Related Experiment Video
Updated: Jun 19, 2026
Photodynamic Therapy with Blended Conducting Polymer/Fullerene Nanoparticle Photosensitizers
Published on: October 28, 2015
Potential of Photodynamic Therapy Based on Sugar-Conjugated Photosensitizers
Hiromi Kataoka1, Hirotada Nishie1, Mamoru Tanaka1
1Department of Gastroenterology and Metabolism, Nagoya City University Graduate School of Medical Sciences, Nagoya 467-8601, Japan.
Abstract:
In 2015, the Japanese health insurance approved the use of a second-generation photodynamic therapy (PDT) using talaporfin sodium (TS); however, its cancer cell selectivity and antitumor effects of TS PDT are not comprehensive. The Warburg effect describes the elevated rate of glycolysis in cancer cells, despite the presence of sufficient oxygen. Because cancer cells absorb considerable amounts of glucose, they are visible using positron emission tomography (PET). We developed a third-generation PDT based on the Warburg effect by synthesizing novel photosensitizers (PSs) in the form of sugar-conjugated chlorins. Glucose-conjugated (tetrafluorophenyl) chlorin (G-chlorin) PDT revealed significantly stronger antitumor effects than TS PDT and induced immunogenic cell death (ICD). ICD induced by PDT enhances cancer immunity, and a combination therapy of PDT and immune checkpoint blockers is expected to synergize antitumor effects. Mannose-conjugated (tetrafluorophenyl) chlorin (M-chlorin) PDT, which targets cancer cells and tumor-associated macrophages (TAMs), also shows strong antitumor effects. Finally, we synthesized a glucose-conjugated chlorin e6 (SC-N003HP) that showed 10,000-50,000 times stronger antitumor effects than TS (IC50) in vitro, and it was rapidly metabolized and excreted. In this review, we discuss the potential and the future of next-generation cancer cell-selective PDT and describe three types of sugar-conjugated PSs expected to be clinically developed in the future.
Insights
Next-generation photodynamic therapy (PDT) utilizes sugar-conjugated photosensitizers targeting cancer cells. This approach enhances antitumor effects and induces immunogenic cell death, offering a promising new cancer treatment strategy.
Area of Science:
- Oncology
- Biochemistry
- Immunology
Background:
- Second-generation photodynamic therapy (PDT) using talaporfin sodium (TS) has limitations in cancer cell selectivity and antitumor efficacy.
- The Warburg effect, characterized by elevated glycolysis in cancer cells, presents a metabolic vulnerability exploitable for targeted therapies.
- Positron emission tomography (PET) visualizes cancer cells due to their high glucose uptake, suggesting glucose-based targeting strategies.
Purpose of the Study:
- To develop third-generation PDT agents with enhanced cancer cell selectivity and antitumor effects by leveraging the Warburg effect.
- To synthesize novel sugar-conjugated chlorin-based photosensitizers (PSs) for targeted PDT.
- To evaluate the antitumor efficacy and immunogenic cell death (ICD) induction of these novel PSs.
Main Methods:
- Synthesis of novel sugar-conjugated chlorin derivatives, including glucose-conjugated (tetrafluorophenyl) chlorin (G-chlorin) and mannose-conjugated (tetrafluorophenyl) chlorin (M-chlorin).
- In vitro evaluation of antitumor effects and IC50 values compared to talaporfin sodium (TS).
- Assessment of immunogenic cell death (ICD) induction and potential for combination therapy with immune checkpoint blockers.
Main Results:
- G-chlorin PDT demonstrated significantly stronger antitumor effects than TS PDT and induced ICD.
- M-chlorin PDT effectively targeted both cancer cells and tumor-associated macrophages (TAMs), exhibiting potent antitumor activity.
- A glucose-conjugated chlorin e6 derivative (SC-N003HP) showed 10,000-50,000 times greater in vitro antitumor effects than TS, with rapid metabolism and excretion.
Conclusions:
- Sugar-conjugated photosensitizers represent a promising strategy for next-generation, cancer cell-selective PDT.
- The developed PDT agents induce ICD, suggesting potential for synergistic effects with immunotherapy.
- Further clinical development of these novel sugar-conjugated PSs is anticipated for improved cancer treatment outcomes.
More Related Videos
08:03Anticancer Efficacy of Photodynamic Therapy with Lung Cancer-Targeted Nanoparticles
Published on: December 1, 2016
11:04An In-House-Built and Light-Emitting-Diode-Based Photodynamic Therapy Device for Enhancing Verteporfin Cytotoxicity in a 2D Cell Culture Model
Published on: January 13, 2023
