Thomas Ajesh P, Palanikumar L, Jeena M T, Kim Kibeom, Ryu Ja-Hyoung
Department of Chemistry , School of Natural Sciences , Ulsan National Institute of Science and Technology (UNIST) , Ulsan-44919 , South Korea . Email:
Chem Sci. 2017 Dec 1;8(12):8351-8356. doi: 10.1039/c7sc03169f. Epub 2017 Oct 13.
Mitochondria-targeted cancer therapies have proven to be more effective than other similar non-targeting techniques, especially in photodynamic therapy (PDT). Indocyanine dye derivatives, particularly IR-780, are widely known for their PDT utility. However, poor water solubility, dark toxicity, and photobleaching are limiting factors for these dyes, which otherwise show promise based on their good absorption in the near-infrared (NIR) region and mitochondria targeting ability. Herein, we introduce an indocyanine derivative () that is highly water soluble, exhibiting higher mitochondrial targetability and better photostability than IR-780. Furthermore, electrostatic interactions between the positively charged and negatively charged hyaluronic acid (HA) were utilized to construct a micellar aggregate that is selective towards cancer cells. The cancer mitochondria-targeted strategy confirms high PDT efficacy as proved by and experiments.
线粒体靶向癌症治疗已被证明比其他类似的非靶向技术更有效，尤其是在光动力疗法（PDT）中。吲哚菁染料衍生物，特别是IR-780，因其在PDT中的应用而广为人知。然而，水溶性差、暗毒性和光漂白是这些染料的限制因素，否则基于它们在近红外（NIR）区域的良好吸收和线粒体靶向能力，它们显示出前景。在此，我们介绍一种吲哚菁衍生物（），其具有高水溶性，与IR-780相比表现出更高的线粒体靶向性和更好的光稳定性。此外，利用带正电荷的 与带负电荷的透明质酸（HA）之间的静电相互作用构建了对癌细胞具有选择性的胶束聚集体。如 和 实验所证明的，癌症线粒体靶向策略证实了高PDT疗效。
