New Сhlorin-Terpene Conjugates: Synthesis, Photoinduced and Dark Cytotoxicity

Abstract

The concentrations, at which chlorin-myrtenic (3) and chlorin-camphenylanic (4) conjugates exhibit photoinduced cytotoxicity, differ by more than two orders of magnitude from the concentrations at which these compounds show dark cytotoxicity. In comparison, the difference between the active concentrations under the light and in-the-dark for Photolon is approximately one order of magnitude. This allows to suggest a high potential of the new compounds 3 and 4 for further in vitro and in vivo studies to eventually improve the efficiency and safety of photodynamic therapy of cancer.Keywords: Chlorin e 6 , terpene acids, chlorin-terpene conjugates, dicyclohexylcarbodiimide (DCC), photosensitizers.Новые хлорин -терпеновые конъюгаты: синтез, фотоиндуцированная и темновая цитотоксичность

Copper Сomplexes of Сhlorin Derivatives of Chlorophyll a as Potential Photosensitizers for Medical Purposes

“…The photosensitizing efficiencies of metal-free chlorins, virtually coincides with the data reported earlier. [21,30,31] IC 50 in the cells incubated in the dark exceeds IC 50 in illuminated samples by two or more orders of magnitude. The photodamaging effect of complexes (Cu-1-Cu-3) is somewhat weaker, however, the ability of these compounds to exert a photosensitizing cell killing is manifested quite clearly.…”

“…The dark and photoinduced toxic activity of chlorins was investigated as described in refs. [21,30,31]…”

“…The IC 50 values used for estimation of the dark and photoinduced toxicity in experiments on HeLa cells (Table 1) were determined similarly to refs. [21,30,31] The metal-free chlorins (1-3) as well as their copper complexes (Cu-1-Cu-3) showed distinct photosensitizing effect. The photosensitizing efficiencies of metal-free chlorins, virtually coincides with the data reported earlier.…”