Synthesis of chlorin-based unsaturated fatty acid conjugates: Their in vitro phototoxicity on TC-1 cancer cell line

Chlorin-based photosensitizers in photodynamic therapy are the promising anticancer agents, but some of their properties such as specific-targeting to tumor need to be improved. The aim of this study was to synthesize chlorin-based unsaturated fatty acid conjugates to obtain an optimal photosensitizers. Thus four chlorin-based fatty acid conjugates were successfully synthesized through an esterification reaction using carbodiimide coupling reagents in enough yields. Then, structures of these conjugates were confirmed by 1H NMR, MALDI-MS, and UV–vis spectroscopy. Furthermore, their in vitro phototoxicity and cellular uptake were evaluated on TC-1 lung cancer cell line and HeLa cell line.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Four unsaturated fatty acid conjugates were synthesized for photodynamic therapy. ► Phototoxicity of PDT conjugates was evaluated with TC-1 cell line via MTT assay. ► PDT conjugates cellular uptake was investigated with TC-1 cell line.