Conjugated PDT drug: photosensitizing activity and tissue distribution of PEGylated pheophorbide a was written by Rapozzi, Valentina;Zacchigna, Marina;Biffi, Stefania;Garrovo, Chiara;Cateni, Francesca;Stebel, Marco;Zorzet, Sonia;Bonora, Gian Maria;Drioli, Sara;Xodo, Luigi E.. And the article was included in Cancer Biology & Therapy in 2010.Related Products of 92557-80-7 This article mentions the following:
The design of new photosensitizers with enhanced phototoxicity and pharmacokinetic properties remains a central challenge for cancer photodynamic therapy (PDT). In this study, Pheophorbide a (Pba) has been pegylated to methoxypolyethylene glycol (mPEG-Pba) to produce a soluble photosensitizer that exhibits a higher tissue distribution than free Pba. In vitro studies have shown that mPEG-Pba promotes a fairly strong photosensitizing effect in cancer cells, as previously observed for the unpegylated mol. MPEG-Pba targets the mitochondria where, following photoactivation, ROS are produced which cause a cellular injury by lipid peroxidation The effect of pegylation on the photosensitizer biodistribution has been examined in different selected organs of female mice, at different time points after i.p. administration of the drug (50 μmol/Kg body weight). Other than free Pba, which showed a low tissue accumulation, mPEG-Pba has been detected in significant amounts (8 to 16 μg/mL) in liver, spleen, duodenum and kidney and, 3-5 h after i.p. injection, in moderate amounts (3 to 8 μg/mL) in brain and lung. In vivo optical imaging performed on living female C57/BL6 mice bearing a s.c. melanoma mass, showed that injected mPEG-Pba distributes all over the body, with an higher uptake in the tumor respect to free Pba. Our results indicate that although pegylation somewhat decreases the phototoxicity, it significantly increases the drug solubility and tissue distribution and tumor uptake of mPEG-Pba, making the conjugate an interesting photosensitizer for PDT. In the experiment, the researchers used many compounds, for example, 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7Related Products of 92557-80-7).
2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Related Products of 92557-80-7
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem