Abstract
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 receptor-overexpressing 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.
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