Potentiating effect of glabridin from Glycyrrhiza glabra on GABA A receptors

Hoffmann, Katrin M.; Cabrera-Beltran, Lola Jimena; Ziemba, Paul M.; Hatt, Hanns; Gisselmann, Günter

doi:10.1016/j.bbrep.2016.04.007

Cited by 17 publications

(18 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It has been demonstrated the amount of GABA in the brain tissue is positively associated with the changes in sleep-wake depth ( 64 ). Furthermore, GABA serves inhibitory roles by binding to its receptor ( 65 ) and GABA A R α1 has a sedative effect ( 66 ). It has been reported that the expression of glutamate in cerebral cortex, hypothalamus and hippocampus of in PCPA-induced insomnia rats increased, while the content of 5-HT and GABA decreased compared with the control group ( 23 ).…”

Section: Discussionmentioning

confidence: 99%

Establishment of a rat model with ageing insomnia induced by D‑galactosef and para‑chlorophenylalanine

et al. 2020

View full text Add to dashboard Cite

The current study aimed to establish a rat model of ageing insomnia induced by D-galactose and/or para-chlorophenylalanine. Following establishment of the model, body weights were measured, and Morris water maze and pentobarbital-induced sleep tests were performed. The serum levels of inflammatory mediators and the neural levels of neurotransmitters were detected. The results demonstrated that the body weights of PCPA+D-gal-induced ageing insomnia rats decreased significantly. Ageing insomnia rats exhibited longer latencies to the platform in the Morris water maze tests and fewer target crossings. The sleep latency of the model rats was longer and sleep time was shorter by contrast. The relative expression of hippocampal IL-6, TNF-α, NF-κB and mGluR2 mRNA of the PCPA+D-gal-induced ageing insomnia group was higher, while the relative expression of 5-HT 1A R and GABA A R a1 mRNA were lower. The serum levels of IL-1β, IL-6, TNF-α and brain level of glutamate increased in the PCPA+D-gal-induced ageing insomnia group, while the levels of 5-HT and GABA decreased. In conclusion, memory function, sleep time, expression of inflammatory factors and neurotransmitters are altered in ageing insomnia rats induced by D-galactose and para-chlorophenylalanine, indicating the successful establishment of a murine model of ageing insomnia.

show abstract

Section: Discussionmentioning

confidence: 99%

Establishment of a rat model with ageing insomnia induced by D‑galactosef and para‑chlorophenylalanine

et al. 2020

View full text Add to dashboard Cite

show abstract

“…This finding may help us to understand the antagonistic effect of this tincture ( Herbrechter et al, 2015 ). Another flavonoid from licorice, named glabridin, was identified as a partial antagonist of the 5-HT 3A -receptor and a potentiator of GABA A -receptors ( Herbrechter et al, 2015 ; Hoffmann et al, 2016 ). The antagonistic effect of Mentha canadensis (herba) may be explained through the action of terpenes, which are known to inhibit the 5-HT 3A receptor.…”

Section: Discussionmentioning

confidence: 99%

Kampo Medicine: Evaluation of the Pharmacological Activity of 121 Herbal Drugs on GABAA and 5-HT3A Receptors

et al. 2016

Self Cite

View full text Add to dashboard Cite

Kampo medicine is a form of Japanese phytotherapy originating from traditional Chinese medicine (TCM). During the last several decades, much attention has been paid to the pharmacological effects of these medical plants and their constituents. However, in many cases, a systematic screening of Kampo remedies to determine pharmacologically relevant targets is still lacking. In this study, a broad screening of Kampo remedies was performed to look for pharmacologically relevant 5-HT3A and GABAA receptor ligands. Several of the Kampo remedies are currently used for symptoms such as nausea, emesis, gastrointestinal motility disorders, anxiety, restlessness, or insomnia. Therefore, the pharmacological effects of 121 herbal drugs from Kampo medicine were analyzed as ethanol tinctures on heterologously expressed 5-HT3A and GABAA receptors, due to the involvement of these receptors in such pathophysiological processes. The tinctures of Lindera aggregata (radix) and Leonurus japonicus (herba) were the most effective inhibitory compounds on the 5-HT3A receptor. Further investigation of known ingredients in these compounds led to the identification of leonurine from Leonurus as a new natural 5-HT3A receptor antagonist. Several potentiating herbs (e.g., Magnolia officinalis (cortex), Syzygium aromaticum (flos), and Panax ginseng (radix)) were also identified for the GABAA receptor, which are all traditionally used for their sedative or anxiolytic effects. A variety of tinctures with antagonistic effects Salvia miltiorrhiza (radix) were also detected. Therefore, this study reveals new insights into the pharmacological action of a broad spectrum of herbal drugs from Kampo, allowing for a better understanding of their physiological effects and clinical applications.

show abstract

“…Gamma‐aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the central nervous system, being GABA A receptors a target for anaesthetics and neuroleptic, anxiolytic, and anticonvulsant compounds (Simmler et al, ). G. glabra acts as a modulator of GABA A receptors (Hoffmann, Beltrán, Ziemba, Hatt, & Gisselmann, ), being able to induce sedative and anxiolytic effects. Glabridin was evaluated by examining GABA responses in acutely isolated dorsal raphe neurons of a rat (Jin et al, ).…”

Section: Pharmacological Propertiesmentioning

confidence: 99%

Liquorice (Glycyrrhiza glabra): A phytochemical and pharmacological review

Pastorino

Cornara

Soares

et al. 2018

Phytotherapy Research

518

332

View full text Add to dashboard Cite

In the last years, consumers are paying much more attention to natural medicines and principles, mainly due to the general sense that natural compounds are safe. On the other hand, there is a growing demand by industry for plants used in traditional medicine that could be incorporated in foods, nutraceuticals, cosmetics, or even pharmaceuticals. Glycyrrhiza glabra Linn. belongs to the Fabaceae family and has been recognized since ancient times for its ethnopharmacological values. This plant contains different phytocompounds, such as glycyrrhizin, 18β-glycyrrhetinic acid, glabrin A and B, and isoflavones, that have demonstrated various pharmacological activities. Pharmacological experiments have demonstrated that different extracts and pure compounds from this species exhibit a broad range of biological properties, including antibacterial, anti-inflammatory, antiviral, antioxidant, and antidiabetic activities. A few toxicological studies have reported some concerns. This review addresses all those issues and focuses on the pharmacological activities reported for G. glabra. Therefore, an updated, critical, and extensive overview on the current knowledge of G. glabra composition and biological activities is provided here in order to explore its therapeutic potential and future challenges to be utilized for the formulation of new products that will contribute to human well-being.

show abstract

Potentiating effect of glabridin from Glycyrrhiza glabra on GABA A receptors

Cited by 17 publications

References 19 publications

Establishment of a rat model with ageing insomnia induced by D‑galactosef and para‑chlorophenylalanine

Establishment of a rat model with ageing insomnia induced by D‑galactosef and para‑chlorophenylalanine

Kampo Medicine: Evaluation of the Pharmacological Activity of 121 Herbal Drugs on GABAA and 5-HT3A Receptors

Liquorice (Glycyrrhiza glabra): A phytochemical and pharmacological review

Contact Info

Product

Resources

About