Primary screening of substances-photosensibilizers of the bacteriochlorin range for photodynamic therapy of malignant neoplasms

Plotnikova E.A.1 , Grin M.A.2, Ostroverkhov P.V.2, Pantushenko I.V.2, Yakubovskaya R.I.1, Kaprin A.D.1

1. Hertsen Moscow Institute of Oncology, Moscow, Russia
2. Moscow Technological University, Moscow, Russia
Section: Experimental Study
DOI: 10.18097/PBMC20186403283      PubMed Id: 29964266
Year: 2018  Volume: 64  Issue: 3  Pages: 283-289
This paper presents a primary screening of bacteriochlorin-type compounds with aminoamide, propyl and carbohydrate substituents aimed for development a new generation photosensitizers (PS) for photodynamic therapy of malignant tumors. Absorption and fluorescence spectral characteristics of the compounds, their storage stability in solutions under dark conditions and light exposure, photo-induced and dark cytotoxicity against human HEp2 tumor cells have been studied. It has been shown that the dyes with aminoamide substituents have an absorbtion maximum at 754±2 nm in the long wavelength region and they are not stable during storage (the specific fluorescence intensity decreased by 33-56% during 24 hours). The long wavelength region absorption of the propyl and carbohydrate substituted compounds varied in the range 780-831 nm, they were stable in solutions during storage and under light irradiation. Except the dye with a carbohydrate residue in the exocycle E, all PS exhibited the high photo-induced activity and low level of the dark cytotoxicity. The highest photo-induced cytotoxicity was observed for compounds with aminoamide substituents inthe macrocyclic ring (IC 50 values ranged from 17 nM to49 nM after 2 hour incubation with PS followed by exposure to the 10 J/cm 2 dose of red light). Taking into account the totality of the physico-chemical and biological properties, as well as manufacturability of production, O-propyloxime-N-propoxybacteriopurinimide methyl ester was chosen as the most promising candidate compound for further investigations.
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Keywords: bacteriochlorophyll a, bacteriochlorin, photodynamic therapy, photosensitizers, photo-induced activity in vitro, primary screening

Plotnikova, E. A., Grin, M. A., Ostroverkhov, P. V., Pantushenko, I. V., Yakubovskaya, R. I., Kaprin, A. D. (2018). Primary screening of substances-photosensibilizers of the bacteriochlorin range for photodynamic therapy of malignant neoplasms. Biomeditsinskaya Khimiya, 64(3), 283-289.
This paper is also available as the English translation: 10.1134/S1990750818030058
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