(-)-表没食子儿茶素-3-没食子酸酯 (EGCG) 封装的 NP 增强了对结肠癌细胞系的抗癌活性。
Enhanced anticancer activity of (-)-epigallocatechin-3-gallate (EGCG) encapsulated NPs towards colon cancer cell lines.
发表日期:2024 May 29
作者:
Tanushree Das, Sanchaita Mondal, Sujata Das, Sanjib Das, Krishna DasSaha
来源:
Cellular & Molecular Immunology
摘要:
(-)-表没食子儿茶素-3-没食子酸酯 (EGCG) 是绿茶的一种生物活性多酚,对多种癌细胞具有化学预防作用。携带不同配体的纳米颗粒(NP)能够与不同癌细胞上的受体特异性相互作用,从而有效释放细胞毒性药物。在本研究中,我们使用 PLGA(聚丙交酯-乙交酯)制备了 EGCG 包埋的纳米颗粒。 PEG(聚乙二醇)和叶酸(FA)通过双乳液溶剂蒸发(DESE)方法制备PLGA-EGCG(P-E)、PLGA-PEG-EGCG(PP-E)和PLGA-PEG-FA-EGCG( PPF-E) 纳米制剂已通过 1H NMR 和 FT-IR 技术、AFM、DLS 进行了表征。 PPF-E NPs 的平均尺寸为 220nm。 Zeta 电位分析证实了纳米颗粒的稳定性。用制备的 NP 和游离 EGCG (0-140μM) 处理 HCT 116、HT-29、HCT-15 和 HEK 293 细胞。结果显示,与 HT-29 相比,PPF-E NPs 对人叶酸受体阳性 (FR) 结直肠癌细胞 (CRC) 的递送、摄取和细胞毒性有所改善,主要是对 HCT116,但对叶酸阴性细胞没有改善(FR-) 为 HCT-15。与其他两种 NP 和游离 EGCG 相比,在缺乏 NAC(N-乙酰基-L-半胱氨酸)的情况下,PPF-E NP 可以增强细胞内活性氧 (ROS) 水平,提高 DNA 碎片水平,并在较高剂量下增加细胞凋亡。总之,PPF-E NPs 在 HCT 116 细胞中比 PP-E、P-E 和游离 EGCG 发挥更大的功效。
(-)-Epigallocatechin-3-gallate (EGCG), a bioactive polyphenol of green tea has chemo- preventive effects against various cancer cells. Nanoparticles (NPs) carrying different ligands are able to specifically interact with their receptors on different cancer cells can provide effective release of cytotoxic drugs. In the present study we have prepared EGCG entrapped nanoparticles using PLGA (poly lactide-co-glycolide). PEG (poly ethylene glycol) and Folic acid (FA) via double emulsion solvent evaporation (DESE) method and the prepared PLGA-EGCG (P-E), PLGA-PEG-EGCG (PP-E) and PLGA-PEG-FA-EGCG (PPF-E) Nanoformulations had been characterized with 1H NMR and FT-IR techniques, AFM, DLS. PPF-E NPs showed an average size of 220nm. Analysis of Zeta potential confirmed the stability of NPs. HCT 116, HT-29, HCT-15, and HEK 293 cells were treated with both the prepared NPs and free EGCG (0-140μM). Result showed PPF-E NPs had improved delivery, uptake and cell cytotoxicity towards in Human folic acid receptor- positive (FR+) colorectal cancer cells (CRCs) as mainly on HCT116 compared to HT-29, but not on the folic acid - negative cells (FR -) as HCT-15. PPF-E NPs enhanced intracellular reactive oxygen species (ROS) level in absence of NAC (N-acetyl-l-cysteine), elevated DNA fragmentation level, and increased apoptotic cell death at higher doses compared to other two NPs and free EGCG. In conclusion PPF-E NPs exerted greater efficacy than PP-E, P-E and free EGCG in HCT 116 cells.