Advances in Research Methods of Pharmacodynamic Substances in Traditional Chinese Medicines and Their Application in the Teaching of Traditional Chinese Medicine Analysi

With the continuous progress of science and technology,the research methods of pharmacodynamic substances in traditional Chinese medicine are developing,and the application of these methods in teaching is becoming more and more extensive.By introducing these research methods into the classroom,teachers can help students to deeply understand the nature and mechanism of action of pharmacodynamic substances in traditional Chinese medicine,and improve their interest in and knowledge of traditional Chinese medicine.This paper introduces the definition of pharmacodynamic substances in traditional Chinese medicine,research methods,and their application in the teaching of traditional Chinese medicine analysis.

Applications of HPLC/MS in the analysis of traditional Chinese medicines

In China, traditional Chinese medicines （TCMs） have been used in clinical applications for thousands of years. The successful hyphenation of high-performance liquid chromatography （HPLC） and mass spectrometry （MS） has been applied widely in TCMs and biological samples analysis. Undoubtedly, HPLC/MS technique has facilitated the understanding of the treatment mechanism of TCMs. We reviewed more than 350 published papers within the last 5 years on HPLC/MS in the analysis of TCMs. The present review focused on the applications of HPLC/MS in the component analysis, metabolites analysis, and pharmacokinetics of TCMs etc. 50% of the literature is related to the component analysis of TCMs, which show that this field is the most popular type of research. In the metabolites analysis, HPLC coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry has been demonstrated to be the powerful tool for the characterization of structural features and fragmentation behavior patterns. This paper presented a brief overview of the applications of HPLC/MS in the analysis of TCMs. HPLC/MS in the fingerprint analysis is reviewed elsewhere.

Rapid bioluminescence assay for monitoring rat CES1 activity and its alteration by traditional Chinese medicines

In traditional Chinese medicine herbs(TCM),including Radix Salviae Miltiorrhizae(Danshen),Radix Puerariae Lobatae(Gegen),Radix Angelicae Sinensis(Danggui),and Rhizoma Chuanxiong(Chuanxiong)are widely used for the prevention and treatment of cardiovascular diseases and also often co-administered with Western drugs as a part of integrative medicine practice.Carboxylesterase 1(CES1)plays a pivotal role in the metabolisms of pro-drugs,Since(S)-2-(2-(6-dimethylamino)-benzothiazole)-4,5-dihydrothiazole-4-carboxylate(NLMe)has recently been identified by us as a selective CES1 bioluminescent sensor,we developed a rapid method using this substrate for the direct measurement of CES1 activity in rats.This bioluminescence assay was applied to determine CES1 activity in rat tissues after a two-week oral administration of each of the four herbs noted above.The results demonstrated the presence of CES1 enzyme in rat blood and all tested tissues with much higher enzyme activity in the blood,liver,kidney and heart than that in the small intestine,spleen,lung,pancreas,brain and stomach.In addition,the four herbs showed tissue-specific effects on rat CES1 expression.Based on the CES1 biodistribution and its changes after treatment in rats,the possibility that Danshen,Gegen and Danggui might alter CES1 activities in human blood and kidney should be considered.In summary,a selective and sensitive bioluminescence assay was developed to rapidly evaluate CES1 activity and the effects of orally administered TCMs in rats.

Screening of new non-nucleoside reverse transcriptase inhibitors of HIV-1 based on traditional Chinese medicines database

HIV- 1 RT is an important target for the treatment of AIDS. There are two major classes of antiviral agents that inhibit HIV- 1 RT have been identified, nucleoside RT inhibitors （NRTIs） and non-nucleoside RT inhibitors （NNRTIs）. In this report, a noval class of non-nucleoside compound with potential RT inhibitory activity were found from the traditional Chinese medicines database （TCMD） using a combination of virtual screening, docking, molecular dynamic simulations, where results were ranked by scoring function of the docking tool. The result indicates that M4753 （a compound derived from TCMD） has not only the lowest bonding energy but also the best match in geometric conformation with the forthcoming NNRTIs. Accordingly M4753 might possibly become a promising lead compound of NNRTIs for AIDS therapy.

Selectivity of New β-Cyclodextrin Derivatives as CGC Stationary Phases and Application for the Analysis of Volatile Compounds in Traditional Chinese Medicines

New cyclodextrin derivatives （CDs）, heptakis（2, 6-di- O-methyl-3- O-methoxymethyl）-β-CD （ Ⅰ ） and heptakis（2, 3, 6-tri-O-methoxymethyl）-β-CD （ Ⅱ ）, were investigated for their chromatographic performance as stationary phases for capillary gas chromatography （CGC）. Both of the CDs exhibited good selectivity and satisfactory separation for test mixtures and aromatic positional isomers, and volatile compounds from Ligusticurn chuanxiong Hort. Additionally, the selectivity and elution orders of major compounds were compared with a well-recognized commercial column on the basis of the results by gas chromatography-mass spectrometry （GC-MS）. The present work demonstrates the good selectivity of the two new CDs and can be used as GC stationary phases for the separation of positional isomers and analytes in complex samples.

Advances in Research of Toxic Traditional Chinese Medicines in the Treatment of Malignant Tumors

Combating poison with poison is an important method of traditional Chinese medicine to treat malignant tumors.This study reviews the experimental research on anti-tumor effects of toxic traditional Chinese medicines in recent years.It summarizes the action mechanism of toxic traditional Chinese medicines for the treatment of malignant tumors,including:inhibiting tumor cell proliferation and angiogenesis,inducing tumor cell apoptosis and differentiation,reversing tumor cell multidrug resistance(MDR),inhibiting tumor cell invasion and metastasis,and enhancing the body's immune functions.Finally,it discusses the research and development prospects of toxic traditional Chinese medicines as new anti-tumor drugs.

Establish a Three-dimensional Fluorescent Fingerprint Database of Traditional Chinese Medicines

Objective:To set up a database of three-dimensional fluorescence spectra of traditional Chinese medicines,Screening of medicinal materials by three-dimensional fluorescence spectroscopy,Methods:The paper Summarizes the three-dimensional fluorescence fingerprints,screens medicinal materials on basis of verifying the three-dimensional fluorescence spectra of the reference crude herbs of the national standard Chinese medicines,and combines with visual basic6.0 and microsoft access 2003 technology system to construct a three-dimensional fluorescence fingerprint database of TCMs.Results:the identification and quality control of traditional Chinese medicines(TCMs)was accuately and swiftly achieved.Conclusion:The relevant analysis on the operating system of database and the three-dimensional fluorescence spectrum database of TCMs indicates that this operating system can provide convenient channels for the inspection,verification and quality control of TCMs.

Status and Development Trend of Evaluation of Post-Marketing Traditional Chinese Medicines in China

Evaluation of traditional Chinese medicines after the market has achieved fruitful results after years of development.The real-world research concept has been first proposed by Chief Researcher Xie Yanming in 2010 and to 2020 with the approval of the National Medical Products Administration to use real-world evidence to support drug development and review in 2020.Real-world data application and transformation continue to cause heated discussions in the industry.Real-world research concepts have been added new motivation into the evaluation of Chinese medicines after they are marketed.The development of the Chinese patent medicine industry is facing unprecedented opportunities and challenges.

Effects of 105 traditional Chinese medicines on the detection ofβ-agonists in medicine extracts and swine urine based on colloidal gold immunochromatographic assay

Colloidal gold immunochromatographic assay(CGIA)is commonly used for the on-site detection ofβ-agonists that are sometimes used illegally as feed additives in swine diets.However,few studies have evaluated the causes of false-positive results that sometimes occur when applying CGIA in agricultural settings.In this study,we investigated if this false-positive phenomenon is related to the addition of certain traditional Chinese medicines(TCMs)to swine feed.We established and verified an extraction method for TCMs,and then applied CGIA to detectβ-agonists in the extracts of 105 TCMs and in the urine of swine dosed with TCMs,respectively.Liquid chromatography-tandem mass spectrometry was used to validate the results of the urine samples tested positive forβ-agonists using CGIA.The results were also verified using TCMs and colloidal gold test strips produced by different manufacturers.The extracts of Citri Reticulatae Pericarpium Viride,Citri Reticulatae Pericarpium,Magnoliae Officinalis Cortex,Chaenomelis Fructus,and Rhodiolae Crenulatae Radix Et Rhizoma were tested positive forβ-agonists.Meanwhile,the addition of Citri Reticulatae Pericarpium Viride and Citri Reticulatae Pericarpium to swine feed resulted in false-positive results forβ-agonists in swine urine.The results provide a new way to explain false-positive CGIA results and provide valuable information for livestock feeding programs.

Mechanisms of traditional Chinese medicines in the treatment of allergic rhinitis using a network biology approach

Objective:To systematically explore the effect and mechanism of traditional Chinese herbs in the treatment of allergic rhinitis.Methods:Magnolia flower,xanthium fruit,astragalus root,paniculate cynanchum,scutellaria root,cicada molting,stephania root,small centipeda herb,and licorice root as traditional Chinese herbs are widely used to treat allergic rhinitis.With multiple database integration and entity grammar systems,a molecular interaction network of traditional Chinese herbs for treating allergic rhinitis was established.Bioinformatics approaches were adopted to integrate relevant data and biological information by multiple databases.Molecular interaction network of Chinese herbs for treating allergic rhinitis was constructed based on entity grammar systems model.The network was then used for elucidating the antiallergic rhinitis mechanism of the Chinese herbs on the molecular level.The subnetworks were also extracted to explicitly display the pathway and targets where effective components acted on.Results:Traditional Chinese herbs could influence various pathological aspects in allergic rhinitis including the production of pro-inflammatory substances,such as histamine and cytokine interleukin-4(IL-4),interleukin-13(IL-13),lowering immunoglobulin E(IgE)level or blocking antigen binding,altering the biological processes of IgE,modulating the balance of T helper(Th)or other cells by cell proliferation and differentiation,mediating cellecell signaling and second-messenger-mediated signaling,stabilizing the cell membrane,and affecting regulation of cellular defense response.Conclusion:The research theoretically confirms the mechanism of anti-allergic rhinitis by traditional Chinese herbs,provides important fundamental research information for treatment of allergic rhinitis,and may serve as a reference for new drug development and effective ingredients of compatibility.

Comparative study on the anti-tuberculous effect and mechanism of the traditional Chinese medicines NiuBeiXiao He extract and JieHeWan

Background:The traditional Chinese medicine NiuBeiXiaoHe(NBXH)extract and Chinese medicine preparation JieHeWan(JHW)exhibit anti-tuberculosis(TB)effects.The anti-TB effect of NBXH was compared with that of JHW to elucidate the mechanism of action of NBXH.Methods:BALB/c mice aged 6-8 weeks were randomly divided into a normal control group,TB model group,JHW treatment group,and NBXH treatment group.After 3 and 13 weeks of treatment,the therapeutic effect in each group was evaluated by comparing lung histopathology,lung and liver colony counts,the number of spots representing effector T cells secreting IFN-γin an enzyme-linked immunospot assay(ELISPOT),and the levels of Th1,Th2,and Th17 cytokines,which were measured by a cytometric bead array(CBA).Mouse RNA samples were subjected to transcriptome sequencing.Results:After 13 weeks of treatment,the mean histopathological lesion area of the NBXH group was significantly smaller than that of the TB model group(P<0.05).Compared with those in the TB model group,the lung colony counts in the JHW and NBXH groups were significantly decreased(P<0.05),and the IL-2 and IL-4 levels in the NBXH group were significantly increased(P<0.05).NBXH partly restored significant changes in gene expression caused by Mycobacterium tuberculosis(M.tuberculosis)infection.According to GO and KEGG analyses,the changes in biological process(BP),cell composition(CC)and molecular function(MF)terms and in signaling pathways caused by NBXH and JHW treatment were not completely consistent,but they were mainly related to the immune response and inflammatory response in the mouse TB model.Conclusions:NBXH had therapeutic effects similar to those of JHW in improving lung histopathology,reducing lung colony counts,and regulating the levels of cytokines.NBXH restored significant changes in gene expression and repaired cell damage caused by M.tuberculosis infection by regulating immune-related pathways,which clarified the mechanism of action of NBXH.

Computer Handling of Chemical and Biological Data of Traditional Chinese Medicines

A specialty database has been established at The Hong Kong University of Science and Technology to handle the chemical and biological data of medicinal plants and other natural products from scientific literatures. Designed as a relational system capable of analyzing, comparing, and correlating data, the system can retrieve information in assimilated tabular formats. The database can provide information supports to researchers in the fields of medicinal chemistry, biochemistry, pharmacology, botany and other disciplines of natural products research.

Determination of components in traditional Chinese medicines associated with promoting or inhibiting urinary stone formation

Objective:To measure oxalate,calcium,and sodium contents of traditional Chinese medicines(TCMs)that are commonly used to prevent and dissolve urinary stones to exclude the possibility that long-term use of such medicines promotes stone formation.The second objective was to measure citrate,potassium,and magnesium contents in the same medicines to provide possible clues about the mechanisms of prevention and dissolution of urinary stones by TCMs.Methods:Ten of the most commonly-used TCMs for preventing and dissolving urinary stones were chosen and subjected to ion chromatography(IC)to measure water-soluble and total oxalate and citrate contents.Inductively coupled plasma atomic emission spectrometry(ICPAES)was used to measure calcium,potassium,magnesium,and sodium contents in a water extract and in digestion liquid.Results:Average contents of water-soluble oxalate,calcium,and sodium in the water extract were 41.92,84.32,and 22.82 mg/100 g,respectively,far below the normal dietary intake of adults in China.The average contents of citrate and magnesium in water extracts were 268.99 and 66.65 mg/100 g,respectively,below the recommended intake for adults.These ion contents are therefore insufficient to inhibit the formation of urinary stones.The average content of potassium in the water extract was 867.71 mg/100 g,which was relatively abundant,so taking the prescription used in this experimental protocol can increase the body’s potassium content to some extent.Conclusions:Long-term use of TCMs would not increase the risk of urinary stone formation.The potassium content in TCMs is high,which is one possible reason for the prevention of urinary stones by TCMs.

An Overview on The Antiviral Traditional Chinese Medicines

Traditional Chinese Medicine(TCM)owns a long history of fighting viral diseases.TCM has acumulated a large amount of clinical experiences to treat viral diseases.Inner Canon of the Yellow Emperor(Huangdi Neijing,300 BC)mentioned:When the five epidemics arrive,they are all infected by the same disease,regardless of their size,and have similar symptoms.Treatise on Cold Pathogenic Diseases(Shanghan Lun,220 AD)described the plague sweeping across the country and killed almost all people.And,numerous prescriptions in Treatise on Cold Pathogenic Diseases(Shanghan Lun)were used until today.Pestilence Theory(Wenyi Lun,1642)written by Wu Youxing differed from Treatise on Cold Pathogenic Diseases in its analysis of the characteristics of epidemics and therapeutic methods.A large number of classical antiviral traditional Chinese medicines and recipes have been accumulated.On the ground of traditional Chinese medicine,modern scientific methods were used to screen out a large number of antiviral traditional Chinese medicines to find new antiviral contents or form new recipes.Despite the disputation around the researchers,TCM provided effective therapeutics in the fight against the Coronavirus Disease(2019 COVID-19)epidemic in China.It demonstrated the potential advantages of Chinese medicines as antiviral medicines with broad research value and prospects.

Gain deeper insights into traditional Chinese medicines using multidimensional chromatography combined with chemometric approaches

Traditional Chinese medicines(TCMs)possess a rich historical background,unique theoretical framework,remarkable therapeutic efficacy,and abundant resources.However,the modernization and internationalization of TCMs have faced significant obstacles due to their diverse ingredients and unknown mechanisms.To gain deeper insights into the phytochemicals and ensure the quality control of TCMs,there is an urgent need to enhance analytical techniques.Currently,two-dimensional(2D)chromatography,which incorporates two independent separation mechanisms,demonstrates superior separation capabilities compared to the traditional one-dimensional(1D)separation system when analyzing TCMs samples.Over the past decade,new techniques have been continuously developed to gain actionable insights from complex samples.This review presents the recent advancements in the application of multidimensional chromatography for the quality evaluation of TCMs,encompassing 2D-gas chromatography(GC),2D-liquid chromatography(LC),as well as emerging three-dimensional(3D)-GC,3D-LC,and their associated data-processing approaches.These studies highlight the promising potential of multidimensional chromatographic separation for future phytochemical analysis.Nevertheless,the increased separation capability has resulted in higher-order data sets and greater demands for data-processing tools.Considering that multidimensional chromatography is still a relatively nascent research field,further hardware enhancements and the implementation of chemometric methods are necessary to foster its robust development.

Traditional Chinese medicines derived natural inhibitors of ferroptosis on ischemic stroke

Ischemic stroke(IS)is a globally prevalent cerebrovascular disorder resulting from cerebral vessel occlusion,leading to significant morbidity and mortality.The intricate pathological mechanisms underlying IS complicate the development of effective therapeutic interventions.Ferroptosis,a form of programmed cell death(PCD)characterized by iron overload and accumulation of lipid peroxidation products,has been increasingly recognized as a key contributor to IS pathology.Traditional Chinese medicines(TCMs)have long been utilized in the management of IS,prompting extensive research into their potential as sources of natural ferroptosis inhibitors.This review investigates the critical role of ferroptosis in IS and provides a comprehensive analysis of current research on natural ferroptosis inhibitors identified in TCMs,aiming to lay a theoretical groundwork for the development of innovative anti-IS therapies.

Effects and mechanisms of traditional Chinese medicines on functional dyspepsia: A review

Functional dyspepsia(FD) is a common and frequently occurring disease in clinic. With the infuence of environmental factors, social factors and dietary factors, the incidence rate of FD in the general population is yearly increasing. Traditional Chinese medicine has a long history and far-reaching infuence in the treatment of FD. It can prevent and treat FD in the form of multiple-components, targets and channels,with obvious effect and prominent advantages. This article starts with the common syndrome types of FD, and discusses the research progress of single Chinese medicine, effective ingredients and the mechanism of traditional Chinese medicines in treating FD, in order to provide a theoretical basis for the treatment of FD with traditional Chinese medicines.

Traditional Chinese medicines for non-small cell lung cancer: Therapies and mechanisms

The most common subtype of lung cancer is non-small cell lung cancer(NSCLC), which has a poor prognosis and seriously threatens the health of human beings. The multidisciplinary comprehensive treatment model has gradually become the mainstream of NSCLC treatment. Traditional Chinese medicine(TCM) can be used effectively either as an adjunctive therapy or alone throughout the NSCLC therapy,which has a significant impact on survival, quality of life, and reduction of toxicity. Therefore, this paper reviewed the theoretical basis, the latest clinical application, and combined treatment mechanisms in order to explore the advantage stage of TCM treatment and the synergistic therapeutic mechanisms.

The traditional Chinese medicines treat chronic heart failure and their main bioactive constituents and mechanisms

Chronic heart failure(CHF)is a severe public health problem with increasing morbidity and mortality,any treatment targeting a single session is insufficient to tackle this.CHF is characterized by reduced cardiac output resulting from neurohumoral dysregulation and cardiac remodeling,which might be related to oxidative stress,inflammation,endoplasmic reticulum stress,apoptosis,autophagy,mitochondrial function,and angiogenesis.These molecular mechanisms interact with each other through crosstalk.Historically,Chinese medicinal herbs have been widely applied in the treatment of CHF,and therapeutic effects of Chinese medicinal herbs and their ingredients have been scientifically confirmed over the past decades.Traditional Chinese medicine(TCM)with multiple components can confront the different pathogenesis of CHF through multiple targets.This review analyzes commonly used TCM patent drugs and TCM decoctions that are applicable to different stages of CHF based on clinical trials.Diverse bioactive ingredients in Chinese medicinal herbs have been found to treat CHF via multiple molecular mechanisms.This review comprehensively covers the key works on the effects and underlying mechanisms of TCM,herbal ingredients and synergistic effects of constituent compatibility in treating CHF,providing additional ideas to address this threat.

Network pharmacology approaches for research of Traditional Chinese Medicines

Pharmacodynamics material basis and effective mechanisms are the two main issues to decipher the mechnisms of action of Traditional Chinese medicines(TCMs)for the treatment of diseases.TCMs,in“multi-component,multi-target,multi-pathway”paradigm,show satisfactory clinical results in complex diseases.New ideas and methods are urgently needed to explain the complex interactions between TCMs and diseases.Network pharmacology(NP)provides a novel paradigm to uncover and visualize the underlying interaction networks of TCMs against multifactorial diseases.The development and application of NP has promoted the safety,efficacy,and mechanism investigations of TCMs,which then reinforces the credibility and popularity of TCMs.The current organcentricity of medicine and the“one disease-one target-one drug”dogma obstruct the understanding of complex diseases and the development of effective drugs.Therefore,more attentions should be paid to shift from“phenotype and symptom”to“endotype and cause”in understanding and redefining current diseases.In the past two decades,with the advent of advanced and intelligent technologies(such as metabolomics,proteomics,transcriptomics,single-cell omics,and artificial intelligence),NP has been improved and deeply implemented,and presented its great value and potential as the next drug-discovery paradigm.NP is developed to cure causal mechanisms instead of treating symptoms.This review briefly summarizes the recent research progress on NP application in TCMs for efficacy research,mechanism elucidation,target prediction,safety evaluation,drug repurposing,and drug design.