MOLECULES
·
2020
·Vol. 25
·期 20
·4702
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IF 3.267
Nan Zhang,Mu Luo,Lei He,Lei Yao
Gardenia jasminoidesEllis is a famous fragrant flower in China. Previous pharmacological research mainly focuses on its fruit. In this study, the essential oil of the flower of ‘Shanzhizi’, which was a major variety for traditional Chinese medicine use, was extracted by hydro distillation and analyzed by GC-MS. Mouse anxiety models included open field, elevated plus maze (EPM), and light and dark box (LDB), which were used to evaluate its anxiolytic effect via inhalation. The involvement of monoamine system was studied by pretreatment with neurotransmitter receptor antagonists WAY100635, flumazenil and sulpiride. The monoamine neurotransmitters contents in the prefrontal cortex (PFC) and hippocampus after aroma inhalation were also analyzed. The results showed that inhalation ofG. jasminoidesessential oil could significantly elevated the time and entries into open arms in EPM tests and the time explored in the light chamber in LDB tests with no sedative effect. WAY100635 and sulpiride, but not flumazenil, blocked its anxiolytic effect. Inhalation ofG. jasminoidesessential oil significantly down-regulated the 5-HIAA/5-HT in the PFC and reduced the 5-HIAA content in hippocampus compared to the control treatment. In conclusion, inhalation of gardenia essential oil showed an anxiolytic effect in mice. Monoamine, especially the serotonergic system, was involved in its anxiolytic effect.Keywords:Gardenia jasminoides;essential oil;inhalation;anxiolytic effect;serotonergic neurotransmission
研究领域:
药理学
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神经科学
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植物化学
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DOI
PubMed
高影响因子
MOLECULES
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2018
·Vol. 23
·期 9
·2329
·
IF 3.098
Shao-Nan Wang,Yong-Sheng Ding,Xiao-Jie Ma,Cheng-Bowen Zhao,Ming-Xuan Lin,Jing Luo,Yi-Nan Jiang,Shuai He,Jian-You Guo,Jin-Li Shi
Zhi zhu xiang(ZZX for short) is the root and rhizome ofValeriana jatamansiJones, which is a Traditional Chinese Medicine (TCM) used to treat various mood disorders for more than 2000 years, especially anxiety. The aim of the present work was to identify the bioactive chemical markers inZhi zhu xiangimproving anxiety in rats by a fingerprint-efficacy study. More specifically, the chemical fingerprint of ZZX samples collected from 10 different regions was determined by High Performance Liquid Chromatography (HPLC) and the similarity analyses were calculated based on 10 common characteristic peaks. The anti-anxiety effect of ZZX on empty bottle stimulated rats was examined through the Open Field Test (OFT) and the Elevated Plus Maze Test (EPM). Then we measured the concentration of CRF, ACTH, and CORT in rat’s plasma by the enzyme-linked immune sorbent assay (ELISA) kit, while the concentration of monoamine and metabolites (NE, DA, DOPAC, HVA, 5-HT, 5-HIAA) in the rat’s cerebral cortex and hippocampus was analysed by HPLC coupled with an Electrochemical Detector. At last, the fingerprint-efficacy study between chemical fingerprint and anti-anxiety effect of ZZX was accomplished by partial least squares regression (PLSR). As a result, we screened out four compounds (hesperidin, isochlorogenic acid A, isochlorogenic acid B and isochlorogenic acid C) as the bioactive chemical markers for the anti-anxiety effect of ZZX. The fingerprint-efficacy study we established might provide a feasible way and some elicitation for the identification of the bioactive chemical markers for TCM.Keywords:anti-anxiety;Valeriana jatamansiJones;fingerprint-efficacy relationship;PLSR
研究领域:
中药学
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神经生物学
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药理学
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PubMed
高影响因子
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
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2018
·Vol. 98
·期 13
·4885-4894
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IF 2.379
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
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植物化学
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DOI
高影响因子
MOLECULES
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2025
·Vol. 30
·期 16
·3400
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IF 4.6
Lina Hu,Mengjiao Li,Zheng Liu,Hui Yan,Xuekun Wang,Shiben Wang
To discover novel, potent anticonvulsant compounds, a series of compounds containing triazole structural fragments were synthesized and evaluated for their anticonvulsant activity. Compounds6f(maximal electroshock (MES), 50% effective dose (ED50) = 13.1 mg/kg; subcutaneous pentylenetetrazole (scPTZ), ED50= 19.7 mg/kg) and6l(MES, ED50= 9.1 mg/kg;scPTZ, ED50= 19.0 mg/kg) showed the best activity in MES andscPTZ tests. The results of an affinity test showed that the potent compounds had better binding to the GABAAreceptors. The results of an inhibitory neurotransmitter GABA content test in brain tissue indicated that compounds6fand6lexerted anticonvulsant activity which may be associated with the increase of GABA content in the rat brain. Elevated plus maze (EPM) assay results showed that compounds6fand6lpossessed anxiolytic effects, and their effects correlated with the binding sites of benzodiazepines (BZs) in the GABAAreceptors. Molecular docking was performed to investigate the interactions of the studied compound6lwith the GABAAreceptors on the molecular level.
研究领域:
药物化学
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药理学
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神经科学
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有机合成
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DOI
PubMed
高影响因子
Biomaterials Science
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2021
·Vol. 9
·期 13
·4765-4777
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IF 6.843
Shu Li,Chen Guo,Xingjiao Zhang,Xiaojing Liu,Jing Mu,Chunxia Liu,Yali Peng,Min Chang
Anxiety disorders are the most common mental diseases and can greatly disrupt everyday life. Although there has been substantial research on anxiety disorders, novel therapeutics are needed. Neuropeptide S (NPS) is a potential therapeutic candidate owing to its strong anxiolytic activity; however, some disadvantages, such as its poor metabolic stability and inability to cross the blood–brain barrier (BBB), limit its use in the clinic. Herein, inspired by nose-to-brain drug delivery strategies, an endogenous 20-amino-acid-long mNPS peptide was modified by incorporating palmitic acid into its functional Lys12 side chain (M-3), which was expected to facilitate nose-to-brain penetration and exert a prolonged anxiolytic-like effect compared to mNPS. We found that M-3 assembled into nanofibers that retained the bioactivity of NPS and exhibited obvious improvements in metabolic stability. Notably, as expected, self-assembled M-3 was able to penetrate into the brain and exert anxiolytic effects. The elevated plus-maze (EPM) results further revealed that M-3 could produce prolonged anxiolytic-like effects in mice. In vivo imaging studies revealed that self-assembled M-3 could be efficiently transported from the nasal cavity to the brain. Furthermore, when intranasally administered, this molecule exhibited a significantly prolonged anxiolytic-like effect, which further illustrated that this molecule has a potent nose-to-brain penetration in vivo. Overall, this self-assembled nanofiber showed potent nose-to-brain penetration ability and prolonged bioactivity.
研究领域:
神经科学
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药理学
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分子生物学
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PubMed
高影响因子
Advanced Science
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2024
·
IF 14.3
Ping-Fen Yang,Tai-Lei Nie,Xia-Nan Sun,Lan-Xin Xu,Cong Ma,Fang Wang,Li-Hong Long,Jian-Guo Chen
Physical exercise has beneficial effect on anxiety disorders, but the underlying molecular mechanism remains largely unknown. Here, it is demonstrated that physical exercise can downregulate the S-nitrosylation of gephyrin (SNO-gephyrin) in the basolateral amygdala (BLA) to exert anxiolytic effects. It is found that the level of SNO-gephyrin is significantly increased in the BLA of high-anxiety rats and a downregulation of SNO-gephyrin at cysteines 212 and 284 produced anxiolytic effect. Mechanistically, inhibition of SNO-gephyrin by either Cys212 or Cys284 mutations increased the surface expression of GABA A R γ2 and the subsequent GABAergic neurotransmission, exerting anxiolytic effect in male rats. On the other side, overexpression of neuronal nitric oxide synthase in the BLA abolished the anxiolytic-like effects of physical exercise. This study reveals a key role of downregulating SNO-gephyrin in the anxiolytic effects of physical exercise, providing a new explanation for protein post-translational modifications in the brain after exercise.
研究领域:
神经科学
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分子生物学
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行为科学
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PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2025
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IF 6.2
Si-Yi Han,Hong-Fu Zhao,Zi-Ying Zhao,Jing-Zhi Yu,Ying-Hua Zhang,Zhi-Shen Mu
Food-derived protein peptides with γ-aminobutyric acid transaminase (GABA-T) inhibitory activity possess the promising ability to alleviate anxiety and have become a market focus. This study prepared casein hydrolysate with valid GABA-T inhibitory activity using ultrasound-assisted enzymatic hydrolysis and obtained novel GABA-T inhibitory peptides through isolation and purification. The results demonstrated that ultrasonic pretreatment significantly improved the casein hydrolysis efficiency, enhanced GABA-T inhibitory activity by 19.32%, and allowed retention of 42.37% of the initial inhibitory activity after gastrointestinal digestion. Through peptidomics analysis, five novel GABA-T inhibitory peptides were identified from casein hydrolysate, including FFVAPFPE, VYPFPGPIPN, HLPLPL, FLPYPY, and WQVL (2.79 ± 0.14 to 8.49 ± 0.26 mM). Molecular docking results revealed that these five peptides bind to GABA-T through hydrogen bonds and hydrophobic interactions, with the Arg422 residue potentially serving as the key active site for GABA-T inhibition. This study demonstrates significant potential for both the high-value utilization of casein and the development of antianxiety functional foods targeting GABA-T.
研究领域:
食品科学
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生物化学
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神经药理学
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肽类研究
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酶学
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PubMed
高影响因子
PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
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2022
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IF 5.201
Lina Ruan,Kaiyu Guan,Yue Wang,Ming Gu,Yue Chen,Lisha Cai,Ruixuan Ye,Zhengwei Huang,Anqi Guo,Zhengkang Su,Xi Li,Jianchun Pan
Post-traumatic stress disorder (PTSD) is a serious mental disease featured by a stress dysfunction that occurs after an individual has faced intense mental stress, often accompanied by anxiety and chronic pain. Currently, the mainstream drug for PTSD is serotonin reuptake inhibitors (SSRIs), however, their pain management for patients is limited. Baicalein , a Chinese traditional herbal medicine, has shown promising results in treating anxiety, depression, and pain. In this study, we found that baicalein may alleviate single prolonged stress (SPS)-induced PTSD-like behaviors in mice without altering baseline nociceptive sensitivity or activity. Meanwhile, baicalein increased the noradrenaline (NE) and serotonin (5-HT) content and decreased the ratio of 5-hydroxyindoleacetic acid (5-HIAA)/5-HT by inhibiting the activity of monoamine oxidase A (MAO-A) in SPS-induce mice. The anxiolytic and antinociceptive effects induced by baicalein were totally abolished by 5-HT depleting agents. Moreover, the anxiolytic effects of baicalein could be abolished by the 5-HT 1A receptor antagonist WAY-100635, and the analgesic effects could be abolished by delta-opioid receptor antagonists in the spinal. Taken together, our study provides compelling evidence that baicalein reversed anxiety-like behaviors and neuropathic pain in PTSD through serotonergic system and spinal delta-opioid receptors.
研究领域:
药理学
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神经科学
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精神病学
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传统中药
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DOI
PubMed
高影响因子
Journal of Essential Oil Bearing Plants
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2022
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IF 1.971
Yuanyuan Zhang,Lin Zhang,Yongbin Meng,Yuangang Zu,Feng Han,Xiuhua Zhao
The utilization of natural product resources is significant for economic growth and health care. Herein, Cinnamomum longepaniculatum essential oil (CLEO) was isolated by microwave-assisted hydrodistillation (MAH). The composition of CLEO was determined by gas chromatography/mass spectrometry (GC/MS), and the antibacterial, nematicidal and anxiolytic activities of CLEO were evaluated. GC/MS results revealed that 33 compounds were identified, accounting for 99.87% of the total identified compounds. The major components of CLEO were monoterpenes, including β-myrcene (22.55%), eucalyptol (11.59%), α-pinene (11.56%), terpinen-4-ol (8.63%). Further research found that CLEO can inhibit the growth of Staphylococcus aureus (MIC 7.13 mg/mL, MBC 14.25 mg/mL), Escherichia coli (MIC 14.25 mg/mL, MBC 57 mg/mL), and Pseudomonas aeruginosa (MIC 14.25 mg/mL, MBC 28.50 mg/mL), the zone of inhibition were 17.49 ± 0.51 mm, 13.35 ± 0.27 mm and 15.15 ± 0.31 mm, respectively. CLEO could increase cell membrane permeability and make β-galactosidase, protein and other substances leak from the cell. Importantly, CLEO was first used to kill pine wood nematodes (PWN, Bursaphelenchus xylophilus). It was found that CLEO was toxic to B. xylophilus (LC50=30.81 mg/mL), and PWN treated with CLEO rapidly died and extended. Furthermore, CLEO was used in anxiolytic for the first time. CLEO inhalation can effectively relieve anxiety-like behaviors in open-field test (OFT) and elevated plus-maze test (EPT), and restore neurotransmitters (5-HT, NE, GABA) in brain tissue to normal levels. This study provides a strategy for the industrial production of CLEO and discovers its potential role in food transportation and preservation, forest pest control, and relief of emotional disorders such as anxiety and stress, which are beneficial to health care and economic development and provides a basis for broader application of CLEO.
研究领域:
药理学
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植物科学
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微生物学
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神经科学
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DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2023
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IF 5.4
Jiaqi Xie,Yihong Li,Yulu Liang,Hongqian Kui,Can Wang,Jianmei Huang
Ethnopharmacological relevance Platycladi Semen was recorded in Shen Nong's Herbal Classic and was considered a herbal medicine with low toxicity after long-term medication. Multiple traditional Chinese medicine prescriptions containing Platycladi Semen have been used to treat insomnia. Modern clinical practitioners commonly use Platycladi Semen to treat anxiety disorders, but there are few studies on its composition and anxiolytic mechanisms. Aim of the study To describe the main components of Platycladi Semen and investigate its anxiolytic effects and mechanisms. Materials and methods The main components of Platycladi Semen were characterized by liquid chromatography-mass spectrometry (LC-MS) and gas chromatography-mass spectrometry (GC-MS). The anxiolytic effects of oral Platycladi Semen were evaluated in chronic unpredictable mild stress (CUMS) induced mice. To explore the anxiolytic mechanisms of Platycladi Semen , serum non-targeted metabolomics combined with network pharmacology and molecular docking was performed. Results Fourteen compounds were identified in the 50% methanol extract and 11 fatty acid derivatives were identified in the methyl-esterified fatty oil of Platycladi Semen . In CUMS mice, both the aqueous extract and fatty oil of Platycladi Semen had anxiolytic effects, which were shown by the increase in the time and frequency of mice entering the open arm in the elevated plus maze (EPM) experiment. Through serum non-targeted metabolomics, 34 differential metabolites were identified, and lipid metabolic pathways such as sphingolipid metabolism, steroidogenesis, alpha-linoleic acid, and linoleic acid metabolism were enriched. Through network pharmacology, 109 targets of the main components in Platycladi Semen were identified, and the ‘neuroactive ligand-receptor interaction’ and ‘lipid metabolism’ were enriched. The molecular docking results showed that the main components in Platycladi Semen could bind to the key targets such as peroxisome proliferator-activated receptor delta (PPARD), peroxisome proliferator-activated receptor alpha (PPARA), fatty acid binding protein 5 (FABP5), fatty acid binding protein 3 (FABP3), peroxisome proliferator-activated receptor gamma (PPARG), arachidonate 5-lipoxygenase (ALOX5) and fatty acid amide hydrolase (FAAH). Conclusion This study indicated that Platycladi Semen has anxiolytic effects, and the anxiolytic mechanisms may be the regulation of lipid metabolism and the neuroactive ligand-receptor interaction.
研究领域:
药理学
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代谢组学
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中药学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
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