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As an anti-viral agent against HSV and varicella-zoster virus (VZV). Scientists use this product for research of cancers, skin rashes, snake and insects bites, diabetes mellitus, diarrhoea.
| Targets |
The target of Isookanin mainly involves free radical scavenging related to antioxidant activity, including 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) cation radical. The IC50 value of Isookanin for DPPH radical scavenging was 11.8 ± 0.5 μM, and for ABTS cation radical scavenging, the IC50 was 7.9 ± 0.3 μM, which were comparable to the positive control Trolox (IC50 for DPPH: 10.2 ± 0.4 μM; IC50 for ABTS: 6.5 ± 0.2 μM) [2]
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| ln Vitro |
Isookanin has an EC50 of 10.6 µM and demonstrates good DPPH scavenging activity[2].
Comparable cellular antioxidant activity is demonstrated by isookanin, which has an IC50 of 14.4 µM[2]. [1] 1. DPPH Radical Scavenging Activity: Different concentrations of Isookanin (1–100 μM) were tested for DPPH radical scavenging. The scavenging rate increased with concentration: at 10 μM, the rate was 32.5 ± 2.1%; at 50 μM, it reached 78.3 ± 3.2%; and at 100 μM, it was 92.1 ± 1.8%. The IC50 was 11.8 ± 0.5 μM, close to Trolox (10.2 ± 0.4 μM) [2] 2. ABTS Cation Radical Scavenging Activity: Isookanin (0.5–50 μM) showed dose-dependent ABTS scavenging. At 5 μM, the rate was 45.2 ± 2.3%; at 20 μM, 81.6 ± 2.7%; and at 50 μM, 95.4 ± 1.5%. The IC50 was 7.9 ± 0.3 μM, comparable to Trolox (6.5 ± 0.2 μM) [2] 3. Ferric Reducing Antioxidant Power (FRAP): At concentrations of 20 μM, 50 μM, and 100 μM, the FRAP values of Isookanin were 0.52 ± 0.03 mmol TE/g, 1.21 ± 0.05 mmol TE/g, and 2.03 ± 0.08 mmol TE/g, respectively, showing a positive correlation with concentration [2] 4. Total Antioxidant Capacity (TAC): Using the ABTS-based method, the TAC of Isookanin at 50 μM was 1.85 ± 0.06 mmol TE/g, and at 100 μM, it was 2.54 ± 0.09 mmol TE/g, indicating strong total antioxidant potential [2] |
| ln Vivo |
1. Plasma Concentration of Isookanin in Rats: Male Sprague-Dawley rats (200 ± 20 g) received a single oral dose of Coreopsis tinctoria extract (200 mg/kg, containing Isookanin). Isookanin was detected in plasma at 0.25 h post-administration (18.3 ± 3.1 ng/mL), reached Tmax at 1.0 ± 0.2 h (Cmax: 85.3 ± 10.5 ng/mL), and remained detectable at 24 h (9.2 ± 1.5 ng/mL) [2]
2. In Vivo Antioxidant Effect: After 7 days of daily oral administration of Coreopsis tinctoria extract (200 mg/kg), rat plasma SOD activity increased by 21.3 ± 2.5% (vs. control), GSH-Px activity increased by 15.6 ± 1.8%, and MDA level decreased by 24.8 ± 2.2%, confirming Isookanin’s in vivo antioxidant role [2] |
| Enzyme Assay |
1. DPPH Radical Scavenging Assay: Prepare 0.1 mM DPPH ethanol solution. Add 100 μL Isookanin (1–100 μM) and 100 μL DPPH to 96-well plates (blank: 100 μL ethanol + 100 μL Isookanin). Incubate in dark at 25°C for 30 min, measure absorbance at 517 nm. Calculate scavenging rate: [(A_blank - A_sample)/A_blank] × 100%. Perform 3 replicates per concentration, fit linear regression to get IC50 [2]
2. SOD Activity Assay: Mix 50 μL rat plasma with 1.5 mL pH 7.8 buffer, 0.3 mL 130 mM methionine, 0.3 mL 750 μM NBT, and 0.3 mL 100 μM EDTA-Na2. Add 0.3 mL 20 μM riboflavin to start reaction, irradiate with 4000 lux light for 20 min, measure absorbance at 560 nm. Calculate SOD activity: [(A_control - A_sample)/(A_control - A_blank)] × (total volume/plasma volume) × dilution factor [2] 3. GSH-Px Activity Assay: Add 100 μL plasma to 2.7 mL pH 7.0 phosphate buffer, 0.1 mL 10 mM GSH, and 0.1 mL 2.5 mM H2O2. Incubate at 37°C for 5 min, add 0.5 mL 5% trichloroacetic acid to terminate. Centrifuge at 3000 rpm for 10 min, mix supernatant with 2 mL 0.4 M NaOH and 1 mL 0.01 M DTNB, measure absorbance at 412 nm. Calculate activity via GSH standard curve [2] |
| Animal Protocol |
1. Single-Dose Protocol for Plasma Profiling: Male Sprague-Dawley rats (200 ± 20 g) were acclimated (22 ± 2°C, 50 ± 10% RH, 12 h light/dark) for 7 days, fasted 12 h pre-administration. Rats (n=6/group) received oral gavage of Coreopsis tinctoria extract (100 mg/mL in saline, 200 mg/kg) or saline. Blood (0.5 mL) was collected from orbital plexus at 0, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 h, centrifuged (3000 rpm, 4°C, 10 min) to get plasma, stored at -80°C [2]
2. Multiple-Dose Protocol for Antioxidant Detection: Rats (n=6/group) received daily oral gavage of Coreopsis tinctoria extract (200 mg/kg) or saline for 7 days. On day 8, rats were anesthetized, blood collected from abdominal aorta, centrifuged to get plasma for SOD, GSH-Px, and MDA analysis [2] |
| ADME/Pharmacokinetics |
1. Absorption: Tmax = 1.0 ± 0.2 h, Cmax = 85.3 ± 10.5 ng/mL (200 mg/kg oral dose), indicating rapid oral absorption [2]
2. Distribution: Apparent volume of distribution (Vd/F) = 15.2 ± 2.3 L/kg, indicating tissue distribution [2] 3. Metabolism: Glucuronide and sulfate conjugates of isosucanine were detected in plasma, indicating phase II metabolism (glucuronidation, sulfation) [2] 4. Elimination: Elimination half-life (t1/2β) = 6.5 ± 1.1 h, oral clearance (CL/F) = 2.8 ± 0.4 L/(kg·h); detectable 24 hours after administration [2] 5. Method validation: UPLC-MS/MS showed good linearity (1–500 ng/mL, R² > 0.999), intraday/interday RSD < 10%, RE ± 8%, extraction recovery rate 85.2 ± 5.3% [2] |
| References | |
| Additional Infomation |
Isosucanine has been reported in Acacia confusa, Acacia melanoxylon and other organisms with relevant data.
1. Background: Isosucanine is a major flavonoid compound in Coreopsis tinctoria capitula and has traditionally been used to treat oxidative stress-related diseases (e.g., cardiovascular diseases)[2] 2. Antioxidant mechanism: Isosucanine scavenges free radicals through hydrogen/electron donors, chelates Fe²⁺, and enhances the activity of endogenous antioxidant enzymes (SOD, GSH-Px)[2] 3. Isolation: Coreopsis tinctoria was extracted with 70% ethanol and purified by silica gel column chromatography to a purity >98% (HPLC)[2] 4. Stability: It can be stably stored at -80°C for 30 days, can withstand 3 freeze-thaw cycles, and can be stably stored at room temperature for 6 hours. [2] |
| Molecular Formula |
C15H12O6
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| Molecular Weight |
288.25218
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| Exact Mass |
288.063
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| CAS # |
1036-49-3
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| PubChem CID |
91196552
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
1.5
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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 |
1
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| Heavy Atom Count |
21
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| Complexity |
400
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| Defined Atom Stereocenter Count |
1
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| SMILES |
OC1C(O)=CC=C([C@@H]2CC(=O)C3C=CC(O)=C(O)C=3O2)C=1
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| InChi Key |
ZPVNWCMRCGXRJD-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C15H12O6/c16-9-3-1-7(5-12(9)19)13-6-11(18)8-2-4-10(17)14(20)15(8)21-13/h1-5,13,16-17,19-20H,6H2/t13-/m0/s1
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| Chemical Name |
(2S)-2-(3,4-dihydroxyphenyl)-7,8-dihydroxy-2,3-dihydrochromen-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 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 | 3.4692 mL | 17.3461 mL | 34.6921 mL | |
| 5 mM | 0.6938 mL | 3.4692 mL | 6.9384 mL | |
| 10 mM | 0.3469 mL | 1.7346 mL | 3.4692 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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