Gentianine has been shown to have a protective effect on hippocampal CA1 neurons in rats subjected to recurrent febrile convulsion(FC).The present study sought to explore the possible mechanism of gentianine by intr...Gentianine has been shown to have a protective effect on hippocampal CA1 neurons in rats subjected to recurrent febrile convulsion(FC).The present study sought to explore the possible mechanism of gentianine by intraperitoneally injecting gentianine into rats with warm water-induced FC.The results revealed that neuronal organelle injury was slightly ameliorated in the hippocampal CA1 region.The level of glutamate was decreased,but the level of γ-aminobutyric acid was increased,as detected by ninhydrin staining.In addition,glutamate acid decarboxylase expression in hippocampal CA1 was increased,as determined by immunohistochemistry.The results demonstrated that gentianine can ameliorate FC-induced neuronal injury by enhancing glutamate acid decarboxylase activity,decreasing glutamate levels and increasing γ-aminobutyric acid levels.展开更多
Objective:Encephalopathy is increasingly threatening human health.It is correspondingly one of the concerns of society and medical community.As a natural source,traditional Chinese medicine has tremendous beneficial o...Objective:Encephalopathy is increasingly threatening human health.It is correspondingly one of the concerns of society and medical community.As a natural source,traditional Chinese medicine has tremendous beneficial outcomes in various diseases including encephalopathy.Gentianine,a Chinese herbal compound,shows effectiveness in many diseases exclusively in inflammation.Therefore,this in vitro research was carried out to find its effectiveness in encephalopathy.Methodology:Ligand and proteins were searched and downloaded from ChemDraw and protein database,respectively.Sybyl-X2.0 docking software and its various functions were used to prepare ligand and proteins.Finally,gentianine was docked with proteins using Sybyl-X2.0 docking software.Results:Gentianine was docked with 20 protein targets.Compounds with C-score of 5 were selected.A total of three kinds of protein docked with gentianine(ABCC1,C-reactive protein[CRP],and NKX5-2)were selected.ABCC1 was expressed in the brain and was related to seizures and stroke.CRP was an inflammatory biomarker and related to seizures,epilepsy,stroke,and Parkinson’s disease.NKX2–5 was also known as cardiac transcription and related to cerebral palsy,Alzheimer’s disease,and stroke.All these targets were related to encephalopathy.Conclusion:Molecular docking findings in this study lead to the suggestion that gentianine might be helpful in treating encephalopathy.This study is expected to provide a solution to find potential anti-encephalopathy compounds.展开更多
基金the Key Project of Technology of Ministry of Education, No. 2007029
文摘Gentianine has been shown to have a protective effect on hippocampal CA1 neurons in rats subjected to recurrent febrile convulsion(FC).The present study sought to explore the possible mechanism of gentianine by intraperitoneally injecting gentianine into rats with warm water-induced FC.The results revealed that neuronal organelle injury was slightly ameliorated in the hippocampal CA1 region.The level of glutamate was decreased,but the level of γ-aminobutyric acid was increased,as detected by ninhydrin staining.In addition,glutamate acid decarboxylase expression in hippocampal CA1 was increased,as determined by immunohistochemistry.The results demonstrated that gentianine can ameliorate FC-induced neuronal injury by enhancing glutamate acid decarboxylase activity,decreasing glutamate levels and increasing γ-aminobutyric acid levels.
基金supported by the National Natural Science Foundation of China(No.82004085)the Double First-Class Personnel Office-Research Fund of Scientific Research Team(1000061020051)+1 种基金University Nursing Program for Young Scholars with Creative Talents in Heilongjiang Province(UNPYSCT-2018032)Chunhui program from Ministry of Education(HLJ2019039)。
文摘Objective:Encephalopathy is increasingly threatening human health.It is correspondingly one of the concerns of society and medical community.As a natural source,traditional Chinese medicine has tremendous beneficial outcomes in various diseases including encephalopathy.Gentianine,a Chinese herbal compound,shows effectiveness in many diseases exclusively in inflammation.Therefore,this in vitro research was carried out to find its effectiveness in encephalopathy.Methodology:Ligand and proteins were searched and downloaded from ChemDraw and protein database,respectively.Sybyl-X2.0 docking software and its various functions were used to prepare ligand and proteins.Finally,gentianine was docked with proteins using Sybyl-X2.0 docking software.Results:Gentianine was docked with 20 protein targets.Compounds with C-score of 5 were selected.A total of three kinds of protein docked with gentianine(ABCC1,C-reactive protein[CRP],and NKX5-2)were selected.ABCC1 was expressed in the brain and was related to seizures and stroke.CRP was an inflammatory biomarker and related to seizures,epilepsy,stroke,and Parkinson’s disease.NKX2–5 was also known as cardiac transcription and related to cerebral palsy,Alzheimer’s disease,and stroke.All these targets were related to encephalopathy.Conclusion:Molecular docking findings in this study lead to the suggestion that gentianine might be helpful in treating encephalopathy.This study is expected to provide a solution to find potential anti-encephalopathy compounds.