Dehydrocostus Lactone

Catalog No.S3615

For research use only.

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.

Dehydrocostus Lactone Chemical Structure

CAS No. 477-43-0

Selleck's Dehydrocostus Lactone has been cited by 3 Publications

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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 Research:[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 Research:[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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 230.30
Formula

C15H18O2

CAS No. 477-43-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C=C1CCC2C(C3C1CCC3=C)OC(=O)C2=C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05337254 Completed Drug: Dihydroergotamine Migraine|Migraine With Aura|Migraine Without Aura Satsuma Pharmaceuticals Inc. March 5 2021 Phase 1
NCT03874832 Completed Drug: Dihydroergotamine Migraine With Aura|Migraine Without Aura|Migraine Satsuma Pharmaceuticals Inc. September 11 2018 Phase 1
NCT03451162 Completed Drug: DHES0815A Breast Cancer Genentech Inc. April 17 2018 Phase 1
NCT01468558 Completed Drug: MAP0004|Drug: IV DHE|Drug: Ketoconazole Healthy Allergan|MAP Pharmaceuticals Inc. a wholly owned subsidiary of Allergan July 2010 Phase 1
NCT02862886 Completed Other: myometrium biopsy Pregnancy Centre Hospitalier Universitaire Dijon July 2010 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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