1. Metabolic Enzyme/Protease Apoptosis Autophagy NF-κB Immunology/Inflammation MAPK/ERK Pathway
  2. MMP Apoptosis Autophagy NF-κB TNF Receptor COX Toll-like Receptor (TLR) SOD ASK1 JNK
  3. Ecliptasaponin A

Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors.

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Ecliptasaponin A

Ecliptasaponin A Chemical Structure

CAS No. : 78285-90-2

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Based on 1 publication(s) in Google Scholar

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Description

Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors[1][2][3][4][5][6][7].

IC50 & Target[2][7]

MMP-9

 

MMP-13

 

MMP-2

 

NF-κB

 

COX-2

 

TLR4

 

In Vitro

Ecliptasaponin A (5-20 μM) inhibits the HMGB1/TLR4/NF-κB pathway to play a protective role on H9C2 cells of oxygen-glucose deprivation (OGD)[3].
Ecliptasaponin A (0-120 μM, 24-48 h) exhibits dose- and time-dependent inhibition of H460 and H1975 cells viability and colony formation ability[4].
Ecliptasaponin A (0-30 μM, 24 h) induces apoptosis through the activation of ASK1/JNK pathway and autophagy in H460 and H1975 cells[4].
Ecliptasaponin A (5-30 μM, 48 h) inhibits ECM and MMP13 expression in human kidney-2 (HK-2) cells induced by transforming growth factor-beta1 (TGFβ1)[5].
Ecliptasaponin A (0-25 μM) targets the protein ESR1 to increase the viability and reduce apoptosis in Cyclophosphamide (HY-17420)-induced damage in AW-CCH252 cells[6].
Ecliptasaponin A (10-50 ng/mL, 25 h) shows the reduced expression of all osteoarthritis -related molecules in IL-1β-stimulated SW1353 cells[7].

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

Cell Viability Assay[4]

Cell Line: H460 and H1975 cells
Concentration: 0, 20, 40, 60, 80, 100 and 120 μM
Incubation Time: 24 and 48 h
Result: Significantly induced cell death in both dose-dependent and time-dependent ways.

Apoptosis Analysis[4]

Cell Line: H460 and H1975 cells
Concentration: 0, 10, 20 and 30 μM
Incubation Time: 24 h
Result: Dose-dependently increased the proportion of apoptotic cells, with early apoptosis (Annexin V+/PI-) being the predominant type.
Displayed typical apoptotic features: nuclear shrinkage, chromatin condensation, nuclear fragmentation, and the formation of apoptotic bodies.

Western Blot Analysis[4]

Cell Line: H460 and H1975 cells
Concentration: 0, 10, 20 and 30 μM
Incubation Time: 24 h
Result: Increased the Caspase-3/8/9 cleavage products and PARP cleavage.
Increased the LC3-II/I ratio, upregulated Beclin-1 expression, and accelerated the degradation of p62.
Increased the expression of p-ASK1 and p-JNK, and decreased the expression of p-ERK.

Western Blot Analysis[5]

Cell Line: HK-2 cells
Concentration: 20 nM
Incubation Time: 48 h
Result: Inhibited the protein expression of ECM proteins such as FN, Col-1, Col-3, and CTGF.
Specifically inhibited MMP13 rather than MMP10.
Inhibited Col-1, α-SMA, and CTGF.

RT-PCR[5]

Cell Line: HK-2 cells
Concentration: 5, 10, 15, 20, 25, 30 nM
Incubation Time: 48 h
Result: Decreased the expression of type I collagen in a concentration-dependent manner.
Inhibited the gene expression of ECM proteins such as FN, Col-1, Col-3, and CTGF.
Significantly inhibited the mRNA expression of MMP10 (not obvious) and MMP13.

RT-PCR[7]

Cell Line: SW1353 cells
Concentration: 10, 30, 50 ng/mL
Incubation Time: Pretreated at 1 h before IL-1β stimulation (24 h) for 25 h
Result: Decreased the mRNA expression of OA-related molecules (MMP13, TNF-α, IL-1β, COX1/2).

Western Blot Analysis[7]

Cell Line: SW1353 cells
Concentration: 10, 30, 50 ng/mL
Incubation Time: Pretreated at 1 h before IL-1β stimulation (24 h) for 25 h
Result: Decreased the protein expression of OA-related molecules (MMP13, Collagen type II, TNF-α, IL-1β, and COX-2).
Parmacokinetics[1]
Species Dose Route Indicator value
Rat 1000 mg/kg p.o. T1/2 3.34 h
Rat 16000 mg/kg p.o. AUC0-∞ 275.23 μg/L·h
Rat 8000 mg/kg p.o. T1/2 3.02 h
Rat 1000 mg/kg p.o. Tmax 0.28 h
Rat 16000 mg/kg p.o. AUC0-t 269.92 μg/L·h
Rat 8000 mg/kg p.o. Tmax 0.23 h
Rat 1000 mg/kg p.o. Cmax 35.15 μg/mL
Rat 16000 mg/kg p.o. Cmax 246.98 μg/L
Rat 8000 mg/kg p.o. Cmax 110.80 μg/L
Rat 1000 mg/kg p.o. AUC0-t 87.52 μg/L·h
Rat 16000 mg/kg p.o. Tmax 0.25 h
Rat 8000 mg/kg p.o. AUC0-t 124.99 μg/L·h
Rat 1000 mg/kg p.o. AUC0-∞ 129.88 μg/L·h
Rat 16000 mg/kg p.o. T1/2 2.94 h
Rat 8000 mg/kg p.o. AUC0-∞ 127.28 μg/L·h
In Vivo

Ecliptasaponin A (1-18 g/kg, p.o., single dose) is distributed in various tissues, with the concentration order being: liver > spleen > lung > kidney > heart[1].
Ecliptasaponin A (80 mg/kg, p.o., once daily for 28 days) prevents the fibrosis in mice via inhibiting TGF-β1 expression[2].
Ecliptasaponin A (0.5-2.5 mg/kg, intramyocardial injection of the left ventricular myocardium, single dose) demonstrates a cardiac protective role in acute myocardial infarction (AMI) model in mice[3].
Ecliptasaponin A (25-50 mg/kg, i.p., for 21 days) causes a clear suppression of tumor growth in lung cancer-bearing nude mice[4].
Ecliptasaponin A (80 mg/kg, p.o., once daily for 10 days) reduces the renal collagen fiber deposition and renal extracellular matrix (ECM) protein expression in renal fibrosis unilateral ureteral obstruction (UUO) mice[5].
Ecliptasaponin A (200 mg/mL with Specnuezhenide (HY-N0665), p.o., once daily for 30 days) improves the basal characteristics and sex hormone levels premature ovarian failure (POF) mice[6].

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

Animal Model: Pulmonary fibrosis model induced by Bleomycin (HY-108345) established in adult male ICR mice (6-7 weeks)[2]
Dosage: 80 mg/kg
Administration: Oral administration (p.o.), once daily for 28 days
Result: Blocked BLM-induced histological changes of lung tissue.
Decreased the high levels of TGF-β1 and α-SMA.
Animal Model: AMI model induced by underwent left anterior descending coronary artery (LAD) ligation established in male SPF C57/BL6 mice, aged 8-10 weeks and weighing 23-25 g[3]
Dosage: 0.5, 1.25, and 2.5 mg/kg
Administration: Intramyocardial injection of the left ventricular myocardium, single dose
Result: Significantly improved ejection fraction (EF%) and short-axis shortening rate (FS%).
Significantly reduced the area of myocardial infarction.
Reduced myocardial cell apoptosis and inflammatory cell infiltration.
Significantly reduced the expressions of HMGB1 and TLR4, as well as the phosphorylation of p-IkBα and p-P65, and the levels of inflammatory factors IL-1β, IL-6, and TNF-α.
Significantly enriched HMGB1/TLR4/NF-κB pathway.
Animal Model: H460 cells induced xenograft tumor model established in male BALB-c nude mice (4-week-old)[4]
Dosage: 25 and 50 mg/kg
Administration: Intraperitoneal injection (i.p.), for 21 days
Result: Decreased the tumor weight and volume.
No significant biological toxicity.
Animal Model: Renal fibrosis UUO model established in six-week-old C57BL/6 J mice[5]
Dosage: 80 mg/kg
Administration: Oral administration (p.o.), once daily for 10 days
Result: Ameliorated the obstructive kidney weight ratio.
Attenuated histological damage and collagen deposition in the kidneys.
Animal Model: POF model established in SPF-grade female C57 mice, 6-8 weeks[6]
Dosage: 200 mg/mL with Specnuezhenide
Administration: Oral administration (p.o.), once daily for 30 days
Result: Increased the ovarian index and serum estradiol (E2) levels.
Reduced the level of follicle-stimulating hormone (FSH).
Extended the emotional cycle.
Increased the number and diameter of follicles.
Promoted ovarian angiogenesis (increase the expression of CD31 and VEGFA).
Molecular Weight

634.84

Formula

C36H58O9

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1(C)[C@@H](O[C@H]2[C@@H]([C@H]([C@@H]([C@@H](CO)O2)O)O)O)CC[C@]3(C)[C@@]4([H])CC=C5[C@]6([H])CC(C)(C)CC[C@@](C(O)=O)6[C@H](O)C[C@](C)5[C@@](C)4CC[C@@]13[H]

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 (157.52 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 1.5752 mL 7.8760 mL 15.7520 mL
5 mM 0.3150 mL 1.5752 mL 3.1504 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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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 (3.94 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (3.94 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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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: 99.50%

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 (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 1.5752 mL 7.8760 mL 15.7520 mL 39.3800 mL
5 mM 0.3150 mL 1.5752 mL 3.1504 mL 7.8760 mL
10 mM 0.1575 mL 0.7876 mL 1.5752 mL 3.9380 mL
15 mM 0.1050 mL 0.5251 mL 1.0501 mL 2.6253 mL
20 mM 0.0788 mL 0.3938 mL 0.7876 mL 1.9690 mL
25 mM 0.0630 mL 0.3150 mL 0.6301 mL 1.5752 mL
30 mM 0.0525 mL 0.2625 mL 0.5251 mL 1.3127 mL
40 mM 0.0394 mL 0.1969 mL 0.3938 mL 0.9845 mL
50 mM 0.0315 mL 0.1575 mL 0.3150 mL 0.7876 mL
60 mM 0.0263 mL 0.1313 mL 0.2625 mL 0.6563 mL
80 mM 0.0197 mL 0.0984 mL 0.1969 mL 0.4922 mL
100 mM 0.0158 mL 0.0788 mL 0.1575 mL 0.3938 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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Ecliptasaponin A
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