No abstract

Mitochondria have emerged as important targets in cancer therapy due to their key role in regulating energy supply, maintaining redox homeostasis, and intrinsic apoptosis. Curcumin (CUR) has shown promise in inhibiting the proliferation and metastasis of cancer cells by inducing apoptosis and arresting cell cycle. However, the clinical application of CUR has been limited by its low stability and poor tumor selectivity. To address these issues, the novel mitochondria-targeted curcumin derivatives were synthesized through the unilateral coupling (CUR-T) or bilateral coupling (CUR-2T) of curcumin's phenolic hydroxy groups with triphenyl phosphorus via ester bond. The aim was to achieve better stability, higher tumor selectivity, and stronger curative efficacy. The results of stability and biological experiments indicated that both stability and cytotoxicity were arranged in descending order of CUR-2T > CUR-T > CUR. In ovarian cancer cells (A2780 cells), CUR-2T showed well-defined preferential selectivity towards cancer cells and exhibited efficient anticancer efficacy due to its superior mitochondria accumulation ability. Subsequently, the mitochondrial redox balance was disrupted, accompanied by increased ROS levels, decreased ATP levels, dissipated MMP, and increased G 0 /G 1 phase arrest, leading to a higher apoptotic rate. In summary, the results of this study suggest that CUR-2T holds substantial promise for further development as a potential agent for the treatment of ovarian cancer.

Gold nanoparticles (AuNPs) with size of 12 ~ 25 nm were loaded on the dendritic nanotubes (DNTs), which were self‐assembled by the triple‐helix polysaccharides from black fungus (AF1). The characterization results proved that the AuNPs were dispersed on the surface of DNTs without affecting their tubular structure. Due to the dendritic structure, the loading content of AuNPs could arrived at 46.4%. Moreover, the potential anticancer activities of the complex (DNT‐Au) were evaluated by the induction of apoptosis in HepG2 cells. It was found DNT‐Au could be taken up by cells and enter into lysosomes, further inducing apoptosis in HepG2 cells by ROS‐mediated mitochondrial dysfunction. This work was benefit for the development of natural polysaccharide as a substrate to stabilize nanoparticles in biomedical fields.