Data_Sheet_1_Synergistic Effect of Retinoic Acid Polymeric Micelles and Prodrug for the Pharmacodynamic Evaluation of Tumor Suppression.PDF

All-trans retinoic acid (ATRA) is an effective agent that induces differentiation, inhibits cell proliferation, and acts as an anticancer agent. ATRA was successfully conjugated with Pluronic F127 via esterification to enhance its anticancer effects. Pluronic-ATRA showed high cytotoxicity and inhibitory concentrations (IC50) 50% lower than those of ATRA in various breast cancer cell lines (4T1:31.16–8.57 μg/mL; EMT6: 50.48–7.08 μg/mL; MDA-MB-231:37.58–8.99 μg/mL; BT474:25.27–9.09 μg/mL). In combination with chemotherapy, Pluronic-ATRA synergistically enhanced the cytotoxic effects of cisplatin (CDDP). Pluronic-ATRA combined with CDDP effectively suppressed breast tumor growth in vivo. The results of this study demonstrate the potential of Pluronic-ATRA as an anticancer agent that can be used in combination therapy against solid tumors.

全反式维甲酸（ATRA）是一种有效的诱导分化、抑制细胞增殖并具有抗癌作用的药物。通过酯化成功将ATRA与Pluronic F127结合，以增强其抗癌效果。Pluronic-ATRA在多种乳腺癌细胞系中表现出高细胞毒性及抑制浓度（IC50），其值比ATRA低50%（4T1：31.16–8.57 μg/mL；EMT6：50.48–7.08 μg/mL；MDA-MB-231：37.58–8.99 μg/mL；BT474：25.27–9.09 μg/mL）。与化疗药物联合使用时，Pluronic-ATRA与顺铂（CDDP）协同增强了其细胞毒性。Pluronic-ATRA与CDDP联合使用可有效抑制体内乳腺癌肿瘤的生长。本研究结果展示了Pluronic-ATRA作为一种可用于实体瘤联合治疗的抗癌药物的潜力。