Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO).
体内研究
Mice treated with Caffeic acid at a dose of 500 mg/kg display a marked reduction in histamine-induced scratching behavior, recording an average of 30.50±10.87 bouts per hour, with a sample size of six. A lower dose of Caffeic acid (100 mg/kg) shows a non-significant reduction in scratching, indicating a possible decreasing trend (49.40±12.35 bouts per hour, n=5). Chloroquine-induced scratching is significantly decreased following pretreatment with 500 mg/kg of Caffeic acid, registering 161.6±31.42 bouts per hour in five subjects[1].
Additionally, Caffeic acid substantially lowers the expression of 5-LO mRNA in a dose-dependent manner in the hippocampus. Compared to the ischemia-reperfusion (I/R) untreated group, 5-LO protein expression significantly diminishes in the I/R-Caffeic acid-treated group, particularly at 50 mg/kg. Relative to the I/R untreated group, the time taken to locate the platform significantly decreases in both low- and high-dose Caffeic acid-treated groups, with the most notable reduction in the I/R-Caffeic acid 50 mg/kg group (P<0.01). In the low-dose Caffeic acid group, cell injury remains pronounced with a pyknosis ratio of 63.6±2.8%, while in the high-dose group, hippocampal neuron pyknosis significantly decreases, showing a pyknosis ratio of 13.3±3.0%[2].
体外研究
Caffeic acid exhibits inhibitory effects on histamine-induced reactions, with its suppressive impact progressively intensifying at concentrations ranging from 0.1 to 1 mM, indicative of a typical dose-dependent response. In HEK293T-TRPV1 cells, a 1 mM pre-incubation with Caffeic acid significantly curtails capsaicin-triggered responses, whereas at lower concentrations, this inhibitory effect on capsaicin-induced reactions is less pronounced. Calcium imaging experiments reveal that Caffeic acid treatment notably reduces activity in histamine-sensitive dorsal root ganglion (DRG) neurons. With a 1 mM Caffeic acid pretreatment, there is a substantial reduction in the proportion of DRG neurons responsive to histamine, decreasing from 12.5% to 2.1%. Additionally, a 1 mM concentration of Caffeic acid effectively obstructs the intracellular calcium increase induced by allylisothiocyanate (AITC) in TRPA1-expressing cells, also preventing AITC-induced TRPA1 activation[1].
Caffeic Acid/咖啡酸 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Bovine mammary epithelial cells
125 or 250 mg/ml
12 hours
CA pretreatment inhibited E. coli B1-induced inflammatory responses and oxidative stress, and restored lipid homeostasis.
Front Immunol. 2022 Oct 20;13:1005430.
HTB-34 human cervical cancer cells
100 µM
24 hours
Caffeic acid activates AMPK, inhibits cell proliferation, and promotes apoptosis
Int J Mol Sci. 2017 Feb 21;18(2):462.
Colon myofibroblasts CCD-18Co
50 µM, 10 µM, 1 µM
24 hours
Investigated the effects of caffeic acid on COX-2 expression, PGE2 biosynthesis, and inflammatory cytokines/chemokines (IL-8, MCP-1, IL-6) in IL-1β-stimulated colon myofibroblasts. Results: Caffeic acid dose-dependently reduced PGE2 levels (significant at 50 and 10 μM), downregulated COX-2 expression (significant at 50 and 10 μM), and only at 50 μM significantly decreased IL-8 secretion (~27%), with no effect on MCP-1 or IL-6.
Nutrients. 2021 Feb 8;13(2):554.
Primary bovine mammary epithelial cells
10, 25, 50 μg/mL
3 hours pretreatment followed by LPS stimulation for 12 hours
Caffeic acid protected cells from LPS-induced structural damage and apoptosis by inhibiting NF-κB and MAPK activation and reducing proinflammatory cytokine expression
Mediators Inflamm. 2019 Apr 30;2019:1897820.
Primary bovine mammary epithelial cells
10, 25, 50 μg/mL
3 hours pretreatment followed by LPS stimulation for 12 hours
Caffeic acid attenuated LPS-induced structural damage and apoptosis by inhibiting NF-κB and MAPK activation, and reduced proinflammatory cytokine release
Mediators Inflamm. 2019 Apr 30;2019:1897820.
BCPAP cells
16 µg/mL
48 hours
Inhibited BCPAP cell proliferation with an inhibition rate of ~79%
J Nanobiotechnology. 2024 Sep 18;22(1):571.
Rat cortical slices
100 µM
CA prevented induced loss of reductive capacity, cell damage, and oxidative damage.
Int J Mol Sci. 2023 May 24;24(11):9218.
HEK-Gα15/ETA and HEK-Gα15/ETB cells
30, 25, 20, 15, 10, 5 and 0 µM
To test the antagonistic activity of the compounds on ETA and ETB receptors. Results showed that these twin drugs could not antagonize ETA and ETB receptors.
Drug Des Devel Ther. 2020 Mar 5;14:977-992.
HEK-Gα15/AT1 cells
30, 25, 20, 15, 10, 5 and 0 µM
To test the antagonistic activity of compound 1a on Ang II-AT1 receptor, with an IC50 of 340nM.
Drug Des Devel Ther. 2020 Mar 5;14:977-992.
Caffeic Acid/咖啡酸 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Drosophila melanogaster
Dextran sulfate sodium (DSS)-induced ulcerative colitis model
Oral
0.5 mM and 1 mM
Daily administration for 7 days
CA significantly improved the survival rate of UC flies, restored their motility and digestive abilities, protected intestinal morphology and homeostasis, and reduced intestinal cell damage. Additionally, CA alleviated intestinal damage by inhibiting apoptosis mediated by mitochondrial damage and reducing immune overactivation in the intestine.
Drug Des Devel Ther. 2025 Mar 22;19:2157-2172
C57 mice
S. aureus-induced endometritis model
Intraperitoneal injection
10, 20, 30 mg/kg
Uterine tissues were harvested 24 hours later
CA significantly alleviated S. aureus-induced uterine injury, MPO activity, the contents of inflammatory factors TNF-α and IL-1β, and NF-κB activation. Meanwhile, CA significantly inhibited S. aureus-induced ferroptosis, as confirmed by decreased MDA and iron concentration and up-regulated GPX4 expression and GSH level. Furthermore, CA attenuated S. aureus-induced HIF-1α and phosphorylated mTOR expression and increased phosphorylated AMPK expression.
J Cell Mol Med. 2024 Oct;28(20):e70175
BALB/c nude mice
Xenograft model
Tail vein injection
2 mg/kg
5 times per week for 14 days
Significantly inhibited the volume and weight of human papillary thyroid tumors
J Nanobiotechnology. 2024 Sep 18;22(1):571.
Sprague-Dawley rats
D-galactose-induced aging model
Oral gavage
20 or 40 mg/kg
Once daily for 8 weeks
Caffeic acid alleviates memory and hippocampal neurogenesis deficits induced by D-galactose
Nutrients. 2022 May 23;14(10):2169
ICR mice
E. coli or K. pneumoniae infection model
Oral
25 or 50 mg/kg/day
Once daily for 10 days
CA pretreatment improved the survival rate of mice and alleviated inflammatory responses and tissue damage in mammary glands.
Front Immunol. 2022 Oct 20;13:1005430.
Rats
Alzheimer’s disease model
Oral
50 mg/kg
Once daily for 25 days
CA significantly counteracted the worsening of cognitive abilities and induced changes in levels of AChE, glutathione, catalase, lipid peroxidation, and superoxide dismutase.
Int J Mol Sci. 2023 May 24;24(11):9218.
C57BL/6 mice
LPS-induced sepsis model
Intraperitoneal injection
50 mg/kg
Single dose, LPS challenge 6 h later
CA significantly improved the survival rate of septic mice, reduced serum IL-1β and TNF-α levels, and inhibited GSDMD activation in peritoneal macrophages
China, Henan
... 展开 >> The Clinical Medical College, The First Affiliated Hospital of Henan University of Science and Technology
Luoyang, Henan, China, 471003 收起 <<
China, Shandong
... 展开 >>
Qilu Hospital, Shandong University
Recruiting
Jinan, Shandong, China
Contact: Ming Hou, Dr. +86-531-82169114 ext 9879 houming@medmail.com.cn
Principal Investigator: Ming Hou, Dr. 收起 <<
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