| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
IKKβ; COX2
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|---|---|
| ln Vitro |
Dehydrocostus lactone can inhibit PGE2 synthesis in vitro. It significantly reduces COX-2 expression but not COX-1 expression[1]. Glioblastoma (U118, U251 or U87) cells are significantly inhibited in their viability, proliferation, and migration following treatment with DHE. The release of cytochrome c into the cytosol, which activates the caspase signaling pathway, is another way that DHE triggers mitochondria-mediated apoptosis. By blocking IKK phosphorylation by aiming at the ATP-binding site and preventing NF-κB binding and p300 recruitment to the COX-2 promoter, DHE significantly reduces COX-2 expression. DHE inhibits the ability of glioblastoma cells to migrate and form colonies, and it triggers apoptosis via the mitochondrial pathway[2].
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| ln Vivo |
Dehydrocostus lactone inhibits colon cancer cell line colo205-transplanted colorectal cancer xenograft growth in athymic mice. The inhibition effect depends on the dose[1]. Blood-brain barrier (BBB) can be crossed by DHE. In the xenograft nude mouse model, treatment with DHE significantly reduces neoplastic weight and volume without observable adverse effects, and these effects may be mediated by inhibiting the IKKβ/NF-κB/COX-2 signaling pathway[2].
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| Cell Assay |
To obtain a 70% confluent monolayer, cells from the U118 (6×103 cells/well), U251 (8×103 cells/well), and U87 (7×103 cells/well) are counted and allowed to adhere. The cells are then given treatments with DHE at the indicated concentrations. Following 12, 24, 36, or 48 hours of incubation, 10 l of MTT (5 mg/ml) is added to each well, and the cells are then incubated for an additional 4 hours. In order to dissolve the formazan crystals, the medium is then replaced with 100 μl of DMSO. A microplate reader is used to measure the absorbance at 570 nm. At least three times each experiment is run again. By extrapolating from dose-response curves, the IC50 values are determined.
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| Animal Protocol |
The female athymic nude mice (4-6 weeks old) and Sprague Dawley rats (8-10 weeks old)
10 and 20 mg/kg i.p. Two main in vivo protocols were used: a pharmacokinetic study for BBB penetration and an efficacy/toxicity study in a xenograft model. 1. **Blood-Brain Barrier Penetration Study:** - **Animals:** Male Sprague Dawley rats (200-220 g). [2] - **Drug Administration:** Rats received an intraperitoneal injection of DHE (100 mg/kg). [2] - **Sample Collection:** One hour post-injection, rats were anesthetized, and cerebrospinal fluid (CSF) was collected from the cisterna magna. [2] - **Sample Preparation and Analysis:** CSF was mixed with acetonitrile, centrifuged, and the supernatant was dried under nitrogen. The residue was reconstituted and analyzed by LC-MS/MS to detect DHE. [2] 2. **Xenograft Tumor Model (Efficacy and Toxicity):** - **Animals:** Female athymic nude mice (4-6 weeks old). [2] - **Tumor Inoculation:** U87 cells (1 × 10⁷) were subcutaneously injected into the left axillary fossa of each mouse. [2] - **Treatment Protocol:** After two weeks, mice were randomly divided into three groups (n=6/group) and received daily intraperitoneal injections of PBS (control), DHE (10 mg/kg), or DHE (20 mg/kg) for 14 days. [2] - **Monitoring:** Body weight and tumor volume (calculated as V = 1/2 × length × width²) were recorded every 2 days. [2] - **Terminal Procedures:** On day 30, mice were euthanized. Tumors were excised, weighed, and photographed. Tumor tissues were fixed in formalin for immunohistochemical analysis of COX-2, p-p65, and p-IKKβ. [2] |
| References | |
| Additional Infomation |
Dehydroauracene lactone is an organic heterotricyclic compound belonging to the guaiacane sesquiterpene lactone family. Its structure involves the substitution of acrylic acid at the 2-position with a 4-hydroxy-3,8-bis(methylene)decylhydroazine-5-yl group, where the hydroxyl and carboxyl groups undergo a condensation reaction to form the corresponding γ-lactone. It can be used as a metabolite, trypanosome killer, antitumor agent, cyclooxygenase 2 inhibitor, antimycobacterial drug, and apoptosis inducer. It is a sesquiterpene lactone, a guaiacane sesquiterpene compound, an organic heterotricyclic compound, and a γ-lactone. Dehydroauracene lactone has been reported to exist in Ainsliaea uniflora, Costus, and other organisms with relevant data. See also: Burdock root (partial).
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| Molecular Formula |
C15H18O2
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|---|---|
| Molecular Weight |
230.307
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| Exact Mass |
230.13
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| Elemental Analysis |
C, 78.23; H, 7.88; O, 13.89
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| CAS # |
477-43-0
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| Related CAS # |
477-43-0
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| PubChem CID |
73174
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
383.7±42.0 °C at 760 mmHg
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| Melting Point |
59 °C
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| Flash Point |
161.2±25.3 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.536
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
17
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| Complexity |
432
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O1C(C(=C([H])[H])[C@]2([H])C([H])([H])C([H])([H])C(=C([H])[H])[C@]3([H])C([H])([H])C([H])([H])C(=C([H])[H])[C@]3([H])[C@@]12[H])=O
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| InChi Key |
NETSQGRTUNRXEO-XUXIUFHCSA-N
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| InChi Code |
InChI=1S/C15H18O2/c1-8-4-7-12-10(3)15(16)17-14(12)13-9(2)5-6-11(8)13/h11-14H,1-7H2/t11-,12-,13-,14-/m0/s1
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| Chemical Name |
(3aS,6aR,9aR,9bS)-3,6,9-trimethylidene-3a,4,5,6a,7,8,9a,9b-octahydroazuleno[4,5-b]furan-2-one
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| Synonyms |
(-)-Dehydrocostus lactone; Dehydrocostus Lactone
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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: 46~250 mg/mL (199.7~1085.5 mM)
Ethanol: 15~46 mg/mL (65.1 mM~199.7) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.03 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 (9.03 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 (9.03 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 | 4.3420 mL | 21.7099 mL | 43.4197 mL | |
| 5 mM | 0.8684 mL | 4.3420 mL | 8.6839 mL | |
| 10 mM | 0.4342 mL | 2.1710 mL | 4.3420 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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