Dehydrocostus Lactone
(Synonyms: 去氢木香烃内酯; (-)-Dehydrocostus lactone; Epiligulyl oxide) 目录号 : GN10786
Dehydrocostus Lactone是一种可以从Saussurea lappa分离得到的天然倍半萜，能够抑制IKKβ活性、IκBα的磷酸化和降解。
Cas No.:477-43-0
Sample solution is provided at 25 µL, 10mM.
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Dehydrocostus Lactone is a natural sesquiterpene that can be isolated from Saussurea lappa and inhibits the activity of IKKβ, the phosphorylation and degradation of IκBα [1]. Dehydrocostus Lactone can cause cell cycle arrest, induce cell apoptosis, reduce drug resistance, and inhibit angiogenesis of cancer cells [2]. Dehydrocostus Lactone has multiple activities such as anti-inflammatory, antibacterial, anti-tumor, and immunomodulatory [3-4].
In vitro, Dehydrocostus lactone (0-2mg/L; 48h) significantly reduced the viability of DU145 cells in a dose-dependent manner, induced cell apoptosis, and inhibited the expression of anti-apoptotic proteins and increased the expression of pro-apoptotic proteins [5]. Dehydrocostus lactone (0-30μM; 0.5h) treatment could inhibit the phosphorylation of p38 MAPK, MK2 and Akt, the activation of NF-κB, reduce iNOS expression and NO production, and lower the mRNA levels of pro-inflammatory cytokines such as TNF-α, IL-6, IL-1β and IL-12 [6].
In vivo, Dehydrocostus lactone (5-20mg/kg/day; i.p.; single administration) treatment significantly alleviated the pathological damage in mice with acute lung injury induced by lipopolysaccharide (LPS), effectively reduced the infiltration of inflammatory cells and the thickening of the alveolar wall, and decreased the expression of lung cytokines [6]. Dehydrocostus lactone (10, 15 and 20mg/kg/day; 13 days; gavage) treatment alleviated the inflammation in mice with ulcerative colitis (UC) induced by glucose sodium sulfate (DSS), reduced the levels of inflammatory cytokines (TNF-α, IL-1β, MCP-1, MPO, SOD, IL-6, IL-17 and IL-23), downregulated the IL-6/STAT3 inflammatory signaling pathway, and inhibited downstream pathways (XBP1s and α-defensin) [7].
References:
[1] Wang J, Yu Z, Wang C, et al. Dehydrocostus lactone, a natural sesquiterpene lactone, suppresses the biological characteristics of glioma, through inhibition of the NF-κB/COX-2 signaling pathway by targeting IKKβ. Am J Cancer Res. 2017;7(6):1270-1284.
[2] Lohberger, B., Rinner, B., Stuendl, N., et al. Sesquiterpene lactones downregulate G2/M cell cycle regulator proteins and affect the invasive potential of human soft tissue sarcoma cells. PLoS One 8(6), (2013).
[3] Taniguchi M, et al. Costunolide and dehydrocostus lactone as inhibitors of killing function of cytotoxic T lymphocytes. Biosci Biotechnol Biochem. 1995 Nov;59(11):2064-7.
[4] Cantrell CL, et al. Antimycobacterial activities of dehydrocostus lactone and its oxidation products. J Nat Prod. 1998 Oct;61(10):1181-6.
[5] Eun Ji Kim, et al. Apoptosis of DU145 human prostate cancer cells induced by dehydrocostus lactone isolated from the root of Saussurea lappa. Food and Chemical Toxicology Volume 46, Issue 12, December 2008, Pages 3651–3658.
[6] Nie Y, Wang Z, Chai G, et al. Dehydrocostus Lactone Suppresses LPS-induced Acute Lung Injury and Macrophage Activation through NF-κB Signaling Pathway Mediated by p38 MAPK and Akt. Molecules. 2019;24(8):1510.
[7] Zhou Q, Zhang W, He Z, et al. The possible anti‐inflammatory effect of dehydrocostus lactone on DSS‐induced colitis in mice[J]. Evidence‐Based Complementary and Alternative Medicine, 2020, 2020(1): 5659738.
Dehydrocostus Lactone是一种可以从Saussurea lappa分离得到的天然倍半萜，能够抑制IKKβ活性、IκBα的磷酸化和降解 [1]。Dehydrocostus Lactone能够使细胞周期停滞、诱导细胞凋亡、降低耐药性以及抑制癌细胞的血管生成 [2]。Dehydrocostus Lactone具有抗炎、抗菌、抗肿瘤和免疫调节等多种活性 [3-4]。
在体外，Dehydrocostus lactone（0-2mg/L; 48h）以剂量依赖性方式显著降低了DU145细胞的活力，诱导细胞发生凋亡，并抑制抗凋亡蛋白表达、增加促凋亡蛋白表达 [5]。Dehydrocostus lactone（0-30μM; 0.5h）处理能够抑制RAW264.7细胞中p38 MAPK、MK2和Akt的磷酸化、NF-κB的激活，减少iNOS表达和NO产生，并降低了TNF-α、IL-6、IL-1β和IL-12等促炎细胞因子的mRNA水平 [6]。
在体内，Dehydrocostus lactone（5-20mg/kg/day; 腹腔注射; 单次给药）治疗显著减轻了脂多糖（LPS）诱导的急性肺损伤模型小鼠的病理损伤，有效地减少了炎症细胞的浸润和肺泡壁的增厚，并降低了肺部细胞因子的表达 [6]。Dehydrocostus lactone（10, 15 and 20mg/kg/day; 13 days; gavage）治疗减轻了葡萄糖硫酸钠（DSS）诱导的溃疡性结肠炎（UC）模型小鼠的炎症，降低了炎症细胞因子（TNF-α、IL-1β、MCP-1、MPO、SOD、IL-6、IL-17和IL-23）的水平，下调了IL-6/STAT3炎症信号通路，并抑制了下游通路（XBP1s和α-defensin）[7]。
| Cell experiment [1]: | |
Cell lines | DU145 human prostate cancer cells |
Preparation Method | Androgen-insensitive DU145 human prostate cancer cells were maintained in DMEM/F12 containing 10% fetal bovine serum (FBS) with 100,000U/L of penicillin and 100mg/L of streptomycin at 37°C in 5% CO2. To determine the effects of the various extracts and of Dehydrocostus Lactone on the cell viability, we plated cells in multi-well plates with DMEM/F12 containing 10% FBS. After 24h, the cell monolayers were rinsed and serum-deprived for 24h with DMEM/F12 containing 1% charcoal-stripped FBS (serum-deprived medium). The medium was then replaced with fresh serum-deprived medium with or without Dehydrocostus Lactone (0.25–2mg/L), and the cells were cultured for 72h. Viable cell numbers were estimated by the MTT assay. |
Reaction Conditions | 0-2mg/L; 48h |
Applications | Dehydrocostus lactone significantly reduced the viability of DU145 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice (acute lung injury (ALI) model) |
Preparation Method | Lipopolysaccharide was dissolved in PBS, and Dehydrocostus Lactone was dissolved in a solvent (H2O:ethanol:polyoxyethylene hydrogenated castor oil = 8:1:1). After acclimation for around 2 weeks under a specific pathogen-free environment (25 °C, 55% humidity, with adequate food and water), the 8- to 10-week-old male C57/BL6 mice (20 ± 3g) were randomly divided into 5 groups: LPS-induced ALI models were generated by intratracheal administration with of LPS (5mg/kg), while some groups were further received Dehydrocostus Lactone intraperitoneally as a therapeutic agent in in a range from 5 to 20mg/kg. The experimental mice were euthanized 24 hours after being injected with LPS, and then their lung tissues and bronchoalveolar lavage fluid were collected for pathological analysis. |
Dosage form | 5, 10 and 20mg/kg/day; single dose; i.p. |
Applications | Dehydrocostus lactone significantly alleviated the pathological damage in mice with acute lung injury induced by LPS. |
References: | |
| Cas No. | 477-43-0 | SDF | |
| 别名 | 去氢木香烃内酯; (-)-Dehydrocostus lactone; Epiligulyl oxide | ||
| 化学名 | (3aS,6aR,9aR,9bS)-3,6,9-trimethylidene-3a,4,5,6a,7,8,9a,9b-octahydroazuleno[4,5-b]furan-2-one | ||
| Canonical SMILES | C=C1CCC2C(C3C1CCC3=C)OC(=O)C2=C | ||
| 分子式 | C15H18O2 | 分子量 | 230.3 |
| 溶解度 | ≥ 7.85mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3422 mL | 21.7108 mL | 43.4216 mL |
| 5 mM | 868.4 μL | 4.3422 mL | 8.6843 mL |
| 10 mM | 434.2 μL | 2.1711 mL | 4.3422 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Quality Control & SDS
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- Purity: >99.50%
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