Liszbinski Raquel B, Romagnoli Graziela G, Gorgulho Carolina M, Basso Caroline R, Pedrosa Valber A, Kaneno Ramon
Department of Microbiology and Immunology, Institute of Bioscience, UNESP, Botucatu SP 18618-000, Brazil.
Department of Chemistry and Biochemistry, Institute of Bioscience, UNESP, Botucatu SP 18618-000, Brazil.
Materials (Basel). 2020 Jan 14;13(2):375. doi: 10.3390/ma13020375.
The aim of the current study is to present a strategy to improve the efficiency of 5-fluorouracil (5-FU), which is widely used as antineoplastic agent against solid tumors-based on the use of gold nanocarriers to overcome the resistance of colorectal cancer cells. 5-FU was loaded on gold nanoparticles (AuNP) coated with anti-EGFR antibodies in order to target them towards colorectal cancer cells that overexpress epidermal growth factor receptors (EGFR). Physicochemical characterization has shown that AuNP size was approximately 20 nm and that AuNP functionalization led to spherical nanoparticles. Flow cytometry allowed observing that some compounds synthesized by our research group have induced apoptosis/necrosis and impaired the proliferation of colon cancer cell lines 'HCT-116' and 'HT-29'. The antibody/drug combination in AuNP (AuNP 5FU EGFR) has improved the apoptosis rate and impaired cell proliferation in both cell lines, regardless of the exposure time. Overall, these results have shown that AuNP functionalization with monoclonal antibodies focused on delivering 5-FU to tumor cells is an exciting strategy against colorectal cancer.
本研究的目的是提出一种提高5-氟尿嘧啶（5-FU）效率的策略，5-FU作为一种抗实体瘤的抗肿瘤药物被广泛使用，该策略基于使用金纳米载体来克服结肠癌细胞的耐药性。5-FU被负载在涂有抗表皮生长因子受体（EGFR）抗体的金纳米颗粒（AuNP）上，以便将它们靶向到过表达表皮生长因子受体（EGFR）的结肠癌细胞。物理化学表征表明，AuNP的尺寸约为20nm，并且AuNP功能化导致形成球形纳米颗粒。流式细胞术观察到，我们研究小组合成的一些化合物可诱导凋亡/坏死，并损害结肠癌细胞系“HCT-116”和“HT-29”的增殖。AuNP中的抗体/药物组合（AuNP 5FU EGFR）在两种细胞系中均提高了凋亡率并损害了细胞增殖，且与暴露时间无关。总体而言，这些结果表明，用单克隆抗体对AuNP进行功能化以将5-FU递送至肿瘤细胞是一种针对结肠癌的令人兴奋的策略。
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