Dehydrocostus Lactone

Catalog No.S3615 Batch:S361502

Technical Data

Formula	C₁₅H₁₈O₂
Molecular Weight	230.30	CAS No.	477-43-0
Solubility (25°C)*	In vitro	DMSO	46 mg/mL (199.73 mM)
		Ethanol	46 mg/mL (199.73 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Dehydrocostus lactone (DHE), a natural sesquiterpene lactone, inhibits IKKβ activity, IκBα phosphorylation and degradation, coactivators p300 recruitments and p50/p65 NF-κB nuclear translocation, and their DNA binding activity on COX-2 promoter. It has anti-inflammatory, anti-ulcer, immunomodulatory and anti-tumor properties.

Targets

IKKβ ^[2]

COX2 ^[1]

In vitro

Dehydrocostus lactone can inhibit PGE2 synthesis in vitro. It significantly decreases the expression of COX-2, but not that of COX-1^[1]. After treatment with DHE, the glioblastoma (U118, U251 or U87) cells are significantly inhibited in their viability, proliferation and migration. At the meantime, DHE also induces mitochondria-mediated apoptosis by promoting the release of cytochrome c into cytosol, which activating caspase signaling pathway. DHE significantly suppresses COX-2 expression by inhibiting the phosphorylation of IKKβ via targeting the ATP-binding site, thereby abrogating NF-κB binding and p300 recruitment to COX-2 promoter. DHE suppresses clonogenic and migratory ability of glioblastoma cells and induces apoptosis through mitochondrial pathway^[2].

In vivo

Dehydrocostus lactone suppresses the growth of colorecral cancer xenografts transplanted by colon cancer cell line colo205 in athymic mice. The inhibition effect is dose dependent^[1]. DHE can cross blood-brain barrier (BBB). Treatment with DHE markedly inhibits neoplastic weight and volume without the notable adverse effects in the xenograft nude mice model, and these effects may be mediated through inhibition of the IKKβ/NF-κB/COX-2 signaling pathway^[2].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines U118, U251 and U87 cells Concentrations 0, 1, 10, 25, 50 and 100 μM Incubation Time 12, 24, 36 or 48 h Method U118 (6×10³ cells/well), U251 (8×10³ cells/well) and U87 (7×10³ cells/well) cells are counted and allowed to adhere to obtain 70% confluent monolayer. Following this, the cells are treated with different concentrations of DHE as indicated. After incubation for 12, 24, 36 or 48 h, 10 μl of MTT (5 mg/ml) is added to each well and the cells are incubated for another 4 h. Subsequently, the medium is replaced with 100 μl of DMSO to dissolve formazan crystals. The absorbance is measured at 570 nm using a microplate reader. Each experiment is repeated at least three times. The IC50 values are calculated by interpolation from dose-response curves.
Animal Study:^{^[2]}	Animal Models The female athymic nude mice (4-6 weeks old) and Sprague Dawley rats (8-10 weeks old) Dosages 10 and 20 mg/kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
U118, U251 and U87 cells
Concentrations
0, 1, 10, 25, 50 and 100 μM
Incubation Time
12, 24, 36 or 48 h
Method
U118 (6×10³ cells/well), U251 (8×10³ cells/well) and U87 (7×10³ cells/well) cells are counted and allowed to adhere to obtain 70% confluent monolayer. Following this, the cells are treated with different concentrations of DHE as indicated. After incubation for 12, 24, 36 or 48 h, 10 μl of MTT (5 mg/ml) is added to each well and the cells are incubated for another 4 h. Subsequently, the medium is replaced with 100 μl of DMSO to dissolve formazan crystals. The absorbance is measured at 570 nm using a microplate reader. Each experiment is repeated at least three times. The IC50 values are calculated by interpolation from dose-response curves.

Animal Study:^{^[2]}

Animal Models
The female athymic nude mice (4-6 weeks old) and Sprague Dawley rats (8-10 weeks old)
Dosages
10 and 20 mg/kg
Administration
i.p.

References

Selleck's Dehydrocostus Lactone has been cited by 3 publications

Dehydrocostus Lactone Attenuates the Senescence of Nucleus Pulposus Cells and Ameliorates Intervertebral Disc Degeneration via Inhibition of STING-TBK1/NF-κB and MAPK Signaling [ Front Pharmacol, 2021, 12:641098]	PubMed: 33935734
Suppressive effects of dehydrocostus lactone on the toll-like receptor signaling pathways. [ Int Immunopharmacol, 2020, 78:106075]	PubMed: 31812722
Dehydrocostus lactone attenuates osteoclastogenesis and osteoclast-induced bone loss by modulating NF-κB signalling pathway. [ J Cell Mol Med, 2019, 23(8):5762-5770]	PubMed: 31225720

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SHIPPING AND STORAGE
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