NDLI: Luminescent platinum(ii) complexes with self-assembly and anti-cancer properties: hydrogel, pH dependent emission color and sustained-release properties under physiological conditions

Content Provider	Royal Society of Chemistry (RSC)
Author	Chan, Anna On-Yee Yang, Chen Che, Chi-Ming Tsai, Johnson Lui-Lui Lok, Chun-Nam Zou, Taotao Liu, Jia Chen, Tianfeng
Copyright Year	2015
Abstract	Supramolecular interactions are of paramount importance in biology and chemistry, and can be used to develop new vehicles for drug delivery. Recently, there is a surge of interest on self-assembled functional supramolecular structures driven by intermolecular metal–metal interactions in cellular conditions. Herein we report a series of luminescent Pt(II) complexes [Pt(C^N^Npyr)(CNR)]+ [HC^N^Npyr = 2-phenyl-6-(1H-pyrazol-3-yl)-pyridine)] containing pincer type ligands having pyrazole moieties. These Pt(II) complexes exert potent cytotoxicity to a panel of cancer cell lines including primary bladder cancer cells and display strong phosphorescence that is highly sensitive to the local environment. The self-assembly of these complexes is significantly affected by pH of the solution medium. Based on TEM, SEM, ESI-MS, absorption and emission spectroscopy, and fluorescence microscopy together with cell based assays, [Pt(C^N^Npyr)(CNR)]+ complexes were observed to self-assemble into orange phosphorescent polymeric aggregates driven by intermolecular Pt(II)–Pt(II) and ligand–ligand interactions in a low-pH physiological medium. Importantly, the intracellular assembly and dis-assembly of [Pt(C^N^Npyr)(CNR)]+ are accompanied by change of emission color from orange to green. These [Pt(C^N^Npyr)(CNR)]+ complexes accumulated in the lysosomes of cancer cells, increased the lysosomal membrane permeability and induced cell death. One of these platinum(II) complexes formed hydrogels which displayed pH-responsive and sustained release properties, leading to low-pH-stimulated and time-dependent cytotoxicity towards cancer cells. These hydrogels can function as vehicles to deliver anti-cancer agent cargo, such as the bioactive natural products studied in this work.
Starting Page	3823
Ending Page	3830
Page Count	8
File Format	HTM / HTML PDF
ISSN	20416520
Volume Number	6
Issue Number	7
Journal	Chemical Science
DOI	10.1039/c4sc03635b
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Subscribed
Subject Keyword	Spectroscopy Cell membrane Cytotoxicity Drug delivery Fluorescence microscope Phenyl group Bladder cancer Pyrazole Organic chemistry Self-assembly Pyridine Transmission electron microscopy PH SEM Phosphorescence Molecular biology Cancer
Content Type	Text
Resource Type	Article
Subject	Chemistry

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