1. Anti-infection NF-κB Apoptosis
  2. Influenza Virus Fungal NF-κB Apoptosis
  3. Hyperoside

Hyperoside is a NF-κB inhibitor, found from Hypericum monogynum. Hyperoside shows anti-tumor, antifungal, anti-inflammatory, anti-viral, and anti-oxidative activities, and can induce apoptosis.

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Hyperoside Chemical Structure

Hyperoside Chemical Structure

CAS No. : 482-36-0

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Based on 4 publication(s) in Google Scholar

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Description

Hyperoside is a NF-κB inhibitor, found from Hypericum monogynum. Hyperoside shows anti-tumor, antifungal, anti-inflammatory, anti-viral, and anti-oxidative activities, and can induce apoptosis[1][2].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 10 μg/mL
Compound: Compound 7
Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
[PMID: 25862199]
C2C12 EC50
60.5 μM
Compound: 11
Increase in glucose uptake in mouse C2C12 cells incubated for 18 hrs using [3H]-2-deoxy-D-glucose by liquid scintillation counting
Increase in glucose uptake in mouse C2C12 cells incubated for 18 hrs using [3H]-2-deoxy-D-glucose by liquid scintillation counting
[PMID: 22738356]
HeLa IC50
> 10 μg/mL
Compound: Compound 7
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
[PMID: 25862199]
RAW264.7 IC50
> 50 μM
Compound: 16
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA
[PMID: 24679441]
RAW264.7 IC50
48.8 μM
Compound: 16
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis
[PMID: 24679441]
SGC-7901 IC50
> 10 μg/mL
Compound: Compound 7
Cytotoxicity against human SGC7901 cells by MTT assay
Cytotoxicity against human SGC7901 cells by MTT assay
[PMID: 25862199]
In Vitro

Hyperoside (12.5-100 μM; 6-24 h) inhibits MCF-7 and 4T1 cell growth[2].
Hyperoside (25-100 μM; 24 h) induces apoptosis of breast cancer cells[2].
Hyperoside inhibits the activation of the NF-κB signaling pathway via the attenuation of intracellular ROS generation[2].

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

Cell Viability Assay[2]

Cell Line: MCF-7 and 4T1 cells
Concentration: 12.5, 25, 50, 75, or 100 µM
Incubation Time: 6, 12, or 24 h
Result: Inhibited cell growth in a time- and concentration-dependent manner.

Apoptosis Analysis[2]

Cell Line: MCF-7 and 4T1 cells
Concentration: 25, 50 and 100 µM
Incubation Time: 24 h
Result: Increased the expressions of Bax, cleaved caspase-3 and cleaved PARP, and decreased Bcl-2 in mRNA and protein levels.
In Vivo

Hyperoside (intraperitoneal injection; 50 mg/kg; every two day for 18 days) treatment inhibits breast tumor growth in vivo[1].

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

Animal Model: Balb/c mice injected with 4T1 cells[2]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 50 mg/kg; every two day for 18 days
Result: Reduced the average tumor volume compared to the control group.
Decreased Bcl-2 and increased bax and cleaved caspase-3.
Molecular Weight

464.38

Formula

C21H20O12

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1=CC(O)=C(C(C(O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O2)=C(C3=CC=C(O)C(O)=C3)O4)=O)C4=C1

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (269.18 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 2.1534 mL 10.7670 mL 21.5341 mL
5 mM 0.4307 mL 2.1534 mL 4.3068 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Concentration (start)

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C2

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Volume (final)

V2

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: ≥ 2.08 mg/mL (4.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (21.53 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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 +
+
%
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%
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.
 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

Purity: 99.50%

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. 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 2.1534 mL 10.7670 mL 21.5341 mL 53.8352 mL
5 mM 0.4307 mL 2.1534 mL 4.3068 mL 10.7670 mL
10 mM 0.2153 mL 1.0767 mL 2.1534 mL 5.3835 mL
15 mM 0.1436 mL 0.7178 mL 1.4356 mL 3.5890 mL
20 mM 0.1077 mL 0.5384 mL 1.0767 mL 2.6918 mL
25 mM 0.0861 mL 0.4307 mL 0.8614 mL 2.1534 mL
30 mM 0.0718 mL 0.3589 mL 0.7178 mL 1.7945 mL
40 mM 0.0538 mL 0.2692 mL 0.5384 mL 1.3459 mL
50 mM 0.0431 mL 0.2153 mL 0.4307 mL 1.0767 mL
60 mM 0.0359 mL 0.1795 mL 0.3589 mL 0.8973 mL
80 mM 0.0269 mL 0.1346 mL 0.2692 mL 0.6729 mL
100 mM 0.0215 mL 0.1077 mL 0.2153 mL 0.5384 mL
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  • 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.

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Product Name:
Hyperoside
Cat. No.:
HY-N0452
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