Cyanine–Gemcitabine Conjugates as Targeted Theranostic Agents for Glioblastoma Tumor Cells

A small subset of heptamethine dyes (cyanine-7 or Cy7) share an intriguing characteristic: preferential tumor accumulation and retention. These dyes absorb in the near-infrared (NIR) region (above 750 nm) and perform active targeting to deliver therapeutic and toxic cargoes to various tumor models in vivo. In this work, four heptamethines 1 were synthesized, which have a gemcitabine fragment attached to the meso-position of the Cy7 core. Theranostic agent 1a was discovered that localized in glioblastoma tumor cells, has absorption maxima in NIR region, and showed similar therapeutic effect to gemcitabine but at one-third the molar dose.

七甲川染料（heptamethine dyes）中的一个小子集为花青7（cyanine-7，Cy7），具备一项引人关注的特性：可优先在肿瘤部位蓄积并滞留。这类染料可吸收750 nm以上的近红外（NIR）波段光线，并可通过主动靶向策略，将治疗性或细胞毒性负载递送至多种体内肿瘤模型。本研究共合成4种标记为1的七甲川染料，其Cy7核心的中位（meso-position）均连接有吉西他滨（gemcitabine）片段。研究发现诊疗一体化试剂（theranostic agent）1a可定位于胶质母细胞瘤（glioblastoma）细胞，其吸收峰位于近红外波段，且在摩尔剂量仅为吉西他滨三分之一的情况下，即可展现出与之相当的治疗效果。