Biocompatible G-Quadruplex/BODIPY assembly for cancer cell imaging and the attenuation of mitochondria

The G-quadruplex aptamer is a high-order structure formed by folding of guanine-rich DNA or RNA. The recognition and assembly of G-quadruplex and compounds are important to find biocompatible drugs. Herein, triphenylamine conjugated 4, 4-difluoro-4-bora-3a, 4a-diaza-s-indacene (BODIPY) compound (BPTPA) was synthesized, and the interaction of BPTPA with G4 DNA was studied. It is found that BPTPA selectively binds with G(3)T(3) G4 DNA forming a water-compatible nanocomplex (BPTPA-G(3)T(3)). BPTPA-G(3)T(3) can image mitochondria and inhibit the expression of TrxR(2). Cytotoxicity results indicate BPTPA-G(3)T(3) ( )can decrease the membrane potential of mitochondria and inhibit the proliferation of BGC-823 cancer cells. Therefore, BPTPA-G(3)T(3) can be the biocompatible attenuator of mitochondria for cancer image and chemotherapy.