Developing a Novel Indium(III) Agent Based on Human Serum Albumin Nanoparticles: Integrating Bioimaging and Therapy

Zhenlei Zhang; Tongfu Yang; Juzheng Zhang; Wenjuan Li; Shanhe Li; Hongbin Sun; Hong Liang; Feng Yang

doi:10.1021/acs.jmedchem.1c01790

Developing a Novel Indium(III) Agent Based on Human Serum Albumin Nanoparticles: Integrating Bioimaging and Therapy

J Med Chem. 2022 Apr 14;65(7):5392-5406. doi: 10.1021/acs.jmedchem.1c01790. Epub 2022 Mar 24.

Authors

Zhenlei Zhang¹, Tongfu Yang¹, Juzheng Zhang¹, Wenjuan Li¹, Shanhe Li¹, Hongbin Sun², Hong Liang¹, Feng Yang¹

Affiliations

¹ State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin, Guangxi 541004, P. R. China.
² Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, Nanjing, Jiangsu 210009, P. R. China.

PMID: 35324188
DOI: 10.1021/acs.jmedchem.1c01790

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Cell Line, Tumor
Humans
Indium* / pharmacology
Nanoparticles*
Phosphatidylinositol 3-Kinases
Serum Albumin, Human / metabolism

Substances

Indium
Serum Albumin, Human