Transepithelial transport mechanisms of 7,8-dihydroxyflavone, a small molecular TrkB receptor agonist, in human intestinal Caco-2 cells

Food & Function
Yufeng ChenYing Zhang

Abstract

7,8-Dihydroxyflavone (7,8-DHF), as a high-affinity TrkB receptor agonist, has been extensively explored in many human disorders involving brain-derived neurotrophic factor (BDNF) such as Alzheimer's disease, Parkinson's disease, depression, and obesity. However, to date, the transepithelial transport mechanisms of 7,8-DHF in the intestines remain unclear. The aim of our work was to quantify and to characterize in vitro transport of naturally occurring 7,8-DHF distinguished by its physicochemical and pharmacological properties. We discussed the transport mechanisms of 7,8-DHF using the Caco-2 cell model to determine the bi-directional permeability with different environmental factors (time, concentration, pH, metabolic inhibitors etc.). The influx and efflux characteristics of 7,8-DHF were also clarified. 7,8-DHF was poorly transported across Caco-2 cell monolayers by mainly passive diffusion via a transcellular pathway and not a paracellular pathway. The transport of 7,8-DHF was time and concentration-dependent in both the apical (AP) to basolateral (BL) side and the reverse direction. Interestingly, decreasing the pH from 7.4 to 6.0 markedly enhanced 7,8-DHF transport. It is noteworthy that 7,8-DHF transport was strongly inhib...Continue Reading

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