Anticonvulsant screening of luteolin in four mouse seizure models

Shaikh, Mohd Farooq; Tan, Kah Ni; Borges, Karin

doi:10.1016/j.neulet.2013.06.065

Cited by 25 publications

(12 citation statements)

References 24 publications

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“…Given that we now know of flumazenil-insensitive actions of flavonoids on GABA A receptors this is an incorrect conclusion. Luteolin showed no anticonvulsant activity in four mouse seizure models (Shaikh et al, 2013) and improves spatial memory in rats in a scopolamine-induced amnesia model (Yoo et al, 2013). In unpublished studies my colleagues, Katherine Locock and Ushma Trived, have shown that luteolin selectively enhances the action of GABA at human recombinant a2b2g2L over a1b2g2L GABA A receptor expressed in oocytes in an flumazenil-insensitive manner, consistent with a selective action on anxiety (M€ ohler, 2006).…”

Section: Apigenin Hispidulin and Luteolinmentioning

confidence: 91%

Flavonoid nutraceuticals and ionotropic receptors for the inhibitory neurotransmitter GABA

Johnston

2015

Neurochemistry International

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Section: Apigenin Hispidulin and Luteolinmentioning

confidence: 91%

Flavonoid nutraceuticals and ionotropic receptors for the inhibitory neurotransmitter GABA

Johnston

2015

Neurochemistry International

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“…Luteolin (3′,4′,5,7-tetrahydroxyflavone), a flavone contained in chamomile and chrysanthemum, has potent antioxidant, neuroprotective, anxiolytic, and anti-inflammatory properties [ 59 , 60 ] and decreased iNOS levels in PTZ induced seizures. Antioxidant effect of luteolin has not been revealed directly, but the increase of eNOS in brain and other tissues and decrease of iNOS show that luteolin has an indirect antioxidant effect [ 61 ].…”

Section: Flavonoids With Action In the Cnsmentioning

confidence: 99%

The Role of Flavonoids on Oxidative Stress in Epilepsy

Diniz

Silva

Lima-Saraiva

et al. 2015

Oxidative Medicine and Cellular Longevity

134

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Backgrounds. Oxidative stress can result from excessive free-radical production and it is likely implicated as a possible mechanism involved in the initiation and progression of epileptogenesis. Flavonoids can protect the brain from oxidative stress. In the central nervous system (CNS) several flavonoids bind to the benzodiazepine site on the GABAA-receptor resulting in anticonvulsive effects. Objective. This review provides an overview about the role of flavonoids in oxidative stress in epilepsy. The mechanism of action of flavonoids and its relation to the chemical structure is also discussed. Results/Conclusions. There is evidence that suggests that flavonoids have potential for neuroprotection in epilepsy.

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“…For instance, studies have shown that luteolin has antidepressant and analgesic effects that are considered to be mediated by enhancing GABA A R functions68; however, luteolin did not exhibit any pro- or anti-convulsant effects in various animal models of epilepsy22. Furthermore, luteolin has been reported to enhance learning and memory in a neurodegenerative model10.…”

mentioning

confidence: 99%

Luteolin inhibits GABAA receptors in HEK cells and brain slices

Shen

Wang

Chen

et al. 2016

Sci Rep

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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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Anticonvulsant screening of luteolin in four mouse seizure models

Cited by 25 publications

References 24 publications

Flavonoid nutraceuticals and ionotropic receptors for the inhibitory neurotransmitter GABA

Flavonoid nutraceuticals and ionotropic receptors for the inhibitory neurotransmitter GABA

The Role of Flavonoids on Oxidative Stress in Epilepsy

Luteolin inhibits GABAA receptors in HEK cells and brain slices

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