Harmaline是β-谷氨酸类生物碱，可从白扁豆的种子中提取。研究表明，Harmaline展现出对肿瘤细胞的强效细胞毒作用。本研究旨在探究Harmaline在体外对胶质母细胞瘤的抗肿瘤作用。对治疗不同剂量的Harmaline的U-87细胞进行了细胞存活率、细胞凋亡和细胞周期阻滞的评估。同时还评估了活性氧生成和细胞凋亡相关基因mRNA的表达。采用明胶酶体原谱法评估了Harmaline对U-87细胞的抗转移作用，测量了基质金属蛋白酶[MMP]-2/-9的酶活，采用刮痕实验评估细胞迁移反应。流式细胞术证明，Harmaline可以抑制胶质母细胞瘤细胞的增殖，诱导次G1期细胞周期阻滞和凋亡性细胞死亡。Harmaline处理还与细胞周期相关基因p21和p53，以及促凋亡的Bax的上调和ROS的诱导有关。明胶酶体原谱法表明，Harmaline通过抑制MMP-2和-9的表达，强烈抑制了转移的必要步骤。此外，Harmaline处理后U-87细胞的迁移显著降低。我们的数据表明，Harmaline在胶质母细胞瘤细胞中具有潜在的细胞毒活性，能够诱导细胞周期阻滞和凋亡、抑制迁移，可能还具有抑制侵袭和转移的作用。© 2023. 作者（们）授予Springer Nature B.V.独家许可。

Harmaline is a β-carboline alkaloid that can be extracted from the seeds of Peganum harmala. Harmaline has been shown to exhibit a potent cytotoxic effect against tumor cells. In this study, the anti-glioblastoma activity of harmaline was investigated in vitro.Cell viability, apoptosis, and cell cycle arrest were assessed in U-87 cells treated with harmaline at different doses. Reactive oxygen species (ROS) generation and the mRNA expression of apoptosis-associated genes were assessed. The anti-metastatic effect of harmaline on U-87 cells was evaluated by gelatin zymography assay where matrix metalloproteinase [MMP]-2/-9 enzymatic activity was measured, and the scratch assay was used to assess migratory responses. Flow cytometry demonstrated that harmaline could suppress the proliferation and induce sub-G1 cell cycle arrest and apoptotic cell death in glioblastoma cells. Harmaline treatment was also associated with an upregulation of the cell cycle-related genes, p21 and p53, and pro-apoptotic Bax, as well as the induction of ROS. The zymography assay indicated that the essential steps of metastasis were potently suppressed by harmaline through inhibiting the expression of MMP-2 and - 9. In addition, the migration of U-87 cells was significantly reduced after harmaline treatment.Our data suggest a basis for further research of harmaline which has potential cytotoxic activities in glioblastoma cells; inducing cell cycle arrest and apoptosis, repression of migration, possibly invasion, and metastasis.© 2023. The Author(s), under exclusive licence to Springer Nature B.V.