Molecular and Supramolecular Approach to Highly Photocytotoxic Phthalocyanines with Dual Cell Uptake Pathways and Albumin-Enhanced Tumor Targeting.

Abstract

Phototherapy for non-invasive cancer treatment has been extensively studied. An urgent challenge in phototherapy application is to fabricate appropriate targeted agents to achieve efficient therapeutic effect. Herein, a molecular and supramolecular approach for targeting phototherapy was reasonably designed and realized through the axial sulfonate modification of silicon(IV) phthalocyanines (Pcs), followed by supramolecular interaction with albumin. This approach can not only improve the photoactivities (e.g., fluorescence emission and reactive oxygen species production) of the Pcs but also enhance their tumor targeting. Most importantly, one of the deigned Pcs (4) can target HepG2 cells through dual cell pathways, leading to an extremely high phototoxicity with an EC50 (i.e., concentration of Pcs to kill 50% of cells under light irradiation) value of 2.0 nM. This finding presents a feasible strategy to realize efficient targeting phototherapy.

• Authors: Hao Liu, Li-Li Lv, Huang Wen, Dong-Mei Zhao, Juhong Wu, Mei-Rong Ke, Bi-Yuan Zheng, Jinyu Li, Xingshu Li, Jian-Dong Huang
• Journal: ACS applied materials & interfaces (ACS Appl Mater Interfaces) Vol. 14 Issue 25 Pg. 28581-28590 (Jun 29 2022) ISSN: 1944-8252 [Electronic] United States
• PMID: 35709499 (Publication Type: Journal Article)

Chemical References

• Albumins
• Antineoplastic Agents
• Indoles
• Photosensitizing Agents

Topics

• Albumins
• Antineoplastic Agents (therapeutic use)
• Cell Line, Tumor
• Indoles (metabolism, pharmacology)
• Photochemotherapy
• Photosensitizing Agents (therapeutic use)
• Phototherapy