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In order to assure the safety and efficacy of the Chinese Medicines in Europe, the quality of TCM herbals should be guaranteed so that they can be freely imported in the European Union and other Western European Countries which are signatories of the European Pharmacopoeia Convention. Consequently, new Ph Eur TCM herbal drug Monographs should be elaborated, based on preexisting Monographs in the Chinese Pharmacopoeia (ChP) 2010. Such a program has been inaugurated in 2005 by the Ph Eur Groups of Experts 13 A and B (Phytochemistry). Since then good progress has been made, elaborating of about one third of the originally proposed 100 TCM herbals being identified as important monographs for the European Market. Taking into account the many challenges still laying ahead, the establishment of a specialized Working Party (WP) on TCM with specialists and experts from many EU Member States has been decided by the Ph Eur Commission in 2008 which is highly active ever since in the examination and elaboration of new TCM herbal drug monographs, primarily to assure the safety of the European patient and further to provide quality parameters extremely important for all registration and licensing procedures of the respective National Authorities all over Europe. This paper is a survey of results and difficulties obtained so far which has been encountered meanwhile in the elaboration process by the Ph Eur TCM WP of these monographs and will discuss these in detail. Moreover the role of Ph Eur TCM monographs in the European community is addressed.

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Artemisinin represents a showcase example not only for the activity of medicinal herbs deriving from traditional chinese medicine, but for phytotherapy in general. Its isolation from Sweet Wormwood (qinhao, Artemisia annua L.) represents the starting point for an unprecedent success story in the treatment of malaria worldwide. Beyond the therapeutic value against Plasmodium parasites, it turned out in recent years that the bioactivity of artemisinin is not restricted to malaria. We and others found that this sesquiterpenoid also exerts profound anticancer activity in vitro and in vivo. Artemisinin-type drugs exert multi-factorial cellular and molecular actions in cancer cells. Ferrous iron reacts with artemisinin, which leads to the formation of reactive oxygen species and ultimately to a plethora anticancer effects of artemisinins, e.g. expression of antioxidant response genes, cell cycle arrest (G1 as well as G2 phase arrests), DNA damage that is repaird by base excision repair, homogous recombination and non-homologous end-joining, as well as different modes of cell death (intrinsic and extrinsic apoptosis, autophagy, necrosis, necroptosis, oncosis, and ferroptosis). Furthermore, artemisinins inhibit neoangiogenesis in tumors. The signaling of major transcription factors (NF-κB, MYC/MAX, AP-1, CREBP, mTOR etc.) and signaling pathways are affected by artemisinins (e.g. Wnt/β-catenin pathway, AMPK pathway, metastatic pathways, nitric oxide signaling, and others). Several case reports on the compassionate use of artemisinins as well as clinical Phase I/II pilot studies indicate the clinical activity of artemisinins in veterinary and human cancer patients. Larger scale of Phase II and III clinical studies are required now to further develop artemisinin-type compounds as novel anticancer drugs. Abbreviations: ABCB6, ATP-binding Cassette Transporter B6; ABCG2, ATP Binding Cassette Transporter G2; AIF, Apoptosis Inducing Factor; AKT, V-Akt Murine Thymoma Viral Oncogene Homologue; AMPK, AMP-Activated Protein Kinase; Ang-1, Angiotensin 1; ARE, Arteether; ARM, Artemether; ARS, Artemisinin; ART, Artesunate; ATF4, Activating Transcription Factor 4; Bak, Bcl2 Antagonist/Killer 1; Bax, Bcl2-Associated X Protein, Pro-Apoptotic BH3-Only Bcl-2 Family Member; Bcl-2, B-cell CLL/lymphoma 2; Bcl-xL, B-cell CLL/Lymphoma-x Long; BCR/ABL, Breakpoint Cluster Region/Abl Proto-Oncogene; Bid, BH3-Interacting Domain Death Agonist; Bim, Pro-Apoptotic Bcl2- Family Member; BSO, Buthionine Sulfoximine; C/EBP β, CCAAT/Enhancer Binding Protein β; CAM, Chorioallantoic Membrane; CD, Cluster of Differentiation; CDC25B; CDK, Cyclin-Dependent Kinase; CHOP/DDIT, DNA Damage-Inducible Transcript; CIP1/WAF1, CDK-Interacting Protein 1/Wild-Type p53-Activated Fragment 1; c-JUN, Jun Proto-Oncogene; COX2, Cyclooxygenase 2; CREB, Cyclic ATP Responsive Element Binding Protein; DHA, Dihydroartesunate; DNA-PK, DNA-Dependent Protein Kinase; DR5, Death Receptor 5; E2F1, E2F Transcription Factor 1; EA, Ethacrynic Acid; EGFR, Epidermal Growth Factor Receptor; EMT, Epithelial to Mesenchymal Transition; EndoG, Endonuclease G; ERK, Extracellular Signal-Regulated Kinase; FAK, Focal Adhesion Kinase; FAS, Fas Cell Surface Death Receptor; Flt-1, Fms- Related Tyrosine Kinase 1; GADD153, Growth Arrest and DNA Damage-Inducible 153; GRP78, Glucose-Regulated Protein; GSK3 β, Glycogen Synthase Kinase 3 β; HIF-1α, Hypoxia-Inducible Factor-1 α; HPV39, Human Papilloma Virus 39; HR, Homologous Repair; hTERT, Human Telomerase Reverse Transcriptase; hTR, Human Telomerase; HUVEC, Human Umbilical Vein Endothelial Cells; IFN, Interferon; IL, Interleukin; IκBβ, Inhibitor of Kappa B β; JNK, c-Jun N-Terminal Kinase; KDR/flk-1, Kinase Insert Domain Receptor; LC3, Microtubule- Associated Protein 1 Light Chain 3; MAPK, Nitogen-Activated Protein Kinase; MAX, MYC-Associated Factor X; Mcl-1, Myeloid Cell Leukemia 1; MDM2, Mouse Double Minute 2 Homologue; MEK, also known as MAPKK, Mitogen-Activated Protein Kinase Kinase; MMP, Matrix Metalloproteinase; MPNST, Malignant Peripheral Nerve Sheath Tumor; mTOR, Mammalian Target of Rapamycin; MYC, Avian Myelomastosis Viral Oncogene Homologue; NAC, N-Acetyl Cysteine; NFκB, Nuclear Factor Kappa B; NHEJ, Non-Homologous End-Joining; NO, Nitric Oxide; NOXA, Also Known As PMA/P1; Phorbol-12-Myristate-13-Acetate-Induced Protein 1; PARK7, Parkinson Disease Protein 7, Protein Deglycase DJ-1; PARP, Poly ADP Ribose Polymerase; PCNA, Proliferating Cell Nuclear Antigen; PGE2, Prostaglandine E2; PI3-K, Phospoinositide-3 Kinase; PMA, Phorbol-12-Myristate-13-Acetate; RAF, Ras-Associated Factor Proto-Oncogene; RAS, Rat Sarcoma Viral Oncogene Homologue; RKIP, Raf-1 Kinase Inhibitor Protein; ROS, Reactive Oxygen Species, SMAC/DIABLO, IAP-Binding Mitochondrial Protein; TCTP, Translationally Controlled Tumor Protein; TF, Transferrin; TFRC, Transferrin Receptor 1 Gene; TGB1, Triple Gene Block Protein β, TGF-beta, Tumor Growth Factor β, TIMP, Tissue Inhibitor of Metalloproteinase, TNF-α, Tumor Necrosis Factor α, TOPO2 A, DNA Topoisomerase 2 α, TRAIL, Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand, Treg, Regulatory T Cells, VDAC2, Voltage-Dependent Anion Channel 2, VEGF, Vascular Endothelial Growth Factor, VEGFR, Vascular Endothelial Growth Factor Receptor, XIAP, X-Linked Inhibitor of Apoptosis, YY1, Yin Yang 1

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Metabolomics, an omic science in systems biology, is the comprehensive profiling of metabolic changes occurring in living systems and has been widely used in the modern research of traditional Chinese medicine (TCM). TCM is a complex medical science, which reflects rich philosophical dialectical thought, puts the human body into a large system for observation and keeps human in a healthy status. For TCM aroused great interest in the whole world, herbs and Chinese medical formulae (CMF) as treatment methods have also been widely attention. Metabolomics represents a powerful way that provides a dynamic drawing of the phenotype of biological systems via the research of endogenous metabolites, and its methods are similar to those of TCM. This review summarizes the advantages of metabolomics, highlight the key role of biomarkers for drug discovery and development of TCM.

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The interest of Western medicine in Traditional Chinese Medicine (TCM) as a source of drug leads/new drugs to treat diseases without available efficient therapies has been dramatically augmented in the last decades by the extensive work and the outstanding findings achieved within this kind of medicine. The practice of TCM over thousands of years has equipped scientists with substantial experience with hundreds of plants that led to the discovery of artemisinin (qinghaosu), which is extracted from the medicinal plant Artemisia annua L. (qinghao). The unexpected success of artemisinin in combating malaria has drawn strong attention from the scientific community towards TCM. Artemisinin was discovered by Youyou Tu in 1972. Since then, several novel pharmacological activities based on the well-known properties of the sesquiterpene lactone structure with the oxepane ring and an endoperoxide bridge have been unravelled. Beyond malaria, artemisinin and its derivatives (artemisinins) exert profound activities towards other protozoans (Leishmania, Trypanosoma, amoebas, Neospora caninum, and Eimeria tenella), trematodes (Schistosoma, liver flukes), and viruses (human cytomegalovirus, hepatitis B and C viruses). Less clear is the effect against bacteria and fungi. Based on the promising results of artemisinin and the first generation derivatives (artesunate, artemether, arteether), novel drug development strategies have been pursued. These included the synthesis of acetal- and non-acetal-type artemisinin dimeric molecules as well as developing nanotechnological approaches, e.g. artemisinin-based liposomes, niosomes, micelles, solid lipid nanocarriers, nanostructured lipid carriers, nanoparticles, fullerenes and nanotubes. The current review presents an overview on different aspects of artemisinins, including sources, chemistry, biological/pharmacological properties, types of infectious pathogens that are susceptible to artemisinins in vitro and in vivo, in addition to the advancement in their drug delivery systems utilizing pharmaceutical technology. It would be expected that different therapeutic strategies based on the second and third generation artemisinin derivatives and artemisinin-based drug technologies would be available in the near future to treat specific infectious diseases. Abbreviations: ARM: Artemether; ARM-LNP: Artemether-loaded lipid nanoparticles; ART: Artemisinin; ACT: Artemisinin-based combination therapies; AC-PL: Artemisinin-curcumin-loaded PEGylated liposomes; ADPs: Artemisinin dimer piperazine derivatives; A-CL: Artemisinin-loaded conventional liposomes, artemisinin-curcumin-loaded; AST: Artesunate; BBB: Blood-brain barrier; AC-CL: Conventional liposomes; A-PL: artemisinin-loaded PEGylated liposomes; DHA: Dihydroartemisinin; %EE: Entrapment efficiency; GNO: Ground nut oil; kDNA: Kinetoplast; LNs: Lipid nanospheres; NPs: Liposomal nanoparticles; MRT: Mean residence times; MPEG: Methoxy polyethylene glycol; NP: Nanoparticle; NLC: Nanostructured lipid carrier; NCEs: New chemical entities; PSM: Plant secondary metabolites; SNL: Solid lipid nanovectors; TCM: Traditional Chinese Medicine; TR: Transferrin; TNBC: Triple negative breast cancer; VM: Vasculogenic mimicry Received 12 January 2016; Accept 3 May 2016

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Safflower, Carthamus tinctorius L., is an annual oilseed crop that is cultivated on small plots all over the world. The seed oil content ranges from 20% to 45%; the oil is high in linoleic acid, an unsaturated fatty acid that aids in lowering the blood cholesterol level. Thus, safflower has long been used as medical plant in many countries, especially in China and India. However, for industrial purposes, it has long been neglected because of the low seed yield or oil content, until its physical role was revealed. In recent years, research works carried out in many countries mostly focused on improving the seed or oil yield. In this review, after illustrating the fatty acid composition of safflower seed oil as well as the genetic characteristics of safflower and their relationships with agronomic traits, a brief analysis of the current worldwide situation and future prospects of safflower utilization are presented.

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The therapeutic potential of artemisinin (ART) and its derivatives (ARTs) is not limited to malaria but has been recently expanded to other infections with protozoans, trematodes, or viruses as well as to cancer. Due to their limited poor water and oil solubility, rapid degradation by the liver, and short half-life, they have a low bioavailability after oral administration. Consequently, there is a pressing necessity to formulate new ART preparations to raise its bioavailability and efficacy. Nanosized drug delivery systems represent important tools in modern medicine with wide clinical applications, because of their potential modulation of pharmacokinetic and biodistribution. This review focuses on polymer-based systems, lipid-based systems, and inorganic nanoparticles loaded with ARTs. The overall goal of this field of research is to enhance their solubility and stability to improve bioavailability at much lower doses and to increase long-term safety. In addition, the opportunity to reach highly specific site-targeted delivery by these nanocarriers confers a high medicinal value. Remarkably, most of the reported nanoparticulate drug delivery systems are biologically inactive or marginally immunogenic, generating no antigenic or pyrogenic reactions but only partial intrinsic toxicity. As clinical studies in human patients are available so far, there is a pressing need to translate preclinical results on ART-based nanosystems into clinical settings.

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Chronic obstructive pulmonary disease (COPD) is a major chronic disease that seriously endangers public health. Some remarkable results have shown that Chinese medicine has an obvious clinical effect in preventing and treating COPD. To further promote the normative use of Chinese medicine to better guide the clinical diagnosis and treatment of COPD, the World Federation of Chinese Medicine Societies developed a panel to establish the guidelines by systematically evaluating, based on the revision and transformation of Guidelines for Chinese Medicine Diagnosis and Treatment of Chronic Obstructive Pulmonary Disease released by the China Association of Chinese Medicine in 2019 (Standard No: T/CACM 1319-2019), the latest clinical research evidence at home and abroad, formatting the International Clinical Practice Guideline of Chinese Medicine—Chronic Obstructive Pulmonary Disease, and publishing in both Chinese and English. The guidelines consist of 12 parts: preface, introduction, scope, normative references, terms and definitions, disease diagnosis and staging, severity assessment, etiology and pathogenesis, syndrome differentiation and treatment, other treatment, prevention and care, and appendix. They also standardize the contents of traditional Chinese medicine (TCM) etiology and pathogenesis, syndrome differentiation and treatment, and prevention and care of COPD. These guidelines are applicable to clinical respiratory physicians of TCM and integrated traditional Chinese and western medicine. The release of these guidelines will help improve the effect and level of Chinese medicine for COPD.

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The therapeutic potential of artemisinin (ART) and its derivatives (ARTs) is not limited to malaria but has been recently expanded to other infections with protozoans, trematodes, or viruses as well as to cancer. Due to their limited poor water and oil solubility, rapid degradation by the liver, and short half-life, they have a low bioavailability after oral administration. Consequently, there is a pressing necessity to formulate new ART preparations to raise its bioavailability and efficacy. Nanosized drug delivery systems represent important tools in modern medicine with wide clinical applications, because of their potential modulation of pharmacokinetic and biodistribution. This review focuses on polymer-based systems, lipid-based systems, and inorganic nanoparticles loaded with ARTs. The overall goal of this field of research is to enhance their solubility and stability to improve bioavailability at much lower doses and to increase long-term safety. In addition, the opportunity to reach highly specific site-targeted delivery by these nanocarriers confers a high medicinal value. Remarkably, most of the reported nanoparticulate drug delivery systems are biologically inactive or marginally immunogenic, generating no antigenic or pyrogenic reactions but only partial intrinsic toxicity. As clinical studies in human patients are available so far, there is a pressing need to translate preclinical results on ART-based nanosystems into clinical settings.

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Direct analysis in real time (DART) possesses the merits of analyzing sample in its native status with minimal or even no sample pretreatment. In this review, we summarized the recent applications of DART in the field of herbal medicine analysis such as compound detection, species identification, metabolites profiling and initial quantification. DART with the characters of hyper-rapid, easy-hyphenated offers a new research tool for herbal medicines to complete the experimental process in a very simple but still reliable way. It is anticipated that more wide and deep applications of DART in herbal medicine analysis, as rapid quantification, high-throughput active compounds screening, rapid species identification, and fast illegal additives screening will be promising and foreseeable in the near future.

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Background: Edible bird nest (EBN) is a natural food product rich in glycoprotein such as sialic acid, which has been reported to improve brain functions. The EBN is widely consumed due to its higher nutritional contents and antioxidant status; however, an interaction of EBN on brain cell metabolic activity and viability are still unclear. Objective: The objectives of this study were to identify the effect of sialic acid from EBN on the cell viability and to determine the appropriate concentration of sialic acid on cognitive performance in mice. Materials and Methods: The viability of pheochromocytoma and neuroblastoma cell lines were tested using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. For in vivo study, 7-week-old female BALB/c mice were randomly assigned into four treatment groups and were treated with sialic acid for 21 days. At day 22, all mice were tested on cognitive performance by Y-maze test. Results: Treatment concentration of sialic acid extract and sialic acid standard at 60 μg/mL (0.6 ppm) increased cell viability and showed no cytotoxicity effects in pheochromocytoma and neuroblastoma cell lines. In addition, an administration of higher dose of sialic acid at 0.6 ppm in animals improved Y-maze test performance, which they showed significantly higher number of entries and time spent in the novel arm. Conclusion: Thus, the current study shows that the sialic acid extract at 0.6 ppm improved brain cognitive performance in mice associated with an increased viability of pheochromocytoma and neuroblastoma cell lines.

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Following the spirit of Central Committee about the Opinions on Promoting the Inheritance, Innovation, and Development of Traditional Chinese Medicine, Academician Chen Kai-Xian, from Shanghai University of Traditional Chinese Medicine, made a wonderful report on the development of traditional Chinese medicine (TCM) and global medicine. The report deeply elaborated on five aspects: the characteristics and advantages of TCM, the challenges faced by contemporary medicine, the status and role of TCM in the contemporary era, the inheritance and innovation of TCM, and the cooperation and development of “Belt and Road.”

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Pain and inflammatory diseases are important clinical indications of acupuncture, which have been widely accepted in the international community. Previous studies have been focusing on rapid analgesia of acupuncture through the regulation of nervous system, but few studies on the inflammation regulatory mechanisms in which acupuncture inhibits the peripheral sensitization-induced pain. Based on studies concerning acupoint mechanisms of acupuncture actions and related researches on acupuncture regulating neuroendocrine and immune systems, we put forward the scientific hypothesis that acupuncture regulates neuroendocrine-immune (NEI) network and key response media therein, so as to achieve anti-inflammatory and analgesic effects in target organs. We have established a platform for acupuncture at ST36 to alleviate inflammatory pain in adjuvant induced arthritic rats. Based on the complex network analysis of multi-dimensional data from multi-time point and multi-site detection of NEI common signaling molecules, we have clarified the regulatory effects of acupuncture on NEI network and corresponding downstream immune network. Results indicated that monocytes/macrophages are the key targeting cells of acupuncture regulation, and acupuncture may display the anti-inflammatory and analgesic effects by regulating polarization of T cells in lymph nodes and polarization of M1/M2 macrophages in inflamed joints/paws. In addition, we have spotted a key molecule for acupuncture analgesia, CXCL1, as well as clarified the novel central analgesic mechanism of acupuncture mediated by CXCL1/CXCR2 desensitization. Thereby, we have provided novel evidence of the anti-inflammatory and analgesic actions of acupuncture through regulating NEI network and several key substances, highlighting a systemic research paradigm for investigating mechanisms of acupuncture actions.

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Pain and inflammatory diseases are important clinical indications of acupuncture, which have been widely accepted in the international community. Previous studies have been focusing on rapid analgesia of acupuncture through the regulation of nervous system, but few studies on the inflammation regulatory mechanisms in which acupuncture inhibits the peripheral sensitization-induced pain. Based on studies concerning acupoint mechanisms of acupuncture actions and related researches on acupuncture regulating neuroendocrine and immune systems, we put forward the scientific hypothesis that acupuncture regulates neuroendocrine-immune (NEI) network and key response media therein, so as to achieve anti-inflammatory and analgesic effects in target organs. We have established a platform for acupuncture at ST36 to alleviate inflammatory pain in adjuvant induced arthritic rats. Based on the complex network analysis of multi-dimensional data from multi-time point and multi-site detection of NEI common signaling molecules, we have clarified the regulatory effects of acupuncture on NEI network and corresponding downstream immune network. Results indicated that monocytes/macrophages are the key targeting cells of acupuncture regulation, and acupuncture may display the anti-inflammatory and analgesic effects by regulating polarization of T cells in lymph nodes and polarization of M1/M2 macrophages in inflamed joints/paws. In addition, we have spotted a key molecule for acupuncture analgesia, CXCL1, as well as clarified the novel central analgesic mechanism of acupuncture mediated by CXCL1/CXCR2 desensitization. Thereby, we have provided novel evidence of the anti-inflammatory and analgesic actions of acupuncture through regulating NEI network and several key substances, highlighting a systemic research paradigm for investigating mechanisms of acupuncture actions.

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Genus Alpinia consists of over 250 species, which are widely distributed in south and southeast Asia. Many plants of genus Alpinia have been used for thousands of years to treat digestive system diseases and as anti-inflammatory drugs. Phytochemical research on this genus has led to the isolation of different kinds of diarylheptanoids, terpenes triterpenoids, phenylbutanoids, lignans, and flavonoids. Experimental evidences revealed that both the crude extracts and pure constituents isolated from the genus Alpinia exhibit a wide range of bioactivities such as anti-cancer, anti-oxidant, anti-bacterial, anti-viral, cardiovascular, and digestive system protective effects. Here, we summarize the phytochemistry and pharmacology investigation of the genus Alpinia, which can provide reference for further research and drug development.

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Inflammation is a defensive reaction of the human body to numerous detrimental stimuli, including physical trauma, noxious chemicals, as well as microbial agents. Uncontrolled inflammation is the pathological basis of multiple diseases, such as rheumatoid arthritis (RA), neurodegenerative diseases, liver disease, and lung inflammation. Lanostane triterpenoids are natural tetracyclic triterpenoids with significant anti-inflammatory activity. An extensive review of the published literature regarding the phytochemistry and anti-inflammatory pharmacology of lanostane triterpenoids has been performed and analyzed using several search engines, such as SciFinder, Web of Science, Scopus, PubMed, Google Scholar, and ScienceDirect. This review is devoted to naturally occurring lanostane-type triterpenes with anti-inflammatory activity, including their sources, biosynthesis, and mechanism of action. This review also discusses the inflammation-related diseases and the clinical significance of traditional Chinese medicine as multi-target therapeutic agents for the prevention and treatment of inflammatory diseases. In the past 30 years, more than 100 new lanostane-type triterpenes have been reported from the families Schisandraceae, Ganodermataceae, and Polyporaceae. Six compounds, fomitopinic acid A, fomitosides E and F, obtusifoliol, 4α, l4α-dimethyl-5α-ergosta-7,9(11), 24(28)-trien-3 β-ol, and gramisterol exhibited the most potent anti-inflammatory activity against cyclooxygenase-1 (COX-1) and COX-2, with IC₅₀values ranging from 0.087 to 1.15 μM. Some of these compounds exhibited significant activity by mediating the inhibition of the pro-inflammatory cytokines, inducible nitric oxide synthase, and COX-2 expression. This review provides a basis for identifying anti-inflammatory drugs with high selectivity, high potency, and few adverse effects from lanostane-type triterpenes.

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Aristolochic acid (AA) is a group of structurally related nitrophenanthrene carboxylic acids found in many plants that are widely used by many cultures as traditional herbal medicines. AA is a causative agent for Chinese herbs nephropathy, a term replaced later by AA nephropathy. Evidence indicates that AA is nephrotoxic, genotoxic, and carcinogenic in humans; and it also induces tumors in the forestomach, kidney, renal pelvis, urinary bladder, and lung of rats and mice. Therefore, plants containing AA have been classified as carcinogenic to humans (Group 1) by the International Agency for Research on Cancer. In our laboratories, we have conducted a series of genotoxicity and toxicogenomic studies in the rats exposed to AA of 0.1–10 mg/kg for 12 weeks. Our results demonstrated that AA treatments induced DNA adducts and mutations in the kidney, liver, and spleen of rats, as well as significant alteration of gene expression in both its target and nontarget tissues. AA treatments altered mutagenesis- or carcinogenesis-related microRNA expression in rat kidney and resulted in significant changes in protein expression profiling. We also applied benchmark dose (BMD) modeling to the 3-month AA-induced genotoxicity data. The obtained BMDL₁₀(the lower 95% confidence interval of the BMD₁₀that is a 10% increase over the background level) for AA-induced mutations in the kidney of rats was about 7 μg/kg body weight per day. This review constitutes an overview of our investigations on AA-induced genotoxicity and toxicogenomic changes including gene expression, microRNA expression, and proteomics; and presents updated information focused on AA-induced genotoxicity in rodents.

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Inflammation is a defensive reaction of the human body to numerous detrimental stimuli, including physical trauma, noxious chemicals, as well as microbial agents. Uncontrolled inflammation is the pathological basis of multiple diseases, such as rheumatoid arthritis (RA), neurodegenerative diseases, liver disease, and lung inflammation. Lanostane triterpenoids are natural tetracyclic triterpenoids with significant anti-inflammatory activity. An extensive review of the published literature regarding the phytochemistry and anti-inflammatory pharmacology of lanostane triterpenoids has been performed and analyzed using several search engines, such as SciFinder, Web of Science, Scopus, PubMed, Google Scholar, and ScienceDirect. This review is devoted to naturally occurring lanostane-type triterpenes with anti-inflammatory activity, including their sources, biosynthesis, and mechanism of action. This review also discusses the inflammation-related diseases and the clinical significance of traditional Chinese medicine as multi-target therapeutic agents for the prevention and treatment of inflammatory diseases. In the past 30 years, more than 100 new lanostane-type triterpenes have been reported from the families Schisandraceae, Ganodermataceae, and Polyporaceae. Six compounds, fomitopinic acid A, fomitosides E and F, obtusifoliol, 4α, l4α-dimethyl-5α-ergosta-7,9(11), 24(28)-trien-3 β-ol, and gramisterol exhibited the most potent anti-inflammatory activity against cyclooxygenase-1 (COX-1) and COX-2, with IC₅₀values ranging from 0.087 to 1.15 μM. Some of these compounds exhibited significant activity by mediating the inhibition of the pro-inflammatory cytokines, inducible nitric oxide synthase, and COX-2 expression. This review provides a basis for identifying anti-inflammatory drugs with high selectivity, high potency, and few adverse effects from lanostane-type triterpenes.

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Herbal medicines may benefit from metabolomics studies, and applying metabolomics may provide answers about which herbal interventions may be effective for individuals, which metabolic processes are triggered, and the subsequent chemical pathways of activity. Physalis pubescens L (PPL) is an herbal fruit for one year living plant and has been developed into healthy function’s food. However, the mechanisms of health functions are still unclear. To comprehensively and holistically assess its anti-fatigue and antioxidant effects, a novel integrative metabolomics approach was applied. In this study, we present metabolomics analysis applying ultra performance liquid chromatography coupled to quadrupole with time-of-flight mass spectrometry (UPLC-Q/TOF-MS) to determine metabolite alterations after oral administration PPL to rats. Fifteen metabolites in urine were identified as potential biomarkers. Pattern analysis of the UPLC-Q/TOF-MS data disclosed that PPL could relieve fatigue rats by ameliorating the disturbance in amino acids metabolism and energy metabolism, alleviating the oxidative stress from reactive oxygen species and the inflammatory damage, and recovering the destructed regulation. Based on these results, we demonstrated that PPL is a promising source of natural anti-fatigue and antioxidants material for use in functional foods and medicines.

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Quality control of traditional Chinese medicine (TCM) begins with elucidation of its chemical basis. The root of Stephania tetrandra, Stephaniae Tetrandrae radix (STR; Fang-Ji), has long been utilized as an antirheumatic, analgesic, and diuretic TCM. Powerful analytical strategies that would enable a multicomponent characterization of STR are still lacking. In the present study, we established a rapid, reliable, and enhanced profiling approach, using ultra-high performance liquid chromatography coupled with ion mobility/quadrupole time-of-flight mass spectrometry (MS) and automatic peak annotation facilitated by computational matching of an in-house library. This approach was used to characterize the multicomponents of STR. Good chromatographic separation was achieved within 17 min on a reversed-phase BEH C18 column eluted with acetonitrile/0.1% ammonium hydroxide in water, whereas data-independent high-definition MS^E in the positive mode was applied to acquire the MS² data using a Vion™ IM-QTOF instrument, which, in theory, could cover all the profiled precursor ions. To overcome the interference of three predominant peaks, a knockout strategy was utilized by automated valve switching. An in-house library of 163 compounds was established and incorporated into the UNIFI™ platform. By applying this method, we could identify or tentatively characterize 76 alkaloids from the methanolic extract of STR, including 14 aporphine-type, four morphine-type, 48 bisbenzylisoquinoline-type, seven tetrahydroprotoberberine-type, one protopine-type, one benzylisoquinoline-type, and one other. For each component, four-dimensional information, such as retention time, collision cross-section, high-accuracy MS¹, and high-accuracy MS² data, was utilized to achieve the systematic multicomponent characterization of STR.

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Objective: Quality control of traditional Chinese medicine (TCM) begins with the chemical basis elucidation. The root of Stephania tetrandra has long been utilized as an antirheumatic, analgesic, and diuretic TCM, Stephaniae Tetrandrae Radix (STR; Fang-Ji). Powerful analytical strategies enabling its multicomponent characterization is still rare. Methods: A rapid, reliable, and enhanced profiling approach, by ultra-high performance liquid chromatography coupled with ion mobility/quadrupole time-of-flight mass spectrometry (UHPLC/IM-QTOF-MS) and automatic peak annotation facilitated by computational matching of in-house library, was established and utilized to characterize the multicomponents from STR. A knockout strategy was utilized by automated valve switching to overcome the interference of predominant peaks. Results: Good chromatographic separation was achieved within 17 min on a reversed-phase BEH C18 column eluted with acetonitrile/0.1% ammonium hydroxide in water, while data-independent high-definition MS^E (HDMS^E) in positive mode was applied to acquire the MS² data by using a VionTM IM-QTOF instrument, which in theory, could cover all the profiled precursor ions. An in-house library of 163 compounds was established and incorporated into the UNIFITM platform. By feat of these efforts, we were able to identify or tentatively characterize 76 alkaloids from the methanolic extract of STR, including 14 aporphine-type, four morphine-type, 48 bisbenzylisoquinoline-type, seven tetrahydroprotoberberine-type, one protopine-type, one benzylisoquinoline-type, and one other. Four-dimensional information, such as the retention time, collision cross section (CCS), high-accuracy MS1 and MS2 data, for each component was provided. Conclusions: The systematic multicomponent characterization of STR was accomplished with high coverage, high degree of automation, and high reliability.

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The objective of the study is to systematically evaluate the efficacy of four Chinese patent medicines in combination with angiotensin-converting enzyme inhibitors/angiotensin receptor blockers (ACEI/ARB) in the treatment of early diabetic nephropathy (DN). Retrospectively, previously published randomized controlled trials (RCTs) of four different Chinese patent medicines combined with ACEI or ARB in the treatment of patients with early DN were searched overall from databases. The data were analyzed by R, Generate Mixed Treatment Comparisons and STATA softwares. A total of 78 RCTs were finally included. Network meta-analysis showed that the total effective rate of the Jinshuibao capsule-ACEI/ARB combination group and Huangkui capsule-ACEI/ARB combination groups were better than the others; Jinshuibao capsule-ACEI/ARB combination group reduced the 24-h urinary protein excretion (24-h UTP), urine microalbumin excretion rate (UAER), serum creatinine (Scr), and glycosylated hemoglobin (HbAlc) values. The Huangkui capsule-ACEI/ARB combination demonstrated a better reduction of (blood urea nitrogen [BUN]). Reduced incidences of adverse effects were only observed on treatment with Bailing capsule-ACEI/ARB combination. In early DN, combination of Jinshuibao capsule-ACEI/ARB provided the highest effective rate; moreover, it could reduce the 24-h values of UTP, UAER, Scr, and HbAlc; Huangkuai capsule-ACI/ARB combination group showed a good effect on reducing BUN. Bailing capsule-ACEI/ARB combination group had reduced the incidences of adverse reactions.

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Objective: The study objective was to observe the effect of Dachaihu decoction and its “prescription elements” on intestinal flora of model rats with nonalcoholic fatty liver disease (NAFLD). Materials and Methods: Healthy male Sprague-Dawley rats were randomly divided into the following seven groups (n = 105): normal, model, pioglitazone hydrochloride (PH), Shuganlidan, Jianpihuatan, Tongfuxiezhuo, and dachaihu decoction (DD). 16SrRNA high-throughput IIlumina sequencing platform was used for sequencing, and bioinformatics analysis of rat intestinal flora was done. Results: Compared with the normal group, rats in the model, PH, Shuganlidan, Jianpihuatan, Tongfuxiezhuo, and DD groups showed significant differences in the intestinal microflora structure. The microorganisms that play an important role in the normal group are Ruminococcaceae, Oscillospira, Lactobacillales, Lactobacillaceae, Lactobacillus, bacilli, Ruminococcus, TM7, Spirochaetes, Clostridium, Elusimicrobia, Elusimicrobiaceae, Elusimicrobiales, Lactobacillus helveticus, Lactobacillus reuteri, Elusimicrobium, RF39, and Christensenellaceae; in the model group are Ruminococcus gnavus; in the PH group are Prevotella, Paraprevotellaceae, and Blautia; in the Jianpihuatan group are Bacteroidetes, Bacteroidia, Bacteroidales, Roseburia, Rikenellaceae, and Stridium methylpentosum; in the TongfuXiezhuo group are Bacteroidaceae, Bacteroides, Porphyromonadaceae, Parabacteroide, 4C0d_2, Cyanobacteria, YS2, Parabacteroides distasonis, Bacteroides uniformis, Verrucomicrobiaceae, Verrucomicrobiae, Verrucomicrobiales, Akkermansia, Akkermansia muciniphila, Coprobacillus, Parabacteroides gordonii, Blautia producta, and Ruminococcus torques; and in the DD group are Erysipelotrichales, Erysipelotrichi, and Erysipelothrichaceae. Conclusion: The Tongfuxiezhuo prescription elements of the DD significantly improved the intestinal flora of rats with NAFLD, improving the relative abundance of beneficial bacteria in the intestinal flora of NAFLD rats such as Bacteroides, Sartre genus, Vibrio pseudobutyrate bacteria, and Akkermansia muciniphila. This subsequently improved the glucose and lipid metabolism in NAFLD rats, reducing fat deposition in the liver, inhibiting intestinal inflammatory reaction, and maintaining the integrity of intestinal mucosal barrier. The action target is the intestinal axis of “intestinal–hepatic axis.”

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The objectives of this study are to conduct a comprehensive literature search and bibliometric analysis to identify the breadth and volume of pharmacological and clinical studies on pine pollen (Pinus pollen) and to identify the potential effects and the use of pine pollen. Three Chinese electronic databases and two English electronic databases were searched for pharmacological and clinical studies on pine pollen. Data were extracted and analyzed and included publication year, authors, study type, pharmacological research topics or clinical diseases/conditions, usage and type of preparation, authors' conclusions, and adverse effects. Of 239 publications identified, 180 were pharmacological studies, 37 were clinical trials, and 22 were reviews. Numbers of publications increased particularly from 2004 onward. The top 10 most frequent topics in pharmacological studies were immune regulation, antisenility, antioxidation, liver protection, inhibiting prostate hyperplasia, inhibiting tumor cell proliferation, lowering blood glucose, lowering blood lipids, antifatigue, and improving intestinal function. The top 10 most frequent clinical diseases treated or where pine pollen was used as an adjuvant were bedsores, diaper dermatitis, hyperlipidemia, oral mucositis, eczema, hyperplasia of prostate, hypertension, prostatitis, type 2 diabetes mellitus, and radiodermatitis. Eight trials reported no adverse events associated with pine pollen, one reported mild gastrointestinal reactions, but symptoms disappeared without special management. There have been an increasing number of publications on pine pollen during the past 20 years. Pharmacological studies have shown many potential benefits, and clinical studies have indicated some positive effects when it is either used as a single herb or as an adjuvant to treat disease. Its use as a topical agent, especially for skin diseases, was notable.

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Radix achyranthis bidentatae (RAB), a member of the Amaranthaceae family, has been widely used in Traditional Chinese Medicine for 1000s of years. Increasing interest in RAB-derived medicinal has led to the discovery of additional triterpenoid saponins, phytoecdysones, polysaccharides, and many other compounds, as well as investigations into their pharmacology. A large number of pharmacological studies have shown RAB and its active components possess a range of pharmacological activities, including anti-tumor, anti-fertility, anti-senile, and anti-inflammatory effects. This review is an up-to-date summary and synthesis of the uses of RAB from phytochemical and pharmacological perspectives.

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