| Description | Eurycomalactone is a natural product isolated from Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor( IC50 of 0.5 μM). Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα. |
| In vitro | Eurycomalactone(ECL),从长叶黄精(Eurycoma longifolia Jack)中分离出的一种活性蛋白,已被证明具有抗癌活性。ECL对非小细胞肺癌细胞A549和COR-L23显示出选择性的细胞毒性,与正常肺成纤维细胞相比。克隆存活结果显示,辐射前ECL处理与辐射协同作用,显著减少了A549和COR-L23的集落数。ECL处理降低了cyclin B1和CDK1/2的表达,导致细胞周期在敏感的G/M阶段停滞。此外,ECL显著延迟了辐射诱导的DNA双链断裂(DSBs)的修复。在A549细胞中,ECL预处理不仅延迟了辐射诱导的γ-H2AX焦点的消解,还阻止了DSB位点53BP1焦点的形成。此外,ECL预处理还降低了两种非小细胞肺癌细胞中DNA修复蛋白Ku-80和KDM4D的表达。因此,这些效应导致辐照细胞凋亡增加。因此,ECL通过诱导G/M阶段阻滞和延迟X射线诱导的DSBs修复,使非小细胞肺癌细胞对X射线敏感。ECL作为增加针对非小细胞肺癌(NSCLC)放射治疗(RT)效率的辐射增敏剂,具有巨大的潜力。 |
| Target activity | NF-κB:0.5 μM |
| molecular weight | 348.39 |
| Molecular formula | C19H24O6 |
| CAS | 23062-24-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (157.87 mM) |
| References | 1. Cytotoxic activity of quassinoids from Eurycoma longifolia.Nat Prod Commun. 2010 Jul;5(7):1009-12. 2. Dukaew N , Konishi T , Chairatvit K , et al. Enhancement of Radiosensitivity by Eurycomalactone in Human NSCLC Cells through G2/M Cell Cycle Arrest and Delayed DNA Double-strand Break Repair[J]. Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics, 2019. |