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Antitumor effects of a novel glucose-conjugated bacteriochlorin for photodynamic therapy
Yasunari Sasaki1, Mamoru Tanaka2, Yuki Kojima1
1Department of Gastroenterology and Metabolism, Nagoya City University Graduate School of Medical Science, Nagoya, Aichi, Japan.
Abstract:
Photodynamic therapy (PDT) is a minimally invasive cancer treatment that employs photosensitizers (PSs) activated by light to generate cytotoxic reactive oxygen species (ROS). Talaporfin sodium (TS), widely used in Japan, has shown limited efficacy in advanced tumors, highlighting the need for novel PSs. We developed a glucose-conjugated bacteriochlorin derivative, Glc-TFPB, designed to enhance tumor selectivity via the Warburg effect and to enable deep tissue penetration owing to its near-infrared absorption. In vitro, Glc-TFPB exhibited time-dependent cellular uptake, predominantly in lysosomes, and induced significant ROS generation and apoptosis upon PDT. Compared with TS, Glc-TFPB-PDT demonstrated markedly higher cytotoxicity 24 h after administration (IC50: 1.10 µM vs 13.60 µM). In vivo fluorescence analysis revealed peak tumor accumulation at 24 h after administration, consistent with optimal treatment timing. PDT with Glc-TFPB significantly suppressed tumor growth in xenografted mice, with greater efficacy at 24 h than at 2 h after administration. These findings indicate that Glc-TFPB is a promising next-generation PS with improved tumor selectivity, deeper tissue penetration, and superior photodynamic efficacy, supporting its potential for clinical translation.
Insights
A novel glucose-conjugated photosensitizer, Glc-TFPB, shows enhanced tumor selectivity and efficacy in photodynamic therapy (PDT). This next-generation agent offers improved cancer treatment potential compared to existing therapies.
Area of Science:
- Biochemistry
- Oncology
- Photomedicine
Background:
- Photodynamic therapy (PDT) uses photosensitizers (PSs) to generate reactive oxygen species (ROS) for cancer treatment.
- Current PSs like talaporfin sodium (TS) have limitations in treating advanced tumors.
Purpose of the Study:
- To develop and evaluate a novel glucose-conjugated bacteriochlorin derivative (Glc-TFPB) as a next-generation PS.
- To assess Glc-TFPB's tumor selectivity, deep tissue penetration, and photodynamic efficacy.
Main Methods:
- In vitro studies assessed cellular uptake, ROS generation, and cytotoxicity of Glc-TFPB.
- In vivo studies utilized fluorescence imaging for tumor accumulation and evaluated tumor growth suppression in xenograft models.
- Compared Glc-TFPB-PDT efficacy with talaporfin sodium (TS)-PDT.
Main Results:
- Glc-TFPB demonstrated time-dependent cellular uptake, lysosomal localization, and significant ROS generation and apoptosis induction.
- Glc-TFPB-PDT exhibited superior in vitro cytotoxicity compared to TS-PDT (IC50: 1.10 µM vs 13.60 µM).
- In vivo studies showed peak tumor accumulation at 24 hours and significant tumor growth suppression, with greater efficacy at 24h than 2h post-administration.
Conclusions:
- Glc-TFPB is a promising next-generation PS with enhanced tumor selectivity via the Warburg effect and deep tissue penetration due to near-infrared absorption.
- Glc-TFPB-PDT demonstrates superior efficacy, supporting its potential for clinical translation in cancer therapy.
