二甲脲乙酸地米滋（DIZE）是一种经FDA认可的小分子，被用于治疗非洲睡眠病。体内研究表明，DIZE可能对各种人类疾病有利。然而，关于DIZE对人类癌细胞的影响，目前资料非常有限。本研究旨在使用人子宫颈癌细胞株Hela，研究DIZE的细胞毒性反应。WST-1细胞增殖试验显示，DIZE以剂量依赖的方式抑制Hela细胞的存活能力，并且观察到的反应与Ki67和PCNA细胞增殖标志物的下调有关。乙酸地米滋处理后的细胞经吖啶橙乙锭和JC-10染料染色显示细胞死亡和线粒体内部电位（Ψm）丧失，与DMSO（溶剂）对照相比。DIZE处理后的细胞免疫荧光染色结果显示升高的caspase 3活性。DIZE处理后的细胞下调了G1/S相关基因CCNA2和CDC25A、S期相关基因MCM3和PLK4，以及G2/S期转换/有丝分裂相关基因Aurka和PLK1的mRNA表达。这些效应与Furin、c-Myc和FOXM1致癌基因的mRNA表达下调相关。这些结果表明，DIZE可能在其他癌症类型中产生影响，是首个评估DIZE对人子宫颈癌细胞影响的研究。© 2023 Wiley Periodicals LLC.

Diminazene aceturate (DIZE) is an FDA-listed small molecule known for the treatment of African sleeping sickness. In vivo studies showed that DIZE may be beneficial for a range of human ailments. However, there is very limited information on the effects of DIZE on human cancer cells. The current study aimed to investigate the cytotoxic responses of DIZE, using the human carcinoma Hela cell line. WST-1 cell proliferation assay showed that DIZE inhibited the viability of Hela cells in a dose-dependent manner and the observed response was associated with the downregulation of Ki67 and PCNA cell proliferation markers. DIZE-treated cells stained with acridine orange-ethidium and JC-10 dye revealed cell death and loss of mitochondrial membrane potential (Ψm), compared with DMSO (vehicle) control, respectively. Cellular immunofluorescence staining of DIZE-treated cells showed upregulation of caspase 3 activities. DIZE-treated cells showed downregulation of mRNA for G1/S genes CCNA2 and CDC25A, S-phase genes MCM3 and PLK4, and G2/S phase transition/mitosis genes Aurka and PLK1. These effects were associated with decreased mRNA expression of Furin, c-Myc, and FOXM1 oncogenes. These results suggested that DIZE may be considered for its effects on other cancer types. To the best of our knowledge, this is the first study to evaluate the effect of DIZE on human cervical cancer cells.© 2023 Wiley Periodicals LLC.