Liang Simin, Zhou Xiaojia, Cai Duo, Rodrigues-Lima Fernando, Chi Jianxiang, Wang Li
Department of Hematology, The First Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Department of Hematology, The Third Affiliated Hospital of Chongqing Medical University, Chongqing, China.
Front Cell Dev Biol. 2021 Sep 9;9:685954. doi: 10.3389/fcell.2021.685954. eCollection 2021.
Chidamide (CDM), a novel histone deacetylase inhibitor, is currently used for patients with peripheral T-cell lymphoma. Aspirin (ASA), an anti-inflammatory drug, has been shown to exert anticancer activity. Herein, we investigated the effect of CDM combined with ASA on myelodysplastic syndromes-derived acute myeloid leukemia (AML-MDS) cells and explored the underlying mechanism. The putative targets of CDM and ASA were predicted by network pharmacology approach. GO functional and KEGG pathway enrichment analyses were performed by DAVID. Furthermore, experimental validation was conducted by Cell Counting Kit-8 assay, Flow cytometry and Western blotting. Network pharmacology analysis revealed 36 AML-MDS-related overlapping genes that were targets of CDM and ASA, while 10 hub genes were identified by the plug-in cytoHubba in Cytoscape. Pathway enrichment analysis indicated CDM and ASA significantly affected PI3K/AKT signaling pathway. Functional experiments demonstrated that the combination of CDM and ASA had a remarkable synergistic anti-proliferative effect by blocking the cell cycle in G0/G1 phase and inducing apoptosis. Mechanistically, the combination treatment significantly down-regulated the phosphorylation levels of PI3K and AKT. In addition, insulin-like growth factor 1 (IGF-1), an activator of PI3K/AKT pathway, reversed the effects of the combination treatment. Our findings suggested that CDM combined with ASA exerted a synergetic inhibitory effect on cell growth by inactivating PI3K/AKT pathway, which might pave the way for effective treatments of AML-MDS.
西达本胺(CDM)是一种新型组蛋白去乙酰化酶抑制剂,目前用于治疗外周T细胞淋巴瘤患者。阿司匹林(ASA)是一种抗炎药物,已被证明具有抗癌活性。在此,我们研究了CDM联合ASA对骨髓增生异常综合征衍生的急性髓系白血病(AML-MDS)细胞的影响,并探讨了其潜在机制。通过网络药理学方法预测了CDM和ASA的潜在靶点。使用DAVID进行基因本体(GO)功能和京都基因与基因组百科全书(KEGG)通路富集分析。此外,通过细胞计数试剂盒-8法、流式细胞术和蛋白质免疫印迹法进行实验验证。网络药理学分析揭示了36个与AML-MDS相关的重叠基因,这些基因是CDM和ASA的靶点,而通过Cytoscape中的cytoHubba插件鉴定出10个核心基因。通路富集分析表明,CDM和ASA显著影响PI3K/AKT信号通路。功能实验表明,CDM与ASA联合使用通过阻断细胞周期于G0/G1期并诱导凋亡,具有显著的协同抗增殖作用。机制上,联合治疗显著下调了PI3K和AKT的磷酸化水平。此外,PI3K/AKT通路的激活剂胰岛素样生长因子1(IGF-1)逆转了联合治疗的效果。我们的研究结果表明,CDM联合ASA通过使PI3K/AKT通路失活对细胞生长发挥协同抑制作用,这可能为AML-MDS的有效治疗铺平道路。