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| Targets |
Signal transducer and activator of transcription 1 (STAT1), Signal transducer and activator of transcription 3 (STAT3) [1]
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| ln Vitro |
- Treatment of mouse splenocytes with Kurarinone (5, 10, 20 μM) dose-dependently inhibited Th1 cell differentiation, as evidenced by reduced frequency of IFN-γ-producing CD4⁺ T cells and decreased IFN-γ secretion (detected by ELISA) [1]
- Kurarinone (5, 10, 20 μM) dose-dependently suppressed Th17 cell differentiation, resulting in decreased frequency of IL-17A-producing CD4⁺ T cells and reduced IL-17A secretion (detected by ELISA) [1] - Western blot analysis showed that Kurarinone (10, 20 μM) inhibited phosphorylation of STAT1 and STAT3 in anti-CD3/anti-CD28-stimulated splenocytes without affecting total STAT1/STAT3 protein levels [1] - Quantitative real-time PCR (qPCR) results indicated that Kurarinone (10, 20 μM) downregulated the mRNA expression of T-bet (Th1-specific transcription factor) and RORγt (Th17-specific transcription factor) in stimulated splenocytes [1] - Kurarinone did not affect the viability of splenocytes at concentrations up to 20 μM (detected by CCK-8 assay) [1] |
| ln Vivo |
- In MOG35-55-induced experimental autoimmune encephalomyelitis (EAE) mice, intraperitoneal administration of Kurarinone (20 mg/kg) significantly reduced the clinical scores of EAE from day 10 to day 25 post-immunization compared with the vehicle control group [1]
- Histopathological analysis of spinal cords from EAE mice showed that Kurarinone (20 mg/kg) treatment decreased the infiltration of inflammatory cells (including CD4⁺ T cells, macrophages) and reduced demyelination [1] - ELISA results revealed that Kurarinone (20 mg/kg) reduced the levels of IFN-γ and IL-17A in the spinal cord homogenates and serum of EAE mice [1] - qPCR analysis indicated that Kurarinone (20 mg/kg) downregulated the mRNA expression of T-bet, RORγt, IFN-γ, and IL-17A in the spinal cords of EAE mice [1] - Western blot analysis showed that Kurarinone (20 mg/kg) inhibited phosphorylation of STAT1 and STAT3 in the spinal cords of EAE mice [1] |
| Cell Assay |
- Splenocytes were isolated from C57BL/6 mice and cultured in complete RPMI 1640 medium. For Th1 cell differentiation, splenocytes were stimulated with anti-CD3 (2 μg/mL) and anti-CD28 (1 μg/mL) antibodies, plus IL-12 (10 ng/mL) and anti-IL-4 (10 μg/mL) antibodies, and treated with Kurarinone (5, 10, 20 μM) or vehicle for 72 hours. The frequency of IFN-γ⁺ CD4⁺ T cells was detected by flow cytometry, and IFN-γ secretion was measured by ELISA [1]
- For Th17 cell differentiation, splenocytes were stimulated with anti-CD3 (2 μg/mL) and anti-CD28 (1 μg/mL) antibodies, plus TGF-β (2 ng/mL), IL-6 (20 ng/mL), IL-1β (10 ng/mL), and TNF-α (10 ng/mL), and treated with Kurarinone (5, 10, 20 μM) or vehicle for 72 hours. The frequency of IL-17A⁺ CD4⁺ T cells was detected by flow cytometry, and IL-17A secretion was measured by ELISA [1] - For Western blot analysis, anti-CD3/anti-CD28-stimulated splenocytes were treated with Kurarinone (10, 20 μM) or vehicle for 30 minutes. Cells were lysed, and proteins were separated by SDS-PAGE, transferred to membranes, and probed with antibodies against p-STAT1, STAT1, p-STAT3, STAT3, and β-actin. Bands were visualized and quantified [1] - For qPCR analysis, anti-CD3/anti-CD28-stimulated splenocytes were treated with Kurarinone (10, 20 μM) or vehicle for 24 hours. Total RNA was extracted, reverse-transcribed to cDNA, and qPCR was performed to detect the mRNA expression of T-bet, RORγt, IFN-γ, and IL-17A using specific primers. GAPDH was used as an internal control [1] - Splenocyte viability was assessed by CCK-8 assay. Splenocytes were cultured with Kurarinone (0-20 μM) for 72 hours, then CCK-8 reagent was added, and absorbance at 450 nm was measured [1] |
| Animal Protocol |
- Female C57BL/6 mice (6-8 weeks old) were used to establish the EAE model. Mice were immunized subcutaneously with 200 μg MOG35-55 peptide emulsified in complete Freund's adjuvant (CFA) containing heat-killed Mycobacterium tuberculosis. On the day of immunization and 48 hours later, mice were intraperitoneally injected with 200 ng pertussis toxin [1]
- Mice were randomly divided into vehicle group and Kurarinone treatment group (n=8 per group). Kurarinone was dissolved in DMSO and then diluted with normal saline (final DMSO concentration ≤ 0.1%). The treatment group received intraperitoneal injection of Kurarinone at 20 mg/kg, and the vehicle group received the same volume of vehicle. Administration was initiated on day 3 post-immunization and repeated every 2 days for a total of 5 injections [1] - Clinical scores of EAE mice were evaluated daily from day 7 post-immunization according to a 0-5 scoring system (0 = no symptoms; 1 = tail weakness; 2 = hind limb weakness; 3 = hind limb paralysis; 4 = forelimb weakness; 5 = moribund or death) [1] - On day 25 post-immunization, mice were sacrificed. Spinal cords were collected for histopathological analysis, Western blot, and qPCR. Serum was collected for ELISA detection of cytokine levels [1] |
| Toxicity/Toxicokinetics |
In vivo experiments showed that intraperitoneal injection of matrine (20 mg/kg) did not cause significant weight loss or behavioral abnormalities in EAE mice, indicating no significant acute toxicity at the test dose [1].
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| References | |
| Additional Infomation |
(2S)-(-)-Matrine is a trihydroxyflavanone with the structure (2S)-flavanone substituted with hydroxyl groups at positions 7, 2', and 4', substituted with lavenderyl at position 8, and substituted with methoxy at position 5. It was isolated from the roots of Sophora flavescens and exhibits cytotoxicity against human myeloid leukemia HL-60 cells. It is both a metabolite and an antitumor drug. It is a trihydroxyflavanone, a monomethoxyflavanone, belonging to the 4'-hydroxyflavanone class of compounds. Its function is related to (2S)-flavanones. 7,2',4'-Trihydroxy-8-lavenderyl-5-methoxyflavanone has been reported in Gentiana macrophylla, Robinia pseudoacacia, and other organisms with relevant data. Matrine is a flavonoid compound. Its mechanism of inhibiting EAE progression is related to inhibiting the phosphorylation of STAT1 and STAT3, thereby inhibiting the differentiation and proliferation of Th1 and Th17 cells, and subsequently downregulating the expression of Th1/Th17 specific transcription factors (T-bet, RORγt) and cytokines (IFN-γ, IL-17A) [1]. EAE is a classic animal model of multiple sclerosis, suggesting that matrine may have potential value in treating multiple sclerosis [1].
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| Molecular Formula |
C26H30O6
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|---|---|
| Molecular Weight |
438.513
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| Exact Mass |
438.204
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| CAS # |
34981-26-5
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| PubChem CID |
11982640
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
651.4±55.0 °C at 760 mmHg
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| Melting Point |
117-119℃
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| Flash Point |
219.0±25.0 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.597
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| LogP |
6.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
698
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(=CC[C@H](CC1=C2C(=C(C=C1O)OC)C(=O)C[C@@H](C3=C(C=C(C=C3)O)O)O2)C(=C)C)C
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| InChi Key |
LTTQKYMNTNISSZ-MWTRTKDXSA-N
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| InChi Code |
InChI=1S/C26H30O6/c1-14(2)6-7-16(15(3)4)10-19-21(29)12-24(31-5)25-22(30)13-23(32-26(19)25)18-9-8-17(27)11-20(18)28/h6,8-9,11-12,16,23,27-29H,3,7,10,13H2,1-2,4-5H3/t16-,23+/m1/s1
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| Chemical Name |
(2S)-2-(2,4-dihydroxyphenyl)-7-hydroxy-5-methoxy-8-[(2R)-5-methyl-2-prop-1-en-2-ylhex-4-enyl]-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) |
DMSO : ~50 mg/mL (~114.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.70 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (5.70 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 25.0 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 | 2.2804 mL | 11.4022 mL | 22.8045 mL | |
| 5 mM | 0.4561 mL | 2.2804 mL | 4.5609 mL | |
| 10 mM | 0.2280 mL | 1.1402 mL | 2.2804 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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