Costunolide ((+)-Costunolide) 是一种天然存在的倍半萜内酯，具有抗氧化、抗炎、抗过敏、骨骼重塑、神经保护、促进头发生长、抗癌和抗糖尿病的特性。 Costunolide 可以诱导乳腺癌细胞的细胞周期停滞和凋亡。
| Cas No. | 553-21-9 |
| 别名 | 木香烃内酯; (+)-Costunolide; Costus lactone |
| 化学名 | (3aS,6E,10E,11aR)-6,10-dimethyl-3-methylidene-3a,4,5,8,9,11a-hexahydrocyclodeca[b]furan-2-one |
| Canonical SMILES | CC1=CCCC(=CC2C(CC1)C(=C)C(=O)O2)C |
| 分子式 | C15H20O2 |
| 分子量 | 232.32 |
| 溶解度 | ≥ 35.7 mg/mL in DMSO, ≥ 45.2 mg/mL in EtOH with ultrasonic and warming |
| 储存条件 | Store at -20℃, sealed storage, away from moisture and light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Description:
IC50 Value: 6.2 - 9.8 μg/mL(sarcoma cells viability)[3]
Costunolide, a sesquiterpene lactone, exhibits anti-inflammatory and anti-oxidant properties and mediates apoptosis.
in vitro: Costunolide significantly inhibited RANKL-induced BMM differentiation into osteoclasts in a dose-dependent manner without affecting cytotoxicity. Costunolide did not regulate the early signaling pathways of RANKL, including the mitogen-activated protein kinase and NF-κB pathways. However, costunolide suppressed nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1) expression via inhibition of c-Fos transcriptional activity without affecting RANKL-induced c-Fos expression. The inhibitory effects ofcostunolide were rescued by overexpression of constitutively active (CA)-NFATc1 [1]. Exposure of T24 cells to costunolide was also associated with increased expression of Bax, down-regulation of Bcl-2, survivin and significant activation of caspase-3, and its downstream target PARP [2]. Both costunolide and dehydrocostus lactone inhibited cell viability dose- and time-dependently. IC50 values ranged from 6.2 μg/mL to 9.8 μg/mL. Cells treated with costunolide showed no changes in cell cycle, little in caspase 3/7 activity, and low levels of cleaved caspase-3 after 24 and 48 h [3].
in vivo: Neither costunolide nor alpha-MGBL affected the blood-ethanol elevation in pylorus-ligated rats or that induced by intraperitoneal and intraduodenal ethanol administration [4]. Costunolide and alpha-MGBL suppressed gastric emptying in rats given 20% ethanol and 1% sodium carboxymethyl cellulose.
Clinical trial: N/A |
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