来自Hybanthus enneaspermus (L.) F. Muell.的潜在抗焦虑治疗药物通过调节GABAA-Cl-通道缓解焦虑。- 可能通过调节 GABAA-Cl- 通道来缓解焦虑。

IF 4.4 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Neurochemistry international Pub Date : 2024-07-11 DOI:10.1016/j.neuint.2024.105804
Liesl Maria Fernandes e Mendonça , Arun Bhimrao Joshi , Anant Bhandarkar , Shamshad Shaikh , Samantha Fernandes , Himanshu Joshi , Shrinivas Joshi
{"title":"来自Hybanthus enneaspermus (L.) F. Muell.的潜在抗焦虑治疗药物通过调节GABAA-Cl-通道缓解焦虑。- 可能通过调节 GABAA-Cl- 通道来缓解焦虑。","authors":"Liesl Maria Fernandes e Mendonça ,&nbsp;Arun Bhimrao Joshi ,&nbsp;Anant Bhandarkar ,&nbsp;Shamshad Shaikh ,&nbsp;Samantha Fernandes ,&nbsp;Himanshu Joshi ,&nbsp;Shrinivas Joshi","doi":"10.1016/j.neuint.2024.105804","DOIUrl":null,"url":null,"abstract":"<div><p>Anxiety is a commonly prevailing psychological disorder that requires effective treatment, wherein phytopharmaceuticals and nutraceuticals could offer a desirable therapeutic profile. <em>Hybanthus enneaspermus</em> (L.) F. Muell. is a powerful medicinal herb, reportedly effective against several ailments, including psychological disorders. The current research envisaged evaluating the anxiolytic potential of the ethanolic extract of <em>Hybanthus enneaspermus</em> (EEHE) and its toluene insoluble biofraction (ITHE) employing experimental and computational approaches. Elevated Plus Maze, Light and Dark Transition, Mirror Chamber, Hole board and Open field tests were used as screening models to assess the antianxiety potential of 100, 200 and 400 mg/kg body weight of EEHE and ITHE in rats subjected to social isolation, using Diazepam as standard. The brains of rats exhibiting significant anxiolytic activity were dissected for histopathological and biochemical studies. Antioxidant enzymes like catalase, superoxide dismutase, glutathione-S-transferase, glutathione peroxidase, glutathione reductase; and neurotransmitters <em>viz</em>. monoamines (serotonin, noradrenaline, dopamine), Gamma-aminobutyric acid (GABA), and glutamate were quantified in the different regions of rats’ brain (cortex, hippocampus, pons, medulla oblongata, cerebellum). Chromatographic techniques were used to isolate phytoconstituents from the fraction exhibiting significant activity that were characterized by spectroscopic methods and subjected to <em>in silico</em> molecular docking. ITHE at 400 mg/kg body weight significantly mitigated anxiety in all the screening models (<em>p</em> &lt; 0.05), reduced the inflammatory vacuoles and necrosis (<em>p</em> &lt; 0.05) and potentiated the antioxidant enzymes (<em>p</em> &lt; 0.05). It enhanced the monoamines and GABA levels while attenuating glutamate levels (<em>p</em> &lt; 0.01) in the brain. Three significant flavonoids <em>viz.</em> Quercitrin, Rutin and Hesperidin were isolated from ITHE. <em>In silico</em> docking studies of these flavonoids revealed that the compounds exhibited substantial binding to the GABA<sub>A</sub> receptor. ITHE displayed a promising pharmacological profile in combating anxiety and modulating oxidative stress, attributing its therapeutic virtues to the flavonoids present.</p></div>","PeriodicalId":398,"journal":{"name":"Neurochemistry international","volume":"178 ","pages":"Article 105804"},"PeriodicalIF":4.4000,"publicationDate":"2024-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Potential anxiolytic therapeutics from Hybanthus enneaspermus (L.) F. Muell. - mitigate anxiety by plausibly modulating the GABAA-Cl- channel\",\"authors\":\"Liesl Maria Fernandes e Mendonça ,&nbsp;Arun Bhimrao Joshi ,&nbsp;Anant Bhandarkar ,&nbsp;Shamshad Shaikh ,&nbsp;Samantha Fernandes ,&nbsp;Himanshu Joshi ,&nbsp;Shrinivas Joshi\",\"doi\":\"10.1016/j.neuint.2024.105804\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Anxiety is a commonly prevailing psychological disorder that requires effective treatment, wherein phytopharmaceuticals and nutraceuticals could offer a desirable therapeutic profile. <em>Hybanthus enneaspermus</em> (L.) F. Muell. is a powerful medicinal herb, reportedly effective against several ailments, including psychological disorders. The current research envisaged evaluating the anxiolytic potential of the ethanolic extract of <em>Hybanthus enneaspermus</em> (EEHE) and its toluene insoluble biofraction (ITHE) employing experimental and computational approaches. Elevated Plus Maze, Light and Dark Transition, Mirror Chamber, Hole board and Open field tests were used as screening models to assess the antianxiety potential of 100, 200 and 400 mg/kg body weight of EEHE and ITHE in rats subjected to social isolation, using Diazepam as standard. The brains of rats exhibiting significant anxiolytic activity were dissected for histopathological and biochemical studies. Antioxidant enzymes like catalase, superoxide dismutase, glutathione-S-transferase, glutathione peroxidase, glutathione reductase; and neurotransmitters <em>viz</em>. monoamines (serotonin, noradrenaline, dopamine), Gamma-aminobutyric acid (GABA), and glutamate were quantified in the different regions of rats’ brain (cortex, hippocampus, pons, medulla oblongata, cerebellum). Chromatographic techniques were used to isolate phytoconstituents from the fraction exhibiting significant activity that were characterized by spectroscopic methods and subjected to <em>in silico</em> molecular docking. ITHE at 400 mg/kg body weight significantly mitigated anxiety in all the screening models (<em>p</em> &lt; 0.05), reduced the inflammatory vacuoles and necrosis (<em>p</em> &lt; 0.05) and potentiated the antioxidant enzymes (<em>p</em> &lt; 0.05). It enhanced the monoamines and GABA levels while attenuating glutamate levels (<em>p</em> &lt; 0.01) in the brain. Three significant flavonoids <em>viz.</em> Quercitrin, Rutin and Hesperidin were isolated from ITHE. <em>In silico</em> docking studies of these flavonoids revealed that the compounds exhibited substantial binding to the GABA<sub>A</sub> receptor. ITHE displayed a promising pharmacological profile in combating anxiety and modulating oxidative stress, attributing its therapeutic virtues to the flavonoids present.</p></div>\",\"PeriodicalId\":398,\"journal\":{\"name\":\"Neurochemistry international\",\"volume\":\"178 \",\"pages\":\"Article 105804\"},\"PeriodicalIF\":4.4000,\"publicationDate\":\"2024-07-11\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Neurochemistry international\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0197018624001311\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Neurochemistry international","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0197018624001311","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0

摘要

焦虑症是一种常见的心理疾病,需要有效的治疗,而植物药和营养保健品可以提供理想的治疗效果。据报道,Hybanthus enneaspermus (L.) F. Muell.是一种强效药草,对包括心理障碍在内的多种疾病有效。目前的研究计划采用实验和计算方法,评估芒柄木乙醇提取物(EEHE)及其甲苯不溶生物馏分(ITHE)的抗焦虑潜力。以地西泮为标准,使用高架加迷宫、明暗转换、镜室、洞板和开放场地试验作为筛选模型,评估了 100、200 和 400 mg/Kg 体重的 EEHE 和 ITHE 对受到社会隔离的大鼠的抗焦虑潜力。对表现出明显抗焦虑活性的大鼠大脑进行解剖,以进行组织病理学和生化研究。对大鼠大脑不同区域(皮层、海马、脑桥、延髓、小脑)的抗氧化酶(如过氧化氢酶、超氧化物歧化酶、谷胱甘肽-S-转移酶、谷胱甘肽过氧化物酶、谷胱甘肽还原酶)和神经递质(如单胺(5-羟色胺、去甲肾上腺素、多巴胺)、γ-氨基丁酸(GABA)和谷氨酸)进行了定量分析。使用色谱技术从具有显著活性的部分中分离出植物成分,并通过光谱方法对其进行表征和进行硅学分子对接。在所有筛选模型中,400 毫克/千克体重的 ITHE 都能显著缓解焦虑(p < 0.05),减少炎症空泡和坏死(p < 0.05),并增强抗氧化酶(p < 0.05)。它提高了大脑中的单胺类和 GABA 水平,同时降低了谷氨酸水平(p < 0.01)。三种重要的类黄酮,即从 ITHE 中分离出槲皮素、芦丁和橙皮甙。对这些类黄酮进行的硅对接研究表明,这些化合物与 GABAA 受体有很强的结合力。ITHE 在抗焦虑和调节氧化应激方面显示出良好的药理特性,其治疗功效归功于其中的类黄酮。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

摘要图片

查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Potential anxiolytic therapeutics from Hybanthus enneaspermus (L.) F. Muell. - mitigate anxiety by plausibly modulating the GABAA-Cl- channel

Anxiety is a commonly prevailing psychological disorder that requires effective treatment, wherein phytopharmaceuticals and nutraceuticals could offer a desirable therapeutic profile. Hybanthus enneaspermus (L.) F. Muell. is a powerful medicinal herb, reportedly effective against several ailments, including psychological disorders. The current research envisaged evaluating the anxiolytic potential of the ethanolic extract of Hybanthus enneaspermus (EEHE) and its toluene insoluble biofraction (ITHE) employing experimental and computational approaches. Elevated Plus Maze, Light and Dark Transition, Mirror Chamber, Hole board and Open field tests were used as screening models to assess the antianxiety potential of 100, 200 and 400 mg/kg body weight of EEHE and ITHE in rats subjected to social isolation, using Diazepam as standard. The brains of rats exhibiting significant anxiolytic activity were dissected for histopathological and biochemical studies. Antioxidant enzymes like catalase, superoxide dismutase, glutathione-S-transferase, glutathione peroxidase, glutathione reductase; and neurotransmitters viz. monoamines (serotonin, noradrenaline, dopamine), Gamma-aminobutyric acid (GABA), and glutamate were quantified in the different regions of rats’ brain (cortex, hippocampus, pons, medulla oblongata, cerebellum). Chromatographic techniques were used to isolate phytoconstituents from the fraction exhibiting significant activity that were characterized by spectroscopic methods and subjected to in silico molecular docking. ITHE at 400 mg/kg body weight significantly mitigated anxiety in all the screening models (p < 0.05), reduced the inflammatory vacuoles and necrosis (p < 0.05) and potentiated the antioxidant enzymes (p < 0.05). It enhanced the monoamines and GABA levels while attenuating glutamate levels (p < 0.01) in the brain. Three significant flavonoids viz. Quercitrin, Rutin and Hesperidin were isolated from ITHE. In silico docking studies of these flavonoids revealed that the compounds exhibited substantial binding to the GABAA receptor. ITHE displayed a promising pharmacological profile in combating anxiety and modulating oxidative stress, attributing its therapeutic virtues to the flavonoids present.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
Neurochemistry international
Neurochemistry international 医学-神经科学
CiteScore
8.40
自引率
2.40%
发文量
128
审稿时长
37 days
期刊介绍: Neurochemistry International is devoted to the rapid publication of outstanding original articles and timely reviews in neurochemistry. Manuscripts on a broad range of topics will be considered, including molecular and cellular neurochemistry, neuropharmacology and genetic aspects of CNS function, neuroimmunology, metabolism as well as the neurochemistry of neurological and psychiatric disorders of the CNS.
期刊最新文献
Neuroprotective effects of nutraceuticals and natural products in Traumatic Brain Injury. Polygonatum sibiricum polysaccharides: A promising strategy in the treatment of neurodegenerative disease The wnt/pyruvate kinase, muscle axis plays an essential role in the differentiation of mouse neuroblastoma cells The developing mouse dopaminergic system: Cortical-subcortical shift in D1/D2 receptor balance and increasing regional differentiation. An overview of the relationship between inflammation and cognitive function in humans, molecular pathways and the impact of nutraceuticals
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1