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PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR · 2013 · IF 2.608

Anticonvulsant and sedative effects of paederosidic acid isolated from Paederia scandens (Lour.) Merrill. in mice and rats

Tao Yang,Bin Kong,Jian-Wen Gu,Yong-Qin Kuang,Lin Cheng,Wen-Tao Yang,Jing-Min Cheng,Yuan Ma,Xiao-Kun Yang

This study was designed to evaluate the anticonvulsant and sedative effects of paederosidic acid isolated from Paederia scandens (Lour.) Merrill. in mice and rats. In the present study, anticonvulsant activities of paederosidic acid were evaluated by maximal electroshock and pentylenetetrazole-induced seizures in male mice. Then, pentobarbital sodium-induced sleeping time and locomotor activity tests in mice were used to evaluate the sedative effects of paederosidic acid. Finally, the mechanism of paederosidic acid was explored by evaluating the contents of Glu and GABA in the brain, and Western blot was used to measure GAD65 expression in the mouse brain. Paederosidic acid (5, 10, 20, and 40   mg/kg, ip) had significant anticonvulsant and sedative effects. Moreover, paederosidic acid increased brain gamma-aminobutyric acid and decreased glutamic acid in the brain, and it up-regulated expressions of GAD 65. In conclusion, our results suggest that paederosidic acid may be a promising future therapeutic agent for treatment of epilepsy .

CAS / MDL: 630-93-3 54-95-5
研究领域: 药理学 · 神经科学
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Food Chemistry-X · 2024 · IF 6.5

A modified QuEChERS-based UPLC-MS/MS method for rapid determination of multiple antibiotics and sedative residues in freshwater fish

Yan Yang,Xin Li,Jian Lin,Rong Bao

Antibiotics and sedatives are used in freshwater fish culture and transportation, and residue in freshwater fish pose potential risks to human health. Therefore, a throughput method was developed to detect antibiotic and sedative residues in fish, simultaneously quantifying 68 antibiotics and 9 sedatives in freshwater fish using a modified QuEChERS extraction method and UPLC-MS/MS. Matrix-matched calibrations demonstrated good correlation coefficients (R 2  > 0.995), with a recovery range of 66.2–118.5%. The intra-day and inter-day relative standard deviation (RSD) were below 9.7% and 12.8%, respectively. The limits of detection (LOD) and quantification (LOQ) were 0.08–1.46 μg/kg and 0.25–4.86 μg/kg, respectively. 68.8% of analytes had weak matrix effects, and 13.0% had moderate matrix effects. In addition, diazepam and many types of antibiotics were detected in30 freshwater fish. The validation parameters were in agreement with the acceptable criteria of the Codex guidelines. The method was effective in analyzing antibiotic and sedative residues in freshwater fish.

研究领域: 食品安全 · 分析化学 · 环境科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Arabian Journal of Chemistry · 2022 · IF 6.212

Simultaneous determination of four sedative-hypnotics in human urine based on dendritic structured magnetic nanomaterials

Jing An,Xin Wang,Haojing Song,Tangjuan Zhao,Hongyan Ren,Weijun Kang,Zhanjun Dong,Lingmei Niu,Hongmei Shi

A magnetic solid-phase extraction technique based on magnetic dendritic structured nanoparticles (Fe 3 O 4 @SiO 2 -NH 2 -G5) as adsorbent coupled with ultra-high performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) has been developed to detect diazepam, midazolam, zolpidem, and zaleplon in human urine. With Fe 3 O 4 @SiO 2 -NH 2 as the central core, dendrimer (G5) grafted alternately with cyanuric chloride and imidazole were bonded to the surface of the core to synthesize Fe 3 O 4 @SiO 2 -NH 2 -G5. The morphology and structure of the magnetic materials were characterized by transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), vibrating sample magnetometer (VSM), and dynamic light scattering (DLS). The key parameters affecting the extraction efficiency were optimized. A satisfactory performance was obtained under the optimum extraction conditions. The proposed method was validated, and the limits of detection of zaleplon, diazepam, zolpidem, and midazolam were 0.05, 0.05, 0.02, and 0.02 ng mL −1 , respectively. The linear correlation coefficients r of the four analytes were > 0.996, the intra-day precision was between 2.4 % and 9.4 % with the recoveries between 88.3 % and 104.8 %, and the inter-day precision ranged from 3.9 % to 15.2 % with the recovery in the range of 94.1 %−108.3 %. The magnetic dendritic structure nanomaterial Fe 3 O 4 @SiO 2 -NH 2 -G5 was successfully used to extract sedative-hypnotic drugs from human urine samples. The Fe 3 O 4 @SiO 2 -NH 2 -G5-based magnetic solid-phase extraction method eliminates centrifugation and filtration steps as in conventional extraction. Only one step of vortex dispersion extraction could achieve the separation and purification of the target compounds. The proposed method was simple, rapid, environment-friendly, and suitable for the analysis of sedative-hypnotic drugs in human urine.

CAS / MDL: 288-32-4
研究领域: 分析化学 · 药物分析 · 纳米技术
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FOOD CHEMISTRY · 2022 · IF 9.231

Simultaneous determination of the residues of anesthetics and sedatives in fish using LC-QLIT-MS/MS combined with DSPE

Qin Huang,Hua Zhou,Xianglun Wu,Chenli Song,Jiangang Zheng,Meikang Lei,Pengqian Mu,Pinggu Wu

Liquid chromatography coupled with quadrupole linear ion trap tandem mass spectrometry (LC-QLIT-MS/MS) technology operated in electrospray ionization (ESI) was developed for tracing anesthetic (AETs) and sedatives (SDTs) in fish. Sampling procedure was achieved by using acetonitrile extraction followed by dispersive solid phase extraction (DSPE) clean-up. Under the optimized laboratory conditions, reliable qualitative confirmation was obtained through the multiple reaction monitoring-information dependent acquisition-enhanced product ion (MRM-IDA- EPI ) mode. Results indicated a favorable linear in the concentration range of 1–100 μg∙kg −1 (0.1–10 μg∙kg −1 for MS-222), with regression coefficient not less than 0.9997. The detection limit ranges from 0.03 to 0.4 μg∙kg −1 (S/N = 3). The validated method was applied to determine AETs and SDTs in fish with satidfied recoveries of 86.3 %–111.7 % and the relative standard deviations (RSD) of 1.9 %–8.9 % (n = 6). Practical samples analysis indicated that the proposed method is simple, rapid, sensitive and accurate for identification of AETs and SDTs.

CAS / MDL: 64-18-6 34819-78-8
研究领域: 分析化学 · 食品安全
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF FOOD SCIENCE · 2025 ·Vol. 90 ·期 2 ·e70042 · IF 3.4

Effect of Eurotium cristatum fermentation on chemical composition and hypoglycemic and sedative activities of Anji Baicha (Camellia sinensis)

Yue Qiu,Xiaolin Liu,Zhiye Huang,Fei Lyu,Xinyu Hu,Shenghua Han,Hao Ren,Anqiang Zhang

Anji Baicha ( Camellia sinensis ), one of the top 10 teas in China, possesses old leaves rich in bioactive ingredients yet is frequently discarded due to inferior taste. This study evaluated the effects of fermentation with Eurotium cristatum , a probiotic known to enhance bioactivity, on the primary nutrients and on the hypoglycemic and sedative properties of old leaves of Anji Baicha. Results indicated a considerable reduction in free amino acids and tea polyphenols post-fermentation. Conversely, the concentrations of flavonoids and theabrownins increased significantly, showing a positive correlation with the in vitro hypoglycemic effect. The contents of L-theanine and γ-aminobutyric acid (γ-GABA), known for their sedative effects, increased after fermentation, while caffeine and glutamate, renowned for their neural stimulation effect, decreased. Molecular docking revealed that L-theanine and γ-GABA may act as a sedative and sleep aid by competing for receptors with caffeine and glutamate, specifically NMDAR2A. This study not only introduces a novel approach for utilizing old leaves of Anji Baicha but also establishes a foundation for further investigating the hypoglycemic, sedative, and sleep-aiding effects of tea fermented with Eurotium cristatum . Practical Application This research offers a sustainable solution for repurposing the underutilized old leaves of Anji Baicha, enhancing their market value and contributing to the circular economy within the tea industry. The fermented tea could be integrated into health-conscious food and beverage products, targeting consumers seeking natural hypoglycemic and sleep-aiding alternatives. Additionally, the findings open avenues for the development of functional teas that cater to specific health needs, such as diabetes management and sleep improvement.

研究领域: 食品科学 · 生物化学 · 植物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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RAPID COMMUNICATIONS IN MASS SPECTROMETRY · 2020 ·Vol. 34 ·期 10 ·e8742 · IF 2.2

Facile preparation of magnetic covalent organic framework–metal organic framework composite materials as effective adsorbents for the extraction and determination of sedatives by high-performance liquid chromatography/tandem mass spectrometry in meat samples

Jichao Liu,Guoliang Li,Di Wu,Yanxin Yu,Jian Chen,Yongning Wu

Rationale Sedatives, which are prone to cause residues in animals, have been abused in modern animal husbandry. Long-term consumption of contaminated meat products would be unfavorable to the human nervous system. Taking into account public health and food safety, it was essential to develop an effective method for the enrichment and detection of sedatives in meat. Methods Fe 3 O 4 @TbBd@ZIF-8 composites were synthesized by using Fe 3 O 4 nanoparticles as a magnetic core and 1,3,5-triformylbenzene (Tb) and benzidine (Bd) as two building blocks to form Fe 3 O 4 @TbBd. Furthermore, the zeolitic imidazolate framework-8 (ZIF-8) was modified on the surface of the Fe 3 O 4 @TbBd. In addition, Fe 3 O 4 @TbBd@ZIF-8 was used as a magnetic solid-phase extraction (MSPE) adsorbent of typical animal sedatives in pork samples. Mass spectrometry analysis was conducted by electrospray ionization triple-quadrupole mass spectrometry in positive-ion multiple reaction monitoring mode. Results By combining the optimized MSPE approach with high-performance liquid chromatography/tandem mass spectrometry (HPLC/MS/MS), an accurate and sensitive method for the determination of sedatives was developed. The method exhibited good linearity in the range of 0.03–70 μg/kg with the correlation coefficient (R 2 ) ranging from 0.9982 to 0.9999, high sensitivity with limits of detection (LODs) ranging from 0.04 to 0.2 μg/kg, and high precision with relative standard deviation (RSD) less than 5.5%. The adsorption behaviors of Fe 3 O 4 @TbBd@ZIF-8 towards sedatives were more suitably described by a pseudo-second-order kinetic and Freundlich isotherm model. Conclusions The proposed MSPE-HPLC/MS/MS method was successfully applied to the determination of sedatives in real samples and showed excellent applicability. Several sedatives were detected in the selected meat samples. The developed method was shown to be facile, sensitive and accurate for sedative detection and also showed great prospects for determination of sedatives from other complex samples.

研究领域: 分析化学 · 食品安全 · 材料科学
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE · 2018 ·Vol. 98 ·期 13 ·4885-4894 · IF 2.379

Sedative–hypnotic and anxiolytic effects and the mechanism of action of aqueous extracts of peanut stems and leaves in mice

Lei Deng,Ai-Min Shi,Qiang Wang

INTRODUCTION Peanut stems and leaves (PSL) have traditionally been used as both a special food and a herbal medicine in Asia. The sedative–hypnotic and anxiolytic effects of PSL have been recorded in classical traditional Chinese literature, and more recently by many other researchers. In a previous study, four sleep-related ingredients (linalool, 5-hydroxy-4′,7-dimethoxyflavanone, 2′- O -methylisoliquiritigenin and ferulic acid), among which 5-hydroxy-4′,7-dimethoxyflavanone and 2′- O -methylisoliquiritigenin were newly found in Arachis species, were screened by ultrahigh-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC/QTOF-MS). In the current study, quantitative examination of the above four ingredients was conducted. Serious fundamental functional studies were done in mice, including locomotor activity, direct sleep tests, pentobarbital-induced sleeping time tests, subthreshold dose of pentobarbital tests and barbital sodium sleep incubation period tests, to determine the material base for the sedative–hypnotic and anxiolytic effects of aqueous extracts of PSL. Furthermore, neurotransmitter levels in three brain regions (cerebrum, cerebellum and brain stem) were determined using UHPLC coupled with triple-quadrupole mass spectrometry (UHPLC/QQQ-MS) in order to elucidate the exact mechanism of action. RESULTS Aqueous extract of PSL at a dose of 500 mg kg −1 (based on previous experience), along with different concentrations of the above four functional ingredients (189.86 µg kg −1 linalool, 114.75 mg kg −1 5-hydroxy-4′,7-dimethoxyflavanone, 32.4mg kg −1 2′- O -methylisoliquiritigenin and 44.44 mg kg −1 ferulic acid), had a sedative−hypnotic effect by affecting neurotransmitter levels in mice. CONCLUSION The data demonstrate that these four ingredients are the key functional factors for the sedative–hypnotic and anxiolytic effects of PSL aqueous extracts and that these effects occur via changes in neurotransmitter levels and pathways. © 2018 Society of Chemical Industry

研究领域: 药理学 · 植物化学
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ANALYTICAL SCIENCES · 2023 ·Vol. 39 ·期 12 ·1939-1946 · IF 1.6

Synthesis of azo-linked covalent organic polymers for pipette tip solid-phase extraction of sedative residues from animal tissues samples

Xiang Jian Jun,Yuan Li Juan,Liao Qie Gen,Zhang Da Wen,Luo Lin Guang

Azo-linked covalent organic polymers (ACOPs) were synthesized by a simple azo reaction, with 2,2ʹ-bis(trifluoromethyl)benzidine and 1,3,5-trihydroxybenzene as the monomers. The preparation process was mild, green, and environmental-friendly, avoiding the use of high temperature, metal catalysis, and harmful organic reagent. The obtained ACOPs were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, thermogravimetric analysis, powder X-ray diffraction, and Brunauer–Emmett–Teller. With the prepared ACOPs as adsorbent, a method of pipette tip solid-phase extraction–liquid chromatography–tandem mass spectrometry detection (PTSPE–LC–MS/MS) was proposed for the analysis of target sedatives in animal tissues. Furthermore, the parameters for the extraction of five sedatives, including the amount of adsorbent, pH value, ion strength, elution solvent and volume, were investigated. Under the optimized conditions, the linear dynamic range was found from 0.1 to 10.0 μg kg −1 , and the limits of detection were ranged from 0.02 to 0.1 μg kg −1 . The method was assessed by the analysis of target sedatives in animal tissues, and the recoveries for the spiked pork muscle and pork liver samples were 84–102% and 83–101%, respectively. The results show that the developed method of PTSPE–LC–MS/MS with ACOPs as adsorbent is efficient for the analysis of trace sedatives in animal tissues. Graphical Abstract

CAS / MDL: 108-73-6
研究领域: 分析化学 · 食品安全
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Pharmaceuticals · 2024 ·Vol. 17 ·期 9 ·1161 · IF 4.3

Beta-Myrcene as a Sedative–Hypnotic Component from Lavender Essential Oil in DL-4-Chlorophenylalanine-Induced-Insomnia Mice

Luge Chen,Yingwei Liu,Dawei Xu,Na Zhang,Yong Chen,Jin Yang,Lijuan Sun

With the increasing prevalence of insomnia-related diseases, the effective treatment of insomnia has become an important health research topic. Lavender (Lavandula angustifoliaMill.) essential oil (LEO) is a commonly used medicine for the treatment of insomnia and neurological disorders. However, neither the active components nor its sedative–hypnotic mechanism have been fully discovered. This study aimed to screen the main active terpenes and discover the possible mechanism of LEO through network pharmacology in the treatment of insomnia-related diseases, as well as to verify our hypothesis in insomnia mice. The results showed that, in LEO’s 15 potential active ingredients, beta-myrcene had strong sedative–hypnotic effects through the serotonergic synaptic pathway according to the network pharmacological prediction. Further, PCPA(DL-4-chlorophenylalanine)-induced insomnia mice were treated with beta-myrcene for one day or seven days. The quiet state of insomnia mice was increased effectively, and the hypnotic effect was enhanced by anaobarbital sodium by prolonging sleep duration, decreasing sleep latency, and increasing the rate of falling asleep. Beta-myrcene reduced the damage to hypothalamic neuron cells induced by PCPA and increased neurotransmitter levels of GABA, 5-HT, and Glu in the serum and hypothalamus of insomnia mice. Meanwhile, beta-myrcene exerted an improvement in insomnia by upregulating relevant genes and protein expression in the serotonergic synaptic pathway. These results support the merit of the sedative–hypnotic activity of LEO. Beta-myrcene, a terpene in LEO, may be the main source of its sedative–hypnotic properties. It may serve as a good potential compound in future clinical studies on coping with insomnia.

研究领域: 药理学 · 神经科学 · 医学
✓ 已验证 DOI PubMed 高影响因子
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FOOD RESEARCH INTERNATIONAL · 2024 · IF 7

Study on chemical characterization and sleep-improvement function of Prunella vulgaris L. based on the functional components

Chang Zhou,Yi-fan Hu,Yan Zhang,Cheng-hao Wang,Xue-jing Liao,Fa-feng Cheng,Yan-yan Jiang

Prunella vulgaris L. (P. vulgaris) has great application value and development prospects in improving sleep. In this study, we continued to evaluate the sleep-improvement function and mechanism of P. vulgaris from both chemical characterization and function based on sleep-improvement functional ingredients, rosmarinic acid and salviaflaside, screened out in the previous stage as the index components. The chemical constituents of P. vulgaris and its phenolic acid fraction were characterized by the UPLC-MS n technology. The quality of the sleep-improvement phenolic acid fraction of P. vulgaris was scientifically evaluated by fingerprints combined with quantitative analysis of rosmarinic acid and salviaflaside. The function of phenolic acid parts of P. vulgaris in improving sleep was verified by different insomnia models including the PCPA-induced insomnia model and surface platform sleep deprivation model. HE staining was used to observe the effect of P. vulgaris on the morphology of nerve cells in different brain regions. In vivo experiments and molecular docking explored the sedative-hypnotic effects of functional ingredients of P. vulgaris . All these results investigated the material basis and mechanism of P. vulgaris to improve sleep from multiple perspectives, which contribute to providing a basis for the development of functional food to improve sleep.

CAS / MDL: 7424-00-2
研究领域: 药理学 · 化学 · 神经科学
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MOLECULAR NUTRITION & FOOD RESEARCH · 2022 ·Vol. 66 ·期 11 ·2100963 · IF 6.575

Cinnamaldehyde Regulates the Generation of γ-aminobutyric Acid to Exert Sedation via Irreversible Inhibition of ENO1 in the Cerebellar Granular Layer

Xiaoyao Ma,Kaixin Liu,Yiman Han,Yongping Bai,Fukui Shen,Mukuo Wang,Wei Wei,Jianfeng Qin,Erwei Hao,Xiaotao Hou,Yuanyuan Hou,Gang Bai

Scope Glutamate (Glu) and γ-aminobutyric acid (GABA) are the major excitatory and inhibitory neurotransmitters that control information flow in the brain. GABA dysfunction is a general vulnerability factor for mental illness. Cinnamaldehyde (CA) is found to have sedation in a mental illness model. However, the specific targets and molecular mechanisms related to the sedative effects of CA have not been elucidated. Methods and Results Metabolomics analysis and target fishing showed CA could increase the expression of GABA in vivo, and α-enolase (ENO1) is the primary target protein of CA associated with sedation. CA mainly binds with ENO1 in the cerebellar granular layer of brain, which influences the first transformations of the input signals arriving in the cerebellar cortex. The α,β-unsaturated aldehyde group of CA blocks the hydroxy group of Ser40, which induces a loss in ENO1 activation. CA also disturbs the glycolysis pathway and influences the tricarboxylic acid cycle and oxidative phosphorylation, which activate gluconeogenesis to provide energy to the brain. This mechanism is verified in zebrafish with ENO1 or glutamic acid decarboxylase (GAD) deficiency. Conclusions CA demonstrates sedation and alleviates GABA dysfunction via covalent binding ENO1, which shows the potential to improve the therapy of mental illness.

研究领域: 神经科学 · 药理学 · 分子生物学 · 生物化学
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NEUROCHEMICAL RESEARCH · 2024 · IF 3.7

Cannabidiol Exerts Sedative and Hypnotic Effects in Normal and Insomnia Model Mice Through Activation of 5-HT1A Receptor

Liu Yu-Meng,Li Jin-Cao,Gu Yong-Fang,Qiu Ren-Hong,Huang Jia-Ying,Xue Rui,Li Shuo,Zhang Yang,Zhang Kuo,Zhang You-Zhi

Cannabis sativa has been used for improving sleep for long history. Cannabidiol (CBD) has drown much attention as a non-addictive psychoactive component in Cannabis sativa extract. However, the effects of CBD on sleep architecture and it’s acting mechanism remains unclear. In the present study, we evaluated the sedative-hypnotic effect of cannabidiol (CBD), assessed the effects of CBD on sleep using a wireless physiological telemetry system. We further explored the therapeutic effects of CBD using 4-chloro-dl-phenylalanine (PCPA) induced insomnia model and changes in sleep latency, sleep duration and intestinal flora were evaluated. CBD shortened sleep latency and increases sleep duration in both normal and insomnia mice, and those effects were blocked by 5-HT 1A receptor antagonist WAY100635. We determined that CBD increases 5-HT 1A receptors expression and 5-HT content in the hypothalamus of PCPA-pretreated mice and affects tryptophan metabolism in the intestinal flora. These results showed that activation of 5-HT 1A receptors is one of the potential mechanisms underlying the sedative-hypnotic effect of CBD. This study validated the effects of CBD on sleep and evaluated its potential therapeutic effects on insomnia.

CAS / MDL: 56-12-2 50-67-9
研究领域: 药理学 · 神经科学 · 睡眠医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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