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| Other Sizes |
| Targets |
STAT3 (Signal Transducer and Activator of Transcription 3); NF-kappaB (Nuclear Factor-kappa B); MMP-9 (Matrix Metalloproteinase-9); p38 MAPK and JNK signaling pathways; iNOS; COX-2. Capillarisin blocks STAT3 activation via induction of SHP-1 and SHP-2 phosphatases and suppresses NF-kappaB-dependent transcriptional activity through p38 MAPK and JNK pathways. It also inhibits pro-inflammatory mediators including iNOS and COX-2 by suppressing LPS-induced ERK, JNK, and NF-kappaB activation.
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| ln Vitro |
There are no notable effects of capillarisin (0~40 μM; 24 hours; SH-SY5Y cells) on the viability of these cells [3]. ..Incubating PI3K/PKB pathway inactivation, capillarisin (40 μM; 24 hours; SH-SY5Y cells) inhibits apoptosis in bupivacaine-challenged SH-SY5Y cells. However, this effect is reversed by LY294002 treatment, which counteracts bupivacaine-induced injury by stimulating the PI3K/PKB pathway[3]. ..In SH-SY5Y cells, capillarisin inhibits oxidative stress caused by bupivacaine by triggering the PI3K/PKB pathway. By triggering the PI3K/PKB pathway, capillarisin prevents endoplasmic reticulum stress and mitochondrial damage brought on by bupivacaine[3].
Capillarisin inhibits the constitutive and inducible STAT3 activation through induction of SHP-1 and SHP-2 tyrosine phosphatases, negatively regulating growth, metastasis, and chemoresistance of tumor cells. It suppresses PMA-induced MMP-9 expression via inhibition of NF-kappaB-dependent transcriptional activity through p38 MAPK and JNK pathways, without affecting MMP-9 enzymatic activity or TIMP-1/-2 expression. Capillarisin also inhibits pro-inflammatory cytokines, iNOS, and COX-2 through suppression of LPS-induced ERK, JNK, and NF-kappaB activation. It has inhibition of in vitro growth of hepatoma cells and protects against t-BHP-induced cytotoxicity in rat primary hepatocytes. |
| ln Vivo |
Strong inhibition of NF-κB mediated genes (iNOS, COX-2) is observed upon pretreatment with capillarisin (20 and 80 mg/kg; ip; 1 hour)[4]. Capillarisin dramatically lowers the plasma resulting to the generation of nitrite. Adenosine 5'-triphosphate (ATP) in plasma and substance P in paw tissue generated by CFA are significantly suppressed by capillarisin[4].
Capillarisin exhibits protective effects on tert-butylhydroperoxide (t-BHP)-induced oxidative damage in rat primary hepatocytes, reducing hepatocyte injury caused by hydrophobic bile acids. It prevents generation of ROS and release of cytochrome c, minimizing hepatocyte apoptosis. Capillarisin has anti-hyperalgesic and anti-allodynic activities via suppression of inflammatory signaling in animal models. It has been shown to exert antiasthmatic activity in neonatal rats via modulating matrix remodeling. In spontaneously hypertensive rats, it may have potential cardiovascular benefits. It also protects SH-SY5Y cells against bupivacaine-induced apoptosis via ROS-mediated PI3K/PKB pathway. |
| Enzyme Assay |
Immunoblotting and reporter assays: Cells are seeded and treated with Capillarisin (concentrations and durations vary). For STAT3 activation studies, cells are stimulated with IL-6 or use constitutive STAT3-active cancer cell lines. Cell lysates are subjected to SDS-PAGE and Western blotting with antibodies against STAT3, p-STAT3 (Tyr705), SHP-1, SHP-2, and downstream targets (survivin, MMP-2, MMP-9). Reporter assays using STAT3-luciferase constructs are used to quantify transcriptional activity. For NF-kappaB studies, p65 nuclear translocation is assessed by immunofluorescence or Western blotting of nuclear fractions. MMP-9 activity can be measured by gelatin zymography. All assays include appropriate positive/negative controls. STAT3 inhibition can be confirmed using selective STAT3 inhibitors as controls.
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: SH-SY5Y cells Tested Concentrations: 0~40 μM Incubation Duration: 24 hrs (hours) Experimental Results: Did not produce any significant changes on the viability of SH-SY5Y cells. Western Blot Analysis[3] Cell Types: SH-SY5Y cells Tested Concentrations: 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced PI3K/PKB pathway inactivation in SH-SY5Y cells. Apoptosis Analysis[3] Cell Types: SH-SY5Y cells Tested Concentrations: 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced inhibition of apoptosis in bupivacaine-challenged SH-SY5Y cells was overturned by LY294002 treatment. For hepatocyte protection studies: Rat primary hepatocytes are isolated and cultured. Cells are pre-incubated with Capillarisin (0.01-1.00 mg/mL) for 2-4 hours, then exposed to t-BHP (0.1-0.5 mM) for 2-4 hours. Cytotoxicity is assessed by LDH release, MTT assay, or trypan blue exclusion. ROS levels are measured using DCFH-DA probe. GSH levels are measured using a commercial assay kit. Cytochrome c release is detected by Western blotting of cytosolic and mitochondrial fractions. Apoptosis is evaluated by caspase-3/7 activity, Annexin V/PI staining, or TUNEL assay. Gene expression of antioxidant enzymes and inflammatory markers can be assessed by qPCR. Each experiment should be performed in triplicate with appropriate controls. |
| Animal Protocol |
Animal/Disease Models: ICR mice[4]
Doses: 20 and 80 mg/kg Route of Administration: Ip; 1 hour Experimental Results: Pretreatment strongly inhibited NF-κB mediated genes (iNOS, COX-2). Animal models: For hepatoprotective studies, rats are treated with Capillarisin (e.g., 10-50 mg/kg, oral or intraperitoneal) for 5-14 days prior to or concurrently with hepatotoxic agent (e.g., CCl4, t-BHP, or bile duct ligation). Blood samples are collected for liver enzyme analysis (ALT, AST, ALP, GGT). Liver tissue is collected for histopathology (H&E staining), oxidative stress biomarkers (MDA, SOD, GSH, catalase), and inflammatory markers (TNF-alpha, IL-6, NF-kappaB). For anti-inflammatory studies, LPS-induced inflammation models are used. Inflammatory markers are measured in serum and tissues. Doses and treatment durations vary depending on the specific model and endpoints. |
| ADME/Pharmacokinetics |
Capillarisin (MW 316.26, formula C1₆H12O₇). Solubility: soluble in DMSO and other organic solvents. For in vivo studies, formulations may include DMSO:PEG300:Tween 80:Saline (10:40:5:45). Storage: Powder at -20degC (stable for 3 years). In solution at -80degC (stable for 1 year). Pharmacokinetic parameters: The compound is likely metabolized by phase I and phase II enzymes. Bioavailability and half-life have not been extensively reported in publicly available literature. LC-MS/MS methods can be used for quantification in biological samples.
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| Toxicity/Toxicokinetics |
Based on its traditional use in herbal medicine, Capillarisin has an acceptable safety profile for research applications at typical doses (10-100 mg/kg in animals). No significant acute toxicity has been reported in available literature. However, comprehensive toxicological studies (including genotoxicity, reproductive toxicity, chronic toxicity) have not been conducted for pure Capillarisin. Standard safety precautions should be taken when handling this compound. It should not be used in humans for therapeutic purposes. Always follow institutional safety guidelines.
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| References |
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| Additional Infomation |
Capillarisin is a coumarin compound. It has been reported that capillary angiotensin exists in Artemisia annua, and relevant data are available for reference.
Capillarisin shows potential as an anti-metastatic agent by suppressing cancer cell invasion through specific inhibition of NF-kappaB-dependent MMP-9 gene expression. It also has hepatoprotective effects by preventing ROS generation and cytochrome c release, thereby minimizing hepatocyte apoptosis. Capillarisin is not a marketed drug and is currently only for research use. Studies suggest it may have therapeutic potential in treating advanced prostate cancer with constitutive STAT3 or IL-6-inducible STAT3 activation. It also shows antiasthmatic activity in neonatal rats via modulating matrix remodeling. Additional research is ongoing to explore its potential in various inflammation-related and liver diseases. |
| Molecular Formula |
C16H12O7
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|---|---|
| Molecular Weight |
316.26
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| Exact Mass |
316.058
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| CAS # |
56365-38-9
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| PubChem CID |
5281342
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
582.6±50.0 °C at 760 mmHg
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| Flash Point |
221.2±23.6 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.695
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| LogP |
2.28
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
469
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C2=C(C=C1O)OC(=CC2=O)OC3=CC=C(C=C3)O)O
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| InChi Key |
NTKNGUAZSFAKEE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12O7/c1-21-16-11(19)6-12-14(15(16)20)10(18)7-13(23-12)22-9-4-2-8(17)3-5-9/h2-7,17,19-20H,1H3
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| Chemical Name |
5,7-dihydroxy-2-(4-hydroxyphenoxy)-6-methoxychromen-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 | 3.1620 mL | 15.8098 mL | 31.6196 mL | |
| 5 mM | 0.6324 mL | 3.1620 mL | 6.3239 mL | |
| 10 mM | 0.3162 mL | 1.5810 mL | 3.1620 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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