Drug intelligence / Profile preview

naringenin

Development stage
Preclinical
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Topical, Intravenous
01

Overview

Naringenin is a naturally occurring flavanone belonging to the flavonoid group of polyphenols. It is widely distributed in citrus fruits such as grapefruit and oranges and also found in tomatoes and other plants. Naringenin exhibits a range of biological activities including antioxidant, anti-inflammatory, anti-diabetic, hepatoprotective, anti-mutagenic, anti-carcinogenic and cardioprotective effects. Mechanistically, it acts by scavenging reactive oxygen species (ROS), modulating immune system activity (notably through inhibition of leukocyte recruitment), suppressing NFκB activation and pro-inflammatory cytokine production in macrophages. Naringenin also activates the nuclear factor erythroid 2–related factor 2 (Nrf2) pathway leading to increased expression of detoxification and antioxidant proteins such as HO-1. Additionally, it can modulate transient receptor potential channels involved in pain signaling (TRPV1/TRPM3/TRPM8) and enhance insulin sensitivity by affecting protein kinase C signaling pathways[2][6][8]. Despite its promising pharmacological profile for conditions like cardiovascular disease or liver disorders, its clinical application is limited by poor water solubility and low bioavailability[5]. Naringenin may interact with cytochrome P450 enzymes—especially CYP3A4—potentially altering the metabolism of various drugs[3][5].

Other names
(S)-naringenin5,7-dihydroxy-2-(4-hydroxyphenyl)-2,3-dihydrochromen-4-oneCAS 480-41-1CAS480-41-1CAS-480-41-1
02

Targets

CYP19A1 (Aromatase)CYP3A4 (Cytochrome P450 3A4)KEAP1 (Kelch-like ECH-associated protein 1)

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