Forsythiaside A, a phenylethanoid glycoside procured from Forsythia suspensa fruits, can be administered orally. It acts as a COX-2 inhibitor and possesses anti-inflammatory, antioxidant, and neuroprotective properties. Forsythiaside A is instrumental in thwarting neuroinflammation and apoptosis prompted by Aβ25-35, rendering it potentially useful in Alzheimer's disease studies. Additionally, it stimulates the Nrf2/HO-1 signaling pathway and mitigates asthma induced by ovalbumin in murine models[1][2][3].
体外研究
Forsythiaside A, at a concentration of 30 μM, inhibits COX-2 with an inhibition rate of 72% [2].
Forsythiaside A (80 μM; 30 minutes) increases the content of endogenous 2-AG by decreasing the expression of MAGL in organotypic hippocampal slice cultures treated with Aβ25-35 (5 μM; 2 hours) [2].
Forsythiaside A (80 μM; 30 minutes) prevents Aβ25-35-induced neuroinflammation in a CB1R-dependent manner [2].
Forsythiaside A (2.5-10 μg/mL; 12 hours) inhibits the Nrf2 signaling pathway in pulmonary epithelial cells [3].
Forsythoside A/连翘酯苷A 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Colon epithelial cells SW620
25, 50, 100 μM
24 hours
Forsythiaside A inhibited TNF-α-induced inflammation and epithelial barrier damage in SW620 cells by suppressing NF-κB/MLCK/MLC2 signaling pathway.
J Adv Res. 2024 Jun;60:183-200
Lung epithelial cells A549
50, 100, 200 μM
24 hours
Forsythiaside A inhibited TNF-α-induced inflammation and epithelial barrier damage in A549 cells by suppressing NF-κB/MLCK/MLC2 signaling pathway.
J Adv Res. 2024 Jun;60:183-200
Macrophage RAW264.7
50, 100, 200 μM
24 hours
Forsythiaside A inhibited LPS-induced inflammation in RAW264.7 macrophages by suppressing TLR4/MAPK/NF-κB signaling pathway.
J Adv Res. 2024 Jun;60:183-200
Rat basophilic leukemia-2H3 cells (RBL-2H3)
50, 100, 150 μg/mL
1 hour
To evaluate the effect of forsythoside A and forsythoside B on mast cell degranulation. Results showed that forsythoside A and forsythoside B slightly stimulated mast cell degranulation, as indicated by a slight increase in the cell index (CI).
Int J Mol Sci. 2019 Dec 12;20(24):6266
Human umbilical vein endothelial cells (HUVECs)
50, 100, 150 μg/mL
1 hour
To evaluate the effect of forsythoside A and forsythoside B on endothelial barrier function. Results showed that forsythoside A and forsythoside B significantly increased the permeability of FITC-dextran, indicating disruption of the endothelial barrier.
Int J Mol Sci. 2019 Dec 12;20(24):6266
Huh-7 cells
30 µM
10 minutes to 6 hours
To confirm the effect of FA on AMPK activity, results showed that FA induced time-dependent phosphorylation of AMPK and ACC.
Int J Mol Sci. 2023 Dec 1;24(23):17033
HepG2 cells
1, 3, 10, 30 µM
12 hours
To evaluate the protective effect of FA against AA + iron-induced cytotoxicity, results showed that FA increased cell viability in a concentration-dependent manner.
Int J Mol Sci. 2023 Dec 1;24(23):17033
BV2 cells
40 μM and 80 μM
3 h pretreatment followed by 24 h co-exposure
FA treatment decreased the formation of the pro-inflammatory factors IL-6, IL-1β, and NO in LPS-stimulated BV2 cells
Int J Biol Sci. 2022 Feb 28;18(5):2075-2090
HT22 cells
40 μM and 80 μM
3 h pretreatment followed by 24 h co-exposure
FA treatment significantly improved cell viability in erastin-exposed HT22 cells and decreased MDA levels
Int J Biol Sci. 2022 Feb 28;18(5):2075-2090
N2a cells
40 μM and 80 μM
3 h pretreatment followed by 24 h co-exposure
FA treatment significantly improved mitochondrial function and inhibited lipid peroxidation in Aβ1-42-exposed N2a cells
Int J Biol Sci. 2022 Feb 28;18(5):2075-2090
HEK 293T-TRPV1 cells
0.1, 1, 10 µg/mL
2 hours
FT-A inhibited CAP-induced PGE2 and IL-8 secretion and calcium influx.
Int J Biol Sci. 2017 Jan 1;13(1):65-75
MDBK cells
20–320 μM
48 hours
FTA significantly inhibited BVDV replication in MDBK cells, reduced BVDV E2 protein and mRNA levels, and decreased the number of infected cells and virus particle production.
Int J Mol Sci. 2022 Aug 20;23(16):9390
Forsythoside A/连翘酯苷A 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
ICR mice
LPS-induced acute lung injury model
Intragastric administration
20, 40, 80 mg/kg
Administered 1 h before modeling and at 24 h and 48 h after modeling, lasting for 72 hours
Forsythiaside A alleviated LPS-induced acute lung injury by regulating PPAR-γ/RXR-α complex to inhibit inflammation and epithelial barrier damages in lung and colon.
J Adv Res. 2024 Jun;60:183-200
Male APP/PS1 double transgenic AD mice
APP/PS1 double transgenic AD mice
Oral administration
30 mg/kg
Once daily for 42 days
FA treatment ameliorated memory and cognitive impairments and suppressed Aβ deposition and p-tau levels in the brain
Int J Biol Sci. 2022 Feb 28;18(5):2075-2090
Mice
Yeast-induced pyrexia mice model
Intraperitoneal injection
2, 4, 8 mg/kg
Single dose
FT-A significantly reduced rectal temperature in yeast-induced pyrexia mice and inhibited PGE2 and IL-8 production.
Int J Biol Sci. 2017 Jan 1;13(1):65-75
C57BL/6 male mice
LPS-induced septic acute kidney injury model
Intraperitoneal injection
40 mg/kg
Administered 1 hour before LPS injection, lasted for 24 hours
To evaluate the protective effect of Forsythiaside A on sepsis-induced acute kidney injury, results showed that Forsythiaside A significantly attenuated pathological kidney injuries, reduced serum BUN and creatinine levels, inhibited the expression of proinflammatory cytokines IL-1β, IL-6, and TNF-α in the kidney, and reduced cell apoptosis
BMC Complement Med Ther. 2023 Feb 3;23(1):35
C57BL/6J and TLR7−/− mice
Influenza A virus FM1 strain infection model
Intragastric
20 mg/kg
Once daily for 5 days
Forsythiaside A improves Influenza A virus infection through the TLR7 signaling pathway and reduces inflammatory response
BMC Complement Med Ther. 2022 Jun 22;22(1):164
ICR mice
Vascular leakage model
Intravenous injection
50, 100 mg/kg
Single administration, observed for 30 minutes
To evaluate the effect of forsythoside A and forsythoside B on vascular permeability in mice. Results showed that forsythoside A and forsythoside B induced dose-dependent vascular leakage, as indicated by EB extravasation. Forsythoside A exhibited a stronger effect than forsythoside B, while forsythoside E did not cause significant reactions.
Int J Mol Sci. 2019 Dec 12;20(24):6266
C57BL/6N mice
CCl4-induced liver injury model
Oral
10 and 30 mg/kg
Once daily for three days
To evaluate the protective effect of FA against CCl4-induced liver injury, results showed that oral administration of FA significantly inhibited CCl4-induced liver injury.
Int J Mol Sci. 2023 Dec 1;24(23):17033
BALB/c mice
BVDV infection model
Intraperitoneal injection
60 mg/kg
Once at 0, 7, and 14 days
When synergistically immunized with the vaccine, FTA as an immune enhancer significantly alleviated pathological damage in BVDV-infected mice, reduced viral load in the spleen, and increased specific antibody levels.
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