Khatib Zadeh Zahra, Arab Samaneh, Kazemi Sohrab, Arabhalvaei Mohadeseh, Afraz Elham Sadat, Bahraminasab Marjan
Student Research Committee, Semnan University of Medical Sciences, Semnan, Iran.
Department of Tissue Engineering and Applied Cell Sciences, School of Medicine, Semnan University of Medical Sciences, Semnan, Iran.
Clin Transl Oncol. 2025 Apr 12. doi: 10.1007/s12094-025-03886-1.
Head and neck cancer, as one of the most common cancers, causes the death of many people worldwide every year. The current approaches to treat this cancer have not been successful, and recurrence, drug-resistance development, side effects, and high treatment costs are important problems necessitating the need for more effective drugs and treatment approaches. Epigallocatechin gallate (EGCG) is the most plentiful and biological-active catechin in green tea with proved anticancer effect. However, the stability, low bioavailability, and short half-life, limits its clinical use. Nanocarrier development may overcome these deficiencies by improving pharmacokinetics and pharmacodynamics. Therefore, this study aimed to examine the nano-emulsion containing EGCG for their anticancer activity. First, EGCG nano-emulsion was prepared, which was then characterized by dynamic light scattering (DLS), zeta potential, and Fourier transform infrared spectroscopy (FTIR). The toxicity of the nano-emulsion on the TSCC-1 cancer cell line was assessed by MTT and LDH assays. Cell migration rate, colony-formation ability, the apoptosis rate, and the expression level of BAX, BCL2, and VEGF genes after treatment of cancer cells were assessed. Moreover, the effect of EGCG nano-emulsion on the spheroid growth of TSCC-1 cells in three-dimensional (3D) culture was investigated. The FTIR results demonstrated the presence of EGCG in the nano-emulsion. The size and zeta potential of the nano-emulsion with and without EGCG were 17.53 ± 1.62 nm and - 0.166 ± 0.169 mV, and 14.0 ± 2.3 nm and - 0.266 ± 0.169 mV, respectively. The sustained drug release was observed. Moreover, the MTT assay exhibited that the cytotoxicity of the nano-emulsion was significant at a concentration of 80 µg/mL on TSCC-1 cells. The colony-formation assay revealed no colonies in the groups treated with nano-emulsion containing EGCG compared to the control group. The scratch test also showed the ability of nano-emulsion to inhibit cell migration. Furthermore, the induction of delayed apoptosis by 88.3 ± 3.18% was observed in the group treated with EGCG nano-emulsion at a concentration of 80 µg/mL. The expression of BCL2 and VEGF genes significantly decreased, while that of BAX gene increased. Moreover, the 3D culture showed a decrease in the size and growth of spheroids in the EGCG nano-emulsion-treated group compared to the control group. The results showed that the nano-emulsion containing EGCG has significant anticancer activity (TSCC-1) and may be a suitable treatment option for the management of squamous cell carcinoma of the head and neck.
头颈癌是最常见的癌症之一，每年在全球导致许多人死亡。目前治疗这种癌症的方法并不成功，复发、耐药性产生、副作用和高昂的治疗成本是重要问题，这使得需要更有效的药物和治疗方法。表没食子儿茶素没食子酸酯（EGCG）是绿茶中含量最丰富且具有生物活性的儿茶素，已证实具有抗癌作用。然而，其稳定性、低生物利用度和短半衰期限制了它的临床应用。纳米载体的开发可能通过改善药代动力学和药效学来克服这些不足。因此，本研究旨在检测含EGCG的纳米乳剂的抗癌活性。首先，制备了EGCG纳米乳剂，然后通过动态光散射（DLS）、zeta电位和傅里叶变换红外光谱（FTIR）对其进行表征。通过MTT和LDH测定评估纳米乳剂对TSCC-1癌细胞系的毒性。评估癌细胞处理后细胞迁移率、集落形成能力、凋亡率以及BAX、BCL2和VEGF基因的表达水平。此外，研究了EGCG纳米乳剂对TSCC-1细胞在三维（3D）培养中球体生长的影响。FTIR结果证明纳米乳剂中存在EGCG。含EGCG和不含EGCG的纳米乳剂的粒径和zeta电位分别为17.53±1.62nm和-0.166±0.169mV，以及14.0±2.3nm和-0.266±0.169mV。观察到药物的持续释放。此外，MTT测定表明，纳米乳剂在浓度为80μg/mL时对TSCC-1细胞具有显著的细胞毒性。集落形成测定显示，与对照组相比，用含EGCG的纳米乳剂处理的组中没有集落。划痕试验也显示纳米乳剂具有抑制细胞迁移的能力。此外，在浓度为80μg/mL的EGCG纳米乳剂处理组中观察到延迟凋亡诱导率为88.3±3.18%。BCL2和VEGF基因的表达显著降低，而BAX基因的表达增加。此外，3D培养显示，与对照组相比，EGCG纳米乳剂处理组中球体的大小和生长有所减小。结果表明，含EGCG的纳米乳剂具有显著的抗癌活性（针对TSCC-1），可能是头颈部鳞状细胞癌治疗的合适选择。
