The evaluations of Tc-99m cyclopentadienyl tricarbonyl triphenyl phosphonium cation for multidrug resistance

作者：Chen, Shuting; Zhang, Ying; Li, Xiaoyan; Jia, Hongmei; Lu, Jie^*

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(15): 3551-3554.

DOI：10.1016/j.bmcl.2017.05.053

• Phosphonium cation
• Multidrug resistant
• P-glycoprotein
• Multidrug resistant protein 1
• SPECT

A triphenylphosphonium cation, [Tc-99m] Technetium cyclopentadienyltricarbonyl-6-hexanoyl-triphenylphosphonium cation ([Tc-99m] 3) was prepared to target multidrug resistance (MDR). The radiotracer was evaluated in the MDR-negative MCF-7 and MDR-positive MCF-7/ADR cell lines in vitro, as well as animal models in vivo. [Tc-99m] 3 was proofed to be a substrate of P-glycoprotein and multidrug resistant protein 1, and showed a higher accumulation in the MDR-negative MCF-7 cells compared to 99mTc-sestamibi in vitro. The MCF-7 tumor-to-MCF-7/ADR tumor ratio of [Tc-99m] 3 was similar to 3 at 1 h p. i. in the biodistribution study. These results demonstrated the capability of the radiotracer to detect multidrug resistance in tumor cells.

• 出版日期2017-8-1
• 单位北京师范大学