| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Epimedokoreanin B targets cancer cells through endoplasmic reticulum (ER) stress-mediated apoptosis accompanied by autophagosome accumulation. It inhibits the growth of lung cancer cells through this mechanism. The compound also exhibits anti-inflammatory and antibacterial activities. It significantly inhibits the formation of advanced glycation end-products (AGEs), preventing clinical complications of diabetes mellitus. Epimedokoreanin B is a natural flavonoid with multiple biological activities.
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| ln Vitro |
Compound 6, epimedokoreanin B, exhibited noteworthy suppression of lung cancer cell growth (A549, Calu1, and H1299) over a 48-hour period at 3.13–25 μM. Human bronchial epithelial cells BEAS-2B are not harmed by epimedokoreanin B [1]. Treatment with epimedokoreanin B decreased the migration and proliferation of A549 and NCI-H292 cells, which was accompanied with cytoplasmic vacuolation. Epimedokoreanin B-treated cells showed autophagosome accumulation together with autophagic flux obstruction, which is consistent with endoplasmic reticulum stress [2]. In human monocyte-derived macrophages (HMDM), Epimedokoreanin B (5 μM; 24 hours) reduces the production of IL-10, a known M2 marker, and CD163 expression, suggesting that it prevents M2 polarization. STAT3 activity in HMDMs is inhibited by epimedokoreanin B [4].
In vitro, Epimedokoreanin B exhibits anticancer activity in human NSCLC A549 and NCI-H292 cells. It inhibits the growth of lung cancer cells through ER stress-mediated apoptosis accompanied by autophagosome accumulation. The compound inhibits the proliferation of MCF-7 breast cancer cells and HepG2 liver cancer cells in a dose-dependent manner. It also possesses anti-inflammatory and antibacterial activities, with DPPH radical scavenging activity. |
| ln Vivo |
In the LM8 tumor-bearing mouse model, epimedokoreanin B (20 mg/kg; oral; three times per week; for 17 days) suppresses tumor growth [4].
In vivo, Epimedokoreanin B inhibits tumor growth in an LM8 tumor-bearing murine model. It is administered thrice a week for 17 days. These results support its potential as an anticancer agent. The compound's ability to inhibit tumor growth in vivo makes it a valuable tool for studying cancer biology and developing anticancer therapies. However, specific published in vivo protocols are not detailed in the available literature. |
| Enzyme Assay |
The in vitro cytotoxicity assay for Epimedokoreanin B is conducted in cancer cell lines including NSCLC A549, NCI-H292, MCF-7, and HepG2 cells. Cells are treated with varying concentrations of the compound for 48-72 hours. Cell viability is measured using standard assays such as MTT or CellTiter-Glo. Apoptosis is assessed by flow cytometry using Annexin V/PI staining, caspase activity assays, and detection of DNA fragmentation. ER stress is evaluated by Western blotting for ER stress markers such as CHOP, GRP78, and PERK. Autophagy is assessed by LC3-II accumulation.
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| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: A549, Calu1 and H1299 cells Tested Concentrations: 3.13 μM, 6.25 μM, 12.5 μM and 25.0 μM Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated significate inhibitory effect on proliferation against lung cancer cell A549, Calu1 and H1299. Western Blot Analysis[4] Cell Types: Human monocyte-derived macrophages (HMDMs) Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dramatically suppressed IL-10-induced JAK1/STAT3 activation.and H1299. Cellular assays for Epimedokoreanin B are conducted in NSCLC A549, NCI-H292, MCF-7, and HepG2 cell lines. Cells are treated with varying concentrations of the compound for 48-72 hours. Cell viability and proliferation are measured using standard assays. Apoptosis is assessed by flow cytometry, caspase activity, and DNA fragmentation. ER stress is evaluated by Western blotting for ER stress markers. Autophagy is assessed by LC3-II Western blotting and autophagosome visualization. Antibacterial activity is assessed using standard broth microdilution assays. |
| Animal Protocol |
Animal/Disease Models: Female C3H mice (8-10 weeks old) injected with LM8 cells[4]
Doses: 20 mg/kg Route of Administration: Oral administration; thrice a week; for 17 days Experimental Results: Inhibited tumor growth. In vivo studies for Epimedokoreanin B are conducted in an LM8 tumor-bearing murine model. The compound is administered thrice a week for 17 days. Efficacy is assessed by measuring tumor growth inhibition over time. Pharmacodynamic markers such as apoptosis and ER stress are evaluated in tumor tissues. However, specific published in vivo protocols are not detailed in the available literature. The compound is primarily used as a research tool for studying anticancer mechanisms. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Epimedokoreanin B is not extensively reported in publicly available sources. The compound has a molecular weight of 536.57 g/mol and a molecular formula of C₃₀H₃₂O₉. As a flavonoid, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life and bioavailability are not available in the current literature for this research compound. Storage conditions are typically at -20°C.
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| Toxicity/Toxicokinetics |
Toxicity data for Epimedokoreanin B is limited in publicly available sources. In the LM8 tumor-bearing murine model, the compound was administered thrice a week for 17 days. As with all research compounds, Epimedokoreanin B is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays in normal cell lines and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References |
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| Additional Infomation |
Epimedokoreanin B is a commonly used ingredient in traditional herbal medicine.
Epimedokoreanin B (EKB) is an isoprenylated flavonoid isolated from Korean Epimedium. It exhibits anticancer activity in NSCLC A549 and NCI-H292 cells through ER stress-mediated apoptosis accompanied by autophagosome accumulation. It inhibits the proliferation of MCF-7 and HepG2 cells. In vivo, it inhibits tumor growth in an LM8 tumor-bearing murine model. Epimedokoreanin B also possesses anti-inflammatory, antibacterial, and DPPH radical scavenging activities. It has a molecular formula of C₃₀H₃₂O₉ and a molecular weight of 536.57 g/mol. |
| Molecular Formula |
C25H26O6
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|---|---|
| Molecular Weight |
422.47
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| Exact Mass |
422.172
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| CAS # |
161068-53-7
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| PubChem CID |
21147600
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
665.9±55.0 °C at 760 mmHg
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| Flash Point |
228.2±25.0 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.650
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| LogP |
6.59
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
745
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=CCC1=C(C(=CC(=C1)C2=CC(=O)C3=C(C=C(C(=C3O2)CC=C(C)C)O)O)O)O)C
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| InChi Key |
QLZMBCVLWOJASJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H26O6/c1-13(2)5-7-15-9-16(10-21(29)24(15)30)22-12-20(28)23-19(27)11-18(26)17(25(23)31-22)8-6-14(3)4/h5-6,9-12,26-27,29-30H,7-8H2,1-4H3
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| Chemical Name |
2-[3,4-dihydroxy-5-(3-methylbut-2-enyl)phenyl]-5,7-dihydroxy-8-(3-methylbut-2-enyl)chromen-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3670 mL | 11.8352 mL | 23.6703 mL | |
| 5 mM | 0.4734 mL | 2.3670 mL | 4.7341 mL | |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.3670 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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