Capelôa Tânia, Caramelo Francisco, Fontes-Ribeiro Carlos, Gomes Célia, Silva Ana P
Laboratory of Pharmacology and Experimental Therapeutics, Faculty of Medicine, University of Coimbra, Azinhaga de Santa Comba, Celas, 3000-548, Coimbra, Portugal.
Neurotox Res. 2014 Oct;26(3):216-27. doi: 10.1007/s12640-014-9464-1. Epub 2014 Mar 21.
Glioblastoma multiforme (GBM) is the most common and malignant primary brain tumor with a high mortality rate. Doxorubicin (DOX) and methotrexate (MTX) showed to be effective against a wide range of tumors, but its use in GBM treatment is limited in part due to the inability to cross the blood-brain barrier (BBB). Based on recent studies demonstrating that methamphetamine (METH) increases BBB permeability, we hypothesized that it could be used as a pharmacological tool to allow the entry of potential therapeutic drugs into the brain. Nevertheless, before attempting this approach it is crucial to understand the cytotoxicity of such drug combinations. Herein, we evaluated the effects of METH on cell viability, migration, chemotaxis, and cell cycle, as well as its modulator effects on DOX or MTX-induced cytotoxicity in a human U118 GBM cell line. Our results demonstrated that both chemotherapeutic drugs DOX and MTX induced a pronounced decrease in cell viability, migration, and chemotaxis, and led to a cell cycle arrest at G2 and S phases, respectively. Additionally, METH (1 μM) neither interfered with U-118 cell viability, migration, or cell cycle nor modified DOX- or MTX-induced cytotoxicity. Noteworthy, METH by itself impaired cell chemotaxis with a similar effect to that induced by DOX or MTX alone. Overall, we can conclude that both DOX and MTX are highly cytotoxic against GBM cells and that METH, at a concentration previously shown to increase endothelial cell permeability without leading to cell death, does not interfere with the cytotoxicity of both chemotherapeutic drugs.
多形性胶质母细胞瘤(GBM)是最常见且恶性程度最高的原发性脑肿瘤,死亡率很高。阿霉素(DOX)和甲氨蝶呤(MTX)对多种肿瘤显示出有效,但它们在GBM治疗中的应用受到限制,部分原因是无法穿过血脑屏障(BBB)。基于最近的研究表明甲基苯丙胺(METH)可增加血脑屏障通透性,我们推测它可作为一种药理学工具,使潜在的治疗药物进入大脑。然而,在尝试这种方法之前,了解此类药物组合的细胞毒性至关重要。在此,我们评估了METH对人U118 GBM细胞系的细胞活力、迁移、趋化性和细胞周期的影响,以及其对DOX或MTX诱导的细胞毒性的调节作用。我们的结果表明,两种化疗药物DOX和MTX均导致细胞活力、迁移和趋化性显著降低,并分别导致细胞周期在G2期和S期停滞。此外,METH(1μM)既不干扰U-118细胞的活力、迁移或细胞周期,也不改变DOX或MTX诱导的细胞毒性。值得注意的是,METH本身会损害细胞趋化性,其效果与单独使用DOX或MTX诱导的效果相似。总体而言,我们可以得出结论,DOX和MTX对GBM细胞均具有高度细胞毒性,而METH在先前显示可增加内皮细胞通透性而不导致细胞死亡的浓度下,不会干扰两种化疗药物的细胞毒性。