Multifunctional Nanoaggregates Composed of Active CPUL1 and a Triphenylphosphine Derivative for Mitochondria-Targeted Drug Delivery and Cell Imaging

Jing Liu; Fei Ji; Zhuolu Xia; Chunhua Zhang; Changshun Zhao; Yanfei Li; Xiang Zhou; Dechun Huang; Wei Chen; Feng Jiang

doi:10.1002/cmdc.202100632

Multifunctional Nanoaggregates Composed of Active CPUL1 and a Triphenylphosphine Derivative for Mitochondria-Targeted Drug Delivery and Cell Imaging

ChemMedChem. 2022 Mar 18;17(6):e202100632. doi: 10.1002/cmdc.202100632. Epub 2021 Nov 16.

Authors

Jing Liu¹, Fei Ji¹, Zhuolu Xia¹, Chunhua Zhang¹, Changshun Zhao¹, Yanfei Li¹, Xiang Zhou¹, Dechun Huang¹, Wei Chen¹, Feng Jiang¹

Affiliation

¹ Department of Pharmaceutical Engineering, China Pharmaceutical University, Nanjing, 210009, China.

PMID: 34750966
DOI: 10.1002/cmdc.202100632

Abstract

We report that active substance (CPUL1) and triphenylphosphine (TPP) derivative could self-assemble into multifunctional nanoaggregates (CPUL1-TPP NAs) through electrostatic and π-π stacking interactions. CPUL1 was wrapped tightly inside the nanoparticles as well as CPUL1 and TPP derivative self-assembled into stable and compact nanoparticles in water. The positive surface charge of CPUL1-TPP NAs made them much easier to be endocytosed to enter cytoplasm, accumulate in the mitochondria and induce cell apoptosis based on their mitochondria targeting ability, fluorescence property and fast cell uptake characteristic, which showed better antitumor efficacy on HUH7 hepatoma cells in vitro than that of free CPUL1.

Keywords: Carrier-free; Cell imaging; Drug delivery; Mitochondria-targeting; Nanoaggregate.

Publication types

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

MeSH terms

Antineoplastic Agents* / metabolism
Antineoplastic Agents* / pharmacology
Drug Delivery Systems
Mitochondria / metabolism
Nanoparticles*
Organophosphorus Compounds / pharmacology

Substances

Antineoplastic Agents
Organophosphorus Compounds
triphenylphosphine