Amino acid derivatives of natural chlorins as a platform for the creation of targeted photosensitizers in oncology

Objectives . This study aims to obtain the amino acid derivatives of chlorophyll a and bacteriochlorophyll for targeted delivery pigments tumor foci. will increase biocompatibility and, as result, reduce toxic side effects. In addition photodynamic efficiency, an additional cytotoxic effect is expected obtained conjugates photosensitizers (PSs) with acids. owing participation latter in intracellular biochemical processes, including interaction components glutathione antioxidant system, leading vulnerability cells oxidative stress. Methods this work, we have implemented optimization structure highly efficient infrared PS based on O-propyloxim-N-propoxybacteriopurpurinimide (DPBP), absorbing at 800 nm showing efficacy treatment deep-seated pigmented tumors, by introducing L-lysine, L-arginine, methionine sulfoximine (MSO), buthionine (BSO) methyl esters. The compounds was proved mass spectrometry nuclear magnetic resonance spectroscopy, photoinduced cytotoxicity studied vitro HeLa cell line. Results Conjugates DPBP acids their derivatives, such lysine, arginine, MSO, BSO been prepared. chelating ability conjugate lysine shown, its Sn(IV) complex obtained. Conclusions Biological testing MSO showed 5–6-fold compared parent PS. Additionally, high internalization found, dark (in absence irradiation) DPBP-MSO DPBP-BSO increased fourfold initial compound. can be explained processes cell.