摘要

Innovative and personalized therapeutic approaches result from the identification and control of individual aberrantly expressed genes at the transcriptional and post-transcriptional level. Therefore, it is of high interest to establish diagnostic, therapeutic and theranostic strategies at these levels. In the present study, we used the Diels-Alder Reaction with inverse electron demand (DARinv) click chemistry to prepare a series of cyclic RGD-BioShuttle constructs. These constructs carry the near-infrared (NIR) imaging agent Cy7 and the chemotherapeutic agent temozolomide (TMZ). We evaluated their uptake by and their efficacy against integrin αvβ3-expressing MCF7 human breast carcinoma cells. In addition, using a mouse phantom, we analyzed the suitability of this targeted theranostic agent for NIR optical imaging. We observed that the cyclic RGD-based carriers containing TMZ and/or Cy7 were effectively taken up by αvβ3-expressing cells, that they were more effective than free TMZ in inducing cell death, and that they could be quantitatively visualized using NIR fluorescence imaging. Therefore, these targeted theranostic agents are considered to be highly suitable systems for improving disease diagnosis and therapy.

译文

创新和个性化的治疗方法是在转录和转录后水平识别和控制个体异常表达基因的结果。因此,在这些水平上建立诊断、治疗和治疗策略是非常有意义的。在目前的研究中,我们使用具有反向电子需求 (DARinv) 点击化学的 Diels-Alder 反应来制备一系列循环 RGD-生物穿梭结构。这些构造携带近红外 (NIR) 显像剂 Cy7 和化疗药物替莫唑胺 (TMZ)。我们评估了它们对整合素 α v β3 表达的 MCF7 人乳腺癌细胞的摄取和疗效。此外,使用小鼠体模,我们分析了这种靶向治疗剂对近红外光学成像的适用性。我们观察到,含有 TMZ 和/或 Cy7 的基于 RGD 的环状载体被 α v β3 表达细胞有效吸收,在诱导细胞死亡方面比游离 TMZ 更有效, 并且可以使用近红外荧光成像对它们进行定量可视化。因此,这些靶向治疗药物被认为是非常适合改善疾病诊断和治疗的系统。

Temozolomide

肿瘤 脑癌 药物
概述  :  

替莫唑胺胶囊,又叫蒂清胶囊、泰道,是一种用于治疗脑癌的美国进口的药物,可以通过增强放化疗作用,让脑癌患者可以更好地对抗癌细胞。主要成份是替莫唑胺,其化学名为:3,4-二氢-3-甲基-4-氧代咪唑[5,1-d]并1,2,3,5-四嗪-8-甲酰胺。由默沙东公司研发生产,是一种硬胶囊剂,内容物为类白色至淡粉色颗粒状粉末。蒂清是目前唯一治疗脑胶质瘤的口服胶囊制剂,针对性强、特异性高,可透过血脑屏障,是治疗脑胶质瘤及转移瘤的特效药。两年多的临床观察及研究工作显示,蒂清治疗脑胶质瘤效果显著,同时具有延长

Temozolomide

释    义   n. 替莫唑胺

例    句   At recurrence temozolomide is effective for anaplastic tumors; well-tolerated and probably equally effective is PCV used as adjuvant therapy. 对于复发的病人,替莫唑胺对间变胶质瘤是有效的。作为辅助治疗,它和PCV方案有同等的效果。

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