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Inulicin (1-O-Acetylbritannilactone), a naturally occurring compound isolated from Inula Britannica L., is a novel and potent inhibitor of the hyperplasia of neointima, acting by modulating the balance of MMP-2 and TIMP-2. It reduced melanin production in a dose-dependent manner with IC50 value of 13.3 uM. Inulicin inhibits VEGF-mediated activation of Src and FAK, also inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
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| ln Vitro |
Inulicin (1-O-Acetylbritannilactone) controls VEGF-Src-FAK signaling, which prevents angiogenesis and the proliferation of lung cancer cells. The growth, migration, and development of capillary structures in cultured human umbilical vascular endothelial cells (HUVECs) are all inhibited by ulicin in a dose-dependent manner. Cell growth suppression and Src-FAK inactivation are the outcomes of inulicin treatment for A549 NSCLC cells. Src and FAK phosphorylation in A549 lung cancer cells is used to investigate the possible impact of inulicin. When A549 cells are treated with inulicin (5 μM and 10 μM), significant high levels of Src and FAK phosphorylations are seen. The growth of cancer cells depends on both FAK and Src. Accordingly, corresponding Inulicin therapy significantly inhibits the development of A549 cells as measured by the MTT assay and the clonogenicity lab. Inulicin exhibits dose-dependent anti-A549 cell growth action once more[1]. Vascular smooth muscle cells (VSMCs) are not able to respond inflammatoryally when inulicin (1-O-Acetylbritannilactone) is extracted from Inula britannica-F. Blockade of NF-κB activation and translocation, as well as suppression of PGE2 synthesis and COX-2 expression induced by lipopolysaccharide (LPS) are among the concentration-dependent effects of inulicin (5, 10, 20 μM). Inulicin also directly prevents active NF-κB from attaching to particular DNA cis-elements[2].
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| ln Vivo |
Inulicin (1-O-Acetylbritannilactone; 12 mg/kg/day) administered as a single dose significantly inhibits the growth of A549 xenografts in nude mice. The production of in vivo microvessels and Src activation in xenograft tumors treated with inulicin are likewise markedly reduced. Using a xenograft model of naked mice, the possible in vivo activity of inulicin is examined. Inulicin (12 mg/kg/day, ip) at a single dose significantly suppresses the development of A549 xenografts in naked mice. Moreover, the weights of tumors treated with inulicin are significantly lower than those of tumors treated with vehicles. Interestingly, mice's body weights remain unchanged after inulicin administration[1].
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| References |
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| Additional Infomation |
1-O-Acetylbritannilactone is a terpene lactone.
Britannilactone 1-O-acetate has been reported in Inula japonica and Pentanema britannicum with data available. |
| Molecular Formula |
C17H24O5
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| Molecular Weight |
308.36946
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| Exact Mass |
308.162
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| CAS # |
33627-41-7
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| PubChem CID |
75528891
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
483.1±45.0 °C at 760 mmHg
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| Flash Point |
173.1±22.2 °C
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| Vapour Pressure |
0.0±2.8 mmHg at 25°C
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| Index of Refraction |
1.521
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| LogP |
2.12
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
519
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1=C([C@H]([C@H]2[C@@H](C1)OC(=O)C2=C)O)[C@@H](C)CCCOC(=O)C
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| InChi Key |
QKUFZFLZBUSEHN-CZLJMHDISA-N
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| InChi Code |
InChI=1S/C17H24O5/c1-9(6-5-7-21-12(4)18)14-10(2)8-13-15(16(14)19)11(3)17(20)22-13/h9,13,15-16,19H,3,5-8H2,1-2,4H3/t9-,13+,15+,16+/m0/s1
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| Chemical Name |
[(4S)-4-[(3aS,4S,7aR)-4-hydroxy-6-methyl-3-methylidene-2-oxo-3a,4,7,7a-tetrahydro-1-benzofuran-5-yl]pentyl] 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~324.29 mM)
Ethanol : ~50 mg/mL (~162.14 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.11 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 (8.11 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 (8.11 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: ≥ 2.5 mg/mL (8.11 mM) (saturation unknown) in 10% EtOH + 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 EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 5: ≥ 2.5 mg/mL (8.11 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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. Solubility in Formulation 6: ≥ 2.5 mg/mL (8.11 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2429 mL | 16.2143 mL | 32.4286 mL | |
| 5 mM | 0.6486 mL | 3.2429 mL | 6.4857 mL | |
| 10 mM | 0.3243 mL | 1.6214 mL | 3.2429 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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