Dihydroparadol
Dihydroparadol is a iNOS inhibitor with an IC50 of 7.24 μM, and it is found in ginger. Dihydroparadol partially inhibits the catalytic activity of iNOS, blocks the nuclear translocation of NF-κB p65, reduces NF-κB activity, and attenuates lipopolysaccharide-induced degradation of IκB-α, thereby inhibiting NF-κB-mediated iNOS gene expression and protein production. Dihydroparadol inhibits lipopolysaccharide-induced nitric oxide production in macrophages and exhibits anti-inflammatory activity. Dihydroparadol increases ABCA1 protein abundance by elevating mRNA levels and reducing proteasomal degradation, and also increases ABCG1 protein abundance by enhancing protein stability. Dihydroparadol promotes cholesterol efflux from cholesterol-loaded macrophages via apolipoprotein A1-mediated and plasma-mediated pathways. Dihydroparadol inhibits PDGF-induced vascular smooth muscle cell proliferation, shows no cytotoxicity to vascular smooth muscle cells within the tested concentration range, and does not interfere with endothelial cell proliferation. Dihydroparadol can be used in the research of inflammatory diseases, atherosclerosis and cardiovascular diseases.
For research use only. We do not sell to patients.
- CAS No.: 143111-84-6
- Formula: C17H28O3
- Molecular Weight:280.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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iNOS 7.24 μM (IC50) |
NF-κB |
IKK-α |
Dihydroparadol (0.035-175 μM; 1 h pretreatment, followed by 20 h LPS stimulation) potently inhibits lipopolysaccharide-induced nitric oxide production in RAW 264.7 murine macrophage cells with an IC50 of 7.24 μM, without reducing cell viability[1].
Dihydroparadol (0.35-17.5 μM; 1 h at 37°C) partially inhibits the catalytic activity of lipopolysaccharide-induced inducible nitric oxide synthase from RAW 264.7 murine macrophage cell homogenates, with inhibition plateauing at ~3.5 μM and a maximum inhibition of 14.8%[1].
Dihydroparadol (3.5-17.5 μM; 1 h pretreatment, followed by 20 h LPS stimulation) inhibits lipopolysaccharide-induced inducible nitric oxide synthase protein expression at 17.5 μM and enzyme activity with an IC50 of 0.88 μM in RAW 264.7 murine macrophage cells[1].
Dihydroparadol (0.35-17.5 μM; 1 h pretreatment, followed by 30 min LPS stimulation) inhibits lipopolysaccharide-induced IκB-α degradation in RAW 264.7 murine macrophage cells at concentrations of 3.5 μM and 17.5 μM[1].
Dihydroparadol (0.35-17.5 μM; 1 h pretreatment, followed by 30 min LPS stimulation) inhibits lipopolysaccharide-induced NF-κB p65 nuclear translocation in RAW 264.7 murine macrophage cells, with significant inhibition observed at concentrations of 3.5 μM and 17.5 μM[1].
Dihydroparadol (0.035-17.5 μM; 1 h pretreatment, followed by 4 h LPS stimulation) concentration-dependently inhibits lipopolysaccharide-induced NF-κB transcriptional activity in RAW 264.7 murine macrophage cells[1].
Dihydroparadol (rac-[5]-dihydroparadol) (30 min) inhibits PDGF-induced proliferation of primary rat aortic vascular smooth muscle cells with an IC50 of 10 μM[3].
Dihydroparadol (30 min) inhibits PDGF-induced proliferation of primary rat aortic vascular smooth muscle cells with an IC50 of 4.11 μM, as measured by crystal violet biomass staining[3].
Dihydroparadol (Up to 30 μM; 30 min) does not induce significant cytotoxicity in primary rat aortic vascular smooth muscle cells at concentrations up to 30 μM[3].
Dihydroparadol (Up to 30 μM; 48 h) does not interfere with the viability of human umbilical vein endothelial cells (HUVECtert) at concentrations up to 30 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7 murine macrophage cells
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Concentration:3.5-17.5 μM (iNOS protein expression); 0.035-100 μM (iNOS activity measurement)
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Incubation Time:1 h pretreatment, followed by 20 h LPS stimulation
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Result:Inhibited LPS-induced iNOS protein levels at 17.5 μM (but not 3.5 μM), confirmed by densitometric analysis.
Concentration-dependently inhibited LPS-induced iNOS enzyme activity with an IC50 of 0.88 μM.
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Cell Line:RAW 264.7 murine macrophage cells
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Concentration:0.35-17.5 μM
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Incubation Time:1 h pretreatment, followed by 30 min LPS stimulation
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Result:Significantly inhibited LPS-induced IκB-α degradation at 3.5 μM (94.6% of control) and 17.5 μM (130% of control).\nIncreased cytoplasmic NF-κB p65 levels to 79.7% of control and reduced nuclear NF-κB p65 levels to 69.8% of LPS-stimulated control at 3.5 μM.
Reduced nuclear NF-κB p65 levels to 37.8% of LPS-stimulated control at 17.5 μM, a level comparable to positive control PDTC.
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Cell Line:Primary rat aortic vascular smooth muscle cells (VSMC)
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Concentration:Up to 30 μM
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Incubation Time:30 min h (post-PDGF stimulation)
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Result:Showed no significant cytotoxicity toward VSMC, as measured by LDH release, at concentrations up to 30 μM.
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Cell Line:Human umbilical vein endothelial cells (HUVECtert)
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Concentration:Up to 30 μM
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Incubation Time:30 min h
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Result:Showed no significant negative effect on HUVECtert viability at concentrations up to 30 μM.
Chemical Information
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CAS No. 143111-84-6
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Molecular Weight 280.40
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Formula C17H28O3
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SMILES
OC1=CC=C(CCC(CCCCCCC)O)C=C1OC
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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.
Purity & Documentation
References
[1]. Aktan F, et al. Gingerol metabolite and a synthetic analogue Capsarol inhibit macrophage NF-kappaB-mediated iNOS gene expression and enzyme activity. Planta medica. 2006 Jun;72(8):727-34. [Content Brief]
[2]. Wang D, et al. 6-Dihydroparadol, a Ginger Constituent, Enhances Cholesterol Efflux from THP-1-Derived Macrophages. Molecular nutrition & food research. 2018 Jul;62(14):e1800011. [Content Brief]
[3]. Liu R, et al. Identification and characterization of [6]-shogaol from ginger as inhibitor of vascular smooth muscle cell proliferation. Molecular nutrition & food research. 2015 May;59(5):843-52. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dihydroparadol Related Classifications
HY-184337 Related Classifications
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