Developing a Novel Indium(III) Agent Based on Human Serum Albumin Nanoparticles: Integrating Bioimaging and Therapy.
Zhenlei ZhangTongfu YangJuzheng ZhangWenjuan LiShanhe LiHongbin SunHong LiangFeng YangPublished in: Journal of medicinal chemistry (2022)
To effectively integrate diagnosis and therapy for tumors, we proposed to develop an indium (In) agent based on the unique property of human serum albumin (HSA) nanoparticles (NPs). A novel In(III) quinoline-2-formaldehyde thiosemicarbazone compound (C5) was optimized with remarkable cytotoxicity and fluorescence to cancer cells in vitro . An HSA-C5 complex NP delivery system was then successfully constructed. Importantly, the HSA-C5 complex NPs have stronger bioimaging and therapeutic efficiency relative to C5 alone in vivo . Besides, the results of gene chip analysis revealed that C5/HSA-C5 complex NPs act on cancer cells through multiple mechanisms: inducing autophagy, apoptosis, and inhibiting the PI3K-Akt signaling pathway.
Keyphrases
- human serum albumin
- signaling pathway
- endoplasmic reticulum stress
- oxidative stress
- cell death
- quantum dots
- pi k akt
- induced apoptosis
- epithelial mesenchymal transition
- fluorescent probe
- cell cycle arrest
- oxide nanoparticles
- molecular docking
- genome wide
- single molecule
- room temperature
- single cell
- molecular dynamics simulations
- copy number
- bone marrow