| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 100mg | |||
| Other Sizes |
| Targets |
- In antifungal activity studies, Magnoflorine exhibits inhibitory effects on Candida species (including Candida albicans, Candida tropicalis, Candida krusei), but no specific molecular target (e.g., enzyme/receptor) or affinity data (IC50/Ki) were reported[1]
- In pro-inflammatory response regulation, Magnoflorine acts via the MyD88-dependent signaling pathway (involved in TLR4-mediated inflammation), but no direct binding affinity to MyD88 or downstream proteins (e.g., NF-κB, MAPK) was provided[2] |
|---|---|
| ln Vitro |
- Magnoflorine inhibited the growth of 8 clinical isolates of Candida albicans, with minimum inhibitory concentrations (MICs) ranging from 16 to 64 μg/mL; it also suppressed Candida tropicalis (MIC: 32 μg/mL) and Candida krusei (MIC: 64 μg/mL) growth[1]
- At 2×MIC concentration, Magnoflorine reduced the biomass of Candida albicans biofilms by 45% (measured via crystal violet staining) and decreased the viability of biofilm-embedded cells by 38% (XTT reduction assay)[1] - Pro-inflammatory effects in U937 macrophages: - In LPS (1 μg/mL)-activated U937 macrophages, Magnoflorine (10-50 μM) increased TNF-α secretion in a dose-dependent manner: 50 μM Magnoflorine elevated TNF-α levels by 2.8-fold compared to LPS alone (ELISA)[2] - It also upregulated IL-6 (2.1-fold) and IL-1β (1.9-fold) mRNA expression at 50 μM (qRT-PCR) and enhanced the phosphorylation of p65 (NF-κB subunit) and p38 (MAPK) by 2.3-fold and 1.7-fold, respectively (Western blot)[2] - Silencing MyD88 via siRNA abolished the pro-inflammatory effects of Magnoflorine: TNF-α secretion was reduced by 65% compared to non-silenced cells[2] |
| Enzyme Assay |
- Candida growth inhibition assay (MIC determination):
- Candida strains were cultured in RPMI 1640 medium to logarithmic phase, then adjusted to 1×10⁶ CFU/mL.
- Serial dilutions of Magnoflorine (2-128 μg/mL) were added to 96-well plates, followed by equal volumes of Candida suspension.
- Plates were incubated at 35°C for 48 hours, and MIC was defined as the lowest Magnoflorine concentration that completely inhibited visible fungal growth[1]
- MyD88-dependent signaling activation assay (Western blot for phosphorylated proteins): - U937 macrophages were pretreated with Magnoflorine (10-50 μM) for 1 hour, then stimulated with LPS (1 μg/mL) for 30 minutes. - Cells were lysed, and proteins were separated by SDS-PAGE, transferred to PVDF membranes, and probed with antibodies against phospho-p65, phospho-p38, and total p65/p38. GAPDH was used as a loading control[2] |
| Cell Assay |
Candida biofilm inhibition assay:
- Candida albicans was inoculated into 96-well plates and cultured at 35°C for 24 hours to form biofilms.
- Biofilms were treated with Magnoflorine (2×MIC, 32 μg/mL) for 24 hours, then stained with crystal violet (0.1%) for 15 minutes.
- Excess stain was washed off, and absorbance at 570 nm was measured to quantify biomass; XTT reagent was added to assess viable cells via absorbance at 490 nm[1]
- U937 macrophage pro-inflammatory factor detection (ELISA/qRT-PCR): - U937 cells were differentiated into macrophages with PMA (100 nM) for 48 hours, then pretreated with Magnoflorine (10-50 μM) for 1 hour, followed by LPS (1 μg/mL) stimulation for 24 hours. - Cell supernatants were collected for TNF-α/IL-6 detection via ELISA; total RNA was extracted, reverse-transcribed to cDNA, and IL-1β mRNA expression was measured via qRT-PCR (GAPDH as internal control)[2] - MyD88 siRNA transfection assay in U937 cells: - U937 macrophages were transfected with MyD88 siRNA or negative control siRNA using transfection reagent for 48 hours. - Transfected cells were treated with Magnoflorine (50 μM) and LPS (1 μg/mL) for 24 hours, then TNF-α secretion was detected via ELISA to verify MyD88 dependence[2] |
| Toxicity/Toxicokinetics |
In U937 macrophages, concentrations up to 50 μM of magnoflorine did not affect cell viability (MTT assay: cell viability >90% compared to the control group), indicating that it has low cytotoxicity at pro-inflammatory concentrations [2]
|
| References | |
| Additional Infomation |
Magnoliaine is a natural apophene alkaloid, primarily isolated from plants of the Magnoliaceae family (e.g., Magnolia officinalis), and possesses potential natural antifungal and immunomodulatory activities [1][2]. The antifungal mechanism of magnoliaine may involve disruption of the integrity of Candida cell membranes (increased membrane permeability in preliminary tests suggests this), but direct evidence has not yet been provided (e.g., ergosterol content assays) [1]. In LPS-activated macrophages, the pro-inflammatory effect of magnoliaine is TLR4/MyD88 dependent, as it does not enhance the inflammatory response in cells treated with the TLR4 inhibitor (TAK-242) [2].
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| Molecular Formula |
C20H24INO4
|
|---|---|
| Molecular Weight |
469.3133
|
| Exact Mass |
469.075
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| CAS # |
4277-43-4
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| Related CAS # |
(+)-Magnoflorine chloride; 6681-18-1; (+)-Magnoflorine; 2141-09-5
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| PubChem CID |
6451920
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| Appearance |
White to light yellow solid
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| Melting Point |
248-249ºC
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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 |
26
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| Complexity |
498
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[I-].O([H])C1=C(C([H])=C2C([H])([H])C([H])([H])[N+](C([H])([H])[H])(C([H])([H])[H])[C@@]3([H])C([H])([H])C4C([H])=C([H])C(=C(C=4C1=C32)O[H])OC([H])([H])[H])OC([H])([H])[H]
|
| InChi Key |
ODRHNGNRVVELAJ-ZOWNYOTGSA-N
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| InChi Code |
InChI=1S/C20H23NO4.HI/c1-21(2)8-7-12-10-15(25-4)20(23)18-16(12)13(21)9-11-5-6-14(24-3)19(22)17(11)18;/h5-6,10,13H,7-9H2,1-4H3,(H-,22,23);1H/t13-;/m0./s1
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| Chemical Name |
(6aS)-2,10-dimethoxy-6,6-dimethyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinolin-6-ium-1,11-diol;iodide
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| Synonyms |
α-Magnoflorine iodide; Magnoflorine iodide; Thalictrine iodide
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~62.5 mg/mL (~133.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.43 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.43 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 20.8 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: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (21.31 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1308 mL | 10.6539 mL | 21.3079 mL | |
| 5 mM | 0.4262 mL | 2.1308 mL | 4.2616 mL | |
| 10 mM | 0.2131 mL | 1.0654 mL | 2.1308 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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