| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
Boldine targets multiple signaling pathways. It induces cell cycle arrest and apoptosis in T24 human bladder cancer cells via regulation of ERK, AKT, and GSK-3β. It suppresses osteoclastogenesis and improves bone destruction by down-regulating the OPG/RANKL/RANK signal pathway. Boldine also connects the p65-NF-κB and STAT3 signaling pathways in mice to hydrophobic inflammation. It has properties as a Ca2+ entry blocker and acts at α1-adrenoceptors.
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| ln Vitro |
Human bladder cancers T24 are inhibited from growing by boldine (10-500 μM, 24 h)[2]. By controlling ERK, AKT, and GSK-3β, boldine (200, 400 μM, 24 h) stimulates the T24 human bladder tumor G2/cell viability assay [2].
In vitro, boldine reduces cell viability and cell proliferation in T24 human bladder cancer cells. It induces cell cycle arrest and apoptosis in T24 cells via regulation of ERK, AKT, and GSK-3β. Boldine reduces oxidative stress and improves endothelium-dependent relaxation in aortas of diabetic mice largely through inhibiting ROS overproduction. It suppresses osteoclastogenesis and improves bone destruction by down-regulating the OPG/RANKL/RANK signal pathway. |
| ln Vivo |
Boldine (unobstructed, 50 mg/kg for 7 days) connects the p65-NF-κB and STAT3 signaling pathways in mice to the hydrophobic inflammation caused by Dextran Sulfate Sodium (DSS) [3].
In vivo, boldine (50 mg/kg for 7 days) connects the p65-NF-κB and STAT3 signaling pathways in mice to hydrophobic inflammation caused by Dextran Sulfate Sodium (DSS). It has been studied for its potential therapeutic effects in rheumatoid arthritis. Boldine's anti-inflammatory and antioxidant activities suggest potential applications in inflammatory and oxidative stress-related diseases. Its ability to suppress osteoclastogenesis indicates potential for bone-related disorders. |
| Enzyme Assay |
The in vitro activity of boldine is assessed using various cell-based and biochemical assays. For cell viability studies, T24 human bladder cancer cells are cultured in appropriate media and treated with various concentrations of boldine (typically 1-100 µM) for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by flow cytometry using Annexin V/PI staining. The expression of ERK, AKT, and GSK-3β is analyzed by Western blotting using phospho-specific antibodies. For antioxidant studies, ROS production is measured using DCFH-DA fluorescence.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: T24 and RT4 Tested Concentrations: 10, 50, 100, 200, 300,400, 500 μM Incubation Duration: 24 h Experimental Results: Inhibition of cell growth. Apoptosis analysis [2] Cell Types: T24 Tested Concentrations: 200, 400 μM Incubation Duration: 24 hrs (hours) Experimental Results: Caused G2/M phase arrest, cell death Dramatically increased Western Blot analysis [2] Cell Types: T24 Tested Concentrations: 200, 400 μM Incubation Duration: 1,, 3, 24 h Experimental Results: p-ERK levels diminished after 24 hrs (hours) with 200 μM and 3 hrs (hours) and 24 hrs (hours) with 400 μM. Anti-p-CDC2 antibodies did not show any differences in CDC2 phosphorylation status. GSK-3β phosphorylation diminished after 24 hrs (hours) at a concentration of 400 μM. For cellular assays, T24 human bladder cancer cells, macrophages, or osteoclast precursor cells are cultured in appropriate media. Cells are treated with various concentrations of boldine (typically 1-100 µM) for defined periods. Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by flow cytometry using Annexin V/PI staining or by measuring caspase-3/7 activity. The expression of inflammatory mediators (e.g., NF-κB, STAT3) is analyzed by Western blotting or qPCR. Osteoclastogenesis is assessed by TRAP staining of osteoclast precursor cells treated with RANKL and M-CSF in the presence of boldine. |
| Animal Protocol |
Animal/Disease Models: DSS-induced mouse model
Doses: 50 mg/kg Route of Administration: Oral Experimental Results: Reduce the expression of CD 68+ and the activity of myeloperoxidase (MPO), attenuate pro-inflammatory cytokines and malondialdehyde ( MDA) levels increase enzymatic antioxidant activity and inhibit p65-NF-κB and STAT3 activity. In vivo, boldine is typically administered orally or intraperitoneally to animal models. In the DSS-induced colitis model, boldine is administered at 50 mg/kg for 7 days, and the effects on inflammation are assessed by measuring inflammatory markers, histological analysis of colon tissues, and the expression of p65-NF-κB and STAT3 signaling pathways. In models of rheumatoid arthritis or bone destruction, boldine is administered, and bone erosion is assessed by micro-CT or histomorphometry. |
| ADME/Pharmacokinetics |
Boldine has a molecular weight of 327.37 g/mol and a molecular formula of C19H21NO4. It is soluble in DMSO and ethanol. The compound should be stored as a powder at -20°C under desiccated conditions. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results. The compound's natural product origin and its presence in Boldo leaves suggest it may have a favorable safety profile.
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| Toxicity/Toxicokinetics |
Specific toxicity data for boldine is not available in the provided search results. As a natural alkaloid, it is generally considered to have low toxicity based on its long history of use in traditional medicine. However, comprehensive toxicological studies are required to establish its full safety profile. The compound should be used with standard laboratory safety precautions. Its effects on cell viability and apoptosis suggest that it may have cytotoxic effects at high concentrations.
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| References |
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| Additional Infomation |
Boldine is an apophene alkaloid. It has been reported to exist in Litsea glutinosa, Neolitsea konishii, and other organisms with relevant data. See also: Boldine hydrochloride (its active ingredient); Peumus boldus leaf (its part).
Boldine is a natural alkaloid with diverse pharmacological activities, including anti-cancer, anti-inflammatory, antioxidant, and bone-protective effects. It is the major alkaloid of Boldo (Peumus boldus), a plant used in traditional medicine for digestive and liver disorders. Boldine is not approved as a pharmaceutical drug but is available as a research compound and dietary supplement ingredient. Its multiple mechanisms of action make it a compound of significant research interest. |
| Molecular Formula |
C19H21NO4
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|---|---|
| Molecular Weight |
327.3743
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| Exact Mass |
327.147
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| CAS # |
476-70-0
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| PubChem CID |
10154
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
529.3±50.0 °C at 760 mmHg
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| Melting Point |
162-164ºC
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| Flash Point |
273.9±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.639
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| LogP |
2.32
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
461
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1CCC2=CC(=C(C3=C2[C@@H]1CC4=CC(=C(C=C43)OC)O)OC)O
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| InChi Key |
LZJRNLRASBVRRX-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C19H21NO4/c1-20-5-4-10-7-15(22)19(24-3)18-12-9-16(23-2)14(21)8-11(12)6-13(20)17(10)18/h7-9,13,21-22H,4-6H2,1-3H3/t13-/m0/s1
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| Chemical Name |
(6aS)-1,10-dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-2,9-diol
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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) |
DMSO : ~100 mg/mL (~305.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.64 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 (7.64 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 | 3.0546 mL | 15.2732 mL | 30.5465 mL | |
| 5 mM | 0.6109 mL | 3.0546 mL | 6.1093 mL | |
| 10 mM | 0.3055 mL | 1.5273 mL | 3.0546 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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