Department of Molecular Science, School of Medicine, University of Texas Rio Grande Valley, Edinburg, TX 78539, USA.
These authors contributed equally to this work.
Oncotarget. 2022 May 5;13:642-658. doi: 10.18632/oncotarget.28227. eCollection 2022.
Glioblastoma multiforme (GBM) is one of the deadliest cancers of the brain. Its ability to infiltrate healthy brain tissues renders it difficult to remove surgically. Furthermore, it exhibits high rates of radio- and chemoresistance, making the survival rates of patients with GBM poor. Therefore, novel effective therapies for GBM remain urgently in demand. Niclosamide is an anti-helminthic drug and recently it has been receiving attention due to its reported anticancer effects in cancer models, including GBM. Furthermore, camptothecin (CPT) is a naturally-occurring alkaloid and has been previously reported to be a potential chemotherapeutic agent by targeting the nuclear topoisomerase I. In the present study, the possible combined chemotherapeutic effects of niclosamide and CPT on the human glioblastoma cell line U87 MG was investigated by MTT assay and western blot analysis. Niclosamide exhibited synergistic activities with CPT to suppress the proliferation of U87 MG cells. Additionally, niclosamide suppressed cell proliferation and induced cell death mainly by triggering ER stress and autophagy, whilst CPT induced cell apoptosis mainly through p53-mediated mitochondrial dysfunction and activation of the MAPK (ERK/JNK) pathways. Overall, these findings suggest that co-administration of niclosamide and CPT may provide a novel therapeutic treatment strategy for GBM.
多形性胶质母细胞瘤(GBM)是最致命的脑癌之一。它浸润健康脑组织的能力使其难以通过手术切除。此外,它还表现出高放射和化学抗性,使得 GBM 患者的生存率较差。因此,新型有效的 GBM 治疗方法仍然迫切需要。氯硝柳胺是一种抗蠕虫药物,最近由于其在癌症模型中报告的抗癌作用而受到关注,包括 GBM。此外,喜树碱(CPT)是一种天然存在的生物碱,先前已被报道通过靶向核拓扑异构酶 I 作为一种潜在的化疗药物。在本研究中,通过 MTT 测定和 Western blot 分析研究了氯硝柳胺和 CPT 对人胶质母细胞瘤细胞系 U87 MG 的联合化疗作用。氯硝柳胺与 CPT 表现出协同作用,抑制 U87 MG 细胞的增殖。此外,氯硝柳胺主要通过触发内质网应激和自噬来抑制细胞增殖并诱导细胞死亡,而 CPT 主要通过 p53 介导的线粒体功能障碍和 MAPK(ERK/JNK)途径的激活诱导细胞凋亡。总的来说,这些发现表明,氯硝柳胺和 CPT 的联合给药可能为 GBM 提供一种新的治疗策略。