Significant Tumor Inhibition of Trimethyl‐152‐[L‐aspartyl]pheophorbide a in Tumor Photodynamic Therapy≠

Benić, Anita; Kussayeva, Akmaral; Antol, Ivana; Vazdar, Mario; Brkljača, Zlatko; Chen, Dan‐Ye; Yan, Yi‐Jia; Gao, Ying‐Hua; Chen, Zhi‐Long; Margetić, Davor (2025) Significant Tumor Inhibition of Trimethyl‐152‐[L‐aspartyl]pheophorbide a in Tumor Photodynamic Therapy≠. ChemMedChem, 20 (10). ISSN 1860-7179

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Abstract

A novel pheophorbide derivative, trimethyl-152-[L-aspartyl]pheophorbide a was synthesised and investigated for anti-tumor activity. The prepared photosensitizer had good absorption in the phototherapeutic window and high ROS yields. It exhibited excellent phototoxicity higher than reference compound m-THPC when irradiated by 650 nm light in vitro, and obvious photodynamic anti-tumor effect in vivo. It causes cellular apoptosis or necrosis under laser irradiation and localizes in mitochondria, lysosome, and endoplasmic reticulum. The observed high efficacy was rationalized by efficient introduction into the blood by facile transfer through membranes, which is supported by molecular dynamics simulation studies. This work provides a new candidate photosensitizer for anti-cancer treatment.

Item Type:	Article
Uncontrolled Keywords:	photodynamic therapy; pheophorbides
Subjects:	NATURAL SCIENCES > Chemistry > Organic Chemistry NATURAL SCIENCES > Biology > Biochemistry and Molecular Biology
Divisions:	Division of Organic Chemistry and Biochemistry
Projects:	Project title Project leader Project code Project type Prostorne modulacije gvanidina Davor Margetić IP-2022-10-4385 HrZZ
Depositing User:	Lorena Palameta
Date Deposited:	23 Sep 2025 14:56
URI:	http://fulir.irb.hr/id/eprint/10017
DOI:	10.1002/cmdc.202500087

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