2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  3. Phosphodiesterase (PDE) NF-κB Keap1-Nrf2 Reactive Oxygen Species TNF Receptor Nuclear Factor of activated T Cells (NFAT) Akt ERK p38 MAPK NO Synthase Interleukin Related COX JNK
  4. Sappanone A

Sappanone A is an orally active homoisoflavone found in sappan L. Sappanone A is a PDE4 and NF-κB inhibitor with anti-inflammatory and antioxidant effect. Sappanone A induces HO-1 expression through activation of Nrf2 pathway. Sappanone A also inhibits RANKL-induced osteoclastogenesis. Sappanone A has great potential in the research of inflammation-related and cardiovascular .

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Sappanone A Chemical Structure

Sappanone A Chemical Structure

CAS No. : 102067-84-5

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Based on 4 publication(s) in Google Scholar

Sappanone A Related Antibodies

Top Publications Citing Use of Products

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Akt Akt1 Akt2 Akt3

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ERK ERK1 ERK2 ERK5 ERK8

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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nNOS iNOS eNOS

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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COX COX-1 COX-2 COX-3

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JNK1 JNK2 JNK3 JNK

  • Biological Activity

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Description

Sappanone A is an orally active homoisoflavone found in sappan L. Sappanone A is a PDE4 and NF-κB inhibitor with anti-inflammatory and antioxidant effect. Sappanone A induces HO-1 expression through activation of Nrf2 pathway. Sappanone A also inhibits RANKL-induced osteoclastogenesis. Sappanone A has great potential in the research of inflammation-related and cardiovascular [1][2][3][4][5].

Cellular Effect
Cell Line Type Value Description References
RAW264.7 IC50
5.7 μM
Compound: 7
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide generation incubated for 24 hrs
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide generation incubated for 24 hrs
[PMID: 23234407]
RAW264.7 IC50
8.3 μM
Compound: 7
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 24 hrs by ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 24 hrs by ELISA
[PMID: 23234407]
RAW264.7 IC50
9.3 μM
Compound: Sappanone A
Inhibition of LPS-induced NO production in mouse RAW264.7 cells preincubated for 1 hr followed by LPS stimulation for 24 hrs by Griess assay
Inhibition of LPS-induced NO production in mouse RAW264.7 cells preincubated for 1 hr followed by LPS stimulation for 24 hrs by Griess assay
[PMID: 28038832]
In Vitro

Sappanone A (5-30 μM, pretreatment for 1 h, then 24 h) inhibits LPS-induced NO, IL-6 and PGE 2 production in RAW264.7 cells in a concentration-dependent manner (IC50 6.8, 11.2 and 12.6 μM, respectively) without cytotoxicity[1].
Sappanone A (5-30 μM, 24 h) exerts anti-inflammatory effects in RAW264.7 cells by inducing HO-1 expression and inhibits LPS-induced NF-κB activation through activation of Nrf2[2].
Sappanone A (10-40 μM) remarkably inhibits PDE4 enzyme activity and reduces TNF-α production induced by LPS in RAW264.7 macrophages[2].
Sappanone A (0.007-1.0 mM, 40 min) has excellent ability to reduce Fe3+ and complex Fe2+, shows excellent antioxidant activity[2].
Sappanone A (3-30 μM, 7 days) inhibits RANKL-induced osteoclastogenesis in mouse bone marrow-derived macrophage (BMM)[3].
Sappanone A (0-30 μM, 7 days) inhibits RANKL-induced NFATc1 activation and AKT phosphorylation in BMMs[3].
Sappanone A (10-30 μM, pretreatment for 1 hour, then treatment for 24 hours) blocks the NF-κB pathway and inhibits the inflammatory response in the HG-induced mesangial cell model[5].

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

Sappanone A Related Antibodies

RT-PCR[1]

Cell Line: RAW264.7cells
Concentration: 5, 15, 30 μM
Incubation Time: 24 h
Result: Reduced the mRNA levels of iNOS, COX-2, and IL-6 in a concentration-dependent manner.
Increased HO-1 mRNA expression level in a concentration-dependent manner, and HO-1 mRNA increased 3 hours after treatment, peaked at 6 hours, and returned to basal levels at 24 hours.
Induced HO-1 expression by activating Nrf2, resulting in a concentration-dependent increase in the mRNA levels of NQO1 and GCLC.

Western Blot Analysis[3]

Cell Line: BMM cells
Concentration: 0, 3, 10, 30 μM
Incubation Time: 7 days
Result: Increased the phosphorylation levels of ERK, p38 and JNK mitogen-activated protein kinases (MAPKs) in a time-dependent manner and pretreatment.
Inhibited RANKL-induced NFATc1 expression.
In Vivo

Sappanone A (20, 50 mg/kg, i.p., one dose) protects mice from death in the LPS-induced mortality in C57BL/6 mice model[1].
Sappanone A (50, 100 mg/kg, i.p., twice a day for seven consecutive days) significantly reduces LPS-induced mice acute lung injury (ALI) without obvious toxic side effects[2].
Sappanone A (50 mg/kg, i.p., injects every other day for a total of eight days) inhibits osteoclast formation in vivo in the LPS-induced mouse bone loss model[3].
Sappanone A (20 mg/kg, i.p., one dose) can reduce myocardial necrosis and apoptosis and promote the recovery of cardiac function in the myocardial ischemia reperfusion injury (MIRI) rat model[4].
Sappanone A (10-30 mg/kg, i.g., once a day for twelve weeks) reduces renal injury during hyperglycemia in a dose-dependent manner in a Streptozotocin (HY-13753)-induced diabetic mouse model[5].

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

Animal Model: ALI in Institute of Cancer Research mice (male 20-25 g) was established by intratracheal instillation of 0.5 mg/kg LPS in 100 μl saline solution.[2]
Dosage: 50,100 mg/kg
Administration: i.p., twice a day for seven consecutive days, 1 h prior to LPS injection
Result: Significantly reduced the production of TNF-α in lung tissue, protein content in BALF, and MPO activity.
Had a good effect on the growth, development and behavior of mice, and no death or obvious toxic side were observed.
Animal Model: Institute of Cancer Research mice (male 6 weeks) injected with LPS (5 mg/kg)[3]
Dosage: 50 mg/kg
Administration: i.p., injected every other day for a total of eight days
Result: LPS-induced significant decreased in the number of TRAP-positive osteoclasts.
Had a good effect on the growth, development and behavior of mice, and no death or obvious toxic side were observed.
Animal Model: Wistar rats (male 250 g) MIRI model (hearts were isolated and underwent 30-min ischemia, followed by 120-min reperfusion)[4]
Dosage: 20 mg/kg
Administration: i.p., one dose, 1 h prior to heart isolation
Result: Reduce myocardial ischemia-reperfusion injury and myocardial infarction area.
Significantly improved LVDP and ±dp/dt values at 30, 60, and 120 min of reperfusion, indicating that it promoted the recovery of cardiac function after ischemia-reperfusion.
Inhibited ischemia-reperfusion-induced cardiomyocyte apoptosis by reducing cell apoptosis and inhibited the expression of cleaved caspase-3.
Significantly reduced the content of ROS and MDA in ischemic myocardium, and increased the activity of SOD and GSH-Px in ischemic myocardium.
Downregulated the expression of Keap1, decreased the level of Nrf2 in the cytoplasm, and increased the level of Nrf2 in the nucleus, and also activated the transcriptional activity to upregulate the expression of Nrf2 target genes (HO-1 and NQO1).
Enhanced the phosphorylation of Nfr2 through the PKC or PI3K pathway.
Animal Model: Streptozotocin (50 mg/kg, i.p., 5 consecutive days) induced diabetic C57BL/6J mice (20-23 g, 6-8 weeks)[5]
Dosage: 10, 20, 30 mg/kg
Administration: i.g., once a day for twelve consecutive weeks
Result: Showed that the increase of serum creatinine and BUN was significantly attenuated, and the 24-hour urine protein of mice was significantly reduced.
Alleviated the pathological changes in Streptozotocin-treated mice, reduced the production of fibrotic molecules transforming growth factor β1 (TGF-β1) and collagen IV (Col-IV), and decreased the expression of inflammatory cytokines interleukin 1β (IL-1β) and tumor necrosis factor α (TNF-α).
Molecular Weight

284.26

Formula

C16H12O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1/C(COC2=CC(O)=CC=C12)=C/C3=CC=C(O)C(O)=C3
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 (351.79 mM; ultrasonic and warming and heat to 60°C; 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 3.5179 mL 17.5895 mL 35.1791 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 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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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 (7.32 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 (7.32 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.
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: 99.87%

SDS (252 KB)

COA (246 KB) HNMR (294 KB) LCMS (96 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 3.5179 mL 17.5895 mL 35.1791 mL 87.9477 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 mL 17.5895 mL
10 mM 0.3518 mL 1.7590 mL 3.5179 mL 8.7948 mL
15 mM 0.2345 mL 1.1726 mL 2.3453 mL 5.8632 mL
20 mM 0.1759 mL 0.8795 mL 1.7590 mL 4.3974 mL
25 mM 0.1407 mL 0.7036 mL 1.4072 mL 3.5179 mL
30 mM 0.1173 mL 0.5863 mL 1.1726 mL 2.9316 mL
40 mM 0.0879 mL 0.4397 mL 0.8795 mL 2.1987 mL
50 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7590 mL
60 mM 0.0586 mL 0.2932 mL 0.5863 mL 1.4658 mL
80 mM 0.0440 mL 0.2199 mL 0.4397 mL 1.0993 mL
100 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8795 mL
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Sappanone A 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:

Sappanone A102067-84-5Phosphodiesterase (PDE)NF-κBKeap1-Nrf2Reactive Oxygen SpeciesTNF ReceptorNuclear Factor of activated T Cells (NFAT)AktERKp38 MAPKNO SynthaseInterleukin RelatedCOXJNKNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRPKBProtein kinase BExtracellular signal regulated kinasesNitric oxide synthasesNOSILCyclooxygenasec-Jun N-terminal kinaseInflammationRAW264.7 cellsoxidative stressC57BL/6 miceICR miceInhibitorinhibitorinhibit

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