Modifying natural products aiming the increase of their bioavailability (Master thesis)

Διαμαντής, Δημήτριος

Natural products and their derivatives since ancient times have been used by traditional medicine to deal with many diseases. Flavonoids, as an important member of the large family of natural products, possess a rich pharmacological profile including antioxidant, antiviral and anti-tumor properties. The purpose of this postgraduate dissertation is the synthesis, characterization and biological evaluation of modified analogues based on flavonoids in order to increase their bioavailability. Initially, quercetin-2HP-β-CD host-guest complex was studied using a series of analytical techniques including solid state NMR, DOSY NMR, UV-vis spectroscopy and molecular dynamics simulations. The bioactivity of the complex was also evaluated and found that it reduces the cell viability of human T24 bladder cancer cells. Subsequently, the decomplexation of quercetin from the cavity of 2HP-β-CD was spectroscopy investigated in presence of iron species at two different pH values, in which the formation of metal complexes between quercetin and iron was observed. In addition, cyclic voltammetry studies were conducted in which the complex and native quercetin showed the same oxidative profile. Finally, in order to enhance the solubility and the bioavaibility of naringenin and apigenin we synthesized and characterized two prodrugs, trigged by alkaline phosphatase, which will selectively release the native drug, exclusively in cancer cells.
Institution and School/Department of submitter: Πανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείας
Subject classification: Φυσικά προϊόντα
Keywords: Φυσικά προϊόντα,Φλαβονοειδή,Προφάρμακα,Natural products,Flavonoids,Prodrugs
Appears in Collections:Διατριβές Μεταπτυχιακής Έρευνας (Masters)

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