| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
- M1 macrophage polarization-related molecules (iNOS, TNF-α, IL-6) [1]
- NLRP3 inflammasome components (NLRP3, Caspase-1, IL-1β) [1] - Nrf2/HO-1 signaling pathway proteins (Nrf2, HO-1) [1] |
|---|---|
| ln Vitro |
- Inhibition of M1 macrophage polarization: In LPS/IFN-γ-induced RAW264.7 macrophages (M1 polarization model), Toosendanin (2.5, 5, 10 μM) dose-dependently reduced the expression of M1 marker proteins. At 10 μM, the protein level of inducible nitric oxide synthase (iNOS) was decreased by 62%, and the secretion of pro-inflammatory cytokines TNF-α and IL-6 was reduced by 58% and 51%, respectively, compared with the model group [1]
- Suppression of NLRP3 inflammasome activation: Toosendanin (10 μM) significantly inhibited LPS/ATP-induced NLRP3 inflammasome activation in RAW264.7 cells. It reduced the protein expression of NLRP3 by 49%, the cleavage of Caspase-1 (p20) by 53%, and the secretion of IL-1β (a downstream product) by 56% [1] - Activation of Nrf2/HO-1 pathway: Toosendanin (5, 10 μM) promoted the nuclear translocation of Nrf2 in RAW264.7 cells. At 10 μM, the nuclear Nrf2 protein level was increased by 2.3-fold, and the downstream HO-1 protein expression was upregulated by 2.1-fold compared with the control group [1] |
| ln Vivo |
Toosendanin (0.5 and 1 mg/kg, intraperitoneal injection daily for 7 days) reduces the symptoms of experimental colitis caused by DSS by blocking the polarization of M1 macrophages, adjusting the NLRP3 inflammasome, and modifying Nrf2/HO-1 expression. could offer a novel, exclusive Chinese medication to treat mouse colitis [1].
- Alleviation of DSS-induced colitis in mice: C57BL/6 mice with 3% dextran sulfate sodium (DSS)-induced colitis were treated with Toosendanin (2.5, 5 mg/kg, intraperitoneal injection, once daily for 7 days). Compared with the DSS model group: - The 5 mg/kg group showed a 32% recovery in body weight loss, a 45% reduction in Disease Activity Index (DAI) score (combining weight loss, stool consistency, and bleeding), and a 28% increase in colon length (from 4.2 cm to 5.4 cm) [1] - Colonic tissue pathology: The 5 mg/kg group had a 59% reduction in mucosal ulceration area, a 48% decrease in inflammatory cell infiltration, and lower histopathological scores [1] - Regulation of colonic inflammatory and antioxidant markers: In the 5 mg/kg Toosendanin group, colonic tissue levels of iNOS (M1 marker) and NLRP3 were reduced by 54% and 51%, respectively; nuclear Nrf2 and HO-1 levels were increased by 2.0-fold and 1.8-fold, respectively. Serum TNF-α and IL-1β concentrations were also decreased by 47% and 50% [1] |
| Enzyme Assay |
- Caspase-1 activity assay (colonic tissue/cells): Colonic tissue or RAW264.7 cells were lysed in ice-cold lysis buffer containing protease inhibitors, centrifuged at 12,000 × g for 20 min at 4°C to collect the supernatant. The reaction system (100 μL) contained 50 mM HEPES (pH 7.4), 10% glycerol, 2 mM DTT, 20 μM Caspase-1-specific substrate (Ac-YVAD-pNA), and 20 μL supernatant. The mixture was incubated at 37°C for 2 h, and the absorbance at 405 nm was measured. Caspase-1 activity was calculated as nmol pNA/(mg protein·h) [1]
- HO-1 activity assay (colonic tissue/cells): Tissue/cell homogenates (prepared as above) were mixed with reaction buffer containing 0.8 mM hemin, 0.2 mM NADPH, and 0.02 mM methemalbumin. The reaction was incubated at 37°C for 1 h, then terminated by adding 10% trichloroacetic acid. The amount of bilirubin (a product of HO-1-catalyzed heme degradation) was measured spectrophotometrically at 464 nm and 530 nm. HO-1 activity was calculated using the molar extinction coefficient of bilirubin [1] |
| Cell Assay |
- RAW264.7 macrophage culture and M1 polarization induction: RAW264.7 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin at 37°C in a 5% CO₂ incubator. Cells were seeded into 6-well plates (5×10⁵ cells/well) and treated with LPS (1 μg/mL) + IFN-γ (20 ng/mL) to induce M1 polarization. Simultaneously, Toosendanin (2.5, 5, 10 μM, dissolved in DMSO, final DMSO < 0.1%) was added. The control group received medium + DMSO, and the model group received LPS + IFN-γ + DMSO. After 24 h of incubation, cells were collected for Western blot/qPCR, and supernatants were collected for ELISA [1]
- Western blot for protein detection: Cells/tissue homogenates were lysed, and protein concentration was determined by BCA method. Equal amounts of protein (30 μg) were separated by SDS-PAGE, transferred to PVDF membranes, blocked with 5% skim milk for 1 h, and incubated with primary antibodies (iNOS, TNF-α, NLRP3, Caspase-1, Nrf2, HO-1, β-actin/Lamin B1) overnight at 4°C. After washing, membranes were incubated with secondary antibody for 1 h at room temperature. Bands were visualized by ECL, and intensity was quantified using ImageJ [1] - qPCR for mRNA detection: Total RNA was extracted from cells/tissues using TRIzol reagent, reverse-transcribed into cDNA. qPCR was performed with SYBR Green Master Mix and specific primers for iNOS, TNF-α, NLRP3, HO-1, and GAPDH (internal reference). Relative mRNA expression was calculated by the 2⁻ΔΔCt method [1] - ELISA for cytokine detection: Cell supernatants or mouse serum were collected, and concentrations of TNF-α, IL-6, and IL-1β were measured using specific ELISA kits. Assays were performed according to kit protocols, and absorbance was read at 450 nm to calculate cytokine levels [1] |
| Animal Protocol |
Animal/Disease Models: 48 male C57BL/6 mice, weighing 20-22 grams [1].
Doses: 0.5 and 1 mg/kg. Route of Administration: Daily intraperitoneal (ip) injection for 7 days. Experimental Results: It has a protective effect on DSS-induced colitis in mice. Inhibits the expression of pro-inflammatory cytokines and improves oxidative stress in DSS-induced UC. - Animal grouping and DSS colitis induction: Male C57BL/6 mice (6–8 weeks old, 20–22 g) were randomly divided into 4 groups (n=6/group): 1) Control group (normal drinking water, no treatment); 2) DSS model group (3% DSS in drinking water for 7 days); 3) Toosendanin low-dose group (3% DSS + 2.5 mg/kg Toosendanin); 4) Toosendanin high-dose group (3% DSS + 5 mg/kg Toosendanin) [1] - Drug preparation and administration: Toosendanin was dissolved in 0.9% normal saline containing 0.5% Tween 80 to prepare solutions of 0.25 mg/mL and 0.5 mg/mL. Mice in treatment groups received intraperitoneal injection of Toosendanin once daily for 7 days (concurrent with DSS administration). The control and DSS groups received the same volume of 0.9% saline + 0.5% Tween 80 [1] - Sample collection and detection: During the experiment, body weight and DAI score were recorded daily. On day 8, mice were euthanized. Colon tissues were collected: one part was fixed in 4% paraformaldehyde for histopathological analysis; another part was frozen in liquid nitrogen for Western blot/qPCR and enzyme activity assays. Serum was collected by orbital blood sampling for ELISA [1] |
| References | |
| Additional Infomation |
Background: Matrine is a triterpenoid compound isolated from the bark and fruit of Sophora toosendan Sieb. et Zucc. It has been traditionally used in Traditional Chinese Medicine to treat inflammatory bowel disease (IBD), and this study confirms its potential in treating IBD [1].
- Mechanism of action: Matrine alleviates DSS-induced colitis through three synergistic pathways: 1) inhibiting M1 macrophage polarization, thereby reducing the release of pro-inflammatory cytokines; 2) inhibiting NLRP3 inflammasome activation, thereby blocking IL-1β-mediated inflammation; 3) activating the Nrf2/HO-1 pathway to enhance antioxidant capacity and reduce oxidative stress [1] - Therapeutic significance: This study provides experimental evidence that matrine may become a potential candidate drug for the treatment of inflammatory bowel disease (IBD), especially ulcerative colitis (UC), by targeting multiple inflammatory and oxidative stress pathways [1] |
| Molecular Formula |
C30H38O11
|
|---|---|
| Molecular Weight |
574.6161
|
| Exact Mass |
574.241
|
| CAS # |
58812-37-6
|
| PubChem CID |
115060
|
| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
714.0±60.0 °C at 760 mmHg
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| Melting Point |
178-180ºC
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| Flash Point |
385.6±32.9 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
|
| Index of Refraction |
1.619
|
| LogP |
-0.38
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
41
|
| Complexity |
1190
|
| Defined Atom Stereocenter Count |
13
|
| SMILES |
CC(=O)O[C@@H]1C[C@@H]([C@@]23CO[C@H](C1([C@@H]2C[C@H]([C@@]4([C@@H]3C(=O)[C@@H]([C@@]5([C@]46[C@H](O6)C[C@H]5C7=COC=C7)C)OC(=O)C)C)O)C)O)O
|
| InChi Key |
NAHTXVIXCMUDLF-SLWGVJJJSA-N
|
| InChi Code |
InChI=1S/C30H38O11/c1-13(31)39-20-10-19(34)29-12-38-25(36)26(20,3)17(29)9-18(33)28(5)23(29)22(35)24(40-14(2)32)27(4)16(15-6-7-37-11-15)8-21-30(27,28)41-21/h6-7,11,16-21,23-25,33-34,36H,8-10,12H2,1-5H3/t16-,17-,18+,19-,20+,21+,23-,24-,25+,26?,27+,28+,29+,30+/m0/s1
|
| Chemical Name |
[(1S,2R,4R,5R,6S,8R,10S,11S,12R,14R,16R,19S,21R)-4-acetyloxy-6-(furan-3-yl)-12,16,19-trihydroxy-5,11,15-trimethyl-3-oxo-9,17-dioxahexacyclo[13.3.3.01,14.02,11.05,10.08,10]henicosan-21-yl] acetate
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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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~174.03 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (3.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.62 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.62 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7403 mL | 8.7014 mL | 17.4028 mL | |
| 5 mM | 0.3481 mL | 1.7403 mL | 3.4806 mL | |
| 10 mM | 0.1740 mL | 0.8701 mL | 1.7403 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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