Diseases resulting from exaggerated inflammatory responses present a significant peril to human beings,and its pathogenesis and treatment have not been fully elaborated.Traditional Chinese medicine offers the benefit ...Diseases resulting from exaggerated inflammatory responses present a significant peril to human beings,and its pathogenesis and treatment have not been fully elaborated.Traditional Chinese medicine offers the benefit of minimal adverse effects and favorable outcomes in the management of inflammatory diseases.Polygonum cuspidatum,a type of traditional Chinese medicine,refers to the dried rhizomes and roots of the plant species Polygonum cuspidatum from the Polygonaceae family.It has a slightly bitter taste and exhibits a cold nature,exhibiting therapeutic effects such as heat-clearing and detoxification,blood stasis removal and pain relief,phlegm resolution,and cough alleviation.Research has demonstrated that the bioactive constituents found in Polygonum cuspidatum can impede the inflammatory response through the modulation of pertinent pathways.The anti-inflammatory effects of it have been primarily observed in nonalcoholic fatty liver disease,arthritis,ischemic stroke,parkinson’s disease,ulcerative colitis,and diabetes mellitus.This review is conducted by combining papers from the past decade.The anti-inflammatory properties and mechanisms of Polygonum cuspidatum and its natural compounds are summarized.It provides a new theoretical basis for further research on the clinical pharmacological effects of Polygonum cuspidatum.展开更多
Aim To establish reliable methods for evaluating the quality of rhizoma of Polygonum cuspidatum( Huzhang in Chinese). Methods TLC and HPLC were employed for the chemical identification and content determination,respec...Aim To establish reliable methods for evaluating the quality of rhizoma of Polygonum cuspidatum( Huzhang in Chinese). Methods TLC and HPLC were employed for the chemical identification and content determination,respectively. Results A qualitative TLC method and a quantitative HPLC method with piceid as the reference substance were established, respectively. With piceid as the reference substance and ethyl acetate-methanol-formic acid-water ( 19:3:0.5:1) as the mobile phase, a TLC method for the identification of Huzhang from the commonly used crude drugs of the same family was also set up. Conclusion The established TLC method can reasonably appraise the quality of the drug and easily distinguish Huzhang from the other commonly used crude drugs of the same family. The HPLC method for determining piceid is simple, reproducible, accurate, and feasible.展开更多
The present study investigated the chemical composition of ethylacetate extracts from an endophytic actinomycete Streptomyces sp. A0916 and its host Polygonum cuspidatum. A comparative analysis of the antimicrobial an...The present study investigated the chemical composition of ethylacetate extracts from an endophytic actinomycete Streptomyces sp. A0916 and its host Polygonum cuspidatum. A comparative analysis of the antimicrobial and antioxidant properties of the extracts was also conducted. 32 compounds of P. cuspidatum and 23 compounds of Streptomyces sp. A0916 were isolated and identified by GC/MS. Antimicrobial activities of the extracts were evaluated using eight microbial strains(3 Gram-positive bacteria, 3 Gram-negative bacteria, and 2 fungi). The Streptomyces sp. A0916 extracts showed a wide range of antimicrobial activities and presented greater antimicrobial effectiveness than the P. cuspidatum extracts. The minimum inhibitory concentration(MIC) of Streptomyces sp. A0916 extracts against the ampicillin-resistant strain Enterococcus faecium SIIA843 was 32 μg·m L-1. Furthermore, the extracts had greater antimicrobial effect against Gram-positive bacteria than Gram-negative bacteria. Finally, the antioxidant activity of the Streptomyces sp. A0916 extracts was equal to that of the P. cuspidatum extracts. In conclusion, our results suggest that the endophytic actinomycetes of the medicinal plants are an important source of bioactive substances.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
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 rain 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
A novel and efficient extraction/hydrolysis method was developed for the recovery of resveratrol and emodin from a well-known traditional chinese medicinal herb, Polygonum cuspidatum. By using a 85% aqueous acetone so...A novel and efficient extraction/hydrolysis method was developed for the recovery of resveratrol and emodin from a well-known traditional chinese medicinal herb, Polygonum cuspidatum. By using a 85% aqueous acetone solution containing 1.0 mol/L HCl as extractant, extraction of resveratrol and emodin from P. cuspidatum and conversion of resveratrol-3-O-β-glucoside and emodin-8-O-β-D-glucoside into the products could be achieved in one step. The effects of several key parameters including concentration of HCl and acetone, temperature, ratio of solvent to material, extraction duration and extraction times on the process efficiency was systematically investigated. The results showed that the optimal conditions for maximizing the recovery yield were 85% acetone containing 1.0 mol/L HCl as extractant, temperature 70 ℃, ratio of liquid to solid 50 mL /g and extraction duration 30 min. This one-pot extraction/hydrolysis process increased the yield of resveratrol and emodin to 524% and 302%, respectively, compared to a raw sample without hydrolysis. Compared with conventional method, the developed process not only achieved high yield of resveratrol and emodin, but simplified the procedures and reduced time. The results demonstrated that the simultaneous extraction/hydrolysis process is simple and efficient which could act as a useful approach for enhanced recovery of resveratrol and emodin from P. cuspidatum.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
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
Background and aims:Polygonum cuspidatum Sieb.et Zucc.(P.cuspidatum)and its active components have been clinically proven to have anti-hepatocellular carcinoma effects.However,the potential targets of P.cuspidatum for...Background and aims:Polygonum cuspidatum Sieb.et Zucc.(P.cuspidatum)and its active components have been clinically proven to have anti-hepatocellular carcinoma effects.However,the potential targets of P.cuspidatum for these effects have not yet been revealed.Methods:We used network pharmacology and single-cell transcriptomic analysis with molecular docking to elucidate the active components and targets of P.cuspidatum for hepatocellular carcinoma.Results:CDK1,ESR1,HSP90A11,and MAPK1 were shown to be the key targets of P.cuspidatum for hepatocellular carcinoma.P.cuspidatum was found to be likely correlated with the improved abnormal expression of CDK1 and ESR1 and the poor prognosis of HSP90AA1 and MAPK1.CDK1 was identified as the most potential antihepatocellular carcinoma target of P.cuspidatum.Among the active components of P.cuspidatum,physcion diglucoside was found to have the most potential to treat hepatocellular carcinoma by targeting CDK1.Conclusion:Our study provides novel insights into the anti-hepatocellular carcinoma pharmacological effects of P.cuspidatum,which could serve as a scientific basis for its development as a medicinal resource and the targeting of CDK1 for hepatocellular carcinoma treatment.展开更多
Various active components have been extracted from the root of Polygonum cuspidatum. However, the genetic basis for their activity is virtually unknown. In this study, 25600002 short reads （2.3 Gb） of P. cuspidatum ...Various active components have been extracted from the root of Polygonum cuspidatum. However, the genetic basis for their activity is virtually unknown. In this study, 25600002 short reads （2.3 Gb） of P. cuspidatum root transcriptome were obtained via lllumina HiSeq 2000 sequencing. A total of 86418 urtigenes were assembled de novo and annotated. Twelve, 18, 60 and 54 unigenes were respectively mapped to the mevalonic acid （MVA）, methyl-D-erythritol 4-phosphate （MEP）, shikimate and resveratrol biosynthesis pathways, suggesting that they are involved in the biosynthesis of pharmaceutically important anthra- quinone and resveratrol. Eighteen potential UDP-glycosyltransferase unigenes were identified as the candidates most likely to be involved in the biosynthesis of glycosides of secondary metabolites. Identification of relevant genes could be important in eventually increasing the yields of the medicinally useful constituents of the P. cuspidatum root. From the previously published transcriptome data of 19 non-model plant taxa, 1127 shared orthologs were identified and characterized. This information will be very useful for future functional, phylogenetic and evolutionary studies of these plants.展开更多
Objective: To observe the effects of Chinese medicine(CM) Polygonum cuspidatum(PC) on adenosine 5'-monophosphate-activated protein kinase(AMPK), forkhead box O3α(FOXO3α), Toll-like receptor-4(TLR4), NACHT, LRR a...Objective: To observe the effects of Chinese medicine(CM) Polygonum cuspidatum(PC) on adenosine 5'-monophosphate-activated protein kinase(AMPK), forkhead box O3α(FOXO3α), Toll-like receptor-4(TLR4), NACHT, LRR and PYD domains-containing protein 3(NLRP3), and monocyte chemoattractant protein-1(MCP-1) expression in a rat model of uric acid-induced renal damage and to determine the molecular mechanism. Methods: A rat model of uric acid-induced renal damage was established, and rats were randomly divided into a model group, a positive drug group, and high-, medium-, and low-dose PC groups(n=12 per group). A normal group(n=6) was used as the control. Rats in the normal and model groups were administered distilled water(10 m L·kg^(–1)) by intragastric infusion. Rats in the positive drug group and the high-, medium-, and low-dose PC groups were administered allopurinol(23.33 mg·kg^(–1)), and 7.46, 3.73, or 1.87 g·kg^(–1)·d^(–1) PC by intragastric infusion, respectively for 6 to 8 weeks. After the intervention, reverse transcription polymerase chain reaction, Western blot, enzyme linked immunosorbent assay, and immunohistochemistry were used to detect AMPK, FOXO3α, TLR4, NLRP3, and MCP-1 m RNA and protein levels in renal tissue or serum. Results: Compared with the normal group, the m RNA transcription levels of AMPK and FOXO3α in the model group were significantly down-regulated, and protein levels of AMPKα1, pAMPKα1 and FOXO3α were significantly down-regulated at the 6 th and 8 th weeks(P<0.01 or P<0.05). The m RNA transcription and protein levels of TLR4, NLRP3 and MCP-1 were significantly up-regulated(P<0.01 or P<0.05). Compared with the model group, at the 6 th week, the mRNA transcription levels of AMPK in the high-and medium-dose groups, and protein expression levels of AMPKα1, p AMPKα1 and FOXO3α in the high-dose PC group, AMPKα1 and p AMPKα1 in the mediumdose PC group, and p AMPKα1 in the low-dose PC group were significantly up-regulated(P<0.01 or P<0.05); the m RNA transcription and protein levels of TLR4 and NLRP3 in the 3 CM groups, and protein expression levels of MCP-1 in the medium-and low-dose PC groups were down-regulated(P<0.01 or P<0.05). At the 8 th week, the m RNA transcription levels of AMPK in the high-dose PC group and FOXO3α in the medium-dose PC group, and protein levels of AMPKα1, p AMPKα1 and FOXO3α in the 3 CM groups were significantly up-regulated(P<0.01 or P<0.05); the m RNA transcription levels of TLR4 in the medium-and low-dose PC groups, NLRP3 in the high-and low-dose PC groups and MCP-1 in the medium-and low-dose PC groups, and protein expression levels of TLR4, NLRP3 and MCP-1 in the 3 CM groups were down-regulated(P<0.01 or P<0.05). Conclusion: PC up-regulated the expression of AMPK and its downstream molecule FOXO3α and inhibited the biological activity of TLR4, NLRP3, and MCP-1, key signal molecules in the immunoinflammatory network pathway, which may be the molecularmechanism of PC to improve hyperuricemia-mediated immunoinflammatory metabolic renal damage.展开更多
基金supported by grants from Zhejiang Chinese Medicine University affiliated hospital research project(2023FSYYZZ18)scientific research item(2022FH001),School of Life Sciences,Zhejiang Chinese Medicine University.
文摘Diseases resulting from exaggerated inflammatory responses present a significant peril to human beings,and its pathogenesis and treatment have not been fully elaborated.Traditional Chinese medicine offers the benefit of minimal adverse effects and favorable outcomes in the management of inflammatory diseases.Polygonum cuspidatum,a type of traditional Chinese medicine,refers to the dried rhizomes and roots of the plant species Polygonum cuspidatum from the Polygonaceae family.It has a slightly bitter taste and exhibits a cold nature,exhibiting therapeutic effects such as heat-clearing and detoxification,blood stasis removal and pain relief,phlegm resolution,and cough alleviation.Research has demonstrated that the bioactive constituents found in Polygonum cuspidatum can impede the inflammatory response through the modulation of pertinent pathways.The anti-inflammatory effects of it have been primarily observed in nonalcoholic fatty liver disease,arthritis,ischemic stroke,parkinson’s disease,ulcerative colitis,and diabetes mellitus.This review is conducted by combining papers from the past decade.The anti-inflammatory properties and mechanisms of Polygonum cuspidatum and its natural compounds are summarized.It provides a new theoretical basis for further research on the clinical pharmacological effects of Polygonum cuspidatum.
基金TheNinth Five yearNationalKeyScientificandTech nicalProgramofChinaNo.99 92 9 0 1 3 1
文摘Aim To establish reliable methods for evaluating the quality of rhizoma of Polygonum cuspidatum( Huzhang in Chinese). Methods TLC and HPLC were employed for the chemical identification and content determination,respectively. Results A qualitative TLC method and a quantitative HPLC method with piceid as the reference substance were established, respectively. With piceid as the reference substance and ethyl acetate-methanol-formic acid-water ( 19:3:0.5:1) as the mobile phase, a TLC method for the identification of Huzhang from the commonly used crude drugs of the same family was also set up. Conclusion The established TLC method can reasonably appraise the quality of the drug and easily distinguish Huzhang from the other commonly used crude drugs of the same family. The HPLC method for determining piceid is simple, reproducible, accurate, and feasible.
基金supported by Department of Science and Technology of Sichuan Province,China(No.2014 JY0199)
文摘The present study investigated the chemical composition of ethylacetate extracts from an endophytic actinomycete Streptomyces sp. A0916 and its host Polygonum cuspidatum. A comparative analysis of the antimicrobial and antioxidant properties of the extracts was also conducted. 32 compounds of P. cuspidatum and 23 compounds of Streptomyces sp. A0916 were isolated and identified by GC/MS. Antimicrobial activities of the extracts were evaluated using eight microbial strains(3 Gram-positive bacteria, 3 Gram-negative bacteria, and 2 fungi). The Streptomyces sp. A0916 extracts showed a wide range of antimicrobial activities and presented greater antimicrobial effectiveness than the P. cuspidatum extracts. The minimum inhibitory concentration(MIC) of Streptomyces sp. A0916 extracts against the ampicillin-resistant strain Enterococcus faecium SIIA843 was 32 μg·m L-1. Furthermore, the extracts had greater antimicrobial effect against Gram-positive bacteria than Gram-negative bacteria. Finally, the antioxidant activity of the Streptomyces sp. A0916 extracts was equal to that of the P. cuspidatum extracts. In conclusion, our results suggest that the endophytic actinomycetes of the medicinal plants are an important source of bioactive substances.
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 rain 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Supported by the National Natural Science Foundation of China(No.2113600921506221)
文摘A novel and efficient extraction/hydrolysis method was developed for the recovery of resveratrol and emodin from a well-known traditional chinese medicinal herb, Polygonum cuspidatum. By using a 85% aqueous acetone solution containing 1.0 mol/L HCl as extractant, extraction of resveratrol and emodin from P. cuspidatum and conversion of resveratrol-3-O-β-glucoside and emodin-8-O-β-D-glucoside into the products could be achieved in one step. The effects of several key parameters including concentration of HCl and acetone, temperature, ratio of solvent to material, extraction duration and extraction times on the process efficiency was systematically investigated. The results showed that the optimal conditions for maximizing the recovery yield were 85% acetone containing 1.0 mol/L HCl as extractant, temperature 70 ℃, ratio of liquid to solid 50 mL /g and extraction duration 30 min. This one-pot extraction/hydrolysis process increased the yield of resveratrol and emodin to 524% and 302%, respectively, compared to a raw sample without hydrolysis. Compared with conventional method, the developed process not only achieved high yield of resveratrol and emodin, but simplified the procedures and reduced time. The results demonstrated that the simultaneous extraction/hydrolysis process is simple and efficient which could act as a useful approach for enhanced recovery of resveratrol and emodin from P. cuspidatum.
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.
基金Supported by National Training Program of Innovation and Entrepreneurship for Undergraduates(202410145118).
文摘Background and aims:Polygonum cuspidatum Sieb.et Zucc.(P.cuspidatum)and its active components have been clinically proven to have anti-hepatocellular carcinoma effects.However,the potential targets of P.cuspidatum for these effects have not yet been revealed.Methods:We used network pharmacology and single-cell transcriptomic analysis with molecular docking to elucidate the active components and targets of P.cuspidatum for hepatocellular carcinoma.Results:CDK1,ESR1,HSP90A11,and MAPK1 were shown to be the key targets of P.cuspidatum for hepatocellular carcinoma.P.cuspidatum was found to be likely correlated with the improved abnormal expression of CDK1 and ESR1 and the poor prognosis of HSP90AA1 and MAPK1.CDK1 was identified as the most potential antihepatocellular carcinoma target of P.cuspidatum.Among the active components of P.cuspidatum,physcion diglucoside was found to have the most potential to treat hepatocellular carcinoma by targeting CDK1.Conclusion:Our study provides novel insights into the anti-hepatocellular carcinoma pharmacological effects of P.cuspidatum,which could serve as a scientific basis for its development as a medicinal resource and the targeting of CDK1 for hepatocellular carcinoma treatment.
基金supported by the National Science and Technology Major Program (Grant No.2008ZX10005-004)
文摘Various active components have been extracted from the root of Polygonum cuspidatum. However, the genetic basis for their activity is virtually unknown. In this study, 25600002 short reads （2.3 Gb） of P. cuspidatum root transcriptome were obtained via lllumina HiSeq 2000 sequencing. A total of 86418 urtigenes were assembled de novo and annotated. Twelve, 18, 60 and 54 unigenes were respectively mapped to the mevalonic acid （MVA）, methyl-D-erythritol 4-phosphate （MEP）, shikimate and resveratrol biosynthesis pathways, suggesting that they are involved in the biosynthesis of pharmaceutically important anthra- quinone and resveratrol. Eighteen potential UDP-glycosyltransferase unigenes were identified as the candidates most likely to be involved in the biosynthesis of glycosides of secondary metabolites. Identification of relevant genes could be important in eventually increasing the yields of the medicinally useful constituents of the P. cuspidatum root. From the previously published transcriptome data of 19 non-model plant taxa, 1127 shared orthologs were identified and characterized. This information will be very useful for future functional, phylogenetic and evolutionary studies of these plants.
基金Supported by the National Natural Science Foundation of China(No.81473516 and No.30973918)
文摘Objective: To observe the effects of Chinese medicine(CM) Polygonum cuspidatum(PC) on adenosine 5'-monophosphate-activated protein kinase(AMPK), forkhead box O3α(FOXO3α), Toll-like receptor-4(TLR4), NACHT, LRR and PYD domains-containing protein 3(NLRP3), and monocyte chemoattractant protein-1(MCP-1) expression in a rat model of uric acid-induced renal damage and to determine the molecular mechanism. Methods: A rat model of uric acid-induced renal damage was established, and rats were randomly divided into a model group, a positive drug group, and high-, medium-, and low-dose PC groups(n=12 per group). A normal group(n=6) was used as the control. Rats in the normal and model groups were administered distilled water(10 m L·kg^(–1)) by intragastric infusion. Rats in the positive drug group and the high-, medium-, and low-dose PC groups were administered allopurinol(23.33 mg·kg^(–1)), and 7.46, 3.73, or 1.87 g·kg^(–1)·d^(–1) PC by intragastric infusion, respectively for 6 to 8 weeks. After the intervention, reverse transcription polymerase chain reaction, Western blot, enzyme linked immunosorbent assay, and immunohistochemistry were used to detect AMPK, FOXO3α, TLR4, NLRP3, and MCP-1 m RNA and protein levels in renal tissue or serum. Results: Compared with the normal group, the m RNA transcription levels of AMPK and FOXO3α in the model group were significantly down-regulated, and protein levels of AMPKα1, pAMPKα1 and FOXO3α were significantly down-regulated at the 6 th and 8 th weeks(P<0.01 or P<0.05). The m RNA transcription and protein levels of TLR4, NLRP3 and MCP-1 were significantly up-regulated(P<0.01 or P<0.05). Compared with the model group, at the 6 th week, the mRNA transcription levels of AMPK in the high-and medium-dose groups, and protein expression levels of AMPKα1, p AMPKα1 and FOXO3α in the high-dose PC group, AMPKα1 and p AMPKα1 in the mediumdose PC group, and p AMPKα1 in the low-dose PC group were significantly up-regulated(P<0.01 or P<0.05); the m RNA transcription and protein levels of TLR4 and NLRP3 in the 3 CM groups, and protein expression levels of MCP-1 in the medium-and low-dose PC groups were down-regulated(P<0.01 or P<0.05). At the 8 th week, the m RNA transcription levels of AMPK in the high-dose PC group and FOXO3α in the medium-dose PC group, and protein levels of AMPKα1, p AMPKα1 and FOXO3α in the 3 CM groups were significantly up-regulated(P<0.01 or P<0.05); the m RNA transcription levels of TLR4 in the medium-and low-dose PC groups, NLRP3 in the high-and low-dose PC groups and MCP-1 in the medium-and low-dose PC groups, and protein expression levels of TLR4, NLRP3 and MCP-1 in the 3 CM groups were down-regulated(P<0.01 or P<0.05). Conclusion: PC up-regulated the expression of AMPK and its downstream molecule FOXO3α and inhibited the biological activity of TLR4, NLRP3, and MCP-1, key signal molecules in the immunoinflammatory network pathway, which may be the molecularmechanism of PC to improve hyperuricemia-mediated immunoinflammatory metabolic renal damage.
