Drug intelligence / Profile preview

luteolin

Development stage
Phase 2
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Luteolin is a naturally occurring flavonoid found in many plants, including celery, parsley, and chamomile. It exhibits a wide range of pharmacological activities such as anti-inflammatory, antioxidant, neuroprotective, analgesic, anti-allergic, antibacterial, antiviral, apoptosis-inducing and chemopreventive effects[1][3][4][8]. Mechanistically, luteolin acts by inhibiting key inflammatory mediators (such as Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and Mitogen-activated protein kinase (MAPK) pathways), reducing oxidative stress through direct scavenging of Reactive oxygen species (ROS) and activation of antioxidant enzymes[1][5][6]. It also modulates the Janus kinase/signal transducer and activator of transcription pathway (JAK/STAT pathway) and enhances transepithelial sodium transport in lung tissue[5], interacts with GABAA receptor for analgesic effects[1], suppresses cAMP-phosphodiesterase activity to reduce inflammation[5], and can induce apoptosis in tumor cells while protecting normal cells from oxidative damage[6]. Luteolin has been studied preclinically for chronic inflammatory diseases (e.g., rheumatoid arthritis), neuropathic pain conditions, respiratory diseases like COPD and ARDS/ALI[1][5], viral infections including COVID-19[8] and RSV pneumonia[5], as well as cancer prevention. While it shows promise for these indications due to its safety profile in preclinical studies,[1] further clinical trials are needed to establish efficacy.

Other names
3',4',5,7-tetrahydroxyflavone
02

Targets

RELA (Nuclear Factor Kappa B Subunit p65)GABRR (GABA-A receptor subunit rho)MEKPDE (Phosphodiesterase family)

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