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Identification of Anxiolytic Potential of Niranthin:In-vivo and Computational Investigations 被引量:1
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作者 Atul R.Chopade Prakash M.Somade +1 位作者 Pratik P.Somade Suraj N.Mali 《Natural Products and Bioprospecting》 CAS 2021年第2期223-233,共11页
Anxiety is an unpleasant state,which can critically decrease the quality of life is often accompanied by nervous behaviour and rumination.Niranthin is a lignan isolated from various Phyllanthus sources.The literature ... Anxiety is an unpleasant state,which can critically decrease the quality of life is often accompanied by nervous behaviour and rumination.Niranthin is a lignan isolated from various Phyllanthus sources.The literature survey on niranthin highlights wide ranges of the therapeutic potentials.In a present study,based on our previous investigations,we evaluated pure,isolated and characterized niranthin as an anxiolytic agent.The niranthin[6-[(2R,3R)-3-[(3,4-dimethoxyphenyl)methyl]-4-methoxy-2-(methoxymethyl)butyl]-4-methoxy-1,3-benzodioxole]was purchased from commercial source and further subjected for assessment of its anxiolytic potentials using popular animal models including Elevated plus-maze model/test(EPM)and Light&Dark Exploration test(L&D).GABA-A receptor mediation was evaluated by pretreating the mice with the GABA-A receptor antagonist Flumazenil before the EPM task.Molecular docking simulation studies(pdb id:4COF)carried out by Vlife QSAR software showed that niranthin(docking score:−62.1714 kcal/mol)have shown comparatively best docking score compared to the standard drug Diazepam(docking score:−63.1568 kcal/mol).To conclude,Niranthin has probable potential in the management of anxiety disorder.Our in-silico and in-vivo analysis(indirectly)indicated the plausible role of GABA mediation for anxiolytic activity.Although,these studies are preliminary,future in depth experimental explorations will be required to use Niranthin as anti-anxiety drug in near future. 展开更多
关键词 PHARMACOLOGY PHYTOCONSTITUENTS niranthin Lignan Anxiolytic activity EPM models
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珠子草素通过调控p38/JNK信号通路抑制肠上皮细胞凋亡保护肠屏障改善克罗恩病样肠炎
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作者 陶露 陈悦 +4 位作者 黄林林 郑旺 宋雪 项平 胡建国 《南方医科大学学报》 北大核心 2025年第11期2483-2494,共12页
目的探讨天然化合物珠子草素(NIR)对克罗恩病样结肠炎的作用及其分子机制。方法采用2,4,6-三硝基苯磺酸(TNBS)诱导小鼠建立结肠炎模型,随机分为4组:WT组注射生理盐水;WT+NIR组腹腔注射NIR(10 mg/kg,1次/d,注射7 d),TNBS组用2.5%TNBS造... 目的探讨天然化合物珠子草素(NIR)对克罗恩病样结肠炎的作用及其分子机制。方法采用2,4,6-三硝基苯磺酸(TNBS)诱导小鼠建立结肠炎模型,随机分为4组:WT组注射生理盐水;WT+NIR组腹腔注射NIR(10 mg/kg,1次/d,注射7 d),TNBS组用2.5%TNBS造模并给予等体积的生理盐水;TNBS+NIR组用2.5%TNBS造模并腹腔注射NIR(10 mg/kg,1次/d,注射7 d),6只/组。用体质量变化、疾病活动指数(DAI)和结肠长度评估NIR的治疗效果。ELISA法和实时定量PCR(qRT-PCR)检测肠黏膜组织炎症因子(IL-6、IL-1β、TNF-α、IL-17A和IL-10)水平。TUNEL染色和Western blotting检测肠上皮细胞凋亡情况及相关蛋白(Bcl-2/Bax)的表达。Western blotting评估紧密连接蛋白(TJ)(ZO-1、Claudin-1)和p38/JNK通路的活化水平,并通过Diprovocim干预实验验证NIR的调控分子机制。结果NIR干预后TNBS小鼠体质量增加,DAI和组织学炎症评分减低,结肠长度增加(P<0.05);ELISA和qRT-PCR结果表明NIR可降低促炎因子(IL-6,IL-1β、IL-17A和TNF-α)的蛋白和mRNA水平,上调抗炎因子IL-10表达水平(P<0.05);TUNEL和Western blotting检测显示NIR可抑制肠上皮细胞凋亡,激活抗凋亡通路(P<0.05);Western blotting结果证实NIR可上调ZO-1和Claudin-1的表达水平,并下调p38和JNK的磷酸化水平(P<0.05);Diprovocim干预可衰减NIR对p38/JNK通路的失活作用。结论NIR可通过调控p38/JNK信号的活化抑制肠上皮细胞凋亡,从而改善小鼠CD样肠炎。 展开更多
关键词 克罗恩病 炎症性肠病 肠上皮细胞凋亡 p38/JNK 珠子草素
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