Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging.,ACS Medicinal Chemistry Letters

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Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-05-18 , DOI: 10.1021/acsmedchemlett.0c00031
Xiangmei Jin ₁ , Jun Zhang ₂ , Xiaoyan Jin ₁ , Lan Liu ₂ , Xizhe Tian ₁

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In this work, a folate receptor (FR)-mediated dual-targeting drug delivery system was synthesized to improve the tumor-killing efficiency and inhibit the side effects of anticancer drugs. We designed and synthesized an FR-mediated fluorescence probe (FA-Rho) and FR-mediated cathepsin B-sensitive drug delivery system (FA-GFLG-SN38). FA-GFLG-SN38 is composed of the FR ligand (folic acid, FA), the tetrapeptide substrate for cathepsin B (GFLG), and an anticancer drug (SN38). The rhodamine B (Rho)-labeled probe FA-Rho is suitable for specific fluorescence imaging of SK-Hep-1 cells overexpressing FR and inactive in FR-negative A549 and 16-HBE cells. FA-GFLG-SN38 exhibited strong cytotoxicity against FR-overexpressing SK-Hep-1, HeLa, and Siha cells, with IC₅₀ values of 2–3 μM, but had no effect on FR-negative A549 and 16-HBE cells. The experimental results show that the FA-CFLG-SN38 drug delivery system proposed by us can effectively inhibit tumor proliferation in vitro, and it can be adopted for the diagnostics of tumor tissues and provide a basis for effective tumor therapy.

中文翻译：

用于选择性癌细胞死亡和成像的叶酸受体靶向和组织蛋白酶 B 敏感的药物递送系统。

在这项工作中，合成了一种叶酸受体（FR）介导的双靶向给药系统，以提高肿瘤杀伤效率并抑制抗癌药物的副作用。我们设计并合成了 FR 介导的荧光探针 (FA-Rho) 和 FR 介导的组织蛋白酶 B 敏感药物递送系统 (FA-GFLG-SN38)。FA-GFLG-SN38 由 FR 配体（叶酸，FA）、组织蛋白酶 B (GFLG) 的四肽底物和抗癌药物 (SN38) 组成。罗丹明 B (Rho) 标记的探针 FA-Rho 适用于过表达 FR 且在 FR 阴性 A549 和 16-HBE 细胞中无活性的 SK-Hep-1 细胞的特异性荧光成像。FA-GFLG-SN38 对 FR 过表达的 SK-Hep-1、HeLa 和 Siha 细胞表现出很强的细胞毒性，IC ₅₀2-3 μM 的值，但对 FR 阴性 A549 和 16-HBE 细胞没有影响。实验结果表明，我们提出的FA-CFLG-SN38给药系统在体外能有效抑制肿瘤增殖，可用于肿瘤组织的诊断，为有效的肿瘤治疗提供依据。

更新日期：2020-05-18

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