Eurycomalactone

SKU: orb1219404

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.Eurycomalactone (ECL), an active quassinoid isolated from Eurycoma longifolia Jack, has been demonstrated to possess anticancer activity. ECL exhibited selective cytotoxicity against the NSCLC cells A549 and COR-L23 compared to the normal lung fibroblast. Clonogenic survival results indicated that ECL treatment prior to irradiation synergistically decreased the A549 and COR-L23 colony number. ECL treatment reduced the expression of cyclin B1 and CDK1/2 leading to induce cell cycle arrest at the radiosensitive G /M phase. Moreover, ECL markedly delayed the repair of radiation-induced DNA double-strand breaks (DSBs). In A549 cells, pretreatment with ECL not only delayed the resolving of radiation-induced γ-H2AX foci but also blocked the formation of 53BP1 foci at the DSB sites. In addition, ECL pretreatment attenuated the expression of DNA repair proteins Ku-80 and KDM4D in both NSCLC cells. Consequently, these effects led to an increase in apoptosis in irradiated cells. Thus, ECL radiosensitized the NSCLC cells to X-ray via G /M arrest induction and delayed the repair of X-ray-induced DSBs. It has a great potential for ECL as an alternative safer radiosensitizer for increasing the RT efficiency against NSCLC.

Images & Validation

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Key Properties

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CAS Number	23062-24-0
MW	348.4
Purity	>98% (HPLC)
Formula	C₁₉H₂₄O₆
SMILES	C[C@]12[C@@]([C@H]([C@@](O3)([H])[C@@](C)([H])[C@]2([H])C3=O)O)([H])[C@]([C@@](C(C)=CC4=O)([H])CC1=O)([C@@H]4O)C
Target	NF-κB
Solubility	In Vitro: DMSO : 100 mg/mL (287.03 mM)

Bioactivity

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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. Eurycomalactone (2.29-156.3 μM; 24 h; A549 and Calu-1 cells) promotes Non-small cell lung cancer (NSCLC) cells apoptosis. 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. Eurycomalactone (2.5-25 μM; 24 h; A549 cells) suppressed the repair of radiation-Induced DNA double-strand breaks. 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. Apoptosis Analysis 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 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. 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. 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. 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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NF-κB

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