α-茄碱是一种配糖生物碱，常见于茄科植物（Solanum）中，对人体有毒性作用。除其他外，已知它可以抑制肿瘤细胞增殖并诱导肿瘤细胞系凋亡。由于其作为肿瘤治疗剂的潜力，当前的研究调查了 α-龙葵碱对头颈鳞状细胞癌 (HNSCC) 的影响。此外，在亚毒性 α-龙葵碱浓度下评估了对人脐静脉内皮细胞 (HUVEC) 的基因毒性和抗血管生成作用。在两种人 HNSCC 细胞系（FaDu 咽癌细胞和 CAL-33 舌癌细胞）以及 HUVEC 中测量了细胞毒性和凋亡率。在 α-龙葵碱处理后 24 小时进行 MTT 和膜联蛋白 V 分析，剂量逐渐增加至 30 µM，以确定细胞毒性浓度。此外，使用单细胞凝胶电泳（彗星测定）分析了 HUVEC 中 1、2、4 和 6 µM 亚毒性浓度的遗传毒性。在毛细管形成试验中评估了对 HUVEC 的抗血管生成作用。 MTT 测定表明 FaDu 和 CAL-33 癌细胞系中浓度依赖性活力丧失的诱导，而膜联蛋白 V 测试表明 α-茄碱诱导的细胞死亡主要与细胞凋亡无关。在 HUVEC 中，细胞毒性作用在较低浓度下发生。在 HUVEC 中，亚毒性剂量下未检测到基因毒性或血管生成抑制。总之，α-茄碱对恶性和非恶性细胞均具有细胞毒作用，但只有在恶性细胞中浓度较高时才能观察到这种作用。与文献中的现有数据相比，肿瘤细胞凋亡不如坏死明显。在良性细胞的亚毒性范围内缺乏基因毒性和抗血管生成作用是有希望的，因为这有利于潜在的治疗应用。然而，总而言之，非恶性细胞中的细胞毒性仍然是 α-茄碱作为人类肿瘤治疗剂应用的严重障碍。版权所有：© 2024 Von Fournier 等人。

α-solanine is a glycoalkaloid that is commonly found in nightshades (Solanum) and has a toxic effect on the human organism. Among other things, it is already known to inhibit tumor cell proliferation and induce apoptosis in tumor cell lines. Due to its potential as a tumor therapeutic, the current study investigated the effect of α-solanine on head and neck squamous cell carcinoma (HNSCC). In addition, genotoxic and antiangiogenic effects on human umbilical vein endothelial cells (HUVECs) were evaluated at subtoxic α-solanine concentrations. Cytotoxicity and apoptosis rates were measured in two human HNSCC cell lines (FaDu pharynx carcinoma cells and CAL-33 tongue carcinoma cells), as well as in HUVECs. MTT and Annexin V analyses were performed 24 h after α-solanine treatment at increasing doses up to 30 µM to determine cytotoxic concentrations. Furthermore, genotoxicity at subtoxic concentrations of 1, 2, 4 and 6 µM in HUVECs was analyzed using single-cell gel electrophoresis (comet assay). The antiangiogenic effect on HUVECs was evaluated in the capillary tube formation assay. The MTT assay indicated an induction of concentration-dependent viability loss in FaDu and CAL-33 cancer cell lines, whereas the Annexin V test revealed α-solanine-induced cell death predominantly independent from apoptosis. In HUVECs, the cytotoxic effect occurred at lower concentrations. No genotoxicity or inhibition of angiogenesis were detected at subtoxic doses in HUVECs. In summary, α-solanine had a cytotoxic effect on both malignant and non-malignant cells, but this was only observed at higher concentrations in malignant cells. In contrast to existing data in the literature, tumor cell apoptosis was less evident than necrosis. The lack of genotoxicity and antiangiogenic effects in the subtoxic range in benign cells are promising, as this is favorable for potential therapeutic applications. In conclusion, however, the cytotoxicity in non-malignant cells remains a severe hindrance for the application of α-solanine as a therapeutic tumor agent in humans.Copyright: © 2024 Von Fournier et al.