An LHRH peptide-conjugated ruthenium(II) complex as tumor-targeted theranostic anticancer agent

作者：Qin, Yafang; Tang, Xingguo; Chen, Jintai; Huang, Jingcong; Wang, Dingding; Zhang, Xianhuan; Zhang, Yangli; Wu, Fenglin^*; Wang, Jinquan^*

来源：Inorganic Chemistry Communication, 2022, 136: 109166.

DOI：10.1016/j.inoche.2021.109166

• Ruthenium(II) complex
• LHRH peptide
• Tumor-targeted
• Theranostic

In the present study, an LHRH peptide-conjugated tumor targeting ruthenium(II) complex (Ru1-LHRH) was synthesized and characterized. Ru1-LHRH selectively targeted the mitochondria of LHRH receptoroverexpressing A2780 tumor cells. In particular, the cytotoxicity of Ru1-LHRH against A2780 cells was approximately 8 times higher than that of nontargeted L02 cells. In addition, this conjugate could perform theranostic functions by simultaneously imaging and killing targeted tumor cells. Further study demonstrated that Ru1-LHRH induced apoptosis by inducing ROS, which involves the activation of the Caspase3/7 protein family. Taken together, Ru1-LHRH exhibited both antitumor and imaging properties, indicating that Ru1-LHRH may be a viable drug candidate as a multifunctional tumor-targeted theranostic anticancer agent.

• 单位
  广东药学院