Panpan Song, Sa Xiao, Yanqing Zhang*, Junbo Xie* and Xusheng Cui Pages 633 - 645 ( 13 )
Background: Flavonoid compounds are one kind of active ingredients isolated from a traditional Chinese herb Zizyphi spinosae semen (ZSS). Studies have shown that ZSS flavonoids have significant antioxidant effects.
Methods: In this study, the Caco-2 cell monolayer model was constructed to investigate the intestinal absorption characteristics and mechanism of Isovitexin (IV), Swertisin (ST), Isovitexin-2''-O-β-D-glucopyranoside (IVG), Spinosin (S), 6'''-p-coumaroylspinosin (6-CS) and 6'''-feruloylspinosin (6-FS).
Results: The results of the bidirectional transport assay showed that the six flavonoids have good intestinal absorption in a near-neutral and 37°C environment, and the absorbability in descending order was 6-FS>6- CS>IVG>S>IV>ST. The results of carrier inhibition experiments and transport kinetics indicated that the absorption mechanism of six flavonoids was energy-dependent monocarboxylate transporter (MCT)-mediated active transport. In particular, the para-cellular pathway also participated in the transport of IV, ST, IVG and S. Furthermore, the efflux process of six flavonoids was mediated by P-glycoprotein (P-gp) and multidrug resistance protein (MRP), which may result in a decrease of bioavailability.
Conclusion: Our findings provide significant information for revealing the relationship between the intestinal absorption mechanism of flavonoids and its structure as well as laying a basis for the research of flavonoid preparations.
Zizyphi spinosae semen, flavonoids, Caco-2 cell model, intestinal absorption, mechanism, transport kinetics.
College of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin, 300134, College of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin, 300134, College of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin, 300134, School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, Shijiazhuang Yiling pharmaceutical Co. Ltd, Hebei, 050035