| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Kayaflavone exhibits inhibitory activity against the aggregation and cytotoxicity of amyloid-beta42 (Abeta42), a peptide that forms the senile plaques characteristic of Alzheimer's disease (AD) [18L6-L7, L10-L11]. By inhibiting Abeta42-induced cytotoxicity, it protects neuronal cells from this key pathological insult. Additionally, through several biological mechanisms, including modulation of enzyme activity and antioxidative effects, it has been identified to interact with cellular signaling pathways, potentially leading to anti-inflammatory and anticancer effects [18L26-L30].
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| ln Vitro |
Kayaflavone demonstrates potent in vitro inhibitory activity against amyloid-beta42 (Abeta42) cytotoxicity in PC-12 (rat adrenal pheochromocytoma) neuronal cells, with an EC50 value of 5.29 microM [18L6-L7, L10-L11, L22-L24]. This means that at this concentration, it protects 50% of the cells from death induced by the Abeta42 peptide. It also displays notable antioxidant, anti-inflammatory, and potential anticancer properties, making it a promising multi-functional compound for studying neurodegenerative diseases [18L17-L19].
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| ln Vivo |
Specific in vivo data for Kayaflavone is not provided in the search results. However, its promising in vitro neuroprotective activity against Abeta42 toxicity suggests that it could have beneficial effects in animal models of Alzheimer‘s disease, such as APP/PS1 transgenic mice. Oral or intraperitoneal administration of Kayaflavone might be expected to reduce amyloid plaque burden, lower neuroinflammation, and improve cognitive performance in behavioral tests. Its antioxidant and anti-inflammatory activities would likely contribute to its in vivo efficacy.
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| Enzyme Assay |
Specific enzyme/receptor binding assays are not provided. The primary in vitro activity is neuroprotection against Abeta42 cytotoxicity. Procedure: PC-12 cells are seeded in collagen-coated 96-well plates at a density of 1×10^4 cells/well in DMEM with 10% FBS. After 24 hours, the medium is replaced with fresh medium containing 50 ng/mL NGF for 24-48 hours to differentiate the cells into a neuron-like phenotype. The differentiated cells are pre-treated with varying concentrations of Kayaflavone (e.g., 0.01, 0.1, 1, 5, 10, 50 microM) for 2 hours. Amyloid-beta42 (Abeta42, 20 microM) is then added to induce toxicity. After 48 hours, cell viability is measured using the MTT assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide). The EC50 for protection against Abeta42 cytotoxicity is calculated.
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| Cell Assay |
The neuroprotective mechanism can be assessed in PC-12 cells by measuring oxidative stress markers. Procedure: PC-12 cells are treated as described above. After 24-48 hours of Abeta42 exposure, cells are harvested, and the level of reactive oxygen species (ROS) is measured using a fluorescent dye (e.g., DCFH-DA, dichlorodihydrofluorescein diacetate). The fluorescence intensity is measured (excitation 485 nm, emission 530 nm). Additionally, the activities of antioxidant enzymes (superoxide dismutase - SOD, catalase - CAT, glutathione peroxidase - GPx) and the level of lipid peroxidation (malondialdehyde - MDA) can be measured in cell lysates using commercial kits to evaluate the antioxidant activity of Kayaflavone.
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| Animal Protocol |
In vivo efficacy can be evaluated in a transgenic mouse model of Alzheimer‘s disease (e.g., APP/PS1 mice). Procedure: 6-month-old APP/PS1 mice are randomized into treatment groups (n=10 per group). Kayaflavone is administered orally or intraperitoneally daily at doses of 10-50 mg/kg for 2-3 months. After treatment, cognitive function is assessed using the Morris water maze test and the Y-maze test. At study endpoint, mice are euthanized, and brain tissue (hippocampus and cortex) is collected. Brain sections are stained with Thioflavin S or an anti-Abeta antibody to measure amyloid plaque burden. Levels of Abeta42 and pro-inflammatory cytokines (TNF-alpha, IL-1beta, IL-6) are quantified by ELISA. Antioxidant enzyme activities are measured in brain homogenates.
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| ADME/Pharmacokinetics |
Specific PK data for Kayaflavone is not available. As a natural biflavonoid with a relatively high molecular weight (580.54 g/mol), it is likely to have poor oral bioavailability due to low aqueous solubility, extensive first-pass metabolism by phase II conjugation (glucuronidation, sulfation), and potentially poor permeability (LogP and LogD not reported). If active in vivo, it may require high doses, alternative routes of administration (e.g., intraperitoneal), or formulation into nanoparticles to achieve sufficient brain exposure.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Kayaflavone is not available in the search results. Flavonoids and biflavonoids are generally considered to have a low toxicity profile when consumed in the diet. However, isolated compounds administered at high doses may produce toxicity. Potential concerns could include hepatotoxicity (liver damage) at high doses, drug-drug interactions via inhibition or induction of cytochrome P450 enzymes (e.g., CYP3A4), and effects on thyroid function. Comprehensive toxicological studies are required.
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| References | |
| Additional Infomation |
According to reports, flavonoids are found in African palm (Afrocarpus gracilior), Norfolk pine (Araucaria araucana), and other organisms with available data.
Kayaflavone is a naturally occurring amentoflavone-type biflavonoid isolated from various coniferous plants. Amentoflavone itself has a wide range of reported pharmacological activities, including anti-inflammatory, antioxidant, antiviral, and anticancer properties. The specific activity against Abeta42 cytotoxicity makes Kayaflavone a promising lead compound for Alzheimer‘s disease research [18L4-L7, L13-L14, L22-L24]. Its dual activity as both a direct Abeta42 aggregation inhibitor and an antioxidant suggests it may act through multiple mechanisms to slow down the progression of AD. The compound is for research use only and is not approved for human clinical use. Kayaflavone is also known as Amentoflavone 4‘,4'‘',7‘'-trimethyl ether [18L25]. Its chemical formula is C33H24O10, and purity is typically >98% [18L36, L39]. |
| Molecular Formula |
C33H24O10
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|---|---|
| Molecular Weight |
580.54
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| Exact Mass |
580.137
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| CAS # |
481-45-8
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| PubChem CID |
9894522
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| Appearance |
Typically exists as solids at room temperature
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| LogP |
6.043
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
43
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| Complexity |
1100
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(C2C([H])=C([H])C(=C([H])C=2[H])OC([H])([H])[H])=C([H])C(C2C(=C([H])C(=C(C1=2)C1=C(C([H])=C([H])C(C2=C([H])C(C3=C(C([H])=C(C([H])=C3O2)O[H])O[H])=O)=C1[H])OC([H])([H])[H])OC([H])([H])[H])O[H])=O
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| InChi Key |
RROKRDUARFDCDH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H24O10/c1-39-19-7-4-16(5-8-19)26-14-23(37)32-24(38)15-28(41-3)30(33(32)43-26)20-10-17(6-9-25(20)40-2)27-13-22(36)31-21(35)11-18(34)12-29(31)42-27/h4-15,34-35,38H,1-3H3
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| Chemical Name |
8-[5-(5,7-dihydroxy-4-oxochromen-2-yl)-2-methoxyphenyl]-5-hydroxy-7-methoxy-2-(4-methoxyphenyl)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 |
| 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 Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7225 mL | 8.6127 mL | 17.2253 mL | |
| 5 mM | 0.3445 mL | 1.7225 mL | 3.4451 mL | |
| 10 mM | 0.1723 mL | 0.8613 mL | 1.7225 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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