2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel Apoptosis Neuronal Signaling MAPK/ERK Pathway NF-κB Immunology/Inflammation Anti-infection
  3. Glutathione S-transferase P-glycoprotein Apoptosis iGluR CaMK p38 MAPK Reactive Oxygen Species (ROS) Bacterial
  4. Coniferyl ferulate

Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC50 = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus.

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Coniferyl ferulate

Coniferyl ferulate Chemical Structure

CAS No. : 63644-62-2

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Based on 1 publication(s) in Google Scholar

Coniferyl ferulate Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC50 = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus[1][2][3][4][5].

IC50 & Target[2]

CaMK II

 

NMDA Receptor

 

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
19.8 μM
Compound: 40; coniferyl ferulate
Antimigratory activity against human MDA-MB-231 cells expressing c-MET assessed as inhibition of HGF-induced cell migration incubated for 24 hrs by Giemsa staining based wound healing assay
Antimigratory activity against human MDA-MB-231 cells expressing c-MET assessed as inhibition of HGF-induced cell migration incubated for 24 hrs by Giemsa staining based wound healing assay
[PMID: 27258622]
MDA-MB-231 IC50
22.3 μM
Compound: 40; coniferyl ferulate
Antiproliferative activity against human MDA-MB-231 cells expressing c-MET assessed as inhibition of HGF-induced cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells expressing c-MET assessed as inhibition of HGF-induced cell growth incubated for 72 hrs by MTT assay
[PMID: 27258622]
MDA-MB-468 IC50
25.6 μM
Compound: 40; coniferyl ferulate
Antiproliferative activity against human MDA-MB-468 cells expressing c-MET assessed as inhibition of HGF-induced cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells expressing c-MET assessed as inhibition of HGF-induced cell growth incubated for 72 hrs by MTT assay
[PMID: 27258622]
In Vitro

Coniferyl ferulate (5-20 μM, 48 h) induces apoptosis and markedly inhibits cells in G1-phase in B-MD-C1 (ADR+/+) cells[1].
Coniferyl ferulate (5-20 μM, 48 h) inhibits the upregulation of MDR1/P-gp caused by Doxorubicin (HY-15142A), and bring the expression of P-gp close to the basal level in B-MD-C1 (ADR+/+) cells[1].
Coniferyl ferulate (0.2-20 μM, 28 h) protects against the decline in cell viability and apoptosis induced by Glutamate (HY-14608), and alleviates cell membrane damage by blocking the NMDA receptor-CaMKII-MAPKs signaling cascade, reducing the level of ROS and enhancing SOD activity in PC12 cells[2].

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

Coniferyl ferulate Related Antibodies

Apoptosis Analysis[1]

Cell Line: B-MD-C1(ADR+/+) cells
Concentration: 5, 10 and 20 μM
Incubation Time: 48 h
Result: Induced apoptosis.

Cell Cycle Analysis[1]

Cell Line: B-MD-C1(ADR+/+) cells
Concentration: 5, 10 and 20 μM
Incubation Time: 48 h
Result: Markedly increased the proportion of cells in G1-phase, decreased the proportion of cells in S-phase.

RT-PCR[1]

Cell Line: B-MD-C1(ADR+/+) cells
Concentration: 5, 10 and 20 μM
Incubation Time: 48 h
Result: Dose-dependently inhibited Doxorubicin-induced MDR1 overexpression.
Brought the expression of P-gp close to the basal level.

Cell Viability Assay[2]

Cell Line: Glutamate-damaged PC12 cells
Concentration: 0.2, 2, 20 μM
Incubation Time: After 4 hours of pre-treatment, with Glutamate for another 24 hours
Result: Concentration-dependently protected the decline in cell viability induced by Glutamate.
Significantly alleviated the damage to the cell membrane caused by Glutamate.

Apoptosis Analysis[2]

Cell Line: Glutamate-damaged PC12 cells
Concentration: 0.2, 2, 20 μM
Incubation Time: After 4 hours of pre-treatment, with Glutamate for another 24 hours
Result: Reduced nuclear shrinkage and PI-positive cells.

Apoptosis Analysis[2]

Cell Line: Glutamate-damaged PC12 cells
Concentration: 0.2, 2, 20 μM
Incubation Time: After 4 hours of pre-treatment, with Glutamate for another 24 hours
Result: Decreased the level of p-NR2B, p-CaMKII, p-JNK and p-p38.
Increased the Bcl-2/Bax ratio and decreased the release of cytochrome C and activation of Caspase-3.
In Vivo

Coniferyl ferulate (25-100 mg/kg, i.g., once daily, for 13-14 days) possesses anti-depressant effect in mice behavioral test[2].
Coniferyl ferulate (50 mg/kg, i.g., once daily, for 4 weeks) attenuates depression-like and anxiety-like behaviors induced by chronic unpredicted mild stress (CUMS), and significantly ameliorates colonic inflammation in mice[3].
Coniferyl ferulate (50 mg/kg, i.g., once daily, for 25 days) alleviates xylene-caused hematopoietic stem and progenitor cell toxicity by inhibiting Mgst2 in mice[4].

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

Animal Model: Behavioral test (tail suspension and forced-swimming test) established in male ICR mice (18-22 g)[2]
Dosage: 25, 50 and 100 mg/kg
Administration: Intragastric administration (i.g.), once daily, for 13 and 14 days
Result: Obviously decreased the immobility time in tail suspension test (TST) and forced swimming test (FST).
Animal Model: CUMS model established in in 8-week-old male C57BL/6 SPF mice (20 g)[3]
Dosage: 50 mg/kg
Administration: Intragastric administration (i.g.), once daily, for 4 weeks
Result: Improved depressive in sucrose preference test (SPT), open field test (OFT), FTS and TST and anxiety-like behaviors in elevated plus-maze test (EPM).
Restored the reduction of intestinal microvilli and alleviated mitochondrial swelling.
Lowered the levels of IL-6, IL-1β, and TNF-α.
Restructured the gut microbiome, and microbial metabolism.
Animal Model: Xylene-induced hematotoxicity model established in male C57BL/6 SPF mice (8 weeks old, 20 g)
Dosage: 50 mg/kg
Administration: Intragastric administration (i.g.), once daily, for 25 days
Result: Significantly reversed the White blood cell count (WBC) reduction induced by xylene.
Restored the proportion of bone marrow LSK cells to the normal level.
Reduced the level of ROS in mitochondria and restored the mitochondrial membrane potential inhibited by xylene.
Acted directly on the Mgst2 target site (KD = 8.0861 kcal/mol).
Molecular Weight

356.37

Formula

C20H20O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC/C=C/C1=CC=C(O)C(OC)=C1)/C=C/C2=CC=C(O)C(OC)=C2
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 (280.61 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 2.8061 mL 14.0304 mL 28.0607 mL
5 mM 0.5612 mL 2.8061 mL 5.6121 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.

  • 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

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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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.02 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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(per animal)

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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: 98.73%

SDS (252 KB)

COA (244 KB) HNMR (255 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
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 2.8061 mL 14.0304 mL 28.0607 mL 70.1518 mL
5 mM 0.5612 mL 2.8061 mL 5.6121 mL 14.0304 mL
10 mM 0.2806 mL 1.4030 mL 2.8061 mL 7.0152 mL
15 mM 0.1871 mL 0.9354 mL 1.8707 mL 4.6768 mL
20 mM 0.1403 mL 0.7015 mL 1.4030 mL 3.5076 mL
25 mM 0.1122 mL 0.5612 mL 1.1224 mL 2.8061 mL
30 mM 0.0935 mL 0.4677 mL 0.9354 mL 2.3384 mL
40 mM 0.0702 mL 0.3508 mL 0.7015 mL 1.7538 mL
50 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4030 mL
60 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1692 mL
80 mM 0.0351 mL 0.1754 mL 0.3508 mL 0.8769 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7015 mL
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Coniferyl ferulate Related Classifications

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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.

Keywords:

Coniferyl ferulate63644-62-2Glutathione S-transferaseP-glycoproteinApoptosisiGluRCaMKp38 MAPKReactive Oxygen Species (ROS)BacterialGlutathione transferasesGSTsP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Ionotropic glutamate receptorsCalmodulin-dependent protein kinasesCalmodulin-dependent kinasesXiaoyaosanAnti-depressionOxidative stressNMDARCaMKIIInhibitorinhibitorinhibit

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