Department of Biomedical Sciences, College of Medicine and Program in Biomedical Science and Engineering, Inha University, Incheon 22332, Republic of Korea.
Department of Biomedical Sciences, College of Medicine and Program in Biomedical Science and Engineering, Inha University, Incheon 22332, Republic of Korea.
Int J Mol Med. 2025 Jan;55(1). doi: 10.3892/ijmm.2024.5458. Epub 2024 Nov 14.
Pancreatic ductal adenocarcinoma (PDAC) is a lethal malignancy with limited therapeutic options. Cisplatin is a primary chemotherapeutic agent utilized in combination with other drugs or radiotherapy for PDAC treatment. However, the severe side effects of cisplatin often necessitate discontinuation of therapy and drug resistance in tumor cells poses significant clinical challenges. Therefore, the development of effective therapeutic strategies is imperative. The present study investigated whether repositioning of the antipsychotic drug aripiprazole could sensitize the anticancer activity of cisplatin in pancreatic cancer at doses calculated by the combination index. The findings indicated that aripiprazole combined with cisplatin to suppress pancreatic cancer cell growth. Notably, the combination notably increased the expression of apoptosis markers, including cleaved caspase‑3, compared with cisplatin alone. Additionally, this combination effectively decreased XIAP and MCL‑1 expression via mitochondrial membrane potential change as revealed by JC‑1 assay, thereby inducing apoptosis. Furthermore, in fluid shear stress assay, the combination of aripiprazole and cisplatin notably inhibited cell adhesion and tumor spheroid formation. Mechanistically, phospho‑kinase array profiles showed that the enhanced anticancer efficacy of the combination treatment could be attributed to the inhibition of STAT3 signaling, which led to a significant reduction in tumor growth in a pancreatic cancer animal model. The results showed that the repositioning of aripiprazole inhibits cancer cell growth by blocking the STAT3 signaling pathway and effectively enhancing cisplatin‑induced apoptosis, thereby suggesting that the combination of aripiprazole and cisplatin may be a potent chemotherapeutic strategy for the treatment of pancreatic cancer.
胰腺导管腺癌(PDAC)是一种致命的恶性肿瘤,治疗选择有限。顺铂是一种主要的化疗药物,与其他药物或放射疗法联合用于 PDAC 治疗。然而,顺铂的严重副作用常常需要停止治疗,并且肿瘤细胞的耐药性也带来了重大的临床挑战。因此,开发有效的治疗策略至关重要。本研究探讨了抗精神病药物阿立哌唑的重新定位是否可以在计算组合指数的剂量下增强顺铂对胰腺癌的抗癌活性。研究结果表明,阿立哌唑与顺铂联合抑制胰腺癌细胞生长。值得注意的是,与单独使用顺铂相比,该联合用药显著增加了凋亡标志物的表达,包括 cleaved caspase-3。此外,通过 JC-1 测定显示,该联合用药通过线粒体膜电位变化有效降低了 XIAP 和 MCL-1 的表达,从而诱导细胞凋亡。此外,在流体切应力试验中,阿立哌唑与顺铂的联合用药显著抑制了细胞黏附和肿瘤球体形成。从机制上讲,磷酸化激酶谱分析表明,联合治疗增强的抗癌效果可归因于 STAT3 信号通路的抑制,这导致胰腺癌动物模型中的肿瘤生长显著减少。结果表明,阿立哌唑的重新定位通过阻断 STAT3 信号通路抑制癌细胞生长,并有效增强顺铂诱导的细胞凋亡,这提示阿立哌唑和顺铂的联合用药可能是治疗胰腺癌的一种有效的化疗策略。