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In the quality control of Chinese medicine， the detection of active components and toxic and harmful components are two important links. Although conventional methods such as high performance liquid chromatography and liquid chromatography-mass spectrometry can accurately quantify the above substances， they have shortcomings such as complicated operation， high costs， inability of detection at any time， difficult detection of insoluble and macromolecular substances. Enzyme-linked immunosorbent assay （ELISA） can adsorb antigens or antibodies on the surface of solid carriers and realize qualitative or quantitative analysis of targets by using the specific reactions of antigens and antibodies. This method is praised for the simple operation， high sensitivity， strong specificity， simple requirements for experimental equipment， a wide application range， and low costs. In recent years， ELISA has been widely used in the quality control of Chinese medicine， especially in the content determination of mycotoxins represented by aflatoxin and the qualitative and quantitative analysis of active components. ELISA plays an increasingly important role with its unique advantages， providing new methods and ideas for the rapid quality examination of large quantities of Chinese medicines. This paper reviews the research progress in ELISA for the quality control of Chinese medicine in recent years and prospects its technical development and application prospects， aiming to provide reference and research ideas for further using this method to ensure the quality， safety， and controllability of Chinese medicine.
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The discovery of drug targets plays a crucial role in drug research. Accurate information of small molecule drug-protein interaction can be provided by label-free target discovery technology without any structural modification at the small molecule. So, the label-free drug target discovery technology had become the powerful tool to discover the targets of drugs. Due to the “multi-component and multi-target” characteristics of traditional Chinese medicines (TCMs), the research on its targets and mechanism had been restricted. Based on potential of the label-free target discovery technology in the research of TCMs, this paper summarized the label-free target discovery technology and its application in TCMs research. It will provide a reference for the discovery of targets of TCMs and a new view for promoting the modernization of TCMs.
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Diabetic retinopathy （DR） is a common complication of diabetes， which causes a great threat to the health of human vision. Recent studies have shown that saponins， polysaccharides and flavonoids in Astragali Radix regulate phosphoinositide 3-kinase/protein kinase B/mammalian target of rapamycin pathway， silent information regulator 1/nuclear factor erythroid 2-related factor 2 pathway， B-cell lymphoma-2 and other signaling pathways by acting on nuclear factor-κB， hypoxia-inducible factor-1α， glial fibrillary acidic protein， glutamine synthetase， aldose reductase， multiple miRNA and other related targets， so as to exert anti- inflammatory， anti-microangiopathy， anti-neurodegenerative disease and anti-apoptosis， and then achieve the purpose of treating DR.
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Perilla frutescens is a widely used medicinal and edible plant with a rich chemical composition throughout its whole plant. The Chinese Pharmacopoeia categorizes P. frutescens leaves(Perillae Folium), seeds(Perillae Fructus), and stems(Perillae Caulis) as three distinct medicinal parts due to the differences in types and content of active components. Over 350 different bioactive compounds have been reported so far, including volatile oils, flavonoids, phenolic acids, triterpenes, sterols, and fatty acids. Due to the complexity of its chemical composition, P. frutescens exhibits diverse pharmacological effects, including antibacterial, anti-inflammatory, anti-allergic, antidepressant, and antitumor activities. While scholars have conducted a substantial amount of research on different parts of P. frutescens, including analysis of their chemical components and pharmacological mechanisms of action, there has yet to be a systematic comparison and summary of chemical components, pharmacological effects, and mechanisms of action. Therefore, this study overviewed the chemical composition and structures of Perillae Folium, Perillae Fructus, and Perillae Caulis, and summarized the pharmacological effects and mechanisms of P. frutescens to provide a reference for better development and utilization of this valuable plant.
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Perilla frutescens/chemistry , Plant Extracts/pharmacology , Seeds/chemistry , Fruit/chemistry , Oils, Volatile/analysis , Plant Leaves/chemistryABSTRACT
Idiopathic pulmonary fibrosis （IPF） is a progressive interstitial lung disease with unknown etiology and poor prognosis. At present， there are few antifibrotic drugs， which have limited efficacy and cause diverse side effects in the treatment of IPF， failing to meet the clinical needs. Therefore， it is urgent to develop more safe and effective drugs to treat IPF. Traditional Chinese medicine （TCM） has garnered increasing attention in recent years in the treatment of IPF due to its unique advantages. Increasing studies have shown that Chinese medicines have remarkable therapeutic effects on IPF and broad application prospects. However， the unclear material basis and mechanism in treating IPF hinders the modernization， internationalization， and clinical application of Chinese medicines. Therefore， it is essential to decipher the mechanism of the active components in Chinese medicines in treating IPF， which has gradually become a hot spot in the research on IPF. Increasing research results have demonstrated that anti-inflammation， anti-oxidation， inhibition of epithelial-mesenchymal transition are involved in the treatment of IPF with these active components， whereas the systematic research and summary remain to be carried out. By reviewing the articles about the treatment of IPF with the active components in Chinese medicines in recent years， this paper summarizes the mechanism and experimental studies and puts forward the existing problems in the research on the mechanism， aiming to provide references for the further basic research on IPF and the development of targerted drugs.
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Rheumatoid arthritis （RA） is a systemic chronic auto-inflammatory disease， characterized by infiltration of inflammatory cells， pannus formation， articular cartilage destruction， and bone matrix destruction. Therefore， improving articular cartilage destruction has an important impact on the treatment of RA. Chinese medicine has a good application effect in improving cartilage destruction of RA due to its characteristics of multiple components， multiple targets， high activity and low side effects. Based on this， the author reviewed relevant literature to summarize the relevant research and mechanism of Chinese medicine and its active components in improving RA cartilage destruction. The results showed that Chinese medicine and its active components can improve RA cartilage destruction by regulating inflammatory factors， phosphatidylinositol 3-kinase/protein kinase B， Wnt/β- catenin， nuclear factor-κB， mitogen-activated protein kinase， Janus kinase 2/signal transduction and activator of transcription 3/ vascular endothelial growth factor， microRNAs， fibroblastic synovial cells.
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Chronic obstructive pulmonary disease （COPD） is a common and frequently-occurring disease of the respiratory system， characterized by persistent respiratory symptoms and airflow restriction， which is prone to attack repeatedly and affect patients' quality of life seriously. At present， the combination of bronchodilators and inhaled corticosteroids is commonly used in clinic. Although these drugs can alleviate the symptoms of COPD patients， there are certain limitations of the difficulty in controlling the course of the disease effectively and reversing the decline of patients' lung function. Therefore， searching for safer and more effective therapeutic drugs has become a hot research topic nowadays. Traditional Chinese medicine （TCM） has remarkable curative effects and advantages in the prevention and therapy of COPD recently. Based on the increasing research and application of the active components of TCM in the therapy of COPD， studies on their pharmacodynamic mechanism are also more in depth. More and more studies have found that the active components of TCM can treat COPD patients effectively， and the mechanism involved mainly includes the anti-inflammatory， the antioxidant， and the inhibition of apoptosis. By searching and screening the domestic and foreign literatures on the treatment of COPD with the active components of TCM in recent years， the active components of TCM including flavonoids， terpenoids， phenols and saponins have been studied as the research objects， and their effects in improving the pulmonary function and oxidative stress， relieving inflammation and inhibiting apoptosis are expounded. Besides， the mechanism of action， signaling pathways and index molecules have been emphatically summarized， in order to provide the ideas for the clinical therapy and the basic research of COPD.
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TCM formulae are the important guidances for clinical application of traditional Chinese medicines, which follow the principles of diagnosis and treatment in TCM. Elucidating the bio-active components of TCM formulae is the key to the modernization and internationalization of traditional Chinese medicines. With the rapid development of modern instruments and technology, many new theories, methods and strategies are emerging, which upgrade the research of TCM formulae into a higher level. Only when the medicinal efficacy, bio-active components, function mechanism of TCM formulae are understood, we can guarantee TCM safety and quality control. In this paper, we summarized the latest modern research thoughts and methods on bio-active components of TCM formulae including formula decomposition study, serum pharmacology and serum pharmacochemistry, association analysis, biochromatography, network pharmacology, metabolomics and proteomics, so as to provide reference for the research and development of TCM in the future.
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Biological Products , Drugs, Chinese Herbal/chemistry , Medicine, Chinese Traditional/methods , Metabolomics , ProteomicsABSTRACT
The effective material basis of Chinese medicine is the key and difficult point in the quality control and modernization research of Chinese medicine. With the increasing application of pharmacophore-based virtual screening in computer-aided drug design, it is possible to employ this technology in the modernization of Chinese medicine. Based on the systematic research method of the pharmacophore model, the present study systematically reviewed the pharmacophore-based technologies and strategies in the identification of active components in Chinese medicine.
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Drug Design , Drugs, Chinese Herbal , Medicine, Chinese TraditionalABSTRACT
This study aims to explore the active components and molecular mechanism of Shenmai Injection in the treatment of atrial fibrillation(AF) based on the application of network pharmacology and molecular docking technology. The chemical components of single herbs of Shenmai Injection were collected from TCMSP and TCMID, with the standard chemical name and PubChem CID(referred to as CID) obtained from PubChem database. The active components were screened using SwissADME, and their targets were predicted using SwissTargetPrediction. Targets related to AF treatment were identified using GeneCards, OMIM, and other databases. Venn diagram was constructed using Venny 2.1 to obtain the intersection targets. The single herb-active component-potential target network was constructed using Cytoscape, and the clusterProfiler R function package was used to perform the gene ontology(GO) and Kyoto encyclopedia of genes and genomes(KEGG) pathway enrichment. The protein-protein interaction(PPI) network of intersection targets was generated based on the STRING database. The hub target protein was identified by visualization using Cytoscape, and then docked to its reverse-selected active components. The analysis showed that there were 65 active components with 681 corresponding targets in Shenmai Injection, 2 798 targets related to AF treatment, and 235 intersection targets involving 2 549 GO functions and 153 KEGG pathways. Finally, hub target proteins, including RAC-alpha serine/threonine-protein kinase(AKT1), phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha(PIK3 CA), and estrogen receptor 1(ESR1), were screened out by PPI network visualization. The molecular docking was performed for 39 active components screened out in reverse, among which 30 active components de-monstrated high affinity. Among them, homoisoflavanoids CID 10871974, CID 5319742, and CID 10361149 had stronger affinity docking with AKT1. This study preliminarily indicates that Shenmai Injection treats AF through multiple components, multiple targets, and multiple pathways. Homoisoflavonoids of Ophiopogon japonicus are its important active components, which target AKT1 to regulate metabolism, inflammation, and apoptosis in AF treatment.
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Humans , Atrial Fibrillation/drug therapy , Drug Combinations , Drugs, Chinese Herbal , Medicine, Chinese Traditional , Molecular Docking SimulationABSTRACT
Isatidis Radix is the dried root of the Isatis indigotica, with pharmacological effects such as heat-clearing and detoxification, cooling blood and pharyngeal relief, antibacterial and anti-inflammatory effects. It is often used clinically to prevent and treat influenza and other diseases. In this paper, relevant domestic and foreign literatures in recent years were summarized, and it was found that Isatidis Radix lignans, indole alkaloids, polysaccharides, etc. were the main active components against influenza virus. Then its pharmacological effects and the mechanism of action were reviewed, providing a basis for in-depth research on the antiviral effect of Isatidis Radix.
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Antiviral Agents/pharmacology , Drugs, Chinese Herbal , Isatis , Orthomyxoviridae , Plant Roots , PolysaccharidesABSTRACT
OBJECTIVE：To establish a method for online detection of antioxidant active components in Glycyrrhiza uroalensis decoction pieces ，and to identify it. METHODS ：The free radical scavenging rate of 1，1-diphenyl-2-trinitrobenzene hydrazine （DPPH）was determined to evaluate the antioxidant activity of G. uralensis decoction pieces. HPLC-UV-DPPH method was used to screen the anti oxidant active components of G. uralensis decoction pieces. HPLC-TOF/MS was used to obtain mass spectrum data and Qualitive Analyst B 06.00 Build 6.0.633.0 software was used to analyze data. Through contrast analysis of UV absorption spectrum，online chromatogram ，mass spectrum information of G. uralensis and the retention time of each compound ，accurate molecular weight ，antioxidant active components were identified by referring to relevant literature. Validation test was also conducted. RESULTS ：DPPH free radical scavenging rate in 8 batches of G. uralensis decoction pieces ranged 55.71％-60.17％. Seven antioxidative active compounds ，including avolomotor ，8-isopentenyl naringin ，yellow lupulin weitone ，isoflavone B ，3′， 4′-dimethoxy3-hydroxy-6-methyl flavone ，glycyrrhizin E and glycyrrhizin H ，could be screened from G. uralensis decoction pieces. After validation ，the peak area of inverted peak generated by online reaction was positively correlated with DPPH free radical scavenging rate. CONCLUSIONS ：Established method is simple and accurate ，and can be used to quickly screen and identify the main antioxidant components of G. uralensis decoction pieces ；the peak area of inverted peak can be used to evaluate the antioxidant active components of G. uralensis decoction pieces.
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Tumor, especially malignant tumor has become one of the major diseases, a serious threat to the health of people around the world. Modern clinical practice shows that the natural active products extracted from traditional Chinese medicine, marine medicine and other natural drugs, such as terpenes, alkaloids, polysaccharides, volatile oils and peptides, can effectively inhibit the growth of tumor cells. In this paper, the active components of natural antitumor products in recent years were summarized and their related mechanism was elucidated, so as to provide theoretical basis for the further development of natural antitumor drugs.
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Three different origins of Anoectochilus roburghii were used as experimental materials to study the effect of three different substrate( peat soil-river sand-peanut shell) radio on survival rate,plant height,stem diameter,plant fresh weight,root number,the longest root length,root diameter,and the contents of polysaccharide,flavonoids,and polyphenol. The results showed that when the substrate ratio was 4 ∶2 ∶2,the survival rate of A. roburghii from different origins was the highest,and the plant height,stem diameter,plant fresh weight,the longest root length and root diameter were also the largest. The cultivation substrate had no significant effect on the polysaccharide content of A. roxburghii and A. formosanus. When the substrate ratio was 4 ∶ 2 ∶ 2,the polysaccharide content of A.chapaensis was significantly lower than that of the other two combinations. When the substrate ratio was 4 ∶2 ∶1,the flavonoid content of A. formosanus was higher than that of the other two combinations. When the substrate ratio was 4 ∶2 ∶2,A. formosanus and A. chapaensis had higher polyphenol content.
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Flavonoids , Orchidaceae , Chemistry , Polyphenols , PolysaccharidesABSTRACT
Objective: To explore the active compounds and integrative mechanism of Scutellaria barbata in treatment of cancer by using network pharmacology. Methods: The active components were screened by five rules of durability. The target proteins of S. barbata were obtained by molecular docking. The main diseases related to S. barbata were obtained by Comparative Toxicogenomics Database (CTD). Then, the compound-target-disease interaction network was built using cytoscape 3.40. After protein-protein interaction analysis, Biological Information Annotation Databases (DAVID) was used to analyze the biological metabolic pathway of target proteins. Results: A total of 72 compounds from S. barbata acted with more than 14 cancer-related targets, and diterpenoids including scutelinquninne D, barbatellarine E, and scutebarbatines A were the main active molecules of S. barbata. Network analysis showed that the active compounds of S. barbata can regulate VEGF signaling pathway, Fc epsilon RI signaling pathway, and FoxO signaling pathway through acting with the key targets protein, such as protein tyrosine phosphatase 1B (PTP1B), carbonic anhydrase 2 (CA2), cyclic protein dependent kinases 2 (CDK2), retinoic acid α receptor (RXRA) and so on. Finally, S. barbata regulated the process of inflammation and tumor angiogenesis for its anticancer effect. Conclusion: S. barbata can show the multi-target and multi-pathway synergistic antitumor activity through anti-inflammation and inhibiting tumor angiogenesis.
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In recent years,with the rapid development of life sciences,changes on the understanding and requirements for innovative drugs of Chinese materia medica (CMM) from the drug approval authorities have been made.In this paper,the discovery,research and development (R & D) approaches for innovative drugs of CMM under new situations were summarized and introduced in details from five aspects as follows.The discovery of innovative drugs from active components of CMMs,active fractions of CMMs and their compound preparations,famous classic prescription,clinically effective prescriptions as well as the famous Chinese patent drugs.This paper puts forward some new ideas for the pharmaceutical researches of innovative drugs of CMM,including the production process,chemical components,quality study,quality standard and stability.This paper provided references for the discovery,R & D of CMM.
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Aim To observe the effects of active com-ponent of Radix Isatidis ( ACRI ) on anti-anoxia and anti-fatigue in mice and investigate its possible mecha-nism. Methods Based on the weights, the mice were randomly divided into 5 groups: blank control group, ACRI 25, 50 and 100 mg·kg-1 groups, positive drug ( American ginseng liquid) control group 3 mL·kg-1 . Drugs were administered to the mice for about 14 con-secutive days, and during the experiment general situa-tions of mice were observed. The experiment of bearing hypoxia at normal pressure and the experiment of swim-ming while weight-bearing were conducted to study the effect of ACRI on anti-anoxia and anti-fatigue in mice. Then the superoxide dismutase ( SOD ) activities, the content of maleic dialdehyde ( MDA ) of mice serum and liver and blood urea nitrogen, blood lactic acid, liver glycogen were detected, in order to investigate its mechanism. Results ACRI decreased the growth rate of body weight in mice significantly, obviously pro-longed the survival time of anoxic mice at normal pres-sure and the swimming time of loaded mice, enhanced the SOD activities of mice blood and liver, decreased the MDA content of mice blood and liver, increased the content of liver glycogen, and decreased the blood urea nitrogen and blood lactic acid in mice after swim-ming. Conclusion ACRI has the anti-anoxia and anti-fatigue functions.
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OBJECTIVE:To study the purification technology of 4 active components from Tripterygium wilfordii by macropo-rous resin. METHODS:The purification abilities of nine macroporous resins(ADS-5,ADS-8,HPD100,HPD300,HPD400, HPD450,HPD700,HPD722 and HPD750) were studied with the adsorption and desorption rates of triptolide,wilforlide,trip-tonide and tripterine as the index by static adsorption and desorption experiments for 4 active components from T. wilfordii,so as to screen optimal macroporous resins. Using transfer rate of active component as index,single factor test was used to investigate the effects of different sampling method,ratio of mixing sample to total resin quantity,ratio of resin to medicinal material,cleaning so-lution(type,amount and cleaning flow rate),diameter- height ratio of resins,eluant(volume,flow rate)on adsorption,so as to determine the optimal elution technology;validation test was also conducted. RESULTS:HPD722 macroporous resin was chosen as adsorption resin;ratio of diameter to height was 1∶10,resin-medicinal material ratio was 1∶2,and ratio of mixing sample to to-tal resin quantity was 1∶10;wet column installing and mixing resin for sample loading were adopted. The macroporous resin was washed with 12 BV 20%ethanol at the rate of 12 BV/h,and then eluted with 12 BV 95%ethanol at the rate of 6 BV/h. The verifi-cation test results showed that the total transfer rate of 4 active components from T. wilfordii was more than 90%(RSD=0.99%, n=3). CONCLUSIONS:The optimized technology is stable and feasible,and suitable for the purification of 4 active components from T. wilfordii.
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Tissue factor (TF), also called tissue thromboplastin, is the principal initiator of physiological blood coagulation and hemostasis and pathological thrombosis, and plays an important role in the formation of various diseases in atherosclerosis, systemic inflammation, angor pectoris, disseminated intravascular coagulation, and tumor angiogenesis and metastasis. Looking for the targets to TF anticoagulant, antithrombotic drug has important theoretical and realistic significance. This summary outlines the research progress of the active components in Chinese materia medica with modulating effects on expression of tissue factor in thrombosis in recent years.
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To explore the anti-atherosclerotic mechanism of active component compatibility of Danshen and Shanzha (SC121) based on network pharmacology and in vitro research validation with cell model. On one hand, according to the chemical structures and pharmacological activities of the compounds reported in Danshen and Shanzha, 5 compounds, i.e., salvianolic acid B, tanshinone ⅡA, tanshinol, epicatechin and procyanidin B2 were chosen and used for network pharmacology analysis. Then the TCMSP（http://lsp.nwsuaf.edu.cn/tcmsp.php）was used for finding the network targets for 5 compounds from SC121. The signaling pathway associated with cardiovascular disease was analyzed by KEGG mapping, the biological process associated with cardiovascular disease was analyzed by Uniprot. And, the mechanism of SC121 was predicted by network pharmacology. In vitro cell model was subsequently performed for validation. HUVEC and RAW264.7 cell injuries and foam cell formation were constructed by ox-LDL, and the intervention effects of SC121 were assayed. The result showed that SC121 not only alleviated the damage of HUVEC and RAW264.7, lowered the ROS level, but also decreased the area of foam cell in a dose-dependent manner, which indicated that SC121 could inhibit the damage of endothelial cells and lower the oxidative stress. The experimental data validated the prediction of network pharmacology, and elucidated the mechanism of SC121's effect on AS.