COMPARATIVE IN VITRO STUDY OF DIFFERENT CLASSES OF PHOTOSENSITIZERS. PYROPHEOPHORBIDES AND CHLORINES

The study evaluates physical, chemical and biological properties of glycosylated derivatives of pyropheophorbide-α and chlorine e₆, cycloimid derivatives of chlorine p₆. Glycosylated derivatives of pyropheophorbide α and chlorine e₆ were characterized by stability in solution without light exposure, but subject to photobleaching during exposure. Derivatives of pyropheophorbide-α showed high photo-induced activity in biological assay, the IC₅₀ value varied from 35±7nM to 82±7 nM (depending on the pendent group and the tumor cell culture). Among the derivatives of chlorine e₆ conjugate with galactose residue in A-pyrrole showed the maximum activity towards HEp2, A549 and HT29 cells (IC_{50 -} 15±8 nM, 70±19 nM and 34±16 nM respectively), its activity 8-10 times exceeding the unconjugated counterpart and the derivatives with different macrocycle modification. Cycloimid derivatives of chlorine p₆ are stable in solution without exposure and relatively stable under light exposure. These compounds showed high photo-induced activity in biological assay (IC₅₀ varied from 35±10 nM to 250±30 nM) significantly exceeding the activity of unmodified derivatives of chlorine p₆.

фотодинамическое воздействие in vitro, производные пирофеофорбида α, производные хлорина е₆ и хлорина р₆, опухолевые клетки, photodynamic effect invitro, derivatives of pyropheophorbide-α, derivatives of chlorine e₆ and chlorine p₆, tumor cells

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