Water Soluble Antioxidant Dextran-Quercetin Conjugate with Potential Anticancer Properties

Area of Science:

• Biomaterials Science
• Polymer Chemistry
• Pharmacology

Background:

• Quercetin, a natural antioxidant, has limited therapeutic applications due to poor water solubility and stability.
• Developing stable, soluble quercetin formulations is crucial for enhancing its bioavailability and therapeutic efficacy.

Purpose of the Study:

• To synthesize a water-soluble quercetin-functionalized dextran polymer.
• To characterize the conjugate's properties, including stability, antioxidant activity, and anticancer efficacy.
• To optimize the conjugation process for improved yield and reduced quercetin oxidation.

Main Methods:

• Conjugation of quercetin to aldehyde-functionalized dextran using an HCl-catalyzed condensation reaction.
• Characterization of the conjugate using NMR spectroscopy (¹H and ¹H-¹³C HSQC).
• In vitro evaluation of antioxidant activity, stability, and cytotoxicity against neuroblastoma and nonmalignant cell lines.

Main Results:

• A water-soluble quercetin-dextran conjugate was successfully synthesized, with conjugation confirmed via NMR.
• The degree of quercetin functionalization was tunable by adjusting reaction temperature and HCl concentration.
• The conjugate exhibited improved stability, retained free-radical scavenging activity, and demonstrated selective cytotoxicity against neuroblastoma cells (SH-SY5Y and BE(2)-C) without affecting nonmalignant MRC-5 cells.

Conclusions:

• The developed quercetin-dextran conjugate overcomes the solubility and stability limitations of native quercetin.
• The conjugate shows significant potential as a targeted therapeutic agent for neuroblastoma.
• Optimization of reaction conditions is key to balancing functionalization, stability, and yield.