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Gadolinium(III) Porphyrinoid Phototheranostics.

Guo-Qing Jin¹, Haoqiang Lai², Zi-Shu Yang¹

¹Beijing National Laboratory for Molecular Sciences, College of Chemistry and Molecular Engineering, Peking University, Beijing, 100871, P. R. China.

Chemistry, an Asian Journal

|March 28, 2022

Summary

This summary is machine-generated.

Gadolinium porphyrinoids show promise as phototheranostic agents, enabling magnetic resonance imaging (MRI) and photodynamic therapy (PDT) with enhanced properties for precision medicine.

Keywords:

Lanthanide chemical biology MRI Metalloporphyrinoid Photodynamic therapy Phototheranostics

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Area of Science:

Biomedical Engineering
Materials Science
Oncology

Background:

Molecular phototheranostics offers non-invasive, precise, and controllable light-based medical treatments.
Gadolinium (Gd³⁺) porphyrinoids are explored for their potential in advanced medical imaging and therapy.

Purpose of the Study:

To develop novel Gd³⁺ porphyrinoids as dual-action agents for MRI and photodynamic therapy (PDT).
To investigate the impact of glycosylation and β-lactonization on the photophysical and imaging properties of Gd³⁺ porphyrinoids.

Main Methods:

Synthesis of Gd³⁺ porphyrinoids with meso-glycosylation and β-lactonization (Gd-1-4-Glu).
Evaluation of photophysical properties, including near-infrared (NIR) absorption and reactive oxygen species (ROS) generation.
Assessment of longitudinal relaxivity (r₁) and in vivo MRI and PDT efficacy in HeLa tumor-bearing mice.

Main Results:

β-lactonization red-shifted absorption to the NIR region and enhanced ROS generation (type I and II pathways).
Modified Gd³⁺ porphyrinoids achieved a high relaxivity of up to 4.3±0.2 mM^-1s^-1.
In vivo studies demonstrated real-time T₁-weighted MRI and effective PDT in tumor-bearing mice.

Conclusions:

Gd³⁺ porphyrinoids with glycosylation and β-lactonization are effective phototheranostic agents.
These agents exhibit improved biocompatibility, photophysical properties, and MRI contrast.
The study highlights the potential of Gd³⁺ porphyrinoids for advanced applications in precision medicine and cancer therapy.