Hypnotic effects and binding studies for GABAA and 5-HT2C receptors of traditional medicinal plants used in Asia for insomnia
- Hypnotic effects and binding studies for GABAA and 5-HT2C receptors of traditional medicinal plants used in Asia for insomnia
- 조승목; Makoto Shimizu; 이창준; 한대석; 정철균; 조진호; 김영명
- Oriental medicinal plant; Hypnotic activity; GABAA receptor; 5-HT2C receptor; Licorice (Glycyrrhiza uralensis Fischer); Silk tree (Albizzia julibrissin Durazzini)
- Issue Date
- Journal of ethnopharmacology
- VOL 132, NO 1, 225-232
- Aim of the study: Many medicinal plants have been used for treatment of insomnia in Asia. However,
scientific evidence and precise mechanism for their sedative-hypnotic activity have not been fully investigated.
Thus, we investigated the binding activity of the oriental plant extracts (mainly from Korea and
Japan) to the well-known molecular targets for sleep regulation, GABAA and 5-HT2C receptors. Following
the binding assay, sedative-hypnotic effects of the extracts with high affinity were examined in an animal
model of sleep.
Materials and methods: Aqueous and ethanol extracts of 15 medicinal plants were tested for binding
at the benzodiazepine site of GABAA receptor and 5-HT site of 5-HT2C receptor. The sedative-hypnotic
effects of selected extracts were evaluated by measuring the sleep latency and sleep duration during
pentobarbital-induced sleep in mice after oral administration of extracts.
Results: In the GABAA assay, the ethanol extracts of licorice and danshen displayed concentrationdependent,
high affinity binding, whereas in the 5-HT2C assay, the ethanol extracts of ginseng and silk
tree showed high affinity. Among these extracts we tested previously uncharacterized licorice and silk
tree for hypnotic effects. We found the ethanol extracts of licorice and silk tree significantly decreased
sleep latency and increased sleep duration in pentobarbital-induced sleep.
Conclusions: We demonstrate for the first time that licorice and silk tree have the sedative-hypnotic
activity possibly by modulating GABAA and 5-HT2C receptors. We propose that licorice and silk tree
might be effective candidates for treatment of insomnia.
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