202803-47-2Relevant academic research and scientific papers
Peptide-targeted dendrimeric prodrugs of 5-aminolevulinic acid: A novel approach towards enhanced accumulation of protoporphyrin IX for photodynamic therapy
Tewari,Dondi,Yaghini,Pourzand,MacRobert,Eggleston
supporting information, (2021/02/26)
Photodynamic therapy (PDT) is a promising approach for the targeted treatment of cancer and various other human disorders. An effective, clinically approved approach in PDT involves the administration of 5-aminolevulinic acid (ALA) to generate elevated levels of the natural photosensitiser protoporphyrin IX (PpIX). The development of prodrugs of ALA is of considerable interest as a means to enhance the efficiency and cell selectivity of PpIX accumulation for PDT applications. In this work a novel peptide-targeted dendrimeric prodrug of 5-aminolevulinic acid (ALA) 13 was synthesised which displays nine copies of ALA on a core structure that is linked to a homing peptide for targeted delivery to a specific cancer cell type. The synthesis was accomplished effectively via a flexible, modular solid phase and solution phase route, using a combination of solid phase peptide synthesis and copper-catalysed azide-alkyne cycloaddition chemistry. The prodrug system shows a sustained and enhanced production of protoporphyrin IX (PpIX) in the MDA-MB-231 cell line that over-expresses the epidernal growth factor receptor (EGFR+) in comparison to equimolar ALA and the corresponding non-targeted ALA dendrimer (nine copies of ALA). This study provides a proof of concept for the development of a new generation of prodrugs for ALA-based photodynamic therapy that can deliver an enhanced ALA payload to specific tissue types.
MULTI-FLUORESCENT SUBSTANCE INCLUDING NOVEL COUMARIN DERIVATIVE, AND LED LIGHT SOURCE-BASED MICROFLUORESCENT QUANTITATIVE BIOSENSOR FOR DIAGNOSIS USING SAME
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Page/Page column, (2014/12/09)
The present invention relates to a novel coumarin derivative, to a method for preparing the same, and a multi-fluorescent substance that includes a plurality of the coumarin derivatives and is able to emit light using an LED light source. A novel coumarin derivative multi-fluorescent substance according to the present invention has an optimal emission wavelength band of 512 nm to 590 nm and thereby is effective in improving a signal intensity and stability since light emission using an LED light source is possible. In addition, higher fluorescence reactivity is exhibited compared to coumarin fluorescent substances known in the related arts since one molecule has a plurality of fluorescent substances, and the problem of the coumarin fluorescent substance possibly binding to a binding site of the antigen of the antibody is solved since fluorescence detection is possible even when a minimum number of fluorescent substance molecules bind to an antibody. Moreover, the novel coumarin derivative multi-fluorescent substance according to the present invention is suitably used in a fluorescent-linked immunosorbent assay (FLISA) and a rapid fluorescent immunochromatographic test (FICT) as an LED-based microfluorescent quantitative biosensor for diagnosis, therefore, diseases such as malaria may be rapidly and quantitatively analyzed.
Synthesis of hyperbranched glycodendrimers incorporating α-thiosialosides based on a gallic acid core
Meunier, Serge J.,Wu, Quigquan,Wang, Sho-Nong,Roy, Rene
, p. 1472 - 1482 (2007/10/03)
Hyperbranched glycodendrimers containing sialic acid residues were synthesized in order to further understand the multivalency effect and its role in carbohydrate-protein interactions. Gallic acid 7 as trivalent core and oligoethylene glycol derivatives as hydrophilic spacers were used to scaffold the dendritic backbones. α-Thiosialoside 16 was conjugated onto N-chloroacetylated dendritic precursors 13, 14, and 26 by nucleophilic substitution to afford trivalent 17, 18, and nonavalent 27 sialodendrimers. Complete sugar deprotection furnished water-soluble α-thiosialodendrimers 21, 22, and 29, which were used in protein-binding studies. Turbidimetric analysis confirmed the strong potential of sialodendrimers 29 having nine readily accessible sialic acid residues to bind, cross-link, and precipitate two different lectins. Preliminary results indicated that nonavalent α-sialodendrimer 29 had a greater affinity towards dimeric wheat germ agglutinin (WGA) and the lectin from the slug Limax flavus (LFA) than the corresponding trivalent glycodendrimers 21 and 22.
