Eurycomalactone (Synonyms: 东革内酯)

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Eurycomalactone  (Synonyms: 东革内酯) 纯度: 98.99%

Eurycomalactone 是一种可以从 Eurycoma longifolia Jack 中分离得到的活性拟松类化合物。Eurycomalactone 是一种有效的NF-κB 抑制剂，其 IC50 值为 0.5 μM。Eurycomalactone 可抑制蛋白合成，降低 cyclin D1 蛋白水平。Eurycomalactone 通过阻滞细胞周期于G2/M 期和延迟 DNA 双链断裂修复来提高放射敏感性。Eurycomalactone 抑制 AKT/NF-κB 信号通路的激活，诱导细胞凋亡并增强对 Cisplatin (HY-17394) 的化疗敏感性。

Eurycomalactone (Synonyms: 东革内酯)

Eurycomalactone Chemical Structure

CAS No. : 23062-24-0

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5 mg ￥4300 In-stock
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生物活性

Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394)[1][2][3].

IC50 & Target

IC50: 0.5 μM (NF-κB)[1]
体外研究
(In Vitro)

Eurycomalactone (24, 48 and 72 h) selectively inhibits the viability of A549 and COR-L23 cells Eurycomalactone inhibits the viability of A549 cells with IC50 values of 20.17, 3.77, and 1.90 μM for 24, 48 and 72 hours, respectively. Eurycomalactone inhibits the viability of COR-L23 cells with IC50 values of 25.02, 2.74, and 1.80 μM for 24, 48 and 72 hours, respectively[1].
Eurycomalactone (2.29-156.3 μM; 24 h; A549 and Calu-1 cells) promotes Non-small cell lung cancer (NSCLC) cells apoptosis[2].
Eurycomalactone (0-25.05 μM; 24 h; A549 and COR-L23 cells) induces cell cycle arrest at the radiosensitive G2/M phase and induces apoptosis in irradiated Non-small cell lung cancer (NSCLC) cells. Eurycomalactone downregulated the key G2/M regulatory proteins in irradiated Non-small cell lung cancer (NSCLC) cells[1].
Eurycomalactone (2.5-25 μM; 24 h; A549 cells) suppressed the repair of radiation-Induced DNA double-strand breaks[1].
Eurycomalactone (2.29-156.3 μM; 24 h; A549 and Calu-1 cells) suppresses AKT/NF-κB activation in Non-small cell lung cancer (NSCLC) cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Eurycomalactone 相关抗体:

Apoptosis Analysis[2]

Cell Line: A549 and Calu-1 cells
Concentration: 2.29, 10.14, 12.02, 20.81, 80.77, and 156.3 μM
Incubation Time: 24 hours
Result: Increased the apoptotic rates in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: A549 and COR-L23 cells
Concentration: 1.57, 2.57, 20.17 and 25.05 μM
Incubation Time: 24 hours
Result: Induced cell cycle arrest at G2/M phase in irradiated cells and increased the sub-G1 population. A549 and COR-L23 cells

Western Blot Analysis[2]

Cell Line: A549 and Calu-1 cells
Concentration: 2.29, 10.14, 12.02, 20.81, 80.77, and 156.3 μM
Incubation Time: 24 hours
Result: Induced the expression levels of active caspase-3 and active PARP (cleaved form), while decreased Bcl-xL and surviving.

Western Blot Analysis[1]

Cell Line: A549 and COR-L23 cells
Concentration: 1.57, 2.57, 20.17 and 25.05 μM
Incubation Time: 24 hours
Result: Downregulated the expression of both G2/M regulatory proteins in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: A549 and COR-L23 cells
Concentration: 2.29, 10.14, 12.02, 20.81, 80.77, and 156.3 μM
Incubation Time: 24 hours
Result: inhibited the expression levels of p(S473)-AKT, total AKT, p(S536)-NF-κB p65 and total NF-κB p65.

分子量

348.39

Formula

C19H24O6
CAS 号

23062-24-0
性状

固体

颜色

White to off-white

中文名称

东革内酯
结构分类
  • Terpenoids
  • Diterpenoids
初始来源
  • 植物
  • 其他科
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (287.03 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8703 mL 14.3517 mL 28.7035 mL
5 mM 0.5741 mL 2.8703 mL 5.7407 mL
10 mM 0.2870 mL 1.4352 mL 2.8703 mL

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储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-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。

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纯度 & 产品资料

纯度: 98.99%

Data Sheet (623 KB) SDS (251 KB)

COA (185 KB) HNMR (159 KB) CNMR (164 KB) RP-HPLC (339 KB)

产品使用指南 (1538 KB)

参考文献

  • [1]. Dukaew N, et, al. Enhancement of Radiosensitivity by Eurycomalactone in Human NSCLC Cells Through G₂/M Cell Cycle Arrest and Delayed DNA Double-Strand Break Repair. Oncol Res. 2020 Mar 27;28(2):161-175.  [Content Brief]

    [2]. Dukaew N, et, al. Inactivation of AKT/NF κB signaling by eurycomalactone decreases human NSCLC cell viability and improves the chemosensitivity to cisplatin. Oncol Rep. 2020 Oct;44(4):1441-1454.  [Content Brief]

    [3]. Malainer C, et, al. Eurycomalactone Inhibits Expression of Endothelial Adhesion Molecules at a Post-Transcriptional Level. J Nat Prod. 2017 Dec 22;80(12):3186-3193.  [Content Brief]

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