Advances in pharmacological effects of jujuboside B / 中国中药杂志

Ziziphi Spinosae Semen(ZSS) is an edible TCM derived from the dried ripe seeds of Ziziphus jujube Mill. var. spinosa(Bunge)Hu ex H. F. Chou(Rhamnaceae), which has the effects of nourishing the heart, tonifying the liver, calming the heart, tranquilizing the mind, arresting sweating, and promoting fluid production, and is widely used in the treatment and health care of diseases related to cardiovascular, nervous, and immune systems. Jujuboside B(JuB), one of the main active ingredients of ZSS, possesses various pharmacological effects with application values. This paper reviewed the chemical structure and pharmacological effects of JuB. JuB has sedative, hypnotic, antitumor, anti-platelet, anti-inflammatory, and other biological activities, which shows the potential thera-peutic effects on insomnia, tumors, coronary artery disease, airway inflammation, and liver injury. However, there are some limitations to the results of current studies. More comprehensive studies, including basic research and clinical trials, need to be carried out to provide more reliable evidence.

Safety on Chloral Hydrate Oral Solution for Sedative and Hypnotic in Children ：A Systematic Review / 中国药房

OBJECTIVE：To systematically evaluate the safety of Chloral hydr ate（CH）oral solution for sedative and hypnotic in children，and to provide evidence-based reference for clinical use. METHODS ：Retrieved from 9 electronic databases （PubMed， Cochrane Library ，Embase，CINAHL，International Pharmaceuticals ，CNKI，CBM，Wanfang Database ，VIP），3 clinical trial registry platforms （Clinical Trials ，Cochrane Clinical Trial Database ，WHO Clinical Trial Database ）and 18 adverse drug reaction （ADR）monitoring systems （ADR monitoring websites of WHO ，USA，Switzerland，China and other countries/areas/international organizations），during the date of database establishment to March 2019，the reports of randomized controlled trials ，cohort studies，case-control studies ，case series studies ，case reports ， cross-sectional studies and adverse reactions monitoring network of chloral hydrate versus other interventions （blank 85503205。E-mail：chenzhehx@163.com control，placebo or other sedative hypnotics ）for children ’s sedative and hypnotic safety were collected. After data extraction of included literatures met inclusion criteria ，quality mail：zhanglingli@scu.edu.cn evaluation of included s tudies with Cochrane bias risk evaluation manual （RCT），Newcastle-Ottawa scale evaluation tool （Cohort study and case control study ），Australian JBI quality assessment tool （case series study and case report study ），Meta-analysis was performed by Rev Man 5.3 software，or descriptive analysis was conducted. RESULTS ：A total of 54 studies were included ，among which there were 13 RCTs，9 cohort studies ，17 case series studies ，13 case reports ，and 2 reports from ADR monitoring network. Based on the results of RCT and cohort studies ， the incidence of Chloral hydrate oral solution adverse events was 7.25％. There was no statistical significance in the incidence of digestive system [RR ＝0.87，95％ CI（0.14，5.42），P＝0.88]，nervous system [RR ＝0.13，95％ CI（0.01，2.41），P＝0.17]， cardiovascular system [RR ＝2.12，95％ CI（0.08，56.57），P＝0.65] adverse event between Chloral hydrate oral solution and midazolam. The incidence of respiratory system adverse events induced by Chloral hydrate oral solution was higher than that of midazolam [RR ＝3.07，95％CI（1.94，4.86），P＜0.01]. There was no statistical significance in the incidence of digestive system adverse events between Chloral hydrate oral solution and diazepam [RR ＝0.71，95％CI（0.47，1.10），P＝0.13]. There was no statistical significance in the incidence of digestive system ，nervous system and cardiovascular system adverse events between Chloral hydrate oral solution and barbiturates （P＞0.05）. CONCLUSIONS ：Chloral hydrate oral solution is similar to midazolam ， diazepam and barbiturates in terms of digestive ，nervous and cardiovascular systems adverse events ，but the incidence of respiratory system adverse events is higher than midazolam.

Sedative and Hypnotic Effects and Transcriptome Analysis of Polygala tenuifolia in Aged Insomnia Rats / 中国结合医学杂志

OBJECTIVE@#To study the sedative and hypnotic effects and underlying mechanisms of Polygala tenuifolia (PT) on treating aged insomnia rats.@*METHODS@#Sixty Sprague-Dawley male rats were divided into 6 groups by a random number table, including control group, model group, diazepam group (0.92 mg/kg), as well as PT low-, medium- and high-dose groups (0.0875, 0.175, 0.35 g/kg, respectively), 10 rats in each group. Aged insomnia rat model was established with subcutaneous injection of D-galactose for 42 days and then intraperitoneal injection of para-chlorophenylalanine for 3 days. PT and diazepam were respectively given to aged insomnia rats by intragastric administration for 7 days after model establishment. Then the rats were investigated by body weight, Morris water maze test, pentobarbital test, enzyme-linked immunosorbent assay, and transcriptome sequencing.@*RESULTS@#Compared with the model group, PT increased the body weight, improved memory ability, and prolonged pentobarbital-induced sleep time of aged insomnia rats (P<0.01 or P<0.05). The medium dose of PT also increased the neurotransmitter levels of 5-hydroxytryptamine (5-HT) and gamma-aminobutyric acid (GABA), and decreased the level of Glu in the hippocampus of aged insomnia rats (P<0.05 or P<0.01). Twenty-four differentially expressed genes (DEGs) were overlapped among model group, medium-dose PT group, and diazepam group in transcriptome analysis. Fuom and Pcp2 were down-regulated by the treatment of medium-dose PT (P<0.01 or P<0.05). The metabolic pathways of PT were relatively less than diazepam (91 vs. 104).@*CONCLUSIONS@#The sedative and hypnotic effects of PT in aged insomnia rats might be related to neuro, metabolism pathways, especially through GABAergic signaling pathway. It provided more effective herb choice for the treatment of senile insomnia.

Evaluation of the sedative and hypnotic effects of H057 / 中国药理学通报

Aim To investigate the sedative and hyp-notic effects of a novel compound H057 . Methods The sedative activity of H057 was investigated by re-cording the spontaneous locomotor activity in mice. The hypnotic property was evaluated by the latency and duration of loss of righting reflex( LORR) in mice and effect of H057 on the sleep onset in subthreshold dos-age of sodium pentobarbital treated mice. The extracel-lular levels of GABA and monoamine neurotransmitters in in cerebral cortex were measured by microdialysis in vivo. Results The spontaneous locomotor activity was decreased by 25% and 66% in H057 ( 5 , 25 mg · kg-1 ,i. p. ) treated mice, respectively. H057 ( 3, 5 mg·kg-1 ,i. p. ) increased the sleep onset to 62. 5%and 87. 5% in subthreshold dosage of sodium pentobar-bital(25 mg·kg-1,i. p. ) treated mice. H057(≥60 mg· kg-1 , i. p. ) could completely induce LORR in mice. The latency of LORR at dose of 60 mg · kg-1 was (24 ± 11) min and the duration of LORR was (96 ± 15 ) min. In vivo mircodialysis revealed that H057 (25 mg·kg-1 , i. p. ) could significantly increase the GABA level by 26% and decrease the 5-HT and NE levels by 50% and 38% in cerebral cortex in mice. Conclusion H057 has potent sedative and hypnotic effects, which may be closely related to the increased content of GABA and the decreased contents of 5-HT and NE in the extracellular fluid in cerebral cortex.

Research progress on Polygalae Radix / 中草药

Polygalae Radix used as Chinese materia medica has a long history. The main chemical constituents include triterpenoid saponins, xanthones, oligosaccharide esters, and so on. The study shows that Polygalae Radix has a wide range of pharmacological activities, such as sedative hypnotic, anticonvulsant, antiaging, antidementia, brain protection, cough expectorant, antidepressant, antibacterial, and anticancer. In this paper, through referring to the domestic and foreign relevant literatures on Polygalae Radix systematically, we summarize the chemical composition, pharmacological activity, and structure activity relationship of Polygalae Radix, which could provide the reference for the further investigation and development of this plant.

Effect of a novel sedative and hypnotic compound B2 on monoamine neurotransmitters levels in mouse brain / 国际药学研究杂志

Objective To study the effect of sedative and hypnotic compound B2 on levels of monoamine neurotransmitters, including norepinephrine (NE), dopamine (DA), and 5-hydroxytryptamine (5-HT) in mouse brain. Methods Mice were randomly divided into vehicle group and B2 group (5 mg/kg, ip), then the contents of NE, DA and 5-HT were detected by high performance liquid chromatography-electrochemical detection (HPLC-ECD). The effects of compound B2 on monoamine oxidase (MAO) activities in mouse hypothalamus, striatum and cortex were detected by colorimetric method. Results B2 (5 mg/kg, ip) could significantly reduce NE contoent in the hypothalamus from (1. 08 ± 0. 09) μgg to (0. 88 ± 0. 07) μgg (P < 0. 01) and reduce DA content in the striatum from (12. 85 ±2. 21) μgg to (8. 44 ± 2. 25) μgg (P < 0. 01). 5-HT content in hypothalamus were significantly decreased from (1. 12 ±0. 12) μgg to (0. 56 ±0. 18) μgg (P < 0. 01). There was no significant difference between two groups in MAO activity. Conclusion The sedative and hypnotic effects of B2 might be mediated by the decrease of monoamine levels in different mouse brain regions.

Nature and flavor pharmacology of Fuling and its components for learning and memory improvement as well as sedative and hypnotic effects / 中草药

Objective: To evaluate the activities of Fuling (the dried sclerotium of Poria cocos) and its components, then its nature and flavor were attributed by traditional Chinese medicine (TCM) theory. Methods: Scopolamine was used to cause learning and memory impairment in mice, and Morris water maze test was used to observe the effects of Fuling and its components on learning and memory of mice, and shaking cage method and pentobarbital sodium were used to evaluate the sedative and hypnotic effects of Fuling and its components. Results: Water decoction of Fuling (crude drug 8.56 g/kg), ethyl acetate, petroleum ether, crude polysaccharides, and refined polysaccharides components could significantly shorten the latency of scopolamine-induced memory impairment in mice to reach the platform; Acetylcholinesterase activity in mice brain was decreased, the effects of the components washed with alcohol and water on latency were less obvious and the individual components of the cerebral index showed an increase in different proportions; Crude drug (42.8 g/kg) water decoction of Fuling could significantly prolong the sleeping time, but had no effect on sleep latency; Crude polysaccharides could significantly shorten the sleep latency while the refined polysaccharides could significantly increase sleeping time; Followed by ethyl acetate components, the petroleum ether components showed a weak antagonistic effect. Conclusion: The learning and memory improvement as well as the sedative and hypnotic effects are associated with Fuling's sweet taste which can tonify spleen to calm nerves; The ethyl acetate, petroleum ether, and polysaccharides components are the basic materials of sweet taste.

Study on Sedative and Hypnotic Effects of Different Eluents of Shuangxiatang / 世界科学技术-中医药现代化

This article was aimed to study the sedative and hypnotic effects of different eluents of Shuangxiatang (SXT). The effects of SXT water decoction, water eluent, 20%, 70% and 95% alcohol eluent on spontaneous ac-tivity and the sleeping induced by subthreshold dose of pentobarbital sodium were measured. The results showed that the SXT decoction, 20% and 95% alcohol eluent can significantly decrease the number of rearing in mice with the percentage of 78.5%, 78.3% and 62.5%, respectively. SXT water eluent and 70% alcohol eluent can significantly decrease the spontaneous activity of mice (P < 0.01), the number of rearing (P < 0.01) and grooming time (P < 0.05). SXT water decoction can significantly shorten sleep latency (P < 0.05), prolong sleep time (P <0.05), and increase rates of sleeping in mice. SXT water eluent can significantly shorten sleep latency in mice (P< 0.05), increase rates of sleeping in mice. SXT water decoction and water eluent have the sedative and hypnotic effects. And the effects are more than alcohol eluents.