1. MAPK/ERK Pathway NF-κB Neuronal Signaling Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis GPCR/G Protein Stem Cell/Wnt
  2. p38 MAPK NF-κB JNK Cholinesterase (ChE) Acyltransferase NO Synthase Interleukin Related TNF Receptor Prostaglandin Receptor ERK COX
  3. Cornuside

Cornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC50 = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.

For research use only. We do not sell to patients.

Cornuside

Cornuside Chemical Structure

CAS No. : 131189-57-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 6 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Cornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC50 = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation[1][2][3].

IC50 & Target[2][3][1]

p38 MAP kinase

 

NF-κB

 

JNK1

 

JNK2

 

AChE

 

BChE

 

iNOS

 

IL-6

 

IL-1β

 

COX-2

 

In Vitro

Cornuside exhibits free radical scavenging activity in a cell-free DPPH assay with an IC50 of 20 μM[1].
Cornuside protects SH-SY5Y cells from H2O2-induced damage by enhancing endogenous antioxidant defense systems[1].
Cornuside (3-30 μM; 30 min) dose-dependently inhibits anti-DNP IgE-mediated histamine release from rat peritoneal mast cells, with significant effects at 10 and 30 μM[2].
Cornuside (3-30 μM; 4 h) dose-dependently inhibits the production and secretion of TNF-α and IL-6 by PMA/A23187-stimulated human mast cells (HMC-1), with significant effects at 10 and 30 μM[2].
Cornuside (3-30 μM; 1 h pre-incubation, 18 h LPS stimulation) dose-dependently inhibits LPS-induced nitric oxide production in RAW 264.7 cells, with maximum inhibition of 67.6% at 30 μM after 18 hours of LPS stimulation[3].
Cornuside (3-30 μM; 1 h pre-incubation, 1 h LPS stimulation) dose-dependently inhibits LPS-induced nuclear translocation of the NF-κB p65 subunit in RAW 264.7 cells after 1 hour of LPS stimulation, with maximum inhibition at 30 μM[3].

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

Western Blot Analysis[2]

Cell Line: human mast cells (HMC-1)
Concentration: 3, 10 and 30 μM
Incubation Time: 4 h (during PMA/A23187 stimulation)
Result: Inhibited protein expression and secretion of TNF-α and IL-6 in a dose-dependent manner, with significant inhibition observed at 10 μM and 30 μM.\n
Inhibited the activation of p38 and JNK in a dose-dependent manner.
Reduced NF-κB p65 levels in the nucleus while increasing NF-κB p65 levels in the cytosol of PMA/A23187-stimulated HMC-1 cells.

ELISA Assay[3]

Cell Line: LPS-stimulated RAW 264.7 macrophage cell line
Concentration: 3, 10, 30 μM
Incubation Time: 1 h pre-incubation, followed by 18 h incubation with LPS
Result: Significantly attenuated LPS-induced PGE2 production in a dose-dependent manner.

Western Blot Analysis[3]

Cell Line: LPS-stimulated RAW 264.7 macrophage cell line
Concentration: 3, 10, 30 μM
Incubation Time: 1 h pre-incubation, followed by 18 h incubation with LPS
Result: Concentration-dependently suppressed LPS-induced protein expressions of iNOS and COX-2.

RT-PCR[3]

Cell Line: LPS-stimulated RAW 264.7 macrophage cell line
Concentration: 3, 10, 30 μM
Incubation Time: 1 h pre-incubation, followed by 6 h incubation with LPS
Result: Concentration-dependently suppressed LPS-induced mRNA expressions of iNOS and COX-2, with levels correlated to protein expression changes.

Western Blot Analysis[3]

Cell Line: LPS-stimulated RAW 264.7 macrophage cell line
Concentration: 3, 10, 30 μM
Incubation Time: 1 h pre-incubation, followed by 1 h incubation with LPS
Result: Dose-dependently inhibited LPS-induced translocation of the p65 subunit of NF-κB from the cytosol to the nucleus.\n
Increased cytoplasmic p65 levels to 80% of vehicle control and decreased nuclear p65 levels to 30% of LPS-only control at 30 μM.
Significantly blocked LPS-stimulated phosphorylation and degradation of IkB-α in a dose-dependent manner.\n
Reduced p-IkB-α levels to 20% of LPS-only control and restored IkB-α levels to 90-100% of vehicle control at 10 and 30 μM.\nSuppressed LPS-stimulated phosphorylations of ERK1/2, p38, and JNK1/2 in a concentration-dependent manner.\n
Reduced p-ERK1/2 levels to 40%, p-p38 levels to 10-15%, and p-JNK1/2 levels to 10-15% of LPS-only control at 30 μM.\n
Left non-phosphorylated ERK1/2, p38, and JNK1/2 expression unaffected.
In Vivo

Cornuside (3-30 mg/kg; p.o.; daily administration for 15 consecutive days) ameliorates scopolamine (HY-N0296)-induced cognitive impairment in mice[1].
Cornuside (50-200 mg/kg; p.o.; single administration) dose-dependently inhibits passive cutaneous anaphylaxis in mice and rats[2].

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

Animal Model: ICR mice (male, 20 g, scopolamine-induced amnesia)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; daily; day 4 to day 19
Result: Significantly improved the learning and memory impairments of mice in the Scopolamine model in water maze, dark avoidance and jumping platform experiments.
Animal Model: Male Sprague-Dawley and Institute of Cancer Research mice[2]
Dosage: 50 mg/kg; 100 mg/kg; 200 mg/kg
Administration: p.o.; single dose 1 hour before antigen challenge
Result: Produced dose-dependent inhibition of passive cutaneous anaphylaxis.
Molecular Weight

542.49

Formula

C24H30O14

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(O)=C(O)C(O)=C1)OCCC(C(C(OC)=O)=COC2OC(C(C(O)C3O)O)OC3CO)C2C=C

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 : 100 mg/mL (184.34 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 1.8434 mL 9.2168 mL 18.4335 mL
5 mM 0.3687 mL 1.8434 mL 3.6867 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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  • Dilution Calculator

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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: ≥ 2.5 mg/mL (4.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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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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

Purity: 99.99%

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 1.8434 mL 9.2168 mL 18.4335 mL 46.0838 mL
5 mM 0.3687 mL 1.8434 mL 3.6867 mL 9.2168 mL
10 mM 0.1843 mL 0.9217 mL 1.8434 mL 4.6084 mL
15 mM 0.1229 mL 0.6145 mL 1.2289 mL 3.0723 mL
20 mM 0.0922 mL 0.4608 mL 0.9217 mL 2.3042 mL
25 mM 0.0737 mL 0.3687 mL 0.7373 mL 1.8434 mL
30 mM 0.0614 mL 0.3072 mL 0.6145 mL 1.5361 mL
40 mM 0.0461 mL 0.2304 mL 0.4608 mL 1.1521 mL
50 mM 0.0369 mL 0.1843 mL 0.3687 mL 0.9217 mL
60 mM 0.0307 mL 0.1536 mL 0.3072 mL 0.7681 mL
80 mM 0.0230 mL 0.1152 mL 0.2304 mL 0.5760 mL
100 mM 0.0184 mL 0.0922 mL 0.1843 mL 0.4608 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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Cornuside
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