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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: 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).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.

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

Dose-response curves and IC50 values of FO (A) and FST (B) in the 5-HT2C receptor binding assay. Each data point is expressed as mean ± SD (n=3).
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f3-bt-23-479: Dose-response curves and IC50 values of FO (A) and FST (B) in the 5-HT2C receptor binding assay. Each data point is expressed as mean ± SD (n=3).

Mentions: Table 2 and 3 presents the % displacement of [3H] flumazenil (GABAA receptor agonist) and [3H] mesulergine (5-HT2C specific agonist) binding with unlabeled FMO obtained with seven concentrations. FST showed moderately dose-dependent activity to GABAA receptor, which displaced over 50% of [3H] flumazenil binding at a concentration of 20 mg/ml. In addition, FO had a weak bonding activity for GABAA receptor at a concentration of 20 mg/ml. The IC50 values of FO and FST were 2.25 ± 1.1 and 1.05 ± 1.15 mg/ml, respectively as seen in Fig. 2. In the 5-HT2C receptor binding assay, FO displayed over 60% of [3H] mesulergine binding at a concentration of 20 mg/ml. FST showed moderately dose-dependent activity in 5-HT2C binding assay similar to its affinity of GABAA receptor, which displaced over 50% of [3H] mesulergine binding at a concentration of 20 mg/ml. The IC50 values for FO and FST were determined to be 1.34 ± 1.11 and 1.56 ± 0.26, respectively as seen in Fig. 3.


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)

Dose-response curves and IC50 values of FO (A) and FST (B) in the 5-HT2C receptor binding assay. Each data point is expressed as mean ± SD (n=3).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

f3-bt-23-479: Dose-response curves and IC50 values of FO (A) and FST (B) in the 5-HT2C receptor binding assay. Each data point is expressed as mean ± SD (n=3).
Mentions: Table 2 and 3 presents the % displacement of [3H] flumazenil (GABAA receptor agonist) and [3H] mesulergine (5-HT2C specific agonist) binding with unlabeled FMO obtained with seven concentrations. FST showed moderately dose-dependent activity to GABAA receptor, which displaced over 50% of [3H] flumazenil binding at a concentration of 20 mg/ml. In addition, FO had a weak bonding activity for GABAA receptor at a concentration of 20 mg/ml. The IC50 values of FO and FST were 2.25 ± 1.1 and 1.05 ± 1.15 mg/ml, respectively as seen in Fig. 2. In the 5-HT2C receptor binding assay, FO displayed over 60% of [3H] mesulergine binding at a concentration of 20 mg/ml. FST showed moderately dose-dependent activity in 5-HT2C binding assay similar to its affinity of GABAA receptor, which displaced over 50% of [3H] mesulergine binding at a concentration of 20 mg/ml. The IC50 values for FO and FST were determined to be 1.34 ± 1.11 and 1.56 ± 0.26, respectively as seen in Fig. 3.

Bottom Line: 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).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.

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