The uptake behaviors of kaempferol and quercetin through rat primary cultured cortical neurons

Abstract

The objective of this study was to investigate whether kaempferol and quercetin could be transported into primary cultured cerebral neurons, to establish a practical HPLC method with UV detection for the two flavonols in the neurons, and to study the uptake and transport behaviors of them through the neurons. The present results showed that the level of kaempferol in the neurons increased linearly and then reached a plateau with incubation time at the high concentration of 10 microg/mL, but not at the other two concentrations of 1 and 0.1 microg/mL. However, the levels of quercetin in the neurons were not detected at the three incubating concentrations, and there was a new peak detected in the cell whose retention time was shorter (3.42 min) than that of quercetin (4.65 min). This phenomenon suggested that quercetin might be transported into the neurons and then metabolized quickly to some derivative. Kaempferol could be transported into the neurons in a concentration- and time-dependent manner when the neurons were incubated with the culture medium containing kaempferol at the high dose. There was an apparent correlation between the concentrations of kaempferol in the medium and in the cell, indicating that the uptake of kaempferol in the cell increased along with its dose (10 microg/mL). However, there was a negative correlation between the concentrations of quercetin in the medium and in the cell. The results suggested that kaempferol and quercetin were disposed by the neurons at different way, and this might be an important factor for their different effects on primary cultured cortical cells.

Facilitating Mitochondrial Calcium Uptake Improves Activation-Induced Cerebral Blood Flow and Behavior after mTBI

“…Kaempferol, a dietary flavonoid compound and a specific enhancer of the mitochondrial Ca 2+ uniporter channel (mCU) (Montero et al, 2004 ), capable of crossing the blood brain barrier and diffusing freely into cells and organelles (Liu et al, 2006 ), was administered in a dose relevant to dietary intake. Dietary therapy is recognized to be advantageous to patients recovering from mild TBI without necessitating hospitalization and intravenous access for drug administration and considered important in preclinical treatment studies of TBI (Elkind et al, 2015 ).…”

Kaempferol Attenuates 4-Hydroxynonenal-Induced Apoptosis in PC12 Cells by Directly Inhibiting NADPH Oxidase

“…Kaempferol can be transported into the neurons in a concentration-dependent manner when the neurons were incubated with the culture medium containing kaempferol (Liu et al, 2006). Because of its permeability in neurons, kaempferol at concentrations of 5 and 10 M might directly bind cytosolic p47 phox and interfere with 4-HNE-induced NOX activity in PC12 cells.…”

Comparison of Quercetin Pharmacokinetics Following Oral Supplementation in Humans

“…The supernatant was diluted with mobile phase and analyzed by HPLC. No stability experiments were performed as quercetin's stability at room temperature has been well documented at pH 4.0 (Moon and others 2008) and in methanol (Liu and others 2006). …”