The use of internalizable derivatives of chlorin E6 for increasing its photosensitizing activity.
Experiments with human hepatoma PLC/PRF/5 cells and human embryo skin fibroblasts involving the use of three different tests (colony formation, Trypan blue exclusion, labeled thymidine incorporation) have demonstrated a significantly higher photosensitizing activity of chlorin e6 conjugates with internalizable ligands as compared to that of chlorin e6 itself. Receptor-mediated internalization of chlorin e6 conjugates ensures a greater photosensitization of cells than binding of those conjugates to cell surface receptors. The suitability of such conjugates that permit the delivery of a photosensitizer to sensitive intracellular targets is discussed.
Russian Research Center of Molecular Diagnostics and Therapy, Moscow.
T V
TV
Akhlynina
A A
AA
Rosenkranz
D A
DA
Jans
P V
PV
Gulak
N V
NV
Serebryakova
A S
AS
Sobolev
D002478:Cells, Cultured; D002735:Chlorophyllides; D005347:Fibroblasts / Q000187:drug effects / Q000528:radiation effects; D006801:Humans; D010777:Photochemistry; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000378:metabolism / Q000494:pharmacology*; D011166:Porphyrins / Q000378:metabolism / Q000494:pharmacology*; D011972:Receptor, Insulin / Q000378:metabolism; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000528:radiation effects
D002735:Chlorophyllides; D017319:Photosensitizing Agents; D011166:Porphyrins; C062985:phytochlorin; D011972:Receptor, Insulin