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Morusin is a prenylated flavonoid isolated from M. australis with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.
| ln Vitro |
Morusin inhibits the growth of human and animal breast cancer cells in a dose- and time-dependent manner. The IC50 values for mouse breast cancer cells (4 T1 and EMT6), human breast cancer cells (MCF-7 and MDA-MB -231), and normal mammary epithelial cells (MCF-10A) are 2.03 and 1.87 μg/mL, respectively, and the maximum inhibition of cell growth (>80%) was found at 8 μg/mL. In a dose-dependent manner, apoptotic cells were markedly upregulated in breast cancer cells treated with morusin [1]. The proliferation and colony formation of human colorectal cancer HT-29 cells are markedly inhibited by muscin. Additionally, morusin promotes the production of IκB-α, suppresses the nuclear translocation of NF-κB and its DNA-binding activity, and inhibits the phosphorylation of IKK-α, IKK-β, and IκB-β. It was also demonstrated that the NF-κB upstream regulators Akt, PDK1, and PI3K were dephosphorylated. Moreover, early time points showed the activation of caspase-8, modifications to the mitochondrial membrane potential, the release of cytochrome c and Smac/DIABLO, and the activation of caspase-9 and -3. Following this, the expression of XIAP and Ku70 is downregulated [2]. Prostate cancer cells' ability to proliferate is inhibited by mususin, whereas normal human prostate epithelial cells are not significantly affected. By preventing STAT3 phosphorylation, nuclear accumulation, and DNA binding activity, morusin also lowers STAT3 activity. Moreover, the expression of STAT3 target genes that encode Cyclin D1, Bcl-xL, Bcl-2, Survivin, and c-Myc is downregulated by morusin. It lowers STAT3 activity, which causes human prostate cancer cells to undergo apoptosis [3].
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| ln Vivo |
Morusin dramatically reduces the rate at which breast cancer spreads. The tumor weights of mice administered 5 and 10 mg/kg morimulin were 0.61±0.23 and 0.41±0.10 g, respectively, and the tumor inhibition rates were 46.5% and 64.1%. The average tumor weight of control mice was 1.14±0.30 g. correspondingly [1].
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| References |
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| Additional Infomation |
Morusin is an extended flavonoid that is flavone substituted by hydroxy groups at positions 5, 2' and 4', a prenyl group at position 3 and a 2,2-dimethyl pyran group across positions 7 and 8. It has a role as a plant metabolite and an antineoplastic agent. It is a trihydroxyflavone and an extended flavonoid.
Morusin has been reported in Morus lhou, Artocarpus tonkinensis, and other organisms with data available. |
| Molecular Formula |
C25H24O6
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|---|---|
| Molecular Weight |
420.4545
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| Exact Mass |
420.157
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| CAS # |
62596-29-6
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| PubChem CID |
5281671
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
656.7±55.0 °C at 760 mmHg
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| Melting Point |
232-235ºC
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| Flash Point |
226.9±25.0 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.636
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| LogP |
6.25
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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 |
3
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| Heavy Atom Count |
31
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| Complexity |
805
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XFFOMNJIDRDDLQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24O6/c1-13(2)5-7-17-22(29)21-19(28)12-20-16(9-10-25(3,4)31-20)24(21)30-23(17)15-8-6-14(26)11-18(15)27/h5-6,8-12,26-28H,7H2,1-4H3
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| Chemical Name |
2-(2,4-dihydroxyphenyl)-5-hydroxy-8,8-dimethyl-3-(3-methylbut-2-enyl)pyrano[2,3-h]chromen-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 |
| 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 (~237.84 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.95 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 (5.95 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 | 2.3784 mL | 11.8920 mL | 23.7840 mL | |
| 5 mM | 0.4757 mL | 2.3784 mL | 4.7568 mL | |
| 10 mM | 0.2378 mL | 1.1892 mL | 2.3784 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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