Target intelligence / Profile preview

Quercetin (QC)

Target
QC
Molecular classification
Flavonoid, Flavonol, Polyphenol, Phytoestrogen
01

Overview

Quercetin is a ubiquitous dietary flavonol and a prominent member of the flavonoid class of polyphenols, found in high concentrations in foods such as onions, apples, and berries [1, 15]. Although often termed a "target" in popular literature, it is fundamentally a bioactive small molecule that exerts pleiotropic effects by binding to and modulating numerous proteins, including kinases, enzymes, and transporters [1, 17]. Its biological roles are diverse, characterized by potent antioxidant activity via free radical scavenging and anti-inflammatory properties through the inhibition of pro-inflammatory cytokines and pathways like NF-κB and cyclooxygenase (COX) [4, 11]. In therapeutic research, quercetin is extensively investigated for its potential in managing chronic conditions such as cancer, diabetes, and cardiovascular diseases [3, 7]. It is particularly noted for its "senolytic" properties, often used in combination with drugs like dasatinib to selectively eliminate senescent cells to combat aging-related pathologies [10]. Despite its broad pharmacological profile and interaction with key survival pathways like PI3K/Akt/mTOR, quercetin's transition to clinical practice is hampered by its poor water solubility, rapid metabolism, and low systemic bioavailability [6, 19].

Other names
3,3',4',5,7-PentahydroxyflavoneSophoretinMeletinXanthaurineQuercetolQuercitinFlavin meletin
02

Mechanism of action

Quercetin acts as a multi-target modulator that inhibits various signaling pathways including PI3K/Akt/mTOR and NF-κB, scavenges reactive oxygen species (ROS), and inhibits multiple protein kinases such as Aurora kinase and Hck. It also modulates the activity of ABC transporters like P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP), and regulates transcription factors such as Nrf2 to enhance antioxidant defenses.

03

Biological functions

AntioxidantSignal transductionApoptosisCell cycleImmune responseEnzyme inhibitionSenolysis
04

Disease associations

CancerInflammationCardiovascular diseaseDiabetesNeurodegenerative diseaseInfection
05

Safety considerations

Poor bioavailabilityPotential for drug-drug interactions through CYP450 and P-gp inhibitionPro-oxidant effects at high concentrationsLack of target specificityLimited clinical evidence for efficacy
06

Interacting drugs

Dasatinib

6 more in the full profile.

07

Biomarkers

Malondialdehyde (MDA)C-reactive protein (CRP)Superoxide dismutase (SOD)p16INK4aGlutathione peroxidase (GPx)

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