Drug intelligence / Profile preview

taxifolin

Development stage
Preclinical
Lead developer
Ametis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Taxifolin is a naturally occurring flavonoid of the flavanonol subclass, also known as dihydroquercetin. It is found in various plants and foods such as grapes, citrus fruits, onions, green tea, olive oil, and herbs like milk thistle[4][7]. Taxifolin exhibits potent antioxidant activity and has demonstrated anti-inflammatory, antimicrobial (including antibacterial and antifungal), anticancer, hepatoprotective, neuroprotective, anti-hyperlipidemic and cardiovascular protective effects in preclinical studies[3][4][5][7][8]. Mechanistically it acts by scavenging free radicals; inhibiting oxidative stress pathways; modulating inflammatory signaling including NF-κB; suppressing COX-2 and iNOS expression; inducing phase II detoxifying enzymes; suppressing cytochrome P450-dependent monooxygenases; inhibiting apoptosis and cancer cell cycle progression[3][4][5]. Taxifolin can inhibit amyloid-β production via the ApoE-ERK1/2 pathway in models of cerebral amyloid angiopathy[3], block protein aggregation relevant to neurodegenerative diseases[6], act as a non-selective opioid receptor antagonist with weak affinity[7], agonize adiponectin receptor 2 (AdipoR2)[7], inhibit degranulation of mast cells via MAPKs/cPLA2/NF-κB pathways[8], regulate glucose metabolism through PI3K/AKT signaling[8] and maintain lipid homeostasis by reducing cholesterol esterification/synthesis[7]. It is not an approved pharmaceutical drug but is considered experimental for multiple indications.

Other names
dihydroquercetin(+)-taxifolin(±)-taxifolin
02

Targets

IleRS (Isoleucyl-tRNA synthetase)NOS2 (Nitric Oxide Synthase 2)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)MOR (Mu opioid receptor)mTOR (Mammalian target of rapamycin kinase)ADIPOR2 (Adiponectin receptor 2)DNA gyrase

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