Chrysin (5,7-dihydroxyflavone) exerts anxiolytic-like effects through GABAA receptors in a surgical menopause model in rats

Rodríguez‐Landa, Juan Francisco; Hernández-López, Fabiola; Cueto‐Escobedo, Jonathan; Herrera-Huerta, Emma Virginia; Rivadeneyra-Domínguez, Eduardo; Bernal-Morales, Blandina; Romero-Avendaño, Elizabeth

doi:10.1016/j.biopha.2018.11.111

Cited by 28 publications

(34 citation statements)

References 46 publications

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“…Those findings resembled the effect of diazepam. At doses of 1, 2, and 4 mg/kg, this flavonoid increased the frequency of entries into, and the time spent in, the open arms of EPM partially through action on GABA A receptors (pretreatment with 1 mg/kg picrotoxin) [49]. On the other hand, neurosteroids and the serotonergic system have also been implicated in the anxiolytic effect of flavonoids, as in the case of puerarin, which increased 5-HT and allopregnanolone levels in the prefrontal cortex and hippocampus in male rats.…”

Section: Flavonoids With Anxiolytic Effectsmentioning

confidence: 96%

Neuropharmacology of Secondary Metabolites from Plants with Anxiolytic and Antidepressant Properties

García-Ríos¹,

Mora-Pérez²,

Ramos-Molina³

et al. 2020

Behavioral Pharmacology - From Basic to Clinical Research

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Depression and anxiety currently rank as the second and fifth most common causes worldwide of years lived with disability-a reality that has intensified the search for new treatments. There are many studies of herbal extracts and secondary metabolites from plants used in traditional medicine due to their antidepressant and anxiolytic properties. Clinical and preclinical studies about some of the mechanisms of action of metabolites like alkaloids, terpenes, flavonoids, and sterols, among others, have documented effects similar to those produced by clinically effective drugs. These metabolites have shown anxiolytic and antidepressant effects in various experimental models of anxiety by interacting with γ-aminobutyric acid subtype A receptors (GABA A-receptors) and by stimulating the serotonergic, noradrenergic, and dopaminergic neurotransmitter systems. These pharmacological effects can be attributed to plant metabolites that share structural similarities with monoamines, which allow them to bind to receptors. The objective of this chapter is to summarize the various mechanisms of action that have been identified in secondary metabolites with anxiolytic and antidepressant properties. Terpenes, alkaloids, flavonoids, and sterols can interact at different levels of the neurotransmission systems involved in the neurobiology of anxiety and depression, suggesting their potential for treating these mental illnesses.

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Section: Flavonoids With Anxiolytic Effectsmentioning

confidence: 96%

Neuropharmacology of Secondary Metabolites from Plants with Anxiolytic and Antidepressant Properties

García-Ríos¹,

Mora-Pérez²,

Ramos-Molina³

et al. 2020

Behavioral Pharmacology - From Basic to Clinical Research

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show abstract

“…В іншому дослідженні на щурах також була показана анксіолітична дія кризину порівняно з діазепамом [49].…”

Section: N№ 4 (106) 2019unclassified

Особливості Лікувальної Тактики При Коморбідності Інсомнії Та Тривоги: В Пошуках Безпечної Альтернативи Бензодіазепінів

Kopchak¹

2021

INJ

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Особливості лікувальної тактики при коморбідності інсомнії та тривоги: в пошуках безпечної альтернативи бензодіазепінів Резюме. У статті подано визначення та сучасні діагностичні критерії інсомнії, висвітлено аспекти спільних патогенетичних механізмів розвитку інсомнії та тривоги. Детально описано підходи до лікування інсомнії. Розглянуто місце Валео-Дорм Дуо-препарату на основі фітофлавоноїду кризину з анксіолітичною дією та мелатоніну в лікуванні пацієнтів із тривогою та інсомнією. Peculiarities of treating patients with insomnia and anxiety comorbidity: in search for a safe alternative to benzodiazepines Abstract. The article presents the definition and modern diagnostic criteria for insomnia, highlights the aspects of common pathogenetic mechanisms of insomnia and anxiety development. Approaches to the treatment of insomnia are described in detail. The place of Valeo-Dorm Duo, a preparation of phyto-flavonoid chrysin with anxiolytic effect and melatonin, in the treatment of patients with anxiety and insomnia is considered.

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“…sedation, amnesia, myorelaxation) that have been attributed to other GABAA modulators (benzodiazepines, ethanol, etc. ); these effects have been evaluated in behavioral models using rodents (Wolfman et al, 1994;Salgueiro et al, 1997;Zanoli et al, 2000;Rodríguez-Landa et al, 2019). Although it has been suggested that presence of the hydroxyl groups in the chrysin structure is the responsible for this pharmacological action, this effect has not been compared with the effects produced by the flavone backbone in preclinical models of anxiety-like behavior.…”

Section: Chrysin (Either Isolated From Passiflora Coerulea Passiflormentioning

confidence: 99%

“…Chrysin is used as a nutraceutical as a "testosterone boosting agent" (a claim that is probably very exaggerated; Gambelunghe et al, 2003), but there is some preclinical evidence that this molecule ameliorates indices of hepatic and renal functioning in diabetic animals (Ramanathan & Thekkumalai, 2014;Yamamoto, 2014). There is also preclinical evidence that this flavonoid exerts anxiolytic-like effects (Wolfman et al, 1994;Salgueiro et al, 1997;Zanoli et al, 2000;Rodríguez-Landa et al, 2019).…”

Section: Introductionmentioning

confidence: 99%

Chrysin, but not flavone backbone, decreases anxiety-like behavior in animal screens

Germán-Ponciano

Costa

Feitosa

et al. 2019

Preprint

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Chrysin (5,7-dihydroxyflavone), a flavonoid present in diverse plants, has a backbone structure shared with the basic structure of the flavones, with additional hydroxyl groups that confers its antioxidant properties and effects at the GABAA receptor complex. However, whether these effects are due to the hydroxyl groups is unknown. Here we report the effects of chrysin or the flavone backbone (1 mg/kg) on rat behavior in the elevated plus-maze (EPM) and a locomotor activity test (LAT), as well as in the zebrafish light/dark test (LDT). Chrysin, but not flavone, increased entries and time in the open arms of the EPM, as well as time on white in the zebrafish LDT. These effects were comparable to diazepam, and were devoid of motor effects in both tests, as well as in the rat LAT. On the other hand, flavone increased risk assessment in the zebrafish LDT and rat EPM, suggesting effects threat information gathering; important species differences suggest new avenues of research. It is suggested that the specific effects of chrysin in relation to flavone are due to its free radical scavenging abilities and/or its action at the GABA A /benzodiazepine receptor complex. Preprint: https://doi.org/10.1101/575514; Data and scripts: https://github.com/lanec-unifesspa/chrysin 1/16 29 behavior. The basic flavone moiety has an hydrogen bond donor site, lipophilic pockets, 30 and an electron rich site (Marder and Paladini, 2002); this last is thought to be 31 important for the binding of both flavonoids and 1,4-benzodiazepines to the central 32 benzodiazepine (BZD) site at GABA A receptors (Marder and Paladini, 2002). Since the 33 chrysin hydroxyl groups are located in one region of the flavone basic ring that is 34 important for the steric interactions associated with binding, this flavonoid is expected 35 to bind BZD sites with a higher affinity than flavone. As a result, while chrysin is 36 2/16 65 measures in the study.

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Chrysin (5,7-dihydroxyflavone) exerts anxiolytic-like effects through GABAA receptors in a surgical menopause model in rats

Cited by 28 publications

References 46 publications

Neuropharmacology of Secondary Metabolites from Plants with Anxiolytic and Antidepressant Properties

Neuropharmacology of Secondary Metabolites from Plants with Anxiolytic and Antidepressant Properties

Особливості Лікувальної Тактики При Коморбідності Інсомнії Та Тривоги: В Пошуках Безпечної Альтернативи Бензодіазепінів

Chrysin, but not flavone backbone, decreases anxiety-like behavior in animal screens

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