Emodin (Frangula emodin) is a naturally occurring anthraquinone present in the roots and barks of numerous plants; exerts antiproliferative effects in Y cells that are regulated by different signaling pathways.

CK2:2 μM.

Emodin，一种蒽醌衍生物，作为竞争性抑制剂，选择性地抑制丝氨酸/苏氨酸激酶案例激酶II(CKII)。其对CKII的活性抑制表现为IC50约2 μM，这比对其他激酶的抑制效力低两到三个数量级。酶动力学分析显示，Emodin作为针对ATP的竞争性抑制剂，抑制CKII活性，其Ki值为7.2 μM[1]。Emodin是一种针对包括白血病、肺癌、人舌鳞状细胞癌、结肠癌、胆囊癌、胰腺癌、乳腺癌、人宫颈癌及肝细胞癌等多种癌症细胞的广谱抑制剂。对A549、HepG2、OVCAR-3、HeLa和Madin-Darby Canine Kidney (MDCK)细胞展现的IC50分别为19.54、12.79、25.82、12.14和5.81 μg/mL。Emodin的抗癌机制涉及多种生物路径，如casein kinase Ⅱ和ERK1/2[2]。Emodin还作为活性氧(ROS)产生剂与顺铂联用，用于对T24和J82人膀胱癌细胞的研究。在剂量依赖和时间依赖的方式下，Emodin能够杀死T24和J82细胞，对HCV-29细胞的毒性较低。为研究T24和J82细胞的化疗敏感性，分别选择了20和15 μM作为24小时内的适宜剂量[3]。

经处理的小鼠，使用Emodin (50 mg/kg) 和 Cisplatin (1 mg/kg)，其肿瘤体积显著小于其他组别。此外，各组之间在体重损失方面没有显著差异，且在肝脏、肾脏和心脏切片中未观察到明显的坏死和异常。这些结果表明，Emodin/Cisplatin联合治疗能显著抑制体内肿瘤生长，且无明显副作用。与体外实验一致，TUNEL实验显示Emodin/Cisplatin组合显著增加异种移植瘤细胞的凋亡。Emodin/Cisplatin联合治疗组也比其他组别有更低的MRP1表达[3]。

Emodin is prepared in DMSO and stored, and then diluted with appropriate medium before use[3]. The T24 human bladder cancer cells, the HCV-29 normal bladder epithelial cells and J82 human bladder cancer cells are are cultured in RPMI 1640 medium supplemented with 10 % fetal bovine serum at 37°C in a humidified atmosphere containing 5 % CO2. Cells are seeded in 96-well plates with 2×104 cells per well. The cells are incubated with Emodin for 24 h at different concentrations (0, 5, 10, 20, 30, 40, 50, 60, 70 μM) and chose the critical concentration (20 μM) treated with cells for 0, 6, 12, 24, 48, 72, 96 h. The cells are incubated with cisplatin for 24 h at different concentrations (0, 0.5, 1.0, 1.5, 2.0, 2.5, 3.0 μg/mL). MTT assay is used to analyze the cell viability. Cells are treated with drugs for 24 h and apoptotic rates are assessed with flow cytometry using AnnexinV-fluorescein isothiocyanate (AnnexinV-FITC)/propidium iodide (PI) kit. Samples are prepared according to the manufacturer's instruction and analyzed by a flow cytometry (FCM) Calibur[3].