Bufalin, a cardiotonic steroid derived from the Chinese toad (Bufo gargarizans), has demonstrated potent anticancer properties across various cancer types, positioning it as a promising therapeutic candidate. However, comprehensive mechanistic studies specific to head and neck cancers have been lacking. Our study aimed to bridge this gap by investigating bufalin’s mechanisms of action in head and neck cancer cells. Using several methods, such as Western blotting, immunofluorescence, and flow cytometry, we observed bufalin’s dose-dependent reduction in cell viability, disruption of cell membrane integrity, and inhibition of colony formation in both HPV-positive and HPV-negative cell lines. Bufalin induces apoptosis through the modulation of apoptosis-related proteins, mitochondrial function, and reactive oxygen species production. It also arrests the cell cycle at the G2/M phase and attenuates cell migration while affecting epithelial–mesenchymal transition markers and targeting pivotal signaling pathways, including Wnt/β-catenin, EGFR, and NF-κB. Additionally, bufalin exerted immunomodulatory effects by polarizing macrophages toward the M1 phenotype, bolstering antitumor immune responses. These findings underscore bufalin’s potential as a multifaceted therapeutic agent against head and neck cancers, targeting essential pathways involved in proliferation, apoptosis, cell cycle regulation, metastasis, and immune modulation. Further research is warranted to validate these mechanisms and optimize bufalin’s clinical application.
蟾毒灵是一种从中华大蟾蜍中提取的强心类固醇，已在多种癌症类型中显示出强大的抗癌特性，使其成为一种有前景的治疗候选药物。然而，针对头颈部癌症的全面机制研究尚显不足。本研究旨在通过探究蟾毒灵在头颈部癌细胞中的作用机制来填补这一空白。通过蛋白质印迹、免疫荧光和流式细胞术等多种方法，我们观察到蟾毒灵在HPV阳性和HPV阴性细胞系中均能剂量依赖性地降低细胞活力、破坏细胞膜完整性并抑制集落形成。蟾毒灵通过调节凋亡相关蛋白、线粒体功能和活性氧生成来诱导细胞凋亡。它还能将细胞周期阻滞在G2/M期，减弱细胞迁移能力，同时影响上皮-间质转化标志物，并靶向包括Wnt/β-catenin、EGFR和NF-κB在内的关键信号通路。此外，蟾毒灵通过将巨噬细胞极化为M1表型发挥免疫调节作用，从而增强抗肿瘤免疫反应。这些发现凸显了蟾毒灵作为多靶点治疗头颈部癌症药物的潜力，其作用涉及增殖、凋亡、细胞周期调控、转移和免疫调节等关键通路。需要进一步研究以验证这些机制并优化蟾毒灵的临床应用。
肿瘤(癌症)患者之家