A uniform experimental design procedure was used to investigate the effects of some operating parameters on the extraction of emodin from Polygonum cuspidatum Sieb. et Zucc. products. Variables tested were volume rati...A uniform experimental design procedure was used to investigate the effects of some operating parameters on the extraction of emodin from Polygonum cuspidatum Sieb. et Zucc. products. Variables tested were volume ratio of material to solvent, size of material, extraction time and temperature and composition of extraction solvent (mixtures of acetone-water). Each variable was tested at seven levels; 7 experiments were performed in random order. Analyses of the extracts were performed by high-performance liquid chromatography with diode array detection(HPLC-DAD). Analytical responses were processed by using a forward regression analysis, in order to find polynomial function describing the relationship between variables and responses. For all the analytes the experimental conditions for providing the highest extraction yield inside the experimental domain considered were found. Finally, a simple, rapid and accurate analytical method was developed for the determination of emodin by high performance liquid chromatography. The separation is achieved within 25 min on an ODS column using methanol and water as gradient mobiles. Emodin can be quantified by using external standard method detecting at 436 nm. Good linearity is obtained with correlation coefficient exceeding 0.9986 and the detection limit and the quantification limit are 1.53 and 3.23 mg/L respectively. This method shows good reproducibility for the quantification of the emodin with intra-day and inter-day relative standard deviation less than 2.3% and 5.6% respectively. Under optimized extraction conditions, the recovery of the standard is 96.5%. The validated method is successfully applied to quantify the emodin in seven Polygonum cuspidatum sieb. Et zucc. products, which provided an idea for the pre-treatment of determination of active compounds in traditional Chinese medicines.展开更多
Background:As a popular Chinese herbal medicine,polygonum cuspidatum is widely used to treat hepatoma in China.Network pharmacology targets biological networks and analyzes the links between drugs,targets,and diseases...Background:As a popular Chinese herbal medicine,polygonum cuspidatum is widely used to treat hepatoma in China.Network pharmacology targets biological networks and analyzes the links between drugs,targets,and diseases in these networks.In this study,network pharmacology was utilized to reveal the potential pharmacological mechanisms of polygonum cuspidatum on hepatoma.Methods:The chemical constituents of polygonum cuspidatum were searched from TCMSP data and target gene names were extracted from UniProt database.The GeneCard,OMIM,PharmGkb,Therapeutic Targets database,and DrugBank database were used to establish a database of hepatoma targets.Common targets for drugs and diseases were obtained from Venn online tools.The protein-protein interaction network was constructed with the STRING database to analyze the related protein interaction relationship.The clusterProfiler R software package was used to enrich the common target proteinsof GO and KEGG to obtained the related functions and pathways.Cytoscape 3.7.2 was used to build a“drug-compound-target-disease”network.Finally,docking of the active components with the core target was carried out.Results:Ten active components of polygonum cuspidatum were obtained,and 108 potential targets for hepatoma were identified.The biological functions of the common target genes of polygonum cuspidatum and hepatoma are shown in GO analysis.Pathways involved in the treatment of hepatoma include virus-related signaling pathways,IL-17 signaling pathways,apoptosis signaling pathways,and PI3K/AKT signaling pathways.Conclusions:The network pharmacology directly shows the“drug-compound-target-disease”effects of polygonum cuspidatum on hepatoma,and provides a basis for studying the mechanism of the effect of polygonum cuspidatum on hepatoma.展开更多
Pulmonary fibrosis(PF)is an irreversible lung disease that is characterized by excessive scar tissue with a poor median survival rate of 2-3 years.The inhibition of transforming growth factor-β receptor type-I(TGF-β...Pulmonary fibrosis(PF)is an irreversible lung disease that is characterized by excessive scar tissue with a poor median survival rate of 2-3 years.The inhibition of transforming growth factor-β receptor type-I(TGF-β RI)by an appropriate drug may provide a promising strategy for the treatment of this disease.Polygonum cuspidatum(PC)is a well-known traditional Chinese herbal medicine which has an anti-PF effect.Accordingly,a combination of high resolution mass spectrometry with an in silico strategy was developed as a new method to search for potential chemical ingredients of PC that target the TGF-β RI.Based on this strategy,a total of 24 ingredients were identified.Then,absorption,distribution,metabolism,and excretion(ADME)-related properties were subsequently predicted to exclude compounds with potentially undesirable pharmacokinetics behaviour.Molecular docking studies on TGF-β RI were adopted to discover new PF inhibitors.Eventually,a compound that exists in PC known as resveratrol was proven to have excellent biological activity on TGF-β RI,with an IC_(50) of 2.211 μM in vitro.Furthermore,the complex formed through molecular docking was tested via molecular dynamics simulations,which revealed that resveratrol had strong interactions with residues of TGF-β RI.This study revealed that resveratrol has significant potential as a treatment for PF due to its ability to target TGF-β RI.In addition,this research demonstrated the exploration of natural products with excellent biological activities toward specific targets via high resolution mass spectrometry in combination with in silico technology is a promising strategy for the discovery of novel drugs.展开更多
Objective:The protective effect of Scutellaria baicalensis Stems and Polygonum Cuspidatum compatibility on lipopolysaccharide(LPS)-induced acute lung injury(ALI)in rats was studied by observing the expression of TRPV1...Objective:The protective effect of Scutellaria baicalensis Stems and Polygonum Cuspidatum compatibility on lipopolysaccharide(LPS)-induced acute lung injury(ALI)in rats was studied by observing the expression of TRPV1 and inflammatory cytokines.Methods:48 male SD rats were randomly divided into 6 groups:control group,model group,dexamethasone group(5mg/kg)and Scutellaria baicalensis Stems-Polygonum Cuspidatum(3.5,7 and 14g/kg).The administration group was gavaged for 7 days,and the control group and model group were given the same amount of 0.9%sodium chloride.On the 8th day,except the control group,rats in other groups were injected with 8mg/kg LPS through caudal vein to induce Ali model.Take the rat lung tissue 6 hours after modeling,and calculate the wet/dry weight ratio(W/D)of the rat lung tissue;HE staining to observe the pathological changes of lung tissue;Determine the content of tumor necrosis factor-α(TNF-α)and interleukin-1β(1L-1β)in alveolar lavage fluid(BALF)and the activity of superoxide dismutase(SOD)in serum;Detect the mRNA and protein expression levels of TRPV1 receptor in rat lung tissue.Results:Compared with the model group,Scutellaria baicalensis Stems-Polygonum Cuspidatum can significantly reduce the damage of lung tissue structure and bleeding state,W/D value and TNF-α、IL-1βThe content of TRPV1 decreased,the level of SOD increased,and the mRNA and protein expression of TRPV1 receptor decreased.Conclusion:The combination of Scutellaria baicalensis Stems-Polygonum has a protective effect on acute lung injury in rats,and its mechanism may be related to down-regulating the expression of TRPV1 and inhibiting the levels of TNF-αand IL-1βin inflammatory cells.展开更多
Polygonum cuspidatum is used as a traditional medicinal herb for the therapy of various diseases including several types of cancers. In the present study, we focused on addressing the anti-cancer activity and molecula...Polygonum cuspidatum is used as a traditional medicinal herb for the therapy of various diseases including several types of cancers. In the present study, we focused on addressing the anti-cancer activity and molecular mechanism of methanol extract of Polygonum cuspidatum (MEPC) in HSC-2 human oral cancer cells. The effect of MEPC on oral cancer cells was estimated by 3-(4,5-dimethylthiazol-20yl)-(3-carboxymethoxyphenyl)-2-(4-sulphophenyl)-2H-tetrazolium (MTS) assay, 4’-6-diamidino-2-phenylindole (DAPI) staining and Western blot analysis. MEPC inhibited the cell viability and induced apoptosis through the induction of death receptor (DR) 5. MEPC also increased the expression of C/EBP homologous protein/growth arrest and the DNA damage-inducible gene 153 (CHOP), a transcription factor induced by ER stress. Thus, we concluded that the induction of CHOP leading to DR5 up-regulation is required for the anti-cancer activity of MEPC in HSC-2 cells and MEPC may be a promising drug candidate for oral cancer.展开更多
Polygonum cuspidatum is a traditional Chinese medicine,and its medicinal part is dry rhizome.It is mainly used to treat damp heat jaundice,burns,carbuncle,ulcer poisoning,amenorrhea,and snake bite.Recent studies have ...Polygonum cuspidatum is a traditional Chinese medicine,and its medicinal part is dry rhizome.It is mainly used to treat damp heat jaundice,burns,carbuncle,ulcer poisoning,amenorrhea,and snake bite.Recent studies have found that P.cuspidatum also contains active ingredients against coronaviruses.This paper reviews the chemical constituents and pharmacological activities of P.cuspidatum,so as to provide a scientific basis for the development and utilization of P.cuspidatum resources in the future.展开更多
[Objectives]To study the toxic effect and antiviral activity of anthraquinone extract of Polygonum cuspidatum on infection of Koi herpes virus(KHV).[Methods]The MTT method and CPE microscopy were used to detect the co...[Objectives]To study the toxic effect and antiviral activity of anthraquinone extract of Polygonum cuspidatum on infection of Koi herpes virus(KHV).[Methods]The MTT method and CPE microscopy were used to detect the common carp brain(CCB)cytotoxicity of the P.cuspidatum anthraquinone extract in 48 h.Eight groups of different concentrations of the P.cuspidatum anthraquinone extract 1.96,3.91,7.28,15.63,31.25,62.5,125,250μg/mL experimental groups and a control group without drug effect were set up.After determining the maximum non-toxic range of the P.cuspidatum anthraquinone extract,the viral replication inhibition test was carried out.[Results]The concentration of the P.cuspidatum anthraquinone extract 31.25μg/mL was recognized as the maximum non-toxic concentration.The survival rate of CCB cells was higher than 80%,and the toxic dose(CC50)of the drug for 50%cell death was(72.67±2.12)μg/mL.The maximum inhibition rate of the P.cuspidatum anthraquinone extract was 78.63%±5.47%at a concentration of 31.25μg/mL,and the 50%effective drug dose(IC50)for inhibiting the virus was(13.67±0.47)μg/mL,and the therapeutic index(TI)was 5.48±0.49.In the direct virus killing test,the highest virus inhibition rate was 32.21%.[Conclusions]Under the experimental conditions,it can be concluded that the P.cuspidatum anthraquinone extract has high anti-KHV activity,and at the same time.It is expected to lay a theoretical foundation for the research of P.cuspidatum anthraquinone extract against KHV.展开更多
Objective A method of TLC-fluorescence spectrophotometry was established to assay the content of polydatin in polygonum cuspidatum sieb. et zucc. Methods: Polydatin was extracted by methanol and separated with chloro...Objective A method of TLC-fluorescence spectrophotometry was established to assay the content of polydatin in polygonum cuspidatum sieb. et zucc. Methods: Polydatin was extracted by methanol and separated with chloroform-acetone-formic acid-water (4∶4∶0.5∶0.2) by thin layer chromatography. The excitation wavelength and emission wavelength were 284 nm and 384 nm, respectively. Results The linear regression equation of the calibration graph was y=7.02179x+4.5143, a linear regression correlative coefficient r=0.9936. Conclusion This method was proved simple, stable and sensitive. It can be used in quality control of herbs.展开更多
目的:运用网络药理学探究虎杖治疗非酒精性脂肪性肝炎(Non-alcoholic steatohepatitis,NASH)的主要活性成分及作用机制。方法:通过中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology,TCMSP)获得虎杖...目的:运用网络药理学探究虎杖治疗非酒精性脂肪性肝炎(Non-alcoholic steatohepatitis,NASH)的主要活性成分及作用机制。方法:通过中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology,TCMSP)获得虎杖主要活性成分,于Pubmed compound数据库下载其结构式并导入Pharmmapper数据库获得成分作用靶点;借助Genecards、OMIM、Disgenet等数据库获得非酒精性脂肪性肝炎的疾病靶点;绘制药物-疾病交集靶点韦恩图,Cytoscape 3.9.1软件构建成分-靶点网络;String数据库获得PPI网络并通过拓扑分析得核心靶点网络,于Metascape数据库对潜在靶点进行GO、KEGG富集分析,微生信在线制图平台绘制气泡图及条形图等。结果:经筛选获得虎杖主要活性成分10个,主要活性成分作用靶点436个,疾病靶点3944个;去重结合得疾病靶点。虎杖抗NASH潜在作用靶点81个,6,8-Dihydroxy-7-methoxyxanthone、luteolin、Physovenine等可能为虎杖作用NASH的主要活性成分;PPI网络拓扑分析得到SRC、RXRA、GRB2、AKT1、RXRB、ESR1、STAT1、JAK2、IGF1、IGF1R等10个核心靶点;GO富集分析主要包含生物过程(Biological process,BP)条目1092个、细胞组分(Cellular component,CC)条目49个、分子功能(Molecular function,MF)条目98个,KEGG分析结果130条,涉及调节细胞对脂质的反应(Cellular response to lipid)、细胞内受体信号通路(Intracellular receptor signaling pathway)等生物过程,通过PI3K/Akt等信号通路发挥作用。结论:虎杖可通过多成分、多靶点、多通路对非酒精性脂肪性肝炎发挥治疗作用,其可能涉及抗炎、抗氧化、抗凋亡、调节代谢、抑制细胞增殖等生物活性。虎杖中的多种活性成分如6,8-Dihydroxy-7-methoxyxanthone、luteolin、Physovenine等可能通过SRC、RXRA、GRB2、AKT1等靶点对信号通路进行调控,涉及多种生物过程,从而发挥抗NASH的作用。展开更多
目的通过网络药理学、分子对接和实验验证探究何首乌-虎杖治疗脑小血管病(cerebral small vessel disease,CSVD)的作用机制。方法运用TCMSP数据库筛选何首乌和虎杖的化学成分及相关靶点蛋白,在GeneCards和OMIM数据库获取痴呆、中风、健...目的通过网络药理学、分子对接和实验验证探究何首乌-虎杖治疗脑小血管病(cerebral small vessel disease,CSVD)的作用机制。方法运用TCMSP数据库筛选何首乌和虎杖的化学成分及相关靶点蛋白,在GeneCards和OMIM数据库获取痴呆、中风、健忘相关靶点,通过Cytoscape构建中药-活性成分-靶点网络图和蛋白相互作用图,再利用DAVID数据库对作用靶点进行京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)通路富集。利用Autodock将关键有效成分和重要靶点进行分子对接,评估其结合活性。最后采用β-淀粉样多肽1-42(amyloidβ_(1-42),Aβ_(1-42))诱导BV-2细胞构建阿尔茨海默病(Alzheimer's disease,AD)细胞模型,采用Western blot法研究何首乌-虎杖对AD细胞模型关键靶点表达的影响。结果筛选出24个化学成分,120个活性成分-疾病共有靶点。KEGG结果涉及磷脂酰肌醇3-激酶/蛋白激酶B(phosphatidylinositol 3-kinase and protein kinase B,PI3K-Akt)、丝裂原激活蛋白激酶(mitogen-activated protein kinase,MAPK)、白介素-17(interleukin-17,IL-17)、缺氧诱导因子(hypoxia-inducible factor-1α,HIF-1)、肿瘤坏死因子(tumor necrosis factor,TNF)等多条炎症相关信号通路。筛选出槲皮素、大黄素、β-谷甾醇、大黄素甲醚、芹菜素5个关键化学成分,c-Jun氨基末端激酶(c-Jun N-terminal kinase,JNK)、TNF-α、细胞肿瘤抗原p53(cellular tumor antigen p53,P53)、白介素-6(interleukin-6,IL-6)和表皮生长因子受体(epidermal growth factor receptor,EGFR)5个关键靶点。分子对接结果显示,上述化合物与靶点的结合能均为负值。实验验证结果显示,何首乌-虎杖能显著抑制AD细胞模型5个关键靶点的表达。结论何首乌-虎杖可能通过调节核心靶点JNK、TNF-α、P53、IL-6抑制炎症反应、抑制细胞凋亡,从而发挥治疗CSVD作用。展开更多
采用网络药理学的方法探究虎杖(Polygonum cuspidatum)治疗糖尿病心肌病(diabetic cardiomyopathy, DCM)的关键靶点和潜在作用机制.通过检索中药系统药理学数据库与分析平台(traditional Chinese medicine systems pharmacology databas...采用网络药理学的方法探究虎杖(Polygonum cuspidatum)治疗糖尿病心肌病(diabetic cardiomyopathy, DCM)的关键靶点和潜在作用机制.通过检索中药系统药理学数据库与分析平台(traditional Chinese medicine systems pharmacology database and analysis platform, TCMSP)和查阅文献,获得虎杖的主要活性成分并预测其潜在的作用靶点.利用GeneCards和在线人类孟德尔遗传(online Mendelian inheritance in man, OMIM)数据库获得DCM的作用靶点,并绘制Venn图获得二者的交集靶点.使用String数据库和CytoScape软件构建虎杖-有效成分-交集靶点网络和蛋白相互作用(protein-protein interaction, PPI)网络.通过注释、可视化和集成发现数据库(the database for annotation, visualization and integrated discovery, DAVID)在线分析工具进行基因本体论(gene ontology, GO)富集分析和京都基因与基因组百科全书(Kyoto encyclopedia of genes and genomes, KEGG)富集分析,共筛选出15个虎杖有效活性成分以及214个治疗DCM的潜在作用靶点,主要涉及脂质和动脉粥样硬化通路、糖尿病并发症中的AGE-RAGE信号通路、IL-17信号通路、HIF-1信号通路、胰岛素抵抗通路、PI3K-Akt信号通路及凋亡通路等.这说明虎杖通过多成分、多靶点、多通路来发挥治疗DCM的作用.展开更多
基金Project (04JJ3081) supported by Hunan Province Natural Science Foundation of China
文摘A uniform experimental design procedure was used to investigate the effects of some operating parameters on the extraction of emodin from Polygonum cuspidatum Sieb. et Zucc. products. Variables tested were volume ratio of material to solvent, size of material, extraction time and temperature and composition of extraction solvent (mixtures of acetone-water). Each variable was tested at seven levels; 7 experiments were performed in random order. Analyses of the extracts were performed by high-performance liquid chromatography with diode array detection(HPLC-DAD). Analytical responses were processed by using a forward regression analysis, in order to find polynomial function describing the relationship between variables and responses. For all the analytes the experimental conditions for providing the highest extraction yield inside the experimental domain considered were found. Finally, a simple, rapid and accurate analytical method was developed for the determination of emodin by high performance liquid chromatography. The separation is achieved within 25 min on an ODS column using methanol and water as gradient mobiles. Emodin can be quantified by using external standard method detecting at 436 nm. Good linearity is obtained with correlation coefficient exceeding 0.9986 and the detection limit and the quantification limit are 1.53 and 3.23 mg/L respectively. This method shows good reproducibility for the quantification of the emodin with intra-day and inter-day relative standard deviation less than 2.3% and 5.6% respectively. Under optimized extraction conditions, the recovery of the standard is 96.5%. The validated method is successfully applied to quantify the emodin in seven Polygonum cuspidatum sieb. Et zucc. products, which provided an idea for the pre-treatment of determination of active compounds in traditional Chinese medicines.
基金funded by Enshi Prefecture Science and Technology Program Research and Development Project(grant no.2019000040).
文摘Background:As a popular Chinese herbal medicine,polygonum cuspidatum is widely used to treat hepatoma in China.Network pharmacology targets biological networks and analyzes the links between drugs,targets,and diseases in these networks.In this study,network pharmacology was utilized to reveal the potential pharmacological mechanisms of polygonum cuspidatum on hepatoma.Methods:The chemical constituents of polygonum cuspidatum were searched from TCMSP data and target gene names were extracted from UniProt database.The GeneCard,OMIM,PharmGkb,Therapeutic Targets database,and DrugBank database were used to establish a database of hepatoma targets.Common targets for drugs and diseases were obtained from Venn online tools.The protein-protein interaction network was constructed with the STRING database to analyze the related protein interaction relationship.The clusterProfiler R software package was used to enrich the common target proteinsof GO and KEGG to obtained the related functions and pathways.Cytoscape 3.7.2 was used to build a“drug-compound-target-disease”network.Finally,docking of the active components with the core target was carried out.Results:Ten active components of polygonum cuspidatum were obtained,and 108 potential targets for hepatoma were identified.The biological functions of the common target genes of polygonum cuspidatum and hepatoma are shown in GO analysis.Pathways involved in the treatment of hepatoma include virus-related signaling pathways,IL-17 signaling pathways,apoptosis signaling pathways,and PI3K/AKT signaling pathways.Conclusions:The network pharmacology directly shows the“drug-compound-target-disease”effects of polygonum cuspidatum on hepatoma,and provides a basis for studying the mechanism of the effect of polygonum cuspidatum on hepatoma.
基金supported by the National Natural Science Foundation of China(Grant Nos.:81703463 and 81603277)the National Key R&D Program of China(Grant No.:U1508220)the Liaoning Distinguished Professor Project for Qing Li,and the Doctoral Scientific Research Foundation of Liaoning Province(Grant No.:20170520199).
文摘Pulmonary fibrosis(PF)is an irreversible lung disease that is characterized by excessive scar tissue with a poor median survival rate of 2-3 years.The inhibition of transforming growth factor-β receptor type-I(TGF-β RI)by an appropriate drug may provide a promising strategy for the treatment of this disease.Polygonum cuspidatum(PC)is a well-known traditional Chinese herbal medicine which has an anti-PF effect.Accordingly,a combination of high resolution mass spectrometry with an in silico strategy was developed as a new method to search for potential chemical ingredients of PC that target the TGF-β RI.Based on this strategy,a total of 24 ingredients were identified.Then,absorption,distribution,metabolism,and excretion(ADME)-related properties were subsequently predicted to exclude compounds with potentially undesirable pharmacokinetics behaviour.Molecular docking studies on TGF-β RI were adopted to discover new PF inhibitors.Eventually,a compound that exists in PC known as resveratrol was proven to have excellent biological activity on TGF-β RI,with an IC_(50) of 2.211 μM in vitro.Furthermore,the complex formed through molecular docking was tested via molecular dynamics simulations,which revealed that resveratrol had strong interactions with residues of TGF-β RI.This study revealed that resveratrol has significant potential as a treatment for PF due to its ability to target TGF-β RI.In addition,this research demonstrated the exploration of natural products with excellent biological activities toward specific targets via high resolution mass spectrometry in combination with in silico technology is a promising strategy for the discovery of novel drugs.
基金Discipline Innovation Team of Shaanxi University of Traditional Chinese Medicine(No.2019-QN02)Project of Shaanxi Provincial Department of Education(Research and Development of Scutellaria Baicalensis Stem and Leaf and Honeysuckle Vine Anti Livestock and Poultry Infection Products)(No.20JC012)。
文摘Objective:The protective effect of Scutellaria baicalensis Stems and Polygonum Cuspidatum compatibility on lipopolysaccharide(LPS)-induced acute lung injury(ALI)in rats was studied by observing the expression of TRPV1 and inflammatory cytokines.Methods:48 male SD rats were randomly divided into 6 groups:control group,model group,dexamethasone group(5mg/kg)and Scutellaria baicalensis Stems-Polygonum Cuspidatum(3.5,7 and 14g/kg).The administration group was gavaged for 7 days,and the control group and model group were given the same amount of 0.9%sodium chloride.On the 8th day,except the control group,rats in other groups were injected with 8mg/kg LPS through caudal vein to induce Ali model.Take the rat lung tissue 6 hours after modeling,and calculate the wet/dry weight ratio(W/D)of the rat lung tissue;HE staining to observe the pathological changes of lung tissue;Determine the content of tumor necrosis factor-α(TNF-α)and interleukin-1β(1L-1β)in alveolar lavage fluid(BALF)and the activity of superoxide dismutase(SOD)in serum;Detect the mRNA and protein expression levels of TRPV1 receptor in rat lung tissue.Results:Compared with the model group,Scutellaria baicalensis Stems-Polygonum Cuspidatum can significantly reduce the damage of lung tissue structure and bleeding state,W/D value and TNF-α、IL-1βThe content of TRPV1 decreased,the level of SOD increased,and the mRNA and protein expression of TRPV1 receptor decreased.Conclusion:The combination of Scutellaria baicalensis Stems-Polygonum has a protective effect on acute lung injury in rats,and its mechanism may be related to down-regulating the expression of TRPV1 and inhibiting the levels of TNF-αand IL-1βin inflammatory cells.
文摘Polygonum cuspidatum is used as a traditional medicinal herb for the therapy of various diseases including several types of cancers. In the present study, we focused on addressing the anti-cancer activity and molecular mechanism of methanol extract of Polygonum cuspidatum (MEPC) in HSC-2 human oral cancer cells. The effect of MEPC on oral cancer cells was estimated by 3-(4,5-dimethylthiazol-20yl)-(3-carboxymethoxyphenyl)-2-(4-sulphophenyl)-2H-tetrazolium (MTS) assay, 4’-6-diamidino-2-phenylindole (DAPI) staining and Western blot analysis. MEPC inhibited the cell viability and induced apoptosis through the induction of death receptor (DR) 5. MEPC also increased the expression of C/EBP homologous protein/growth arrest and the DNA damage-inducible gene 153 (CHOP), a transcription factor induced by ER stress. Thus, we concluded that the induction of CHOP leading to DR5 up-regulation is required for the anti-cancer activity of MEPC in HSC-2 cells and MEPC may be a promising drug candidate for oral cancer.
基金This work was financially supported by National Natural Science Foundation of China(81973284)Scientific Research Projects of the Education Department of Liaoning Province(LJKZ0944).
文摘Polygonum cuspidatum is a traditional Chinese medicine,and its medicinal part is dry rhizome.It is mainly used to treat damp heat jaundice,burns,carbuncle,ulcer poisoning,amenorrhea,and snake bite.Recent studies have found that P.cuspidatum also contains active ingredients against coronaviruses.This paper reviews the chemical constituents and pharmacological activities of P.cuspidatum,so as to provide a scientific basis for the development and utilization of P.cuspidatum resources in the future.
基金the Modern Agricultural Industrial Technology System of the Ministry of Agriculture and Rural Affairs and the Ministry of FinanceProject of Fundamental Research Funds for Jilin Provincial Public Welfare Research Institutes(JSCYJK202102).
文摘[Objectives]To study the toxic effect and antiviral activity of anthraquinone extract of Polygonum cuspidatum on infection of Koi herpes virus(KHV).[Methods]The MTT method and CPE microscopy were used to detect the common carp brain(CCB)cytotoxicity of the P.cuspidatum anthraquinone extract in 48 h.Eight groups of different concentrations of the P.cuspidatum anthraquinone extract 1.96,3.91,7.28,15.63,31.25,62.5,125,250μg/mL experimental groups and a control group without drug effect were set up.After determining the maximum non-toxic range of the P.cuspidatum anthraquinone extract,the viral replication inhibition test was carried out.[Results]The concentration of the P.cuspidatum anthraquinone extract 31.25μg/mL was recognized as the maximum non-toxic concentration.The survival rate of CCB cells was higher than 80%,and the toxic dose(CC50)of the drug for 50%cell death was(72.67±2.12)μg/mL.The maximum inhibition rate of the P.cuspidatum anthraquinone extract was 78.63%±5.47%at a concentration of 31.25μg/mL,and the 50%effective drug dose(IC50)for inhibiting the virus was(13.67±0.47)μg/mL,and the therapeutic index(TI)was 5.48±0.49.In the direct virus killing test,the highest virus inhibition rate was 32.21%.[Conclusions]Under the experimental conditions,it can be concluded that the P.cuspidatum anthraquinone extract has high anti-KHV activity,and at the same time.It is expected to lay a theoretical foundation for the research of P.cuspidatum anthraquinone extract against KHV.
文摘Objective A method of TLC-fluorescence spectrophotometry was established to assay the content of polydatin in polygonum cuspidatum sieb. et zucc. Methods: Polydatin was extracted by methanol and separated with chloroform-acetone-formic acid-water (4∶4∶0.5∶0.2) by thin layer chromatography. The excitation wavelength and emission wavelength were 284 nm and 384 nm, respectively. Results The linear regression equation of the calibration graph was y=7.02179x+4.5143, a linear regression correlative coefficient r=0.9936. Conclusion This method was proved simple, stable and sensitive. It can be used in quality control of herbs.
文摘目的:运用网络药理学探究虎杖治疗非酒精性脂肪性肝炎(Non-alcoholic steatohepatitis,NASH)的主要活性成分及作用机制。方法:通过中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology,TCMSP)获得虎杖主要活性成分,于Pubmed compound数据库下载其结构式并导入Pharmmapper数据库获得成分作用靶点;借助Genecards、OMIM、Disgenet等数据库获得非酒精性脂肪性肝炎的疾病靶点;绘制药物-疾病交集靶点韦恩图,Cytoscape 3.9.1软件构建成分-靶点网络;String数据库获得PPI网络并通过拓扑分析得核心靶点网络,于Metascape数据库对潜在靶点进行GO、KEGG富集分析,微生信在线制图平台绘制气泡图及条形图等。结果:经筛选获得虎杖主要活性成分10个,主要活性成分作用靶点436个,疾病靶点3944个;去重结合得疾病靶点。虎杖抗NASH潜在作用靶点81个,6,8-Dihydroxy-7-methoxyxanthone、luteolin、Physovenine等可能为虎杖作用NASH的主要活性成分;PPI网络拓扑分析得到SRC、RXRA、GRB2、AKT1、RXRB、ESR1、STAT1、JAK2、IGF1、IGF1R等10个核心靶点;GO富集分析主要包含生物过程(Biological process,BP)条目1092个、细胞组分(Cellular component,CC)条目49个、分子功能(Molecular function,MF)条目98个,KEGG分析结果130条,涉及调节细胞对脂质的反应(Cellular response to lipid)、细胞内受体信号通路(Intracellular receptor signaling pathway)等生物过程,通过PI3K/Akt等信号通路发挥作用。结论:虎杖可通过多成分、多靶点、多通路对非酒精性脂肪性肝炎发挥治疗作用,其可能涉及抗炎、抗氧化、抗凋亡、调节代谢、抑制细胞增殖等生物活性。虎杖中的多种活性成分如6,8-Dihydroxy-7-methoxyxanthone、luteolin、Physovenine等可能通过SRC、RXRA、GRB2、AKT1等靶点对信号通路进行调控,涉及多种生物过程,从而发挥抗NASH的作用。
文摘目的通过网络药理学、分子对接和实验验证探究何首乌-虎杖治疗脑小血管病(cerebral small vessel disease,CSVD)的作用机制。方法运用TCMSP数据库筛选何首乌和虎杖的化学成分及相关靶点蛋白,在GeneCards和OMIM数据库获取痴呆、中风、健忘相关靶点,通过Cytoscape构建中药-活性成分-靶点网络图和蛋白相互作用图,再利用DAVID数据库对作用靶点进行京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)通路富集。利用Autodock将关键有效成分和重要靶点进行分子对接,评估其结合活性。最后采用β-淀粉样多肽1-42(amyloidβ_(1-42),Aβ_(1-42))诱导BV-2细胞构建阿尔茨海默病(Alzheimer's disease,AD)细胞模型,采用Western blot法研究何首乌-虎杖对AD细胞模型关键靶点表达的影响。结果筛选出24个化学成分,120个活性成分-疾病共有靶点。KEGG结果涉及磷脂酰肌醇3-激酶/蛋白激酶B(phosphatidylinositol 3-kinase and protein kinase B,PI3K-Akt)、丝裂原激活蛋白激酶(mitogen-activated protein kinase,MAPK)、白介素-17(interleukin-17,IL-17)、缺氧诱导因子(hypoxia-inducible factor-1α,HIF-1)、肿瘤坏死因子(tumor necrosis factor,TNF)等多条炎症相关信号通路。筛选出槲皮素、大黄素、β-谷甾醇、大黄素甲醚、芹菜素5个关键化学成分,c-Jun氨基末端激酶(c-Jun N-terminal kinase,JNK)、TNF-α、细胞肿瘤抗原p53(cellular tumor antigen p53,P53)、白介素-6(interleukin-6,IL-6)和表皮生长因子受体(epidermal growth factor receptor,EGFR)5个关键靶点。分子对接结果显示,上述化合物与靶点的结合能均为负值。实验验证结果显示,何首乌-虎杖能显著抑制AD细胞模型5个关键靶点的表达。结论何首乌-虎杖可能通过调节核心靶点JNK、TNF-α、P53、IL-6抑制炎症反应、抑制细胞凋亡,从而发挥治疗CSVD作用。
文摘采用网络药理学的方法探究虎杖(Polygonum cuspidatum)治疗糖尿病心肌病(diabetic cardiomyopathy, DCM)的关键靶点和潜在作用机制.通过检索中药系统药理学数据库与分析平台(traditional Chinese medicine systems pharmacology database and analysis platform, TCMSP)和查阅文献,获得虎杖的主要活性成分并预测其潜在的作用靶点.利用GeneCards和在线人类孟德尔遗传(online Mendelian inheritance in man, OMIM)数据库获得DCM的作用靶点,并绘制Venn图获得二者的交集靶点.使用String数据库和CytoScape软件构建虎杖-有效成分-交集靶点网络和蛋白相互作用(protein-protein interaction, PPI)网络.通过注释、可视化和集成发现数据库(the database for annotation, visualization and integrated discovery, DAVID)在线分析工具进行基因本体论(gene ontology, GO)富集分析和京都基因与基因组百科全书(Kyoto encyclopedia of genes and genomes, KEGG)富集分析,共筛选出15个虎杖有效活性成分以及214个治疗DCM的潜在作用靶点,主要涉及脂质和动脉粥样硬化通路、糖尿病并发症中的AGE-RAGE信号通路、IL-17信号通路、HIF-1信号通路、胰岛素抵抗通路、PI3K-Akt信号通路及凋亡通路等.这说明虎杖通过多成分、多靶点、多通路来发挥治疗DCM的作用.