Dehydrocostus Lactone

製品コードS3615 バッチS361502

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H18O2
分子量 230.30 CAS No. 477-43-0
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 U118, U251 and U87 cells
濃度 0, 1, 10, 25, 50 and 100 μM
反応時間 12, 24, 36 or 48 h
実験の流れ 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.
動物実験 動物モデル The female athymic nude mice (4-6 weeks old) and Sprague Dawley rats (8-10 weeks old)
投薬量 10 and 20 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。