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Homoeriodictyol is an orally active, bitter-tasting flavanone that can penetrate the blood-brain barrier. Homoeriodictyol enhances synaptic-related protein expression through NCOA4-mediated ferritin autophagy. Homoeriodictyol improves memory impairment in mice by inhibiting the NLRP3 inflammasome. Homoeriodictyol protects human endothelial cells from oxidative damage by activating Nrf2 and inhibiting mitochondrial dysfunction. Homoeriodictyol enhances ROS activity and induces apoptosis, exhibiting anticancer effects. Homoeriodictyol inhibits the survival and migration of androgen-resistant prostate cancer cells in vitro. Homoeriodictyol exerts antinociceptive activity in mice in vivo.
Homoeriodictyol is an orally active, bitter-tasting flavanone that can penetrate the blood-brain barrier. Homoeriodictyol enhances synaptic-related protein expression through NCOA4-mediated ferritin autophagy. Homoeriodictyol improves memory impairment in mice by inhibiting the NLRP3 inflammasome. Homoeriodictyol protects human endothelial cells from oxidative damage by activating Nrf2 and inhibiting mitochondrial dysfunction. Homoeriodictyol enhances ROS activity and induces apoptosis, exhibiting anticancer effects. Homoeriodictyol inhibits the survival and migration of androgen-resistant prostate cancer cells in vitro. Homoeriodictyol exerts antinociceptive activity in mice in vivo[1][2][3][4][5][6].
Activated the nuclear translocation of Nrf2 protein.
Increased protein levels of Nrf2, NQO1, and γGCS, continued to increase Nrf2 protein levels over the 24 hours tested.
Reduce MMP levels.
Reduced cytochrome C protein levels in the cytoplasm and mitochondria.
Inhibited tAIF production and blocks AIF translocation from mitochondria to the nucleus.
Reduced cytochrome C protein levels in the cytoplasm and mitochondria.
Inhibited tAIF production and blocks AIF translocation from mitochondria to the nucleus.
Inhibited H2O2-induced activations of cleaved caspases -3, -9 and PARP.
Induced apoptosis, reduced cell density and disrupted cell morphology, enhanced the efficacy of Docetaxel (HY-B0011) leading to higher apoptosis rates.
Increased the mRNA expression of BAX, CASP3, CASP8, and CYCS, upregulated TP53, along with enhanced expression of caspases in combination with Docetaxel.
Reduced migration, reduced TWIST, SNAIL, and ZEB1 mRNA expression levels by 59%, 68%, and 42%, respectively, compared to untreated cells.
体内実験
Homoeriodictyol (10 mg/kg/d, p.o., 4 weeks) improves Aβ25-35-induced memory impairment by inhibiting the NLRP3 inflammasome to reduce inflammation in AD kunming mice model[2].
Homoeriodictyol (50-μg/kg, i.p., once) exhibits antinociceptive activity through both central and peripheral pathways in swiss albino mice model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Aβ25-35-induced AD kunming mice (Male, 7 weeks old) model[1]
Dosage:
10 mg/kg/d
Administration:
p.o., 4 weeks
Result:
Improved memory impairment and cognitive dysfunction, alleviated hippocampal neuronal damage.
Decreased the levels of Aβ1-40, Aβ1-42, and p-Tau in the hippocampus.
Reduced oxidative stress in the brain, reduced the levels of ROS, apoptosis and MDA, increased the levels of GSH-Px and SOD.
Resulted in increased numbers of NK cells, Th cells, Tc cells, and DCs, and decreased numbers of MDSCs and Treg cells in peripheral blood and splenic tissues.
Had excellent anti-inflammatory effects, reduced the protein expression levels of NLRP3, Caspase-1, and ASC, and the inflammatory factors IL-18 and IL-1β in brain tissue.
Lowered the writhing responses to acetic acid, showed a dose-responsive relation analgesic effect.
Increased the time respond to thermal pain on a hot plate.
Decreased the licking times in both the early and late phases after formalin injection, alleviated pain in the formalin test.
Lessened licking time after Capsaicin (HY-10448) injection, indicating a dose-responsive effect.
Reduced paw licking times, mitigated glutamate-induced pain responses.
DMSO : 50 mg/mL (165.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
3.3082 mL
16.5410 mL
33.0819 mL
5 mM
0.6616 mL
3.3082 mL
6.6164 mL
10 mM
0.3308 mL
1.6541 mL
3.3082 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (12.5 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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