luteolin

Overview

Luteolin is a naturally occurring flavone widely distributed in edible plants and medicinal herbs. It is a dietary polyphenol of interest in biomedical research because of its reported antioxidant and anti-inflammatory properties, as well as broader pharmacological potential. In the recent literature provided, luteolin is also described as a biopharmaceutical classification system (BCS) Class II compound, indicating low aqueous solubility but relatively favorable permeability, a profile that has motivated formulation research to improve its delivery.

Biologically, luteolin has been investigated in relation to oxidative stress, apoptosis, inflammatory signaling, and disease-modifying effects in several experimental settings. Recent studies have explored its activity in cancer, neuroprotection, hearing loss, sepsis-associated encephalopathy, and myocardial infarction repair, often in combination with advanced delivery systems such as nanosuspensions, PEGylated nano-vesicular platforms, nanocomposites, and hydrogels. It has also been quantified as a phytochemical marker in plant materials and herbal preparations, reflecting its importance in natural product analysis and quality control.

Focus of Latest Publications

Recent publications document luteolin's therapeutic potential across multiple organ systems and pathological contexts, with particular emphasis on overcoming its poor aqueous solubility and limited bioavailability through advanced formulation strategies. Studies have explored encapsulation approaches including WPI-Pueraria lobata composite gels, PEGylated aspasomes, lactoferrin-chondroitin sulfate nanoparticles, and nanosuspensions to enhance intestinal absorption, brain penetration, and target-tissue delivery. These delivery platforms consistently demonstrated improved stability, enhanced cellular uptake, and superior bioactivity compared to free luteolin in both in vitro and in vivo models.

In metabolic and systemic inflammation contexts, luteolin-based interventions showed efficacy in adipose tissue dysfunction and insulin resistance. A WPI-encapsulated formulation promoted thermogenic gene expression (UCP1, Pgc-1α, Prdm16, Cidea) in brown adipocytes and restored insulin sensitivity in white adipocytes impaired by inflammatory stimuli, while simultaneously suppressing pro-inflammatory cytokine production (IL-6, TNF-α, IL-1β) in macrophage models. These findings aligned with observations in sepsis-associated encephalopathy, where luteolin-loaded nanocomposites shifted microglia polarization from the pro-inflammatory M1 phenotype toward the anti-inflammatory M2 phenotype via suppression of the TLR4/MyD88/NF-κB pathway.

Luteolin's neuroprotective capacity emerged across stress-related and degenerative contexts. PEGylated luteolin aspasomes administered to chronically stressed rats enhanced spatial memory, attenuated depressive-like behavior, and reduced hippocampal acetylcholinesterase activity while increasing brain-derived neurotrophic factor levels. The flavonoid additionally demonstrated protective effects against noise-induced hearing loss through mitigation of oxidative stress and apoptosis, potentially via regulation of the EGR1/SPRY4 axis.

In cardiac pathology, an injectable hydrogel incorporating luteolin addressed the multifactorial injury cascade following myocardial infarction by simultaneously reducing inflammatory cytokines, alleviating oxidative stress through Nrf2/HO-1 pathway activation, and preserving connexin 43-mediated electrical coupling to reduce arrhythmia incidence. Preliminary evidence also indicated luteolin's potential in oncology, with studies identifying the flavonoid as an inhibitor of cervical cancer cell growth through carbonic anhydrase II suppression. Across diverse formulations and applications, luteolin consistently engaged antioxidant and anti-inflammatory mechanisms involving nuclear factor-kappa B and phosphoinositide 3-kinase signaling.

Key Publications

• NEWJun Biomedical publication details. (PubMed Database, 2026, PMID 42283235)
• Jun Liquid Chromatography-Electrospray Ionization-Tandem Mass Spectrometry Profiling, Antioxidant, Antibacterial, and Antidiabetic Properties of Fagonia cretica L.: Insights From In Vitro and In Silico Approaches. (ChemistryOpen, 2026, PMID 42168772): "Molecular docking identified quercetin, luteolin, and catechin as leading compounds, displaying strong binding affinities across antioxidant, antibacterial, and antidiabetic protein targets-at times surpassing reference ligands."
• May Improving the palatability of Platycodonic Radix for pediatric use: Integrating LC-MS-based bitter component profiling with an HP-β-Cyclodextrin/xylitol taste-masking strategy. (International journal of pharmaceutics, 2026, PMID 42155616): "Docking results indicated that platycodigenin, polygalacic acid, lactone-type platycodins, luteolin, and lignans show high affinity for human bitter taste receptors TAS2R14, TAS2R44, and TAS2R47, confirming a multi-component basis for PR bitterness."
• May Valorization of Pitaya (Selenicereus monacanthus) Peels: Proof of Concept for Food Formulation. (Plant foods for human nutrition (Dordrecht, Netherlands), 2026, PMID 42128980): "It showed a significant content of bioactive flavonoids, with isorhamnetin, rutin, myricetin, quercetin, and luteolin as major identified compounds."
• May PEGylated Flavonoid Aspasomes as a Brain-Targeted Nano-Vesicular Platform for Enhanced Neuroprotection in Stress-Induced Cognitive Dysfunction. (AAPS PharmSciTech, 2026, PMID 42091762): "Luteolin (LUT) is a biologically active flavonoid exhibiting significant therapeutic potential against neurodegenerative disorders such as cognitive impairment."
• May Luteolin Protects Against Noise-Induced Hearing Loss via Mitigating Oxidative Stress and Apoptosis, With Potential Regulation of the EGR1/SPRY4 Axis. (CNS neuroscience & therapeutics, 2026, PMID 42067975): "This study explored the protective effect of luteolin (LL), a natural antioxidant flavonoid, against NIHL and its underlying molecular mechanism."
• Jun A comprehensive insight into optimized ultrasound-assisted extraction of bioactive compounds and antioxidant activities from dandelion (Taraxacum officinale) plant extract using response surface methodology. (Ultrasonics sonochemistry, 2026, PMID 42068787): "Under optimized conditions major bioactive compounds identified and quantified were chlorogenic acid, quercetin, apigenin, luteolin-7-O-glycoside, luteolin, p-coumaric acid, caffeic acid, ferulic acid, cichoric acid, isoetin, and caftaric acid."
• Jun Improvement of aqueous solubility and oral bioavailability of luteolin: a nanosuspension approach. (Drug development and industrial pharmacy, 2026, PMID 42050999): "Luteolin (LT), a naturally occurring flavonoid and biopharmaceutical classification system (BCS) Class II compound, holds broad pharmacological potential."
• May Injectable, Conductive, Multifunctional Hydrogels with Sustained Luteolin Release for Promoting Myocardial Infarction Repair. (ACS applied materials & interfaces, 2026, PMID 42008242): "Constructed from a thermo-/photo-cross-linkable Pluronic F127 diacrylate matrix functionalized with luteolin, recombinant human collagen type I, and MXene nanosheets, FLCM exhibits excellent injectability, electrical conductivity, mechanical robustness, cell affinity, and sustained drug release capability."
• Jun Metabolomics analysis reveals dynamic changes in the quality components and antioxidant activity capacity during variable temperature drying of Jinsihuangju (Chrysanthemum morifolium) tea. (Food research international (Ottawa, Ont.), 2026, PMID 41895980): "likely due to the significant increase in functional components such as luteoloside, isovitexin, luteolin, apigenin 7-O-glucoside."