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Brevilin A is a naturally occurring sesquiterpene lactone isolated from Centipeda minima with anticancer activity. It is an inhibitor of JAK-STAT by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM).
| ln Vitro |
Brevilin A (1–20 μM; 24 h) quantitatively suppresses STAT3 nasal signaling [1]. Loop of Hounsfield amplification is inhibited by Brevilin A (0-50 μM; 24-72 h) [2]. Induction of DU145 and MDA-MB-468 cells was induced by Brevilin A (10 μM) following treatment for 24 hours [1]. Casein 705 phosphate and Brevilin A (12.5 and 25 μM; 24 hours) burst STAT3 in A549R cells
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|---|---|
| ln Vivo |
Brevilin A (lateral gavage; once daily; 10 and 20 mg/kg; 16 days) suppresses intraluminal PI3K/AKT and STAT3 apoptotic signaling as well as the formation of CNE-2 xenograft tumors [2].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: A549R Cells Tested Concentrations: 1-20 μM Incubation Duration: 24 hrs (hours) Experimental Results: In a dose-dependent manner Exhibits inhibition of STAT3 signaling with an IC50 value of 10.6 μM [1]. Cell proliferation assay[2] Cell Types: CNE-2 Cell Tested Concentrations: 0-50 μM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Shows IC50 values in CNE-2 cells treated for 24, 48 and 72 hrs (hours) respectively are 7.93, 2.60 and 22.26 µM. Apoptosis analysis[1] Cell Types: DU145 and MDA-MB-468 Cell Tested Concentrations: 10 µM Incubation Duration: 24 hrs (hours) and 48 hrs (hours) Experimental Results: c-Myc and CyclinD1 diminished after 24 hrs (hours) and 48 hrs (hours) treatment, after 24 hrs (hours) treatment Increased cleavage of PARP. Western Blot Analysis[1] Cell Types: A549R Cells Tested Concentrations: 12.5 and 25 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of STAT3 phosphorylation in A549R cells. |
| Animal Protocol |
Animal/Disease Models: Male BALB/c nude mice injected with CNE-2 cells [2]
Doses: 10 and 20 mg/kg Route of Administration: po (oral gavage); 10 and 20 mg/kg; one time/day; 16-day Experimental Results: with vehicle Compared to controls, mean tumor volume and weight were diminished by 36.3% and 46.0%, respectively, when treated with 20 mg/kg. Inhibited the protein expression of p-AKT and p-STAT3 at both low and high doses. |
| References |
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| Additional Infomation |
Brevilin A has been reported in Arnica longifolia with data available.
See also: Centipeda minima flowering top (part of). |
| Molecular Formula |
C20H26O5
|
|---|---|
| Molecular Weight |
346.42
|
| Exact Mass |
346.178
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| CAS # |
16503-32-5
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| PubChem CID |
12302076
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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 |
494.0±45.0 °C at 760 mmHg
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| Flash Point |
216.0±28.8 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.535
|
| LogP |
2.98
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
|
| Complexity |
676
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C/C=C(/C)\C(=O)O[C@H]1[C@@H]2[C@@H](C(=O)O[C@@H]2C[C@H]([C@H]3[C@]1(C(=O)C=C3)C)C)C
|
| InChi Key |
KUPPZVXLWANEJJ-UXPPPGSFSA-N
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| InChi Code |
InChI=1S/C20H26O5/c1-6-10(2)18(22)25-17-16-12(4)19(23)24-14(16)9-11(3)13-7-8-15(21)20(13,17)5/h6-8,11-14,16-17H,9H2,1-5H3/b10-6-/t11-,12+,13+,14-,16-,17+,20+/m1/s1
|
| Chemical Name |
[(1S,3aR,5R,5aR,8aR,9S,9aR)-1,5,8a-trimethyl-2,8-dioxo-3a,4,5,5a,9,9a-hexahydro-1H-azuleno[6,5-b]furan-9-yl] (Z)-2-methylbut-2-enoate
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| Synonyms |
6-OAP Brevilin-A Brevilin A
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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 (~288.67 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 10 mg/mL (28.87 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 100.0 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. Solubility in Formulation 2: ≥ 6.25 mg/mL (18.04 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 62.5 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: ≥ 6.25 mg/mL (18.04 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 | 2.8867 mL | 14.4333 mL | 28.8667 mL | |
| 5 mM | 0.5773 mL | 2.8867 mL | 5.7733 mL | |
| 10 mM | 0.2887 mL | 1.4433 mL | 2.8867 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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