863892-06-2Relevant academic research and scientific papers
Design, synthesis, and delivery properties of novel guanidine-containing molecular transporters built on dimeric inositol scaffolds
Maiti, Kaustabh K.,Jeon, Ock-Youm,Lee, Woo Sirl,Chung, Sung-Kee
, p. 762 - 775 (2007/10/03)
We have developed a novel class of synthetic molecular transporters that contain eight residues of guanidine with an inositol dimer as the scaffold. The dimers were prepared by connecting two units of myo- or scyllo-inositol via a carbonate or amide linkage, and the multiple units of the guanidine functionality were constructed on the inositol scaffold by means of peracylation with ω-aminocarboxylate derivatives of varying length. Bioassays based on confocal laser scanning microscopy and fluorescence-activated cell sorter analyses indicated that these transporters display a varying degree of membrane translocating ability, and the intracellular localization and mouse-tissue distribution studies strongly suggested that these transporters undergo substantially different mechanistic processes from those of peptide transporters reported to date. It was also shown that doxorubicin, an anticancer antibiotic, can be efficiently delivered into mouse brain by aid of this type of transporter.
Design, synthesis, and membrane-translocation studies of inositol-based transporters
Maiti, Kaustabh K.,Jeon, Ock-Youm,Lee, Woo Sirl,Kim, Dong-Chan,Kim, Kyong-Tai,Takeuchi, Toshihide,Futaki, Shiroh,Chung, Sung-Kee
, p. 2907 - 2912 (2007/10/03)
(Figure Presented) Delivery vehicles: Novel guanidine-containing "transporters" constructed on a dimeric inositol scaffold show significant translocation across the cell membrane and the blood-brain barrier, as well as unique in vitro and in vivo distributions. Doxorubicin was efficiently delivered to mouse-brain tissue by conjugating the compound with such a transporter (see the fluorescence microscopy image).
