Ichikawa Karen, Johnson Hannah M, Curtis Maurice A, Biswas Nandita, Singh Snigdha, Khachatryan Hasmik N, Gater Anastasia E, Lin Simon X, Sperry Jonathan
School of Chemical Sciences, University of Auckland, 23 Symonds Street, Auckland 1010, New Zealand; Centre for Brain Research, University of Auckland, Auckland, New Zealand; Department of Anatomy and Medical Imaging, University of Auckland, Auckland, New Zealand.
School of Chemical Sciences, University of Auckland, 23 Symonds Street, Auckland 1010, New Zealand.
Bioorg Med Chem. 2025 Apr 15;121:118051. doi: 10.1016/j.bmc.2024.118051. Epub 2024 Dec 25.
Glioblastoma multiforme (GBM), classified as a grade IV astrocytoma, is the most aggressive and deadly form of glioma, characterized by rapid progression, extensive genetic heterogeneity, and resistance to conventional therapies. Despite advancements in surgical techniques, radiation therapy, and the frontline chemotherapeutic agent temozolomide, the prognosis for GBM patients remains poor, with a median survival of 15 months and a 5-year survival rate of approximately 7 %. The absence of effective long-term treatments underscores the urgent, unmet clinical need for novel therapeutic strategies to improve patient outcomes. Natural products, particularly alkaloids, have garnered attention as a rich source of bioactive compounds with diverse pharmacological properties. Alkaloids, a structurally diverse group of natural products, are renowned for their chemotherapeutic properties and ability to cross the blood-brain barrier (BBB), making them promising candidates for glioma therapy. This review systematically examines all reported heteroaromatic alkaloids with documented anti-glioma activities, highlighting their mechanisms of action where available. By providing a comprehensive resource, it aims to facilitate the identification and optimisation of alkaloid-based compounds for glioma-targeted drug discovery. Additionally, this review emphasizes the importance of incorporating natural products into the drug development pipeline to address the pressing challenges associated with glioma, particularly GBM treatment.
多形性胶质母细胞瘤(GBM)被归类为IV级星形细胞瘤,是最具侵袭性和致命性的胶质瘤形式,其特征为进展迅速、广泛的基因异质性以及对传统疗法的耐药性。尽管手术技术、放射治疗和一线化疗药物替莫唑胺有所进展,但GBM患者的预后仍然很差,中位生存期为15个月,5年生存率约为7%。缺乏有效的长期治疗凸显了对改善患者预后的新型治疗策略的迫切临床需求。天然产物,特别是生物碱,作为具有多种药理特性的生物活性化合物的丰富来源而受到关注。生物碱是一类结构多样的天然产物,以其化疗特性和穿越血脑屏障(BBB)的能力而闻名,使其成为胶质瘤治疗的有希望的候选药物。本综述系统地研究了所有报道的具有抗胶质瘤活性的杂环芳香生物碱,并在可行的情况下突出了它们的作用机制。通过提供全面的资源,旨在促进用于胶质瘤靶向药物发现的基于生物碱的化合物的鉴定和优化。此外,本综述强调了将天然产物纳入药物开发流程以应对与胶质瘤特别是GBM治疗相关的紧迫挑战的重要性。