Albaconol
Albaconol is a prenylresorcinol compound. Albaconol is isolated from the mushroom A. confluens. Albaconol inhibits NF-κB and DNA topoisomerase II, and induces Apoptosis. Albaconol inhibits IκB-α phosphorylation and p65 nuclear translocation, enhances SOCS1 expression, reduces the production of proinflammatory cytokines and NO, and suppresses the expression of iNOS, MHC-II and co-stimulatory molecules. Albaconol acts as a weak antagonist of hVR1 and rVR1, with IC50 values of 17 µM and 5.5 µM, respectively. Albaconol induces tracheal contraction and desensitization. Albaconol inhibits the growth of tumor cells. Albaconol can be used in pain-related research.
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- CAS No.: 338405-64-4
- Formule: C22H34O3
- Masse moléculaire:346.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Fungal Metabolite |
Topoisomerase II |
iNOS |
MHC II |
Albaconol (0.5-20 μg/mL; 8-53 h) inhibits proliferation of RAW264.7 cells in a dose- and time-dependent manner with an IC50 of 5.55 μg/mL[1].
Albaconol (2.5-7.5 μg/mL; 24 h) at 7.5 μg/mL induces apoptosis of RAW264.7 cells, while concentrations of 2.5 μg/mL and 5.0 μg/mL do not cause significant apoptosis[1].
Albaconol (5.0 μg/mL; 24 h pretreatment, followed by 24 h LPS stimulation) inhibits TNF-α, IL-1β, and IL-6 mRNA expression in both unstimulated and LPS-stimulated RAW264.7 cells[1].
Albaconol (2.5-5.0 μg/mL; 24 h pretreatment, followed by 24 h LPS stimulation) at 5.0 μg/mL inhibits LPS-induced TNF-α, IL-1β, and IL-6 production in RAW264.7 cells, while 2.5 μg/mL albaconol only inhibits LPS-induced IL-1β production[1].
Albaconol (2.5-5.0 μg/mL; 24 h pretreatment, followed by 12-24 h LPS stimulation) at 5.0 μg/mL inhibits LPS-induced iNOS expression and NO production in RAW264.7 cells, while 2.5 μg/mL albaconol has no effect on these endpoints[1].
Albaconol (2.5-50 μg/mL; 24 h) at concentrations ≤10 μg/mL does not induce apoptosis/necrosis in mouse bone marrow-derived CD11c+ dendritic cells, while higher concentrations (20 μg/mL, 50 μg/mL) do trigger apoptotic/necrotic cell death[2].
Albaconol (3.0 μg/mL; 12 h pretreatment, 24 h LPS stimulation) inhibits LPS-induced upregulation of MHC-II (Ia), CD40, CD80, and CD86 expression in mouse bone marrow-derived CD11c+ dendritic cells[2].
Albaconol (up to 50 µM) exhibits no agonistic activity on hVR1-expressing recombinant CHO cells at concentrations up to 50 µM[3].
Albaconol acts as a weak antagonist of hVR1 in hVR1-expressing recombinant CHO cells, with an IC50 of 17 µM[3].
Albaconol acts as a weak antagonist of rVR1, with an IC50 of 5.5 µM, and exhibits no agonistic activity on rVR1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7
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Concentration:0.5-20 μg/mL
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Incubation Time:8-53 h
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Result:Inhibited RAW264.7 cell proliferation in a dose- and time-dependent manner.
Achieved an IC50 value of 5.55 μg/mL.
Induced obvious proliferation inhibition after 24 hours of treatment with 2.5 μg/mL or 5.0 μg/mL.
Maintained inhibitory effect from 24 h to 47 h.
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Cell Line:RAW264.7
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Concentration:2.5-7.5 μg/mL
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Incubation Time:24 h
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Result:Induced significant apoptosis of RAW264.7 cells at 7.5 μg/mL.
Showed no obvious proapoptotic activity at 2.5 μg/mL or 5.0 μg/mL.
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Cell Line:RAW264.7
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Concentration:5.0 μg/mL
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Incubation Time:24 h pretreatment, followed by 24 h LPS stimulation
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Result:Significantly inhibited mRNA expression of TNF-α, IL-1β, and IL-6 in both unstimulated and LPS-stimulated RAW264.7 cells.
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Cell Line:RAW264.7
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Concentration:2.5-5.0 μg/mL
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Incubation Time:24 h pretreatment, followed by 12-24 h LPS stimulation
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Result:Markedly inhibited LPS-induced iNOS mRNA and protein expression, as well as LPS-induced NO production at 5.0 μg/mL.
Showed no inhibitory effect on LPS-induced iNOS expression or NO production at 2.5 μg/mL.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:F1 (BALB/c × C57BL/6)[2]
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Dosage:DC pretreatment
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Administration:in vitro pretreatment; 12 hours prior to LPS stimulation
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Result:Reduced the percentage of OVA-specific KJ1-26+ CD4+ T cells from 9.8% to 0.5%.
Chemical Information
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CAS No. 338405-64-4
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Masse moléculaire 346.50
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Formule C22H34O3
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SMILES
C[C@@]12[C@H]([C@](O)(CC[C@@]1([H])C(C)(CCC2)C)C)CC3=C(C=C(C=C3O)C)O
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Structure Classification
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Initial Source
Albatrellus spp.
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Liu Q, et al. Albaconol, a plant-derived small molecule, inhibits macrophage function by suppressing NF-kappaB activation and enhancing SOCS1 expression. Cellular & molecular immunology. 2008 Aug;5(4):271-8. [Content Brief]
[2]. Liu Q, et al. Plant-derived small molecule albaconol suppresses LPS-triggered proinflammatory cytokine production and antigen presentation of dendritic cells by impairing NF-kappaB activation. International immunopharmacology. 2008 Aug;8(8):1103-11. [Content Brief]
[3]. Hellwig V, et al. Activities of prenylphenol derivatives from fruitbodies of Albatrellus spp. on the human and rat vanilloid receptor 1 (VR1) and characterisation of the novel natural product, confluentin. Archiv der Pharmazie. 2003 Apr;336(2):119-26. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)