Flexible Formation of Nanoparticles: Selectively Self-Assembling with Glycoclusters to Form Nano-Photosensitizers for Multipurpose Bioimaging and Photodynamic Therapy

The smart construction of nano-photosensitizers (PSs) is significant for multipurpose applications, such as bioimaging, efficient photodynamic anti-tumor or anti-bacterial studies. This work reports a flexible self-assembling strategy for the construction of nano-PSs, in which PSs spontaneously form...

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Main Authors: Kai-Li He, Wen-Jia Li, Yu Hu, Lu-Lu Sun, Lei Dong, Jing Xing, Jin Gong, Xiaoming Gong, Hai-Hao Han
Format: Article
Language:English
Published: MDPI AG 2025-03-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/6/1274
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author Kai-Li He
Wen-Jia Li
Yu Hu
Lu-Lu Sun
Lei Dong
Jing Xing
Jin Gong
Xiaoming Gong
Hai-Hao Han
author_facet Kai-Li He
Wen-Jia Li
Yu Hu
Lu-Lu Sun
Lei Dong
Jing Xing
Jin Gong
Xiaoming Gong
Hai-Hao Han
author_sort Kai-Li He
collection DOAJ
description The smart construction of nano-photosensitizers (PSs) is significant for multipurpose applications, such as bioimaging, efficient photodynamic anti-tumor or anti-bacterial studies. This work reports a flexible self-assembling strategy for the construction of nano-PSs, in which PSs spontaneously form amorphous aggregates for killing bacteria, or self-assemble with tetraphenylethene (TPE) based glycoclusters (<b>TPE-Glc<sub>4</sub></b>) to construct glyco-dots for cell imaging and photodynamic anti-tumor studies. Tricyanofuran (TCF) and TPE units were bridged with furan or thiophene moiety to construct two PSs (<b>1</b> and <b>2</b>) with NIR fluorescence in monomers, and a performance of the aggregation-induced generation of reactive oxygen species (AIG-ROS) in an aggregated state. Compared to the large amorphous aggregates (<b>2-a</b>), TPE-based glycoclusters encapsulated with PS form glyco-dots (<b>2-Glc</b>) that exhibit a smaller and more homogeneous hydrated size of approximately 40 nm, as well as enhanced water-solubility and biocompatibility. TPE-glycoclusters facilitate the cellular uptake of <b>2</b> into HepG2 cells, therefore enhancing the NIR fluorescence imaging signal and photodynamic therapy. Meanwhile, <b>2-a</b> exhibits satisfied phototoxicity against <i>Escherichia coli</i>. This work highlights the flexible self-assembly of nano-PSs for multifunctional bioapplications.
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publisher MDPI AG
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spelling doaj-art-a1bc51ae89a24abaae91d588c382e0452025-08-20T02:42:28ZengMDPI AGMolecules1420-30492025-03-01306127410.3390/molecules30061274Flexible Formation of Nanoparticles: Selectively Self-Assembling with Glycoclusters to Form Nano-Photosensitizers for Multipurpose Bioimaging and Photodynamic TherapyKai-Li He0Wen-Jia Li1Yu Hu2Lu-Lu Sun3Lei Dong4Jing Xing5Jin Gong6Xiaoming Gong7Hai-Hao Han8School of Pharmacy, Shandong Second Medical University, Weifang 261053, ChinaShandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, ChinaSchool of Pharmacy, Shandong Second Medical University, Weifang 261053, ChinaShandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, ChinaSchool of Pharmacy, Shandong Second Medical University, Weifang 261053, ChinaSchool of Pharmacy, Shandong Second Medical University, Weifang 261053, ChinaSchool of Pharmacy, Shandong Second Medical University, Weifang 261053, ChinaComprehensive Technical Service Center of Weifang Customs, Weifang 261041, ChinaShandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, ChinaThe smart construction of nano-photosensitizers (PSs) is significant for multipurpose applications, such as bioimaging, efficient photodynamic anti-tumor or anti-bacterial studies. This work reports a flexible self-assembling strategy for the construction of nano-PSs, in which PSs spontaneously form amorphous aggregates for killing bacteria, or self-assemble with tetraphenylethene (TPE) based glycoclusters (<b>TPE-Glc<sub>4</sub></b>) to construct glyco-dots for cell imaging and photodynamic anti-tumor studies. Tricyanofuran (TCF) and TPE units were bridged with furan or thiophene moiety to construct two PSs (<b>1</b> and <b>2</b>) with NIR fluorescence in monomers, and a performance of the aggregation-induced generation of reactive oxygen species (AIG-ROS) in an aggregated state. Compared to the large amorphous aggregates (<b>2-a</b>), TPE-based glycoclusters encapsulated with PS form glyco-dots (<b>2-Glc</b>) that exhibit a smaller and more homogeneous hydrated size of approximately 40 nm, as well as enhanced water-solubility and biocompatibility. TPE-glycoclusters facilitate the cellular uptake of <b>2</b> into HepG2 cells, therefore enhancing the NIR fluorescence imaging signal and photodynamic therapy. Meanwhile, <b>2-a</b> exhibits satisfied phototoxicity against <i>Escherichia coli</i>. This work highlights the flexible self-assembly of nano-PSs for multifunctional bioapplications.https://www.mdpi.com/1420-3049/30/6/1274TPE-glycoclusterself-assemblybiological uptakephotodynamic therapy
spellingShingle Kai-Li He
Wen-Jia Li
Yu Hu
Lu-Lu Sun
Lei Dong
Jing Xing
Jin Gong
Xiaoming Gong
Hai-Hao Han
Flexible Formation of Nanoparticles: Selectively Self-Assembling with Glycoclusters to Form Nano-Photosensitizers for Multipurpose Bioimaging and Photodynamic Therapy
Molecules
TPE-glycocluster
self-assembly
biological uptake
photodynamic therapy
title Flexible Formation of Nanoparticles: Selectively Self-Assembling with Glycoclusters to Form Nano-Photosensitizers for Multipurpose Bioimaging and Photodynamic Therapy
title_full Flexible Formation of Nanoparticles: Selectively Self-Assembling with Glycoclusters to Form Nano-Photosensitizers for Multipurpose Bioimaging and Photodynamic Therapy
title_fullStr Flexible Formation of Nanoparticles: Selectively Self-Assembling with Glycoclusters to Form Nano-Photosensitizers for Multipurpose Bioimaging and Photodynamic Therapy
title_full_unstemmed Flexible Formation of Nanoparticles: Selectively Self-Assembling with Glycoclusters to Form Nano-Photosensitizers for Multipurpose Bioimaging and Photodynamic Therapy
title_short Flexible Formation of Nanoparticles: Selectively Self-Assembling with Glycoclusters to Form Nano-Photosensitizers for Multipurpose Bioimaging and Photodynamic Therapy
title_sort flexible formation of nanoparticles selectively self assembling with glycoclusters to form nano photosensitizers for multipurpose bioimaging and photodynamic therapy
topic TPE-glycocluster
self-assembly
biological uptake
photodynamic therapy
url https://www.mdpi.com/1420-3049/30/6/1274
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