ArticleScientific reports2016
Luteolin inhibits GABAA receptors in HEK cells and brain slices.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 19 citations in OpenAlex.
- Effect of Phenolic Compounds and Terpenes on the Flavour and Functionality of Plant-Based Foods.Nutrients · 2025Review
- Recent Advances in Bioactive Flavonoids-based Nanotherapeutics as Promising Neuroprotectants in Epilepsy.Current aging science · 2025Review
- The Neuroprotective Effect of Rooibos Herbal Tea Against Alzheimer's Disease: A Review.Molecular nutrition & food research · 2025Review
- Luteolin reversed anxiety and depressive-like behavior via modulation of the NF-κB/NLRP3 inflammasome axis in the hippocampus of rats subjected to sleep deprivation.Iranian journal of basic medical sciences · 2024Article
- Antidepressant-Like Effects ofJournal of experimental pharmacology · 2024Article
- Phenolics as GABAMolecules (Basel, Switzerland) · 2022Review
- Flumazenil-Insensitive Benzodiazepine Effects in Recombinant αβ and Neuronal GABABrain sciences · 2020Article
- Anxiolytic and anti-depressant effects of hydroalcoholic extract fromAfrican health sciences · 2019Article
- Structure-Dependent Activity of Natural GABA(A) Receptor Modulators.Molecules (Basel, Switzerland) · 2018Review
- Recent updates on neuropharmacological effects of luteolin.EXCLI journal · 2018Article
- Antidepressant and anxiolytic activity of Lavandula officinalis aerial parts hydroalcoholic extract in scopolamine-treated rats.Pharmaceutical biology · 2017Article
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Modulation of the A type γ-aminobutyric acid receptors (GABAAR) is one of the major drug targets for neurological and psychological diseases. The natural flavonoid compound luteolin (2-(3,4-Dihydroxyphenyl)- 5,7-dihydroxy-4-chromenone) has been reported to have antidepressant, antinociceptive, and anxiolytic-like effects, which possibly involve the mechanisms of modulating GABA signaling. However, as yet detailed studies of the pharmacological effects of luteolin are still lacking, we investigated the effects of luteolin on recombinant and endogenous GABAAR-mediated current responses by electrophysiological approaches. Our results showed that luteolin inhibited GABA-mediated currents and slowed the activation kinetics of recombinant α1β2, α1β2γ2, α5β2, and α5β2γ2 receptors with different degrees of potency and efficacy. The modulatory effect of luteolin was likely dependent on the subunit composition of the receptor complex: the αβ receptors were more sensitive than the αβγ receptors. In hippocampal pyramidal neurons, luteolin significantly reduced the amplitude and slowed the rise time of miniature inhibitory postsynaptic currents (mIPSCs). However, GABAAR-mediated tonic currents were not significantly influenced by luteolin. These data suggested that luteolin has negative modulatory effects on both recombinant and endogenous GABAARs and inhibits phasic rather than tonic inhibition in hippocampus.
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