2. Metabolic Enzyme/Protease Autophagy Apoptosis Immunology/Inflammation NF-κB Epigenetics Cell Cycle/DNA Damage
  3. Drug Metabolite Autophagy Apoptosis Reactive Oxygen Species (ROS) Keap1-Nrf2 MMP Caspase PARP MDM-2/p53
  4. Homoeriodictyol

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.

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Homoeriodictyol

Homoeriodictyol Chemical Structure

CAS No. : 446-71-9

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Based on 1 publication(s) in Google Scholar

Other Forms of Homoeriodictyol:

Homoeriodictyol Related Antibodies

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

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].

IC50 & Target[4]

Caspase 3

 

Caspase-9

 

In Vitro

Homoeriodictyol (0.1-1 μM) increases cell viability, PSD-95, SYN, P62, and FTH levels, and decreases LC3 and NCOA4 levels in Corticosterone (HY-B1618)-induced SH-SY5Y cells[1].
Homoeriodictyol (10 μM/L, 24 h) restores cell viability and migration levels, and reduces inflammatory factor levels in N9 microglial cells[2].
Homoeriodictyol (0-20 μM, 16 h) upregulates the protein levels of Nrf2 and γGCS in MDA-MB-231 cells[3].
Homoeriodictyol (1-5 μM, 12-24 h) prevents mitochondrial dysfunction and apoptosis, reduces MMP, cytochrome C, tAIF, cleaved caspase -3, -9 and PARP levels in H2O2-induced EA.hy926 cells [3].
Homoeriodictyol (0-5 μM, 2-24 h) activats the Nrf2 pathway through inducing Nrf2 at the protein level and enhancing Nrf2 stability in EA.hy926 cells[3].
Homoeriodictyol (100-500 μg/mL, 24 h) shows cytotoxicity and concentration-dependent lysosomal toxicity, enhances intracellular ROS generation and induces mitochondrial dysfunction in MCF-7, HeLa, and HT-29 cells[4].
Homoeriodictyol (500 μg/mL, 24 h) increases the subG1 peaks, increases the expressions of p53, caspase 3, caspase 9, bax, and SOD1 genes in MCF-7, HeLa, and HT-29 cells[4].
Homoeriodictyol (0-250 μM, 24-72 h) reduced cell viability against PC3 cells, with an IC50 of 118.15 μM, induces apoptosis, inhibits cell migration in PC3 cells[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Homoeriodictyol Related Antibodies

ELISA Assay[2]

Cell Line: N9 microglial cells
Concentration: 10 μM/L
Incubation Time: 24 h
Result: Reduced levels of IL-1β and IL-18.

Cell Migration Assay [2]

Cell Line: N9 microglial cells
Concentration: 10 μM/L
Incubation Time: 24 h
Result: Restored migration levels.

Western Blot Analysis[3]

Cell Line: MDA-MB-231 cells
Concentration: 0, 2.5, 5 ,10, 20 μM
Incubation Time: 16 h
Result: Upregulated the protein levels of Nrf2 and γGCS.

Apoptosis Analysis[3]

Cell Line: H2O2-induced EA.hy926 cells
Concentration: 2, 5 μM
Incubation Time: 24 h
Result: Decreased apoptosis cells.

Immunofluorescence[3]

Cell Line: EA.hy926 cells
Concentration: 2, 5 μM
Incubation Time: 12 h
Result: Activated the nuclear translocation of Nrf2 protein.

Western Blot Analysis[3]

Cell Line: EA.hy926 cells
Concentration: 1, 2, 5 μM
Incubation Time: 2, 4, 6, 8, 12, 16 h
Result: 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.

RT-PCR[3]

Cell Line: EA.hy926 cells
Concentration: 1, 2, 5 μM
Incubation Time: 24 h
Result: Did not affect mRNA level of Nrf2, but upregulated the levels of NQO1 and GCLM.

Immunofluorescence[3]

Cell Line: H2O2-induced EA.hy926 cells
Concentration: 2, 5 μM
Incubation Time: 12 h
Result: 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.

Western Blot Analysis[3]

Cell Line: H2O2-induced EA.hy926 cells
Concentration: 1, 2, 5 μM
Incubation Time: 12 h
Result: 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.

Immunofluorescence[4]

Cell Line: MCF-7, HeLa, and HT-29 cells
Concentration: 500 μg/mL
Incubation Time: 24 h
Result: Increased the green fluorescence of DCF, increased the fluorescence of Rh123 fluorescence.

Cell Cycle Analysis[4]

Cell Line: MCF-7, HeLa, and HT-29 cells
Concentration: 500 μg/mL
Incubation Time: 24 h
Result: Increased the subG1 peaks.

RT-PCR[4]

Cell Line: MCF-7, HeLa, and HT-29 cells
Concentration: 100 μg/mL
Incubation Time: 24 h
Result: Increased the expressions of p53, caspase 3, caspase 9, bax, and SOD1 genes.

Apoptosis Analysis[6]

Cell Line: PC3 cells
Concentration: PC3 cells
Incubation Time: 72 h
Result: 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.

Cell Migration Assay [6]

Cell Line: PC3 cells
Concentration: 100 μM
Incubation Time: 24 h
Result: Reduced migration, reduced TWIST, SNAIL, and ZEB1 mRNA expression levels by 59%, 68%, and 42%, respectively, compared to untreated cells.
In Vivo

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.
Animal Model: Swiss albino mice (adult male, 24-28 g) model[5]
Dosage: 50, 100, 150, and 200 μg/kg
Administration: i.p., once
Result: 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.
Clinical Trial
Molecular Weight

302.28

Formula

C16H14O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C[C@@H](C2=CC=C(O)C(OC)=C2)OC3=CC(O)=CC(O)=C13
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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
Concentration Solvent Mass 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
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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (4.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO 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)

    Solubility: ≥ 1.25 mg/mL (4.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.
 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.
Purity & Documentation
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3082 mL 16.5410 mL 33.0819 mL 82.7048 mL
5 mM 0.6616 mL 3.3082 mL 6.6164 mL 16.5410 mL
10 mM 0.3308 mL 1.6541 mL 3.3082 mL 8.2705 mL
15 mM 0.2205 mL 1.1027 mL 2.2055 mL 5.5137 mL
20 mM 0.1654 mL 0.8270 mL 1.6541 mL 4.1352 mL
25 mM 0.1323 mL 0.6616 mL 1.3233 mL 3.3082 mL
30 mM 0.1103 mL 0.5514 mL 1.1027 mL 2.7568 mL
40 mM 0.0827 mL 0.4135 mL 0.8270 mL 2.0676 mL
50 mM 0.0662 mL 0.3308 mL 0.6616 mL 1.6541 mL
60 mM 0.0551 mL 0.2757 mL 0.5514 mL 1.3784 mL
80 mM 0.0414 mL 0.2068 mL 0.4135 mL 1.0338 mL
100 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8270 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

Homoeriodictyol446-71-9Drug MetaboliteAutophagyApoptosisReactive Oxygen Species (ROS)Keap1-Nrf2MMPCaspasePARPMDM-2/p53Matrix metalloproteinasespoly ADP ribose polymeraseSH-SY5Y cellsMDA-MB-231 cellsEA.hy926 cellsMCF-7 cellsHeLa cellsHT-29 cellsPC3 cellsSwiss albino miceAD miceprostate cancerInhibitorinhibitorinhibit

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