Institute of Translational Pharmacology, National Research Council of Italy (CNR), 00133 Rome, Italy.
National Center for Drug Research and Evaluation, Italian National Institute of Health (ISS), 00161 Rome, Italy.
Int J Mol Sci. 2024 Sep 30;25(19):10572. doi: 10.3390/ijms251910572.
Glioblastoma (GBL) is one of the more malignant primary brain tumors; it is currently treated by a multimodality strategy including surgery, and radio- and chemotherapy, mainly consisting of temozolomide (TMZ)-based chemotherapy. Tumor relapse often occurs due to the establishment of TMZ resistance, with a patient median survival time of <2 years. The identification of natural molecules with strong anti-tumor activity led to the combination of these compounds with conventional chemotherapeutic agents, developing protocols for integrated anticancer therapies. Curcumin (CUR), resveratrol (RES), and its glucoside polydatin (PLD) are widely employed in the pharmaceutical and nutraceutical fields, and several studies have demonstrated that the combination of these natural products was more cytotoxic than the individual compounds alone against different cancers. Some of us recently demonstrated the synergistic efficacy of the sublingual administration of a new nutraceutical formulation of CUR+PLD in reducing tumor size and improving GBL patient survival. To provide some experimental evidence to reinforce these clinical results, we investigated if pretreatment with a combination of CUR+PLD can improve TMZ cytotoxicity on GBL cells by analyzing the effects on cell cycle, viability, morphology, expression of proteins related to cell proliferation, differentiation, apoptosis or autophagy, and the actin network. Cell viability was assessed using the MTT assay or a CytoSmart cell counter. CalcuSyn software was used to study the CUR+PLD synergism. The morphology was evaluated by optical and scanning electron microscopy, and protein expression was analyzed by Western blot. Flow cytometry was used for the cell cycle, autophagic flux, and apoptosis analyses. The results provide evidence that CUR and PLD, acting in synergy with each other, strongly improve the efficacy of alkylating anti-tumor agents such as TMZ on drug-resistant GBL cells through their ability to affect survival, differentiation, and tumor invasiveness.
胶质母细胞瘤(GBL)是一种较为恶性的原发性脑肿瘤;目前,它的治疗采用多模态策略,包括手术和放射及化学疗法,主要由替莫唑胺(TMZ)为基础的化疗组成。由于建立了 TMZ 耐药性,肿瘤复发经常发生,患者的中位生存时间<2 年。由于具有很强抗肿瘤活性的天然分子的鉴定,导致这些化合物与常规化疗药物联合使用,从而开发了综合抗癌疗法的方案。姜黄素(CUR)、白藜芦醇(RES)及其糖苷白藜芦醇苷(PLD)广泛应用于制药和营养保健品领域,多项研究表明,这些天然产物的联合使用比单独使用对不同癌症的细胞毒性更强。我们中的一些人最近证明了舌下给予 CUR+PLD 的新营养保健品配方在减少肿瘤大小和提高 GBL 患者生存方面的协同功效。为了提供一些实验证据来加强这些临床结果,我们研究了 CUR+PLD 预处理是否可以通过分析对细胞周期、活力、形态、与细胞增殖、分化、凋亡或自噬相关的蛋白质表达以及肌动蛋白网络的影响,来提高 TMZ 对 GBL 细胞的细胞毒性。使用 MTT 测定法或 CytoSmart 细胞计数器评估细胞活力。使用 CalcuSyn 软件研究 CUR+PLD 的协同作用。通过光学和扫描电子显微镜评估形态,通过 Western blot 分析蛋白质表达。使用流式细胞术进行细胞周期、自噬通量和凋亡分析。结果提供了证据,表明 CUR 和 PLD 通过影响生存、分化和肿瘤侵袭性,协同作用强烈提高了烷基化抗肿瘤药物如 TMZ 对耐药性 GBL 细胞的疗效。