Structure of Phillyrin
CAS No.: 487-41-2
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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.
Phillyrin is a naturally occuring AMPK activity enhancer, isolated and purified from the fruits of Forsythia suspensa.
Synonyms: Forsythin
4.5
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Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 487-41-2 |
Formula : | C27H34O11 |
M.W : | 534.55 |
SMILES Code : | COC1=C(C=CC(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)=C1)[C@@H]3[C@]4([H])[C@@](CO3)([H])[C@H](C5=CC=C(OC)C(OC)=C5)OC4 |
Synonyms : |
Forsythin
|
MDL No. : | MFCD00467090 |
InChI Key : | KFFCKOBAHMGTMW-LGQRSHAYSA-N |
Pubchem ID : | 101712 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
EA.hy926 cells | 20 µM | 1 hour | Phillyrin effectively protects against glycocalyx HS degradation in LPS-stimulated EA.hy926 cells, possibly associated with suppressing the production of reactive oxygen species and decreasing expression levels of cathepsin L and heparanase. | Inflammation. 2020 Apr;43(2):540-551 |
Primary brain microvascular endothelial cells (BMECs) | 40 μg/mL | 12 hours | Evaluate the effect of Phillyrin on BMEC viability and tube formation ability. Results showed that Phillyrin enhanced BMEC viability and tube formation ability | Front Pharmacol. 2021 Oct 20;12:719823 |
Madin-Darby Canine Kidney (MDCK) cells | 100, 50, 25 µM | 12 hourspi and 24 hourspi | Phillyrin suppressed influenza viral replication (Matrixprotein and nucleoprotein mRNA level) and reduced influenza virus-induced cytopathic effect (CPE). | Virol J. 2023 Nov 13;20(1):262 |
HEp-2 cells | 0, 1, 10, 50, 100 µM | 12, 24, 48 hours | To evaluate the effect of PHN on the proliferation and apoptosis of HEp-2 cells. Results showed that PHN alone had little effect on HEp-2 cell proliferation and apoptosis. | Biosci Rep. 2019 Jun 20;39(6):BSR20190459 |
Primary cortical neurons | 20, 40, 80 µM | 2 hours | Phillyrin significantly increased the viability of H2O2-injured neurons, decreased LDH release, downregulated the Bax/Bcl-2 ratio, and reduced procaspase-3, p-Akt-1, and p-mTOR levels. | Bioengineered. 2022 Mar;13(3):7940-7950 |
AML-12 cells | 200 μg/ml | 24 hours | To investigate the effect of Phillyrin on ethanol-induced autophagic flux in AML-12 cells. Results showed that Phillyrin promoted autophagic flux by targeting PDPK1 and inhibiting its Ser241 phosphorylation, thereby reducing intracellular lipid droplet accumulation. | Cell Death Dis. 2022 Nov 23;13(11):991 |
293T cells | 100 μg/ml | 24 hours | To evaluate the effect of Phillyrin on influenza viral RNA polymerase activity, results showed that Phillyrin significantly inhibited viral RNA polymerase activity. | Influenza Other Respir Viruses. 2023 Mar 1;17(3):e13112 |
PC12 cells | 1, 5, 10 μg/ml | 24 hours | To evaluate the protective effect of Phillyrin on H2O2-induced damage in PC12 cells. Results showed that Phillyrin pretreatment significantly increased cell viability, reduced LDH leakage, and inhibited H2O2-induced oxidative stress and apoptosis. | Cell Mol Neurobiol. 2014 Nov;34(8):1165-73 |
MLE-12 cells | 10, 20, 40 µM | 24 hours | To evaluate the protective effect of Phillyrin on LPS-induced pyroptosis in MLE-12 cells. Results showed that PHI pretreatment significantly ameliorated LPS-induced morphological changes, reduced LDH release and PI-positive cell ratio, and inhibited the activation of the NLRP3/caspase-1/GSDMD-dependent pyroptosis signaling pathway. | Acta Biochim Biophys Sin (Shanghai). 2024 Oct 10;57(3):447-462 |
RAW264.7 cells | 0.0015 mg/mL | 24 hours | Evaluate the anti-inflammatory activity of Phillyrin, results showed that Phillyrin significantly inhibited LPS-induced inflammatory cytokine release. | Ultrason Sonochem. 2024 Aug;108:106944 |
Adipose tissue explants | 200 µM | 24 hours | To investigate the effect of Phillyrin on IL-6 production in LPS-stimulated adipose tissue explants. Results showed that Phillyrin significantly reduced LPS-induced IL-6 mRNA levels and secretion. | Front Nutr. 2022 Oct 5;9:956218 |
Primary microglia | 10-40 μg/mL | 4 or 24 hours | Evaluate the effect of Phillyrin on the viability and morphology of microglia. Results showed that all concentrations of Phillyrin had no adverse effects on microglial cell viability and reduced LPS-induced amoeboid cell numbers | Front Pharmacol. 2021 Oct 20;12:719823 |
Madin–Darby Canine Kidney (MDCK) cells | 100 μg/ml | 48 hours | To evaluate the effect of Phillyrin on influenza virus-induced cytopathic effect (CPE), results showed that Phillyrin significantly reduced virus-induced CPE. | Influenza Other Respir Viruses. 2023 Mar 1;17(3):e13112 |
Bone marrow-derived macrophages (BMMs) | 0, 2.5, 5, 10, 20 µM | 5 days | To evaluate the effect of Phillyrin on RANKL-induced osteoclast differentiation. Results showed that Phillyrin significantly inhibited RANKL-induced osteoclast formation and bone resorption activity. | Front Pharmacol. 2019 Oct 17;10:1188 |
Adipose tissue explants | 1-200 µM | 6 hours | To investigate the effect of Phillyrin on IL-6-induced basal lipolysis. Results showed that Phillyrin significantly inhibited IL-6-induced basal lipolysis, with 200 μM completely blocking the effect of IL-6. | Front Nutr. 2022 Oct 5;9:956218 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
C57BL/10ScNJ mice | Traumatic brain injury (TBI) model | Intraperitoneal injection | 10 mg/kg | 1 hour before surgery and daily thereafter for 7 days | Evaluate the effect of Phillyrin on BBB damage in TBI mice. Results showed that Phillyrin reduced TBI-induced BBB damage, decreased Evans blue extravasation, and improved cerebral microvascular integrity | Front Pharmacol. 2021 Oct 20;12:719823 |
BALB/c mice | H1N1 influenza (PR8)-induced pneumonia model | Intraperitoneal injection | 15 mg/kg | Once daily for 6 days | Phillyrin significantly improved the weight loss caused by viral infection, ameliorated pulmonary inflammation, and inhibited the accumulation of multiple cytokines and chemokines in bronchoalveolar lavage fluid. | Virol J. 2023 Nov 13;20(1):262 |
C57BL/6 mice | Cecal ligation and puncture (CLP)-induced septic acute lung injury model | Intragastric administration | 15, 30, 60 mg/kg | Once daily for seven consecutive days | To evaluate the protective effect of Phillyrin on sepsis-induced acute lung injury. Results showed that PHI pretreatment significantly reduced pulmonary edema, systemic/pulmonary inflammation, and pulmonary histological damage, and inhibited the activation of the NLRP3/caspase-1/GSDMD-dependent pyroptosis signaling pathway. | Acta Biochim Biophys Sin (Shanghai). 2024 Oct 10;57(3):447-462 |
C57BL/6 mice | Alcoholic steatohepatitis (ASH) model | Gavage | 15, 45 mg/kg | Once daily for 10 days | To evaluate the protective effect of Phillyrin in the ASH mouse model. Results demonstrated that Phillyrin significantly reduced hepatic lipid droplet accumulation, lowered serum ALT and AST levels, and alleviated liver injury by promoting autophagic flux. | Cell Death Dis. 2022 Nov 23;13(11):991 |
C57BL/6 mice | DSS-induced colitis model | Oral | 12.5, 25.0, and 50.0 mg/kg | Daily administration for 15 days | Phillyrin ameliorates DSS-induced colitis in mice via modulating the gut microbiota and inhibiting the NF-κB/MLCK pathway. The results showed that Phillyrin significantly reduced weight loss, colon shortening, increased secretion of inflammatory factors, increased intestinal permeability, and enhanced disease activity index in mice with ulcerative colitis (UC). Molecular studies determined that Phillyrin mitigates the nuclear translocation of nuclear factor kappa B, thereby downregulating myosin light-chain kinase-driven myosin light-chain phosphorylation, preserving the integrity of the intestinal barrier. 16S rRNA sequencing outcomes suggest that Phillyrin (50 mg/kg) increased the relative abundance of certain probiotic strains, including Lactobacillaceae and Lachnospiraceae. Additionally, Phillyrin supplementation elevated the short-chain fatty acid contents within the intestinal contents of mice with UC. | Microbiol Spectr. 2025 Feb 4;13(2):e0200624 |
C57BL/6J mice | High-fat diet-induced obesity model | Oral gavage | 25 and 50 mg/kg | Once daily for 9 weeks | To evaluate the metabolic effects of Phillyrin in high-fat diet-induced obese mice. Results showed that Phillyrin significantly reduced weight gain, improved insulin sensitivity, decreased hepatic lipid accumulation, and attenuated adipose tissue inflammation and IL-6 production. | Front Nutr. 2022 Oct 5;9:956218 |
Sprague Dawley (SD) rats | MCAO/R model | Gavage | 25, 50, 100 mg/kg | Once daily for three days | Phillyrin significantly reduced cerebral infarction volume, neurological score, and brain water content, and inhibited neuron apoptosis. | Bioengineered. 2022 Mar;13(3):7940-7950 |
C57BL/6 male mice | LPS-induced acute kidney injury model | Intragastric administration | 40 mg/kg/day | Once daily for 7 days | Phillyrin alleviates LPS-induced acute kidney injury by protecting against glycocalyx HS damage and inhibiting inflammatory responses. | Inflammation. 2020 Apr;43(2):540-551 |
C57BL/6 mice | LPS-induced calvarial osteolysis model | Intraperitoneal injection | 5 and 10 mg/kg | Every other day for 7 days | To evaluate the protective effect of Phillyrin on LPS-induced osteolysis. Results showed that Phillyrin significantly inhibited LPS-induced osteolysis, reducing the number of TRAP+ osteoclasts and bone erosion area. | Front Pharmacol. 2019 Oct 17;10:1188 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.87mL 0.37mL 0.19mL |
9.35mL 1.87mL 0.94mL |
18.71mL 3.74mL 1.87mL |
Tags: Phillyrin | Cytochrome P450 | Influenza Virus | Bacterial | CYPs | inhibitor | 487-41-2 |
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