Advance on the absorption, metabolism, and efficacy exertion of quercetin and its important derivatives

Abstract

Quercetin, a dietary flavonol, has been used as potential ingredient in food supplements to promote health. Its health effects are closely related to its bioavailability and further depend on its absorption, metabolism and excretion in vivo. Here, we systematically summarized the absorption and metabolism of quercetin in human intestine, liver, and kidney, highlighting the transport and metabolic pathways, intermediate metabolites, and circulation channels involving quercetin. The bioactivities of quercetin on theintestine, liver, and kidney were also considered. In general, except for passive diffusion, different transporters (e.g., SGLT1,OATPs, and MRPs) participate in the transport of quercetin and its metabolites across biological barriers. Quercetin undergoes phase II metabolism after absorption by the intestine and is finally excreted into bile through liver or urine through kidney. Quercetin can protect the intestinal barrier and modulate the microflora. Moreover, its antioxidant, anti-inflammatory, and anti-fibrotic activities protect the liver and kidney.

Quercetin Liposomal Nanoformulation for Ischemia and Reperfusion Injury Treatment

“…Moreover, it would be interesting to investigate quercetin liposomes' antioxidant effect in hepatic IRI, which could give further insights into the mechanisms responsible for the positive therapeutic outcome obtained in the present work. This would enable a more complete comparison of the mechanism of action of the quercetin liposomal formulation with the mechanisms of free quercetin described in the literature, for example by Hai et al [58], Xu et al [14], and Atef et al [47]. Taken together, the results obtained demonstrate that the combination of quercetin with a liposomal nanocarrier resulted in an in vitro and in vivo enhanced therapeutic effect, validating the potential of this system for hepatic IRI treatment.…”

The Targeting of Noncoding RNAs by Quercetin in Cancer Prevention and Therapy

“…The bioavailability and metabolism of quercetin have been well defined. Only a small quantity of quercetin is absorbed in the stomach, and the main site of absorption is the small intestine [ 28 ]. Quercetin predominantly occurs in glycosidic form after oral intake.…”

Polyphenolic Promiscuity, Inflammation-coupled Specificity: Whether PAINs Filters Mask an Antiviral Asset

“…The most commonly obtained pharmacological assay for concentration of polyphenols or their metabolites is blood plasma analysis, rather than interstitial fluid or intracellular fluid. [37][38][39][40][41][42][43][44][45][46][47][50][51][52][53][54][55][56][57][58][59] 2. A polyphenol's plasma concentration profile alone provides no data on tissue distribution or biotransformation.…”

“…Plasma samples of polyphenols are more frequently obtained from healthy individuals, rather than those suffering from a particular pathology. [37][38][39][40][41][42][43][44][45][46][47][51][52][53][54][55][56][57][58][59] Therefore if any particular pharmaceutical candidate's PK profile achieves significant distribution in organs other than those associated with either the GI tract or renal tract, it would be unascertainable from serum analysis alone. Further, if any particular pathology has an effect on a compound's tissue distribution (whether by causing sequestering in sanctuary sites, or adduct formation with the target in tissue both of which represent an increase in the volume of distribution), then plasma analysis alone remains poorly positioned to provide the relevant readout.…”