Furohyperforin
Furohyperforin is a natural product isolated from Hypericum perforatum L., possessing neuroprotective and antidepressant activities. Furohyperforin acts as an NLRP3 inflammasome inhibitor and also exhibits inhibitory effects on recombinant CYP3A4. Furohyperforin exerts neuroprotective effects against corticosterone-induced neuronal damage. Furohyperforin inhibits the NLRP3 inflammasome cascade and its downstream IL‑1β and GSDMD signaling pathways, and also reduces serum corticosterone levels in mice, regulating HPA axis function. Furohyperforin is applicable for depression-related research.
For research use only. We do not sell to patients.
- CAS No.: 219793-20-1
- Formula: C35H52O5
- Molecular Weight:552.78
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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CYP3A4 |
NLRP3 |
IL-1β |
In Vitro
Furohyperforin inhibits recombinant CYP3A4 enzyme activity with an IC50 of 1.3 μM[1].
Furohyperforin (compound 7) (10 μM) protects SH-SY5Y cells against CORT-induced injury[2].
Furohyperforin (10-50 μM; 24 h) inhibits LPS-induced BV2 cell injury and shows no cytotoxicity to BV2 cells[2].
Furohyperforin exhibits weak inhibitory activity on synaptosomal serotonin uptake in rat brain synaptosomes[4].
Furohyperforin (compound 10) (10 μg/mL; 2 h pretreatment before KCl injury induction) shows no activity against KCl-induced SH-SY5Y cell injury and no activity against CORT-induced PC12 cell injury, indicating that the β-orientation of the substituent is crucial for neuroprotective activity[5].
Furohyperforin (5-20 μM; 30 min) inhibits NLRP3 inflammasome activation in LPS/nigericin-stimulated BV2 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:BV2
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Concentration:5, 10, 20 μM
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Incubation Time:30 min
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Result:Significantly inhibited the release of NLRP3, ASC, caspase-1, and pro-caspase-1.
Reduced the expression levels of IL-1β, pro-IL-1β, and GSDMD.
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Cell Line:BV2
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Concentration:10, 20 μM
10, 20, 50 μM -
Incubation Time:24 h
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Result:Inhibited LPS-induced BV2 cell injury and showed no cytotoxicity to BV2 cells.
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Cell Line:SH-SY5Y, PC12
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Concentration:10 μg/mL
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Incubation Time:2 h pre-treatment prior to 24 h KCl or CORT injury induction
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Result:Was inactive in the KCl-induced SH-SY5Y cell injury model.
Was inactive in the CORT-induced PC12 cell injury model.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 219793-20-1
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Molecular Weight 552.78
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Formula C35H52O5
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SMILES
O=C1[C@@]23C(O[C@@H](C3)C(C)(O)C)=C(C([C@@]1([C@@](C)([C@H](C2)C/C=C(C)\C)CC/C=C(C)/C)C(C(C)C)=O)=O)C/C=C(C)\C
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)