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Sedative-Hypnotic and Receptor Binding Studies of Fermented Marine Organisms.

Joung HY, Kang YM, Lee BJ, Chung SY, Kim KS, Shim I - Biomol Ther (Seoul) (2015)

Bottom Line: In GABAA and 5-HT2C receptor binding assays, FST displayed an effective concentration-dependent binding affinity to GABAA receptor, similar to the binding affinity to 5-HT2C receptor.FO exhibited higher affinity to 5-HT2C receptor, compared with the GABAA receptor.The data demonstrate that FST and FO possess sedative-hypnotic activity possibly by modulating GABAA and 5-HT2C receptors.

View Article: PubMed Central - PubMed

Affiliation: Department of Physiology, College of Medicine, The Catholic University of Korea, Seoul 137-701 ; Department of Science in Korean Medicine, Graduate School, College of Korean Medicine, Kyung Hee University, Seoul 130-701.

ABSTRACT
This study was performed to investigate the sedative-hypnotic activity of γ-aminobutyric acid (GABA)-enriched fermented marine organisms (FMO), including sea tangle (FST) and oyster (FO) by Lactobacillus brevis BJ20 (L. brevis BJ20). FST and FO were tested for their binding activity of the GABAA-benzodiazepine and 5-HT2C receptors, which are well-known molecular targets for sleep aids. We also measured the sleep latency and sleep duration during pentobarbital-induced sleep in mice after oral administration of FST and FO. In GABAA and 5-HT2C receptor binding assays, FST displayed an effective concentration-dependent binding affinity to GABAA receptor, similar to the binding affinity to 5-HT2C receptor. FO exhibited higher affinity to 5-HT2C receptor, compared with the GABAA receptor. The oral administration of FST and FO produced a dose-dependent decrease in sleep latency and increase in sleep duration in pentobarbital-induced hypnosis. The data demonstrate that FST and FO possess sedative-hypnotic activity possibly by modulating GABAA and 5-HT2C receptors. We propose that FST and FO might be effective agents for treatment of insomnia.

No MeSH data available.


Related in: MedlinePlus

Effects of FMO on sleep latency (A) and sleep duration (B) in mice induced by hypnotic dose (40 mg/kg, i.p.) of pentobarbital. Mice received pentobarbital 30 min after administration of FMO. CON: control (saline 10 ml/kg, p.o.) Each column represents the mean ± SEM. *p<0.05, **p<0.01, ***p<0.001, significant as compared to the control group.
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f4-bt-23-479: Effects of FMO on sleep latency (A) and sleep duration (B) in mice induced by hypnotic dose (40 mg/kg, i.p.) of pentobarbital. Mice received pentobarbital 30 min after administration of FMO. CON: control (saline 10 ml/kg, p.o.) Each column represents the mean ± SEM. *p<0.05, **p<0.01, ***p<0.001, significant as compared to the control group.

Mentions: The sedative-hypnotic effects of FMO were tested by measuring the sleep onset and sleep duration time pentobarbital-induced sleep after oral administration of FMO in mice. ANOVA analysis of pentobarbital test revealed that sleep onset and sleep duration time were significantly different across all groups (F5,59=15.394, p<0.001; F5,59=5.459, p<0.01, respectively). The oral administration of FST and FO produced a dose-dependent decrease in sleep latency and increase in sleep duration in mice with hypnotic dose (40 mg/kg) of pentobarbital as seen in Fig. 4. The most pronounced hypnotic activity of FO was observed at 400 mg/kg in the sleep onset time (p<0.05) (Fig. 4A) and sleep duration time (p<0.01) (Fig. 4B), compared to the control group. FST significantly decreased sleep onset time (p<0.05) (Fig. 4A) and increased sleep duration time (p<0.05) (Fig. 4B) at a dose of 400 mg/ml compared with the control mice. However, FST and FO at a low dose (200 mg/kg, p.o) had no significantl hypnotic effects on the sleep onset time. As a positive control, DZP (2 mg/kg, p.o) significantly potentiated the pentobarbital-induced sleep behaviors, compared with control group (p<0.001 for sleep onset time, p<0.05 for sleep duration time).


Sedative-Hypnotic and Receptor Binding Studies of Fermented Marine Organisms.

Joung HY, Kang YM, Lee BJ, Chung SY, Kim KS, Shim I - Biomol Ther (Seoul) (2015)

Effects of FMO on sleep latency (A) and sleep duration (B) in mice induced by hypnotic dose (40 mg/kg, i.p.) of pentobarbital. Mice received pentobarbital 30 min after administration of FMO. CON: control (saline 10 ml/kg, p.o.) Each column represents the mean ± SEM. *p<0.05, **p<0.01, ***p<0.001, significant as compared to the control group.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4556209&req=5

f4-bt-23-479: Effects of FMO on sleep latency (A) and sleep duration (B) in mice induced by hypnotic dose (40 mg/kg, i.p.) of pentobarbital. Mice received pentobarbital 30 min after administration of FMO. CON: control (saline 10 ml/kg, p.o.) Each column represents the mean ± SEM. *p<0.05, **p<0.01, ***p<0.001, significant as compared to the control group.
Mentions: The sedative-hypnotic effects of FMO were tested by measuring the sleep onset and sleep duration time pentobarbital-induced sleep after oral administration of FMO in mice. ANOVA analysis of pentobarbital test revealed that sleep onset and sleep duration time were significantly different across all groups (F5,59=15.394, p<0.001; F5,59=5.459, p<0.01, respectively). The oral administration of FST and FO produced a dose-dependent decrease in sleep latency and increase in sleep duration in mice with hypnotic dose (40 mg/kg) of pentobarbital as seen in Fig. 4. The most pronounced hypnotic activity of FO was observed at 400 mg/kg in the sleep onset time (p<0.05) (Fig. 4A) and sleep duration time (p<0.01) (Fig. 4B), compared to the control group. FST significantly decreased sleep onset time (p<0.05) (Fig. 4A) and increased sleep duration time (p<0.05) (Fig. 4B) at a dose of 400 mg/ml compared with the control mice. However, FST and FO at a low dose (200 mg/kg, p.o) had no significantl hypnotic effects on the sleep onset time. As a positive control, DZP (2 mg/kg, p.o) significantly potentiated the pentobarbital-induced sleep behaviors, compared with control group (p<0.001 for sleep onset time, p<0.05 for sleep duration time).

Bottom Line: In GABAA and 5-HT2C receptor binding assays, FST displayed an effective concentration-dependent binding affinity to GABAA receptor, similar to the binding affinity to 5-HT2C receptor.FO exhibited higher affinity to 5-HT2C receptor, compared with the GABAA receptor.The data demonstrate that FST and FO possess sedative-hypnotic activity possibly by modulating GABAA and 5-HT2C receptors.

View Article: PubMed Central - PubMed

Affiliation: Department of Physiology, College of Medicine, The Catholic University of Korea, Seoul 137-701 ; Department of Science in Korean Medicine, Graduate School, College of Korean Medicine, Kyung Hee University, Seoul 130-701.

ABSTRACT
This study was performed to investigate the sedative-hypnotic activity of γ-aminobutyric acid (GABA)-enriched fermented marine organisms (FMO), including sea tangle (FST) and oyster (FO) by Lactobacillus brevis BJ20 (L. brevis BJ20). FST and FO were tested for their binding activity of the GABAA-benzodiazepine and 5-HT2C receptors, which are well-known molecular targets for sleep aids. We also measured the sleep latency and sleep duration during pentobarbital-induced sleep in mice after oral administration of FST and FO. In GABAA and 5-HT2C receptor binding assays, FST displayed an effective concentration-dependent binding affinity to GABAA receptor, similar to the binding affinity to 5-HT2C receptor. FO exhibited higher affinity to 5-HT2C receptor, compared with the GABAA receptor. The oral administration of FST and FO produced a dose-dependent decrease in sleep latency and increase in sleep duration in pentobarbital-induced hypnosis. The data demonstrate that FST and FO possess sedative-hypnotic activity possibly by modulating GABAA and 5-HT2C receptors. We propose that FST and FO might be effective agents for treatment of insomnia.

No MeSH data available.


Related in: MedlinePlus