Structure of Forsythoside A
CAS No.: 79916-77-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Forsythoside A, a natural product isolated and purified from the fruits of Forsythia suspensa, has anticomplementary, antimicrobial, antiinflammatory and antiendotoxin activities.
Synonyms: Forsythiaside A; Forsythiaside
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CAS No. : | 79916-77-1 |
Formula : | C29H36O15 |
M.W : | 624.59 |
SMILES Code : | O[C@H]([C@H]([C@H](OC(/C=C/C1=CC=C(O)C(O)=C1)=O)[C@@H](CO[C@H]2[C@@H]([C@@H]([C@H]([C@H](C)O2)O)O)O)O3)O)[C@@H]3OCCC4=CC=C(O)C(O)=C4 |
Synonyms : |
Forsythiaside A; Forsythiaside
|
MDL No. : | MFCD08460220 |
InChI Key : | DTOUWTJYUCZJQD-UJERWXFOSA-N |
Pubchem ID : | 5281773 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Description |
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].
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In Vitro:
Cell Line
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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 |
In Vivo:
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. | Int J Mol Sci. 2022 Aug 20;23(16):9390 |
Tags: Forsythiaside A | 2-Arachidonoylglycerol | Cyclooxygenase-2 | Forsythiaside | Long term potentiation | Neuroinflammation | β-Amyloid | Asthma | NF-κB | Nrf2 | inhibitor | 79916-77-1 |
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