Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
9769186 | European Journal of Medicinal Chemistry | 2005 | 12 Pages |
Abstract
Several strategies have been proposed to improve the efficiency of photosensitizers used in photodynamic therapy (PDT). In this context, the synthesis of mono- (1) and di-glucosylated (2) porphyrins, and mono-glucosylated chlorin (3) was performed. HT29Â human adenocarcinoma cells were significantly more sensitive to asymmetric and less hydrophobic glucosylated photosensitizers-mediated PDT (1, 3), compared to tetraphenylporphyrin (TPP). The lowest photosensitivity observed for TPP was consistent with the lowest uptake. Moreover, the most pronounced photodynamic activity measured for 3 was in relation with the improvement of cellular uptake, the singlet oxygen quantum yield and the high extinction coefficient value at 650Â nm compared to porphyrins. Cellular localization analysis showed that 1 and 3 accumulated mainly inside the endoplasmic reticulum.
Keywords
DIOC6EtOHDMAPPDT4-dimethylaminopyridineTFARP-HPLCNaHCO3NHSDCCMgSO4BOCDMFCH2Cl2N-hydroxysuccinimidedicyclohexylcarbodiimidetetramethylsilaneCDCl3EDCIDDQtert-butoxycarbonylTMSchloroform-dTPPNaOHPBSTHFHCl1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride1-hydroxybenzotriazole3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromideBSADMSOMTTTetraphenylporphyrinAdenosine TriphosphateATPbovine serum albuminEthanolEDTAEthylene diamine tetra acetic acidTrifluoroacetic acidhydrochloric acidTetrahydrofuranNMRPhotodynamic therapyIn vitrodimethyl formamideDichloromethaneDimethyl sulfoxidequenching constantsodium bicarbonatei.d.Nuclear magnetic resonance spectroscopyPhosphate buffered salineInternal DiameterMethanolmagnesium sulfateMeOHTargetingsodium hydroxidePorphyrinReversed phase high performance liquid chromatographyChlorinGlucosylation
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Benoît Di Stasio, Céline Frochot, Dominique Dumas, Pascale Even, Jurriaan Zwier, Audrey Müller, Jacques Didelon, François Guillemin, Marie-Laure Viriot, Muriel Barberi-Heyob,