Kascakova et al. PLOS One_Somatostatin_2014

Our aim was to develop an approach to improve PDT by direct conjugation of photosensitizer with the synthetic, metabolically stable somatostatin analogue octreotate. We report on the in vitro cytotoxicity of two Ce6-somatostatin analogue conjugates: Ce6-K3-[Tyr3]-octreotate (1) and Ce6-[Tyr3]-octreotate-K3-[Tyr3]-octreotate (2). Their in vitro quantitative uptake and phototoxicity in sst2+ K562 and WT cells have been compared with those of un-conjugated Ce6.本研究旨在通过将光敏剂（photosensitizer）与合成代谢稳定的生长抑素类似物奥曲肽酸（octreotate）直接偶联，开发一种优化光动力疗法（PDT）的策略。本研究报道了两种Ce6-生长抑素类似物偶联物的体外细胞毒性：Ce6-K3-[Tyr3]-奥曲肽酸（1）与Ce6-[Tyr3]-奥曲肽酸-K3-[Tyr3]-奥曲肽酸（2）。我们将这两种偶联物在sst2阳性K562细胞与野生型（Wild Type，WT）细胞中的体外定量摄取水平及光毒性，与未偶联的Ce6进行了对比分析。