2. Metabolic Enzyme/Protease MAPK/ERK Pathway Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage GPCR/G Protein Immunology/Inflammation Anti-infection Apoptosis Membrane Transporter/Ion Channel NF-κB
  3. Amylases Glycosidase Lipase Dipeptidyl Peptidase p38 MAPK PPAR P2Y Receptor NOD-like Receptor (NLR) SARS-CoV Pyroptosis GLUT Angiotensin-converting Enzyme (ACE) NF-κB
  4. Cichoriin

Cichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC50 values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y14R (IC50 = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2.

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Cichoriin

Cichoriin Chemical Structure

CAS No. : 531-58-8

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Based on 2 publication(s) in Google Scholar

Cichoriin Related Antibodies

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  • Biological Activity

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Description

Cichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC50 values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y14R (IC50 = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2[1][2][3][4].

IC50 & Target[1][5]

PPAR-γ

 

DPP-4

 

GLUT4

 

NLRP3 inflammasome

 

P2Y14 Receptor

 

In Vitro

Cichoriin exhibits favorable binding affinity to multiple diabetes and cardiovascular targets, including α-amylase, α-glucosidase, DPP-IV, PPARγ, AMPK, GLUT-4, ACE and NF-κB, with binding energies ranging from -6.8 to -9.8 kcal/mol[1].
Cichoriin (25-50 μM; 24 h) dose-dependently reduces free fatty acid (FFA)-induced lipid accumulation in HepG2 cells, AML12 cells, and primary mouse hepatocytes[3].
Cichoriin (25-50 μM; 24 h) reduces reactive oxygen species levels in FFA-induced AML12 mouse hepatocytes[3].
Cichoriin (50 μM; 24 h) activates the AMPK pathway by increasing the phosphorylation levels of AMPKα and ACC, and upregulates the expression of CPT-1A in primary mouse hepatocytes treated with free fatty acids (FFA)[3].
Cichoriin (50 μM; 24 h) inhibits the migration and activation of hepatic stellate cells (HSC) (reducing the expression of Col I and α-SMA) in an indirect co-culture system by regulating paracrine signals in primary mouse hepatocytes treated with FFA[3].
Cichoriin (25-50 μM; 24 h) inhibits PDGF-AA secretion from lipotoxic primary mouse hepatocytes[3].
The lipid-lowering, anti-inflammatory, and PDGF-AA inhibitory effects of Cichoriin on free fatty acid (FFA)-treated primary mouse hepatocytes, as well as the anti-fibrotic effect on co-cultivated hepatic stellate cells (HSCs), all depend on the activation of AMPK[3].
Cichoriin (50-200 μM; 24 h) significantly inhibits monosodium urate crystal-induced release of IL-1β and IL-18, as well as protein expression of NLRP3, Caspase-1, GSDMD and ASC in differentiated THP-1 macrophages[5].
Cichorin (50-200 μM; 24 h) effectively inhibits monosodium urate crystal-driven macrophage pyroptosis[5].

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

Cichoriin Related Antibodies

Western Blot Analysis[3]

Cell Line: Primary mouse hepatocytes (with FFA-induced lipotoxicity)
Concentration: 50 μM
Incubation Time: 24 h (concurrent with FFA treatment)
Result: Significantly increased phosphorylation levels of AMPKα and ACC compared to FFA-only treated cells.
Upregulated CPT-1A protein expression compared to FFA-only treated cells.

Cell Migration Assay[3]

Cell Line: Indirect Transwell co-culture of primary mouse hepatocytes and primary mouse hepatic stellate cells (HSCs) (with FFA-induced hepatocyte lipotoxicity)
Concentration: 50 μM
Incubation Time: 24 h (incubation with hepatocytes, prior to co-culture)
Result: Significantly inhibited HSC migration (reduced wound closure rate) compared to FFA-only treated hepatocytes.
Downregulated protein expression of collagen I (Col I) and alpha-smooth muscle actin (α-SMA) in co-cultured HSCs compared to FFA-only treated hepatocytes.

ELISA Assay[3]

Cell Line: Primary mouse hepatocytes (with FFA-induced lipotoxicity)
Concentration: 25 and 50 μM
Incubation Time: 24 h
Result: Reduced FFA-induced PDGF-AA secretion from primary mouse hepatocytes compared to FFA-only treated hepatocytes.

ELISA Assay[5]

Cell Line: THP-1 macrophages
Concentration: 25, 100 and 200 μM
Incubation Time: Pre-treatment for 1 hour, followed by stimulation with sodium urate crystals for 23 hours
Result: Significantly inhibited the release of IL-1β and IL-18.

Western Blot Analysis[5]

Cell Line: THP-1 macrophages
Concentration: 25, 100 and 200 μM
Incubation Time: Pre-treatment for 1 hour, followed by stimulation with sodium urate crystals for 23 hours
Result: Significantly inhibited the protein expression levels of NLRP3, Caspase-1, GSDMD and ASC.
In Vivo

Cichoriin (50-100 mg/kg; p.o.; daily; 4 weeks) mitigates high-fat diet-induced obesity and associated metabolic, oxidative, and histopathological dysfunctions in rats in a dose-dependent manner[2].
Cichoriin (100-200 mg/kg/day; oral gavage; daily; 6 weeks) dose-dependently alleviates GAN diet-induced MASH and associated liver fibrosis in male C57BL/6J mice via AMPK pathway activation[3].

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

Animal Model: Wistar (male, 100-150 g initial weight, high-fat diet-induced obesity)[2]
Dosage: 50 mg/kg; 100 mg/kg
Administration: p.o.; daily; 4 weeks
Result: Reduced body-weight gain to 142 g, BMI to 0.58 g/cm2, liver weight to 7.0 g, visceral fat weight to 4.7 g.
Improved serum lipid profile to total cholesterol 125 mg/dL, triglycerides 48 mg/dL, low-density lipoprotein cholesterol 93 mg/dL, high-density lipoprotein cholesterol 23 mg/dL, LDL-C/HDL-C ratio 4.2.
Lowered hepatic malondialdehyde to 107.2 nmol/g tissue, renal malondialdehyde to 78.4 nmol/g tissue, and increased hepatic reduced glutathione to 271 mg/g tissue, renal reduced glutathione to 286 mg/g tissue.
Upregulated peroxisome proliferator-activated receptor gamma mRNA and protein expression in adipose tissue.
Showed moderate improvement in heart, kidney, and liver tissue architecture with reduced tissue damage compared to HFD controls.
Reduced body-weight gain to 123 g, BMI to 0.55 g/cm2, liver weight to 6.7 g, kidney weight to 1.2 g, heart weight to 0.9 g, visceral fat weight to 3.1 g.
Improved serum lipid profile to total cholesterol 85 mg/dL, triglycerides 40 mg/dL, low-density lipoprotein cholesterol 44 mg/dL, high-density lipoprotein cholesterol 33 mg/dL, LDL-C/HDL-C ratio 1.4.
Normalized serum alanine transaminase, aspartate transaminase, urea, creatinine, and creatine kinase MB levels to near-control values.
Lowered hepatic malondialdehyde to 96.9 nmol/g tissue, renal malondialdehyde to 64.3 nmol/g tissue, and increased hepatic reduced glutathione to 325 mg/g tissue, renal reduced glutathione to 339 mg/g tissue.
Upregulated peroxisome proliferator-activated receptor gamma mRNA and protein expression in adipose tissue to levels comparable to the atorvastatin control.
Showed marked improvement in heart, kidney, and liver tissue architecture with minimal residual damage compared to HFD controls.
Animal Model: C57BL/6J (male, 8-10 weeks old, 20-25 g, GAN diet-induced MASH)[3]
Dosage: 100 mg/kg/day; 200 mg/kg/day
Administration: oral gavage; daily; 6 weeks
Result: Significantly reduced body weight, liver index, and blood glucose levels in a dose-dependent manner.
Decreased serum levels of AST, ALT, LDH, AKP, TC, TG, LDL-C, and NEFA, while increased HDL-C levels.
Attenuated hepatic steatosis, inflammation scores, and NAFLD Activity Score (NAS), with reduced liver lipid content (Oil Red O staining area, hepatic TC, TG).
Lowered hepatic AST, ALT, and LDH levels.
Reduced liver fibrosis, as shown by decreased Masson’s trichrome staining area, hepatic hydroxyproline levels, liver Ishak score, and serum fibrosis biomarkers (HA, LN, Col IV, Pro III).
Dose-dependently suppressed mRNA expression of fibrosis-related genes (Col3a1, Col1a1, Acta2, Tgfb1), reduced Smad2 and Smad4 staining intensity, and downregulated protein expression of α-SMA, TGF-β1, Col III, and Col I.
Decreased hepatic F4/80-positive macrophage density, upregulated hepatic SOD, GSH, and CAT levels, and reduced hepatic MDA content.
Lowered hepatic levels of TNF-α, IL-6, and IL-1β, with downregulated protein levels of p-IKKβ and p-NF-κB p65, and upregulated IκBα.
Enhanced phosphorylation of AMPK (Thr172) and ACC (Ser79) at 200 mg/kg dose, increasing p-AMPK/total AMPK and p-ACC/total ACC ratios.
Reversed GAN diet-induced upregulation of pro-inflammatory factors, fibrogenic markers, and lipogenic enzymes, while restored expression of fatty acid β-oxidation and insulin signaling proteins at 200 mg/kg dose.
Molecular Weight

340.28

Formula

C15H16O9
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=C(C=C2C(C=CC(O2)=O)=C1)O[C@@H]3O[C@@H]([C@H]([C@@H]([C@H]3O)O)O)CO
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (293.88 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 2.9388 mL 14.6938 mL 29.3876 mL
5 mM 0.5878 mL 2.9388 mL 5.8775 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 (sealed storage, away from moisture and 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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Molecular Weight *

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: ≥ 2.5 mg/mL (7.35 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 (7.35 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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(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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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: 99.9%

SDS (252 KB)

COA (251 KB) HNMR (111 KB) CNMR (114 KB) RP-HPLC (174 KB) MS (138 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 (sealed storage, away from moisture and 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 2.9388 mL 14.6938 mL 29.3876 mL 73.4689 mL
5 mM 0.5878 mL 2.9388 mL 5.8775 mL 14.6938 mL
10 mM 0.2939 mL 1.4694 mL 2.9388 mL 7.3469 mL
15 mM 0.1959 mL 0.9796 mL 1.9592 mL 4.8979 mL
20 mM 0.1469 mL 0.7347 mL 1.4694 mL 3.6734 mL
25 mM 0.1176 mL 0.5878 mL 1.1755 mL 2.9388 mL
30 mM 0.0980 mL 0.4898 mL 0.9796 mL 2.4490 mL
40 mM 0.0735 mL 0.3673 mL 0.7347 mL 1.8367 mL
50 mM 0.0588 mL 0.2939 mL 0.5878 mL 1.4694 mL
60 mM 0.0490 mL 0.2449 mL 0.4898 mL 1.2245 mL
80 mM 0.0367 mL 0.1837 mL 0.3673 mL 0.9184 mL
100 mM 0.0294 mL 0.1469 mL 0.2939 mL 0.7347 mL
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Cichoriin 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:

Cichoriin531-58-8AmylasesGlycosidaseLipaseDipeptidyl Peptidasep38 MAPKPPARP2Y ReceptorNOD-like Receptor (NLR)SARS-CoVPyroptosisGLUTAngiotensin-converting Enzyme (ACE)NF-κBDPPPeroxisome proliferator-activated receptorsSARS coronavirusGlucose transporter Nuclear factor-κBNuclear factor-kappaBAML12 cellsSARS-CoV-2porcine pancreatic lipasePPAR-γα-amylaseα-glucosidaseHepG2 cellsprimary mouse hepatocytesAMPKDPP-IVInhibitorinhibitorinhibit

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