Glioblastoma multiforme (GBM) is a prevalent primary brain tumor. However, no specific therapeutic drug has been developed for it. Nuclear factor erythroid 2-related factor 2 (Nrf2) is a crucial transcription factor involved in the cellular response to oxidative stress. Numerous studies have demonstrated that Nrf2 plays a pivotal role in GBM angiogenesis, and inhibiting Nrf2 can significantly enhance patient prognosis. Using virtual screening technology, we examined our in-house library and identified pinosylvin as a potential compound with high activity. Pinosylvin exhibited robust hydrogen bond and Π-Π interaction with Nrf2. Cell experiments revealed that pinosylvin effectively reduced the proliferation of U87 tumor cells by regulating Nrf2 and demonstrated greater inhibitory activity than temozolomide. Consequently, we believe that this study will offer valuable guidance for the future development of highly efficient therapeutic drugs for GBM.

中文翻译：

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用于治疗多形性胶质母细胞瘤的 Nrf2 调节剂的设计、合成和生物学评价

多形性胶质母细胞瘤（GBM）是一种常见的原发性脑肿瘤。然而，尚未开发出针对该疾病的特效治疗药物。核因子红细胞 2 相关因子 2 (Nrf2) 是参与细胞氧化应激反应的关键转录因子。大量研究表明Nrf2在GBM血管生成中发挥着关键作用，抑制Nrf2可以显着改善患者预后。使用虚拟筛选技术，我们检查了我们的内部图书馆，并确定松西林是一种具有高活性的潜在化合物。 Pinosylvin 与 Nrf2 表现出强大的氢键和 Π-Π 相互作用。细胞实验表明，pinosylvin 通过调节 Nrf2 有效减少 U87 肿瘤细胞的增殖，并表现出比替莫唑胺更强的抑制活性。因此，我们相信这项研究将为未来开发高效的 GBM 治疗药物提供有价值的指导。