一种雌激素受体靶向的钌配合物作为用于乳腺癌细胞的双光子光动力治疗剂。

An estrogen receptor targeted ruthenium complex as a two-photon photodynamic therapy agent for breast cancer cells.

机构信息

State Key Laboratory of Fine Chemicals, Dalian University of Technology, No. 2 Linggong Road, High-tech District, Dalian 116024, China.

出版信息

Chem Commun (Camb). 2018 Jun 21;54(51):7038-7041. doi: 10.1039/c8cc03786h.

DOI:10.1039/c8cc03786h

PMID:29873358

Abstract

In this study, we reported a tamoxifen modified Ru(ii) polypyridyl complex (Ru-tmxf) as an estrogen receptor (ER) targeted photosensitizer. Ru-tmxf displays enhanced cellular uptake and PDT efficiency toward breast cancer cells with high ER expression due to the specific targeting of tamoxifen to ER and finally localizes in lysosomes. Moreover, Ru-tmxf can be activated by two-photon excitation, generating 1O2 to damage lysosomes and result in cell death.

摘要

在这项研究中，我们报道了一种他莫昔芬修饰的 Ru(ii) 多吡啶配合物（Ru-tmxf）作为雌激素受体（ER）靶向光敏剂。由于他莫昔芬特异性靶向 ER，Ru-tmxf 显示出对高 ER 表达的乳腺癌细胞增强的细胞摄取和 PDT 效率，并最终定位于溶酶体中。此外，Ru-tmxf 可以通过双光子激发激活，产生 1O2 来破坏溶酶体并导致细胞死亡。