| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| ln Vitro |
In an AhR-based bioassay (Ah-Immunoassay), Brevifolincarboxylic acid showed a marked, dose-dependent inhibitory effect on the activation of the aryl hydrocarbon receptor (AhR) induced by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). The concentration producing AhR activity equal to 70% of the maximal response to TCDD in controls (EC70) was determined to be 3.9 μM.[2]
Brevifolincarboxylic acid was isolated from the n-butanol extract of Potentilla kleiniana Wight et Arn and identified as an α-glucosidase inhibitor through ultrafiltration HPLC-MS screening and subsequent activity validation. In an in vitro α-glucosidase inhibition assay, brevifolincarboxylic acid exhibited an IC50 value of 323.46 ± 8.08 μM, indicating inhibitory activity against the enzyme. Its activity was stronger than that of the reference compound acarbose (IC50 = 332.12 ± 5.52 μM). The study also noted that the esterified form of brevifolincarboxylic acid (ethyl brevifolincarboxylate) showed reduced activity (IC50 = 841.75 ± 12.63 μM), suggesting that esterification may diminish α-glucosidase inhibitory potency.[3] |
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| Enzyme Assay |
An AhR-based bioassay, the Ah-Immunoassay, was used to evaluate the inhibitory effect of vegetable constituents on TCDD-induced AhR activation. The assay uses cytosol containing AhR extracted from mammalian liver cells. Briefly, cytosol was added to sample solutions (compounds dissolved in DMSO at final concentrations of 0.5–50 μM) or DMSO control, preincubated for 20 minutes, and then incubated with TCDD (final concentration 0.025 nM) for 2 hours at 30°C. The formation of the AhR-TCDD complex was determined using an immunoassay kit, and absorbance was measured. AhR activity was calculated relative to controls, and concentration–response curves were plotted. The EC70 value (concentration producing 70% of maximal TCDD response) was calculated from the linear portion of the dose–response curve near the origin.[2]
An in vitro α-glucosidase inhibition assay was performed to evaluate the activity of the compounds. Briefly, α-glucosidase and the substrate p-nitrophenyl-α-D-glucopyranoside (pNPG) were dissolved in phosphate buffer (pH 6.86). The test sample (at various concentrations), α-glucosidase solution, and buffer were mixed and pre-incubated at 37°C for 10 minutes. The reaction was initiated by adding pNPG solution. After incubation at 37°C for 30 minutes, sodium carbonate solution was added to stop the reaction. The absorbance at 405 nm was measured, and the percentage inhibition of enzyme activity was calculated by comparing the absorbance of the sample to a control (without inhibitor). The half-maximal inhibitory concentration (IC50) was determined from the dose-response curve.[3] |
| References |
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| Additional Infomation |
Bruxine carboxylic acid is an isocoumarin compound.
Bruxine carboxylic acid has been reported to exist in Combretum indicum, Phyllanthus virgatus, and other organisms with relevant data. Bruxine carboxylic acid is a plant component isolated from Phyllanthus flexuosus. Molecular modeling shows that bruxine carboxylic acid, like other inhibitory compounds such as apigenin and resveratrol, has a similar molecular size and planar structure to TCDD, which may explain its potential antagonistic activity against AhR. This study suggests that dietary components with AhR inhibitory activity, such as bruxine carboxylic acid, may play a role in mitigating dioxin toxicity by interfering with the AhR activation pathway, thereby reducing related health risks. [2] |
| Molecular Formula |
C13H8O8
|
|---|---|
| Molecular Weight |
292.1978
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| Exact Mass |
292.021
|
| CAS # |
18490-95-4
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| PubChem CID |
9838995
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| Appearance |
Yellow to brown solid powder
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| Density |
2.0±0.1 g/cm3
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| Boiling Point |
758.5±60.0 °C at 760 mmHg
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| Melting Point |
250 °C
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| Flash Point |
296.2±26.4 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.802
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| LogP |
0.99
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
565
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JFJWMFPFMLRLMI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8O8/c14-5-2-4-7(10(17)9(5)16)8-3(12(18)19)1-6(15)11(8)21-13(4)20/h2-3,14,16-17H,1H2,(H,18,19)
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| Chemical Name |
7,8,9-trihydroxy-3,5-dioxo-1,2-dihydrocyclopenta[c]isochromene-1-carboxylic acid
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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) |
DMSO : ~33.33 mg/mL (~114.07 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (2.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4223 mL | 17.1116 mL | 34.2231 mL | |
| 5 mM | 0.6845 mL | 3.4223 mL | 6.8446 mL | |
| 10 mM | 0.3422 mL | 1.7112 mL | 3.4223 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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