Hohenbuehelia serotina polysaccharides self-assembled nanoparticles for delivery of quercetin and their anti-proliferative activities during gastrointestinal digestion in vitro

Abstract

In this study, the self-assembled nanoparticles based on Hohenbuehelia serotina polysaccharides (QC-HSP NPs) were fabricated to encapsulate quercetin for improving its bioavailability. The structural characteristics, physicochemical properties as well as the cytotoxicity activities of QC-HSP NPs during gastrointestinal digestion in vitro were respectively investigated. The results showed that QC-HSP NPs possessed the spherical and smooth surface morphology, with the average particle size of 360 nm and zeta potential of -38.8 mV. Moreover, QC-HSP NPs had excellent physiochemical stabilities, and presented sustained-release characteristics during gastrointestinal digestion in vitro. Compared with undigested ones, QC-HSP NPs after gastrointestinal digestion exhibited the more significant anti-proliferative activity on HeLa cells through accumulation of intracellular ROS, arrest of cell cycle at G2/M phase by regulation of cyclin B1, CDK1, p53 and p21 and induction of apoptosis by ER apoptosis pathway. This study provides a new strategy for designing quercetin-loaded nanoparticles based on natural polysaccharides to improve the bioavailability of quercetin.

Keywords: Anti-proliferative activity; Gastrointestinal digestion; Hohenbuehelia serotina polysaccharides; Physicochemical characteristic; Quercetin.