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Chemical Structure| 487-41-2 Chemical Structure| 487-41-2

Structure of Phillyrin
CAS No.: 487-41-2

Chemical Structure| 487-41-2

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Phillyrin is a naturally occuring AMPK activity enhancer, isolated and purified from the fruits of Forsythia suspensa.

Synonyms: Forsythin

4.5 *For Research Use Only !

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Product Details of Phillyrin

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

Safety of Phillyrin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Phillyrin

epigenetics
PI3K-AKT

Isoform Comparison

Biological Activity

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

Protocol

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

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