mg/ml
16 h
To evaluate the effect of Ferulic Acid-treated microglial supernatants on HRECs tube formation and migration, the results showed that Ferulic Acid-treated microglial supernatants significantly inhibited HRECs tube formation and migration.
Front Immunol. 2022 Sep 2;13:976729.
Skeletal Stem Cells (SSCs)
30 μM
24 h
Ferulic acid significantly rescued the radiation-induced impairment of SSCs by restoring their proliferation, osteogenic differentiation, and self-renewal capacity, and by activating the p38/MAPK and ERK/MAPK pathways.
Stem Cells Transl Med. 2021 Aug;10(8):1217-1231.
Mouse tracheal epithelial cells (MTECs)
0, 25, 50, 100, 200, 400, 800 μM
24 h
To evaluate the effect of Ferulic Acid on the viability of MTECs, results showed that 25-200 μM Ferulic Acid significantly increased cell viability, while 400-800 μM began to show toxic effects.
Respir Res. 2021 Dec 4;22(1):308.
Mouse tracheal epithelial cells (MTECs)
200 μM
24 h
To evaluate the effect of Ferulic Acid on ENaC activity in LPS-induced MTECs, results showed that Ferulic Acid reversed the LPS-induced reduction of ENaC activity.
Respir Res. 2021 Dec 4;22(1):308.
Ferulic Acid/阿魏酸 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Insomnia model
Oral
40 mg/kg
Single dose
The pharmacokinetics and tissue distribution of FA-SMEDDS were evaluated. The results showed that FA-SMEDDS significantly improved the oral bioavailability of FA, reduced its distribution in the kidney, and increased its distribution in the brain.
Int J Nanomedicine. 2020 Mar 25;15:2059-2070
C57BL/6 mice
LPS-induced sepsis model
Intraperitoneal injection
50 mg/kg
Single injection, lasting 6 hours
To investigate the protective effect of ferulic acid on LPS-induced septic mice, results showed that ferulic acid significantly improved the survival rate and reduced the serum concentrations of IL-1β and TNF-α
MedComm (2020). 2023 Apr 20;4(3):e255.
Mice
High-fat diet model
Dietary supplementation
50 mg/kg
8 weeks
To investigate the effect of FA on gut health in mice fed a high-fat diet, results showed that FA reduced lymphocyte infiltration and protected the intestinal epithelial barrier.
Antioxidants (Basel). 2022 Jul 26;11(8):1448.
APP/PS1 mice
Alzheimer's disease model
Drinking water
20 mg/kg
Once daily for 30 days
Ferulic acid counteracts ET1-mediated vasoconstriction, prevents reductions in density and diameter of hippocampal capillaries, and ameliorates Aβ plaque deposition and spatial memory deficits
Neurotherapeutics. 2021 Apr;18(2):1064-1080
APP/PS1 Mice
Alzheimer's Disease Model
Oral
50 mg/kg
Once daily for 4 months
Long-term FA treatment improved behavioral and cognitive functions, reduced Aβ burden, and improved synaptic plasticity in APP/PS1 mice
Neurotherapeutics. 2023 Jul;20(4):1081-1108.
C57BL/6J mice
Oxygen-induced retinopathy (OIR) model
Intragastric administration
50 mg/kg
Twice daily for 5 days (P12 to P17)
To evaluate the inhibitory effect of Ferulic Acid on retinal neovascularization in the OIR model, the results showed that Ferulic Acid significantly reduced the area of retinal neovascular clusters and the number of endothelial cells, and promoted reparative angiogenesis.
Front Immunol. 2022 Sep 2;13:976729.
C57BL/J male mice
LPS-induced tracheal injury model
Intraperitoneally
100 mg/kg
12 hours before and 12 hours after intratracheal administration of LPS
To evaluate the protective effect of Ferulic Acid on LPS-induced tracheal injury, results showed that Ferulic Acid significantly attenuated tracheal injury and restored the structure of tracheal epithelial cells and ENaC expression.
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