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    2022,14(2), DOI: 10.1016/j.chmed.2022.03.005
    Abstract:
    In less than 20 years since the beginning of 21th century, there have been many major outbreaks of SARS, avian influenza, H1N1 flu, Ebola virus, and COVID-19 in the world one after another. These epidemics have caused huge losses of human life and property. Meanwhile, tumors, diabetes, cardiovascular and cerebrovascular diseases, mental diseases and diseases with unknown etiology that were rare in the past have now become common diseases in society. Coupled with the outbreak of major epidemics, they have posed a huge threat to human health and even survival. How to minimize and/or eliminate these threats? The traditional application and modern research of traditional Chinese medicine (TCM) give us a lot of inspiration. This issue has ushered in several excellent papers to continuously spotlight the exciting progress of Chinese herbal medicines in human health and diseases. Both Rosa and Tetrastigma belong to the Eudicots clade Rosids, which possess astounding biodiversity and chemodiversity, followed by highly diverse bioactivities. Their traditional uses and pharmacological activities have been elaborated in two comprehensive reviews (Wang et al., 2022; Zhang et al., 2022a); extracts and compounds of both genera showed the following activities: Antineoplastic and anti-cancer, anti-inflammatory, antioxidant, hepatoprotective, blood sugar regulatory/antidiabetic, antibacterial, antiviral, and cardiovascular protection, and others. Possibly due to the distinct chemical composition, these genera also have some differences in bioactivities, e.g., flavonoids of Rosa displayed the nervous system protection, Rosa also had the anti-aging and hypolipidemic properties, while Tetrastigma showed the analgesic activity. The studies of these pharmacological activities are booming (Gu et al., 2022; Zhang et al., 2022b), as they are aimed at the current common and frequently occurring diseases, including epidemic and pandemic diseases. Promisingly, both Rosa and Tetrastigma had no toxic effect in human subjects, which is especially validated by their long-term uses in folk medicine. Notwithstanding, the drug metabolism and pharmacokinetic studies of both genera, as well as other taxonomic groups with abundant medicinal phytometabolites, should be strengthened to further expound the absorption, distribution, metabolism, excretion and toxicity attributes of botanical extracts and phytometabolites; Q-markers of herbal products (Liu, 2021; Liu et al., 2018) derived from them should also be developed to maximize their health-promoting and therapeutic effects. The specialized metabolites of medicinal plants induced by ecological/environmental factors vary greatly, but meanwhile the specific biosynthetic pathways and related phytometabolites, and even therapeutic efficacy, may have some phylogenetic signals, which is suggested by pharmacophylogeny investigations (Hao et al., 2022). The metabolomic studies of medicinal genera should be further expanded to collect compound information as completely as possible, so as to analyze the correlation between specialized metabolites and molecular phylogeny qualitatively and quantitatively. After superimposing phylogenetic background, the dominance of a specific type of phytometabolites could be found in the specific part of phylogenetic tree, and the evolutionary trajectory of chemodiversity could be revealed, which has important guiding significance for the discovery and development of new/alternative phytomedicine resources. Many phytometabolites are phylogenetically conserved, and their abundance in different taxonomic groups is highly variable; e.g., indole alkaloids are reported in Tetrastigma instead of Rosa (Wang et al., 2022; Zhang et al., 2022a), the ursane-type triterpenoids are abundant in the latter rather than the former, while diterpenoids are trivial in both genera. In addition, the correlation between geographical distributions and therapeutic compounds should also be taken into account to assess the resource value of any taxonomic groups. We could find that some local species which were lately diverged have more diverse specialized metabolites as compared with widespread species firstly diverged, or vice versa. The genetic background and environmental pressure jointly shape the unique metabolome of each taxonomic group. With the explosive increase of the identified compounds in recent years (Gu et al., 2022), we are more confident in the systematic study of variation pattern of chemodiversity in the taxonomic group of interest in the light of evolution. These studies will promote the vitality of TCM supply chain and the sustainable development of Chinese herbal medicine industry.
    2022,14(2), DOI: 10.1016/j.chmed.2022.03.004
    Abstract:
    Traditional Chinese medicines (TCMs) have continued to be a treasure trove. The study of chemodiversity and versatility of bioactivities has always been an important content of pharmacophylogeny. There is amazing progress in the discovery and research of natural components with novel structures and significant bioactivities in 2020. In this paper we review 271 valuable natural products, including terpenoids, steroids, flavonoids, phenylpropanoids, phenolics, nitrogen containing compounds and essential oil, etc., isolated and identified from TCMs published in journals of Chinese Traditional and Herbal Drugs (Zhong Cao Yao) and Chinese Herbal Medicines (CHMs), and focus on their structures, source organisms, and relevant bioactivities, paying special attention to structural characteristics of novel compounds and newly revealed pharmacological properties of known compounds. It is worth noting that natural products with antitumor activity still constitute the primary object of research. Among the reported compounds, two new triterpenoids, i.e., ursolic acid 3-O-β-cis-caffeate and mollugoside E, display remarkable cytotoxicity against PC-9 and HL-60 cell lines, respectively. Three known phenolic compounds, i.e., pyoluteorin, 4-hydroxy-3-methoxy cinnamaldehyde and 3,7-dimethoxy-5-hydroxy-1,4-phenanthrenequinone, exhibit significant cytotoxicity against multiple cell lines. Numerous studies on the free radical scavenging activity of reported compounds are currently underway. In vitro, three known phenolic compounds, i.e., 3,4-O-dicaffeoylquinic acid methyl ester, 3,4,5-O-tricaffeoylquinic acid methyl ester and arbutin, had more considerable antioxidant activities than vitamin C. The anti-inflammatory, anti-diabetic, hypolipidemic, neuroprotective and antimicrobial activities of isolated compounds are also encouraging. The structural characteristics and bioactivities of TCM compounds highlighted here reflect the enormous progress of CHM research in 2020 and will play a positive role in the future drug discovery and development. According to pharmacophylogeny, the phylogenetic distribution of compounds with different natures and flavors can be explored, with view to better mining TCM resources.
    2022,14(2), DOI: 10.1016/j.chmed.2022.01.005
    Abstract:
    The genus Rosa (Rosaceae family) includes about 200 species spread in the world, and this genus shows unique advantages in medicine and food. To date, several scholars concentrated on compounds belonging to flavonoids, triterpenes, tannins, polysaccharide, phenolic acids, fatty acids, organic acids, carotenoids, vitamins. Pharmacological effects such as antineoplastic and anti-cancer properties, anti-inflammatory, antioxidant, liver protection, regulate blood sugar, antimicrobial activity, antiviral activity, as well as nervous system protection and cardiovascular protection were wildly reported. This article reviews the chemical constituents, pharmacological effects, applications and safety evaluations of Rosa plants, which provides a reference for the comprehensive utilization of medicine and food resources and gives a scientific basis for the development of medicinal plants of the genus Rosa.
    2022,14(2), DOI: 10.1016/j.chmed.2022.03.003
    Abstract:
    The genus Tetrastigma belongs to the Vitaceae family and contains over 100 species. This paper reviewed folk uses, chemical constituents, pharmacological activities, and clinical applications of the medicinal plants in the genus Tetrastigma. In addition, the paper also discussed the current problems for the further studies. Up to now, more than 240 compounds were reported from the genus Tetrastigma, covering 74 flavonoids, 14 terpenoids, 19 steroids, 21 phenylpropanoids, 14 alkaloids and others constituents. Among them, flavonoids are the major and the characteristic chemical constituents in this genus. Modern pharmacological studies and clinical practice showed that the extracts and chemical constituents of Tetrastigma species possessed wide pharmacological activities including antitumor, antioxidative, hepatoprotective, antiviral, anti-inflammatory, and analgesic activities. The information summarized in this paper provided valuable clues for discovering new drug for further research and an incentive to expand the research of genus Tetrastigma.
    2022,14(2), DOI: 10.1016/j.chmed.2021.12.003
    Abstract:
    Puerarin (Pue), known as a phytoestrogen, has salient bioactivities and is promising against cardiovascular diseases. This article summarizes the underlying molecular mechanisms of Pue in treating cardiovascular diseases, especially regulating the intracellular signal transduction, influencing ion channels, modulating the expression of microRNA, and impacting on the autophagy, which are mainly involved in the inflammatory signaling pathways, fatty acid/lipid metabolism, oxidative stress, apoptosis, and the like. The protective effect of Pue against cardiovascular diseases mainly involves attenuating the myocardial injury and decreasing the myocardial fibrosis, improving the myocardial ischemia/reperfusion injury, as well as inhibiting the myocardial hypertrophy and atherosclerosis. The molecular mechanisms of Pue’s cardiovascular protective effects for the first time and comment on the state-of-the-art research methods and principles of Pue’s regulation of small molecules were reviewed, so as to provide the rationale for its basic research and clinical applications.
    2022,14(2), DOI: 10.1016/j.chmed.2021.11.003
    Abstract:
    Worldwide, gastric cancer is the second leading cause of cancer deaths and the fifth most common malignant tumor. Gastric cancer is believed to be caused by a variety of factors, such as genetics, epigenetics, and environmental influences. Among the pathogenic factors, inflammation has been considered as one of the main risk factors for gastric cancer. There are currently limited ways to prevent gastric cancer. Although the combined application of aspirin and non-steroidal anti-inflammatory drugs can reduce the risk, it has great side effects and can easily cause gastric perforation or gastric bleeding. Therefore, an alternative plan is urgently needed. Curcumin is the yellow pigment in the rhizome of the plant turmeric. Current studies have found that curcumin has a protective effect on gastric mucosal damage caused by non-steroidal anti-inflammatory drugs, gastric mucosal damage in rats, and gastric mucosal damage caused by stress bleeding and Helicobacter pylori infection. Curcumin shows significant anti-inflammatory and anti-cancer activities by regulating DNA methylation, histone modification, nuclear factor erythrocyte 2 related factor 2 and other related signal pathways. In this article, the latest evidence of curcumin for epigenetic changes in gastric cancer and its potential contribution to gastric cancer were discussed.
    2022,14(2), DOI: 10.1016/j.chmed.2021.11.003
    Abstract:
    Objective: In this study, the aim was to investigate the inhibitory effect of 6,6′-bieckol on the migration and epithelial-mesenchymal transition (EMT) of non-small cell lung cancer (NSCLC) cells, and explore its potential molecular mechanisms. Methods: Cell migration was measured using a CCK8, wound healing, and transwell migration assay. Apoptosis was determined using an Annexin V/propidium iodide staining. Western blotting and immunofluorescence were used to examine the expression level of apoptosis-related proteins and EMT marker proteins. Results: The results showed that 6,6′-bieckol inhibited migration and induced apoptosis of NSCLC cells. Furthermore, 6,6′-bieckol had significantly up-regulated the E-cadherin and down-regulated Snail1 and Twist1 transcriptional levels. 6,6′-Bieckol might inhibit TGF-β-induced EMT by down-regulating Snail1 and Twist1 and up-regulating E-cadherin in lung cancer cells. Conclusion: It was suggested that 6,6′-bieckol has the potential to be developed as a therapeutic candidate for lung cancer.
    2022,14(2), DOI: 10.1016/j.chmed.2021.09.014
    Abstract:
    Objective: To investigate the role of Portulaca oleracea (POL) in promoting revascularization and re-epithelization as well as inhibiting iron aggregation and inflammation of deep tissue pressure injury (DTPI). Methods: The hydroalcoholic extract of POL (P) and aqueous phase fraction of POL (PD) were prepared based on maceration and liquid-liquid extraction. The number of new blood vessels and VEGF-A expression level were assessed using H&E stain and Western blot on injured muscle to examine the role of POL different extracts in vascularization. The iron distribution and total elemental iron of injured muscle were detected using laser ablation inductively coupled plasma mass spectrometry (ICP-MS) and Perls' stainning to determine whether POL extracts can inhibit the iron accumulation. Besides, the ability of POL extracts to promote wound healing by combining re-epithelization time, inflammation degree and collagen deposition area were comprehensively evaluated. Results: In vitro, we observed a significant increase in HUVEC cell viability, migration rate and the number of the tube after P and PD treatment (P < 0.05). In vivo, administration of P and PD impacted vascularization and iron accumulation on injured tissue, evident from more new blood vessels, higher expression of VEGF-A and decreased muscle iron concentration of treatment groups compared with no-treatment groups (P < 0.05). Besides, shorter re-epithelization time, reduced inflammatory infiltration and distinct collagen deposition were associated with administration of P and PD (P < 0.05). Conclusion: POL extract administration groups have high-quality wound healing, which is associated with increased new blood vessels, collagen deposition and re-epithelization, along with decreased iron accumulation and inflammatory infiltration. Our results suggest that that POL extract is beneficial to repair injured muscle after ischemia-reperfusion, highlighting the potential of POL in the DTPI treatment.
    2022,14(2), DOI: 10.1016/j.chmed.2022.03.002
    Abstract:
    Objective: Nonalcoholic fatty liver disease (NAFLD) has become a common chronic liver disease that is harmful to human health. Moreover, there is currently no FDA-approved first-line drug for the treatment of nonalcoholic steatohepatitis (NASH) or NAFLD. Traditional Chinese medicine (TCM) is widely used to ameliorate liver diseases, such as the traditional ancient recipe called Three Flower Tea (TFT), which consists of double rose (Rosa rugosa), white chrysanthemum (Chrysanthemum morifolium), and Daidaihua (Citrus aurantium). However, the mechanisms of the action of TFT are not clear. Therefore, this study aimed to elucidate the mechanisms of TFT against NAFLD in high-fat diet (HFD)-induced rats. Methods: This study utilized bioinformatics and network pharmacology to establish the active and potential ingredient-target networks of TFT. Furthermore, a protein-protein interaction (PPI) network was constructed, and enrichment analysis was performed to determine the key targets of TFT against NAFLD. Furthermore, an animal experiment was conducted to evaluate the therapeutic effect and confirm the key targets of TFT against NAFLD. Results: A total of 576 NAFLD-related genes were searched in GeneCards, and under the screening criteria of oral bioavailability (OB) ≥ 30% and drug-likeness (DL) ≥ 0.18, a total of 19 active ingredients and 210 targets were identified in TFT. Network pharmacology analysis suggested that 55 matching targets in PPIs were closely associated with roles for NAFLD treatment. Through the evaluation of network topology parameters, four key central genes, PPARγ, SREBP, AKT, and RELA, were identified. Furthermore, animal experiments indicated that TFT could reduce plasma lipid profiles, hepatic lipid profiles and hepatic fat accumulation, improve liver function, suppress inflammatory factors, and reduce oxidative stress. Through immunoblotting and immunofluorescence analysis, PPARγ, SREBP, AKT, and RELA were confirmed as targets of TFT in HFD-induced rats. Conclusion: In summary, our results indicated that TFT could prevent and treat NAFLD via multiple targets, including lipid accumulation, antioxidation, insulin sensitivity, and inflammation.
    2022,14(2), DOI: 10.1016/j.chmed.2021.09.013
    Abstract:
    Objective: Network pharmacology combines drug and disease targets with biological information networks based on the integrity and systematicness of the interactions between drugs and disease targets. This study aims to explore the molecular basis of Hanshi Zufei formula for treatment of COVID-19 based on network pharmacology and molecular docking techniques. Methods: Using TCMSP, the chemical constituents and molecular targets of Atractylodis Rhizoma, Citri Reticulatae Pericarpium, Magnoliae Officinalis Cortex, Pogostemonis Herba, Tsaoko Fructus, Ephedrae Herba, Notopterygii Rhizoma et Radix, Zingiberis Rhizoma Recens, and Arecae Semen were investigated. The predicted targets of novel coronavirus were screened using the NCBI and GeneCards databases. To further screen the drug-disease core targets network, the corresponding target proteins were queried using multiple databases (Biogrid, DIP, and HPRD), a protein interaction network graph was constructed, and the network topology was analyzed. The molecular docking studies were also performed between the network’s top 15 compounds and the coronavirus (SARS-CoV-2) 3CL hydrolytic enzyme and angiotensin conversion enzyme II (ACE2). Results: The herb-active ingredient-target network contained nine drugs, 86 compounds, and 49 drug-disease targets. Gene ontology (GO) enrichment analysis resulted in 1566 GO items (P < 0.05), among which 1438 were biological process items, 35 were cell composition items, and 93 were molecular function items. Fourteen signal pathways were obtained by enrichment screening of the KEGG pathway database (P < 0.05). The molecular docking results showed that the affinity of the core active compounds with the SARS-CoV-2 3CL hydrolase was better than for the other compounds. Conclusion: Several core compounds can regulate multiple signaling pathways by binding with 3CL hydrolase and ACE2, which might contribute to the treatment of COVID-19.
    2022,14(2), DOI: 10.1016/j.chmed.2021.09.001
    Abstract:
    Objective: This study was devoted to identifying natural thrombin inhibitors from traditional Chinese medicine (TCM) and evaluating its biological activity in vitro and binding characteristics. Methods: A combination strategy containing molecular docking, thrombin inhibition assay, surface plasmon resonance (SPR) and molecular dynamics simulation were applied to verify the study result. Results: Gallic acid was confirmed as a direct thrombin inhibitor with IC50 of 9.07 μmol/L and showed a significant inhibitory effect on thrombin induced platelet aggregation. SPR-based binding studies demonstrated that gallic acid interacted with thrombin with a KD value of 8.29 μmol/L. Molecular dynamics and binding free energy analysis revealed that thrombin-gallic acid system attained equilibrium rapidly with very low fluctuations, the calculated binding free energies was ?14.61 kcal/mol. Ala230, Glu232, Ser235, Gly258 and Gly260 were the main amino acid residues responsible for thrombin inhibition by gallic acid, providing a mechanistic basis for further optimization. Conclusion: This study proved that gallic acid is a direct thrombin inhibitor with platelet aggregation inhibitory effect, which could provide a basis for the follow-up research and development for novel thrombin inhibitors.
    2022,14(2), DOI: 10.1016/j.chmed.2021.12.004
    Abstract:
    Objective: The current investigation aimed to determine the appropriate dosage form by comparing solid dispersion and liposome to achieve the purpose of improving the solubility and bioavailability of linarin. Methods: Linarin solid dispersion (LSD) and linarin liposome (LL) were developed via the solvent method and the thin film hydration method respectively. The Transwell chamber model of Caco-2 cells was established to evaluate the absorption of drug. The pharmacokinetics of linarin, LSD and LL in rats after ig administration were carried out by high performance liquid chromatography (HPLC) method. Results: The solubility of LSD and LL was severally 3.29 times and 3.09 times than that of linarin. The permeation coefficients of LSD and LL were greater than 10-6, indicating that the absorption of LSD and LL were both better than linarin. The bioavailability of the LSD was 3.363 times higher than that of linarin, and the bioavailability of LL was 0.9886 times higher than that of linarin. Conclusion: The linarin was more suitable for making solid dispersion to enhance its solubility and bioavailability.
    2022,14(2), DOI: 10.1016/j.chmed.2021.01.006
    Abstract:
    Objective: To establish HPLC fingerprints of different parts of chicory stems, leaves, roots, flowers and seeds, and compare the similarities and differences of chemical components in different parts, so as to provide a scientific basis for the comprehensive utilization of chicory. Methods: To establish the HPLC fingerprint of chicory, the chromatographic column was chosen with Agilent ZORBAX Eclipse XDB-C18, the mobile phase was methanol (A) - 0.2% formic acid (B), the flow rate was 1 mL/min, the column temperature was 30 °C, and the detection wavelength was 254 nm. The Similarity Evaluation System of Chromatographic Fingerprint of Traditional Chinese Medicine (2012 Edition) was used to evaluate the similarity of different parts of decoction pieces, and the determination method of multi-component content was established based on fingerprint identification chromatographic peaks, and the determination results were analyzed. Results: The HPLC fingerprinting method of chicory was established. Sixteen chromatographic peaks were identified and 10 of them were identified as: caftaric acid (1), esculin (2), chlorogenic acid (3), esculetin (4), caffeic acid (5), cichoric acid (8), hyperoside (11), rutin (12), isochlorogenic acid C (14) and luteolin (16). The similarity of different parts was 0.084?0.701. At the same time, the total content of detected chemical components was ranked as flower > leaf > stem > root > seed. Roots did not contain caftaric acid, rutin, and luteolin, flowers did not contain luteolin, and seeds did not contain caftaric acid, cichoric acid, and luteolin. The content of cichoric acid in leaves was the most, and esculin in flowers was the most. Conclusion: The results of HPLC fingerprint and multi-component content determination revealed the similarity and difference of different parts of chicory from chemical composition, indicating that there were certain differences in different parts of chicory. The established HPLC fingerprinting method can provide a reference for quality control and evaluation of different parts of the chicory.
    2022,14(2), DOI: 10.1016/j.chmed.2022.03.001
    Abstract:
    Objective: To establish a reliable and sensitive method for evaluating quality of Yiqi Jiangzhi Granules (YQJZG). Methods: Ultra performance liquid chromatography electrospray ionization tandem mass spectrometry (UPLC-ESI-MS/MS) was employed for simultaneous determination of eight marker components. Separation was performed on an AQUITY UPLC? HSS T3 column, the mobile phase consisted of acetonitrile as the organic phase and 0.1% (volume percentage) formic acid as the aqueous. Eight marker components, ginsenoside Rg1 (GRg1), ginsenoside Re (GRe), ginsenoside Rb1 (Gb1), typhaneoside (TEO), isorhamnetin-3-O-neohespeidoside (IN), hesperidin (HPD), aurantio-obtusin-6-O-β-D-glucoside (AG) and curcumin (CCM), were detected by multiple reaction monitoring (MRM) mode. The Chinese Pharmacopoeia (2020 edition) was regarded as the guidance document for this method validation. Results: The method showed good linearity (R2 ≥ 0.9990). The relative standard deviation (RSD) values for the instrument precision, intermediate precision and repeatability were less than 2.91%, 2.88%, and 3.54%, respectively. The average recovery varied from 91.08% to 103.89%, with RSD below 3.81%. Sample solutions were found to be stable within 24 h at 4 °C (RSD < 2.85%). Eight marker components were successfully determined from three batches of YQJZG. Conclusion: The proposed UPLC-ESI-MS/MS method was found to be simple, fast and sensitive, and can be used for the routine quality assessment of YQJZG. Simultaneously, this method may provide a new and powerful tool of quality control for other traditional Chinese medicine analogous formulae.
    2022,14(2), DOI: 10.1016/j.chmed.2021.05.006
    Abstract:
    Objective: To study the chemical constituents from the leaves and twigs of Callicarpa cathayana. Methods: The chemical constituents were isolated and purified by column chromatography on silica gel, MCI gel CHP 20P/P120, Sephadex LH-20, and HPLC. The structures of the compounds were determined by HR-ESI-MS, 1D and 2D NMR data. Results: A total of 24 compounds were isolated from the 85% methanol extract of leaves and twigs of C. cathayana. They were identified as cathayanalactone G (1), a new diterpene, and 23 known compounds as patagonic acid (2), (-)-16-hydroxycledroda-3,13-dien-16,15-olide-18-oic acid (3), 15-methoxypatagonic acid (4), oleanolic acid (5), ursolic acid (6), siaresinolic acid (7), pomolic acid (8), α-amyrin (9), tormentic acid (10), lupeol (11), 5,7-dihydroxy-3,4'-dimethoxyflavone (12), 5,4'-dihydroxy-3,7,3'-dimethoxyfla-vone (13), 5-hydroxy-3,6,7,4'- tetramethoxyflavone (14), salvigenin (15), kaemferol (16), astragalin (17), pinoresinol 4-O-β-D-glucopyranoside (18), paulownin (19), β-sitosterol (20), β-sitosterol β-D-glucopyranoside (21), 5-hydroxy-coumarin (22), isocopoletin (23), and 4-hydroxycinnamic acid (24). Conclusion: Compound 1 is a new labdane diterpene. Compounds 10, 13, 16 and 17 are isolated from the genus Callicarpa for the first time. Compounds 7, 8, 9, 12, 14, 23 and 24 are reported from C. cathayana for the first time.
    2022,14(2), DOI: 10.1016/j.chmed.2022.02.002
    Abstract:
    Objective: To study the active ingredients in the root bark of Aralia echinocaulis. Methods: Three triterpenoid saponins were separated from the 70% ethanol extracts and purified by column chromatography and their structures were determined by spectroscopic analysis. Compound 1 and 3 were evaluated for antioxidant activity by the in vitro DPPH free radical scavenging ability and the protective effect of OH- induced DNA oxidative damage. Results: Compound 1 was a new type of triterpenoid saponin, named as echinocaulisaglycone 3-O-β-D-glucopyranoside (echinocaulisaponin A), and it had good antioxidant activity. Compound 2 was similar to compound 1, named as 1-hydroxyl-echinocaulisaglycone 3-O-β-D-glucopyranoside (echinocaulisaponin B). Compound 3 was also a new type of triterpenoid saponin, named as echinocaulisaglycone II 3-O-α-L-arabinopyranosyl-(1”→4’)-β-D-glucopyranosiduronic acid (echinocaulisaponin C), and its antioxidant activity was weaker than compound 1. Conclusion: In this study, three new compounds were discovered and two of them were carried out in vitro anti-oxidation studies, laying the foundation for further research on the treatment of related diseases (cardiovascular disease, arthritis, age-related macular degeneration, etc.) through anti-oxidation or quenching free radical function.
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    2011,3(2):140-143, DOI: 10.3969/j.issn.1674-6384.2011.02.009
    [Abstract] (1457) [HTML] (0) [PDF 142.79 K] (17134)
    Abstract:
    Objective To study a novel feature extraction method of Chinese materia medica (CMM) fingerprint. Methods On the basis of the radar graphical presentation theory of multivariate, the radar map was used to figure the non-map parameters of the CMM fingerprint, then to extract the map features and to propose the feature fusion. Results Better performance was achieved when using this method to test data. Conclusion This shows that the feature extraction based on radar chart presentation can mine the valuable features that facilitate the identification of Chinese medicine.
    2012,4(1):63-69, DOI: 10.3969/j.issn.1674-6384.2012.01.010
    [Abstract] (1798) [HTML] (0) [PDF 160.29 K] (11357)
    Abstract:
    Objective To identify and analyze the volatile constituents in the leaves and fruits of Ficus carica. Methods Gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) were used. Results The major components detected in volatile oil of the leaves were psoralen (10.12%), β-damascenone (10.17%), benzyl alcohol (4.56%), behenic acid (4.79%), and bergapten (1.99%), etc. The major components detected in volatile oil of the fruits were furfural (10.55%), 5-methyl-2-furaldehyde (10.1%), and benzeneacetaldehyde (6.59%), etc. Conclusion A total of 121 volatile constituents are identified in the leaves and 108 in the fruits of F. carica, among which 103 constituents are identified for the first time in the leaves and 100 in the fruits. Eighteen volatile constituents are identified in both leaves and fruits.
    2010,2(4):272-288, DOI: 10.3969/j.issn.1674-6384.2010.04.005
    [Abstract] (3080) [HTML] (0) [PDF 307.65 K] (10506)
    Abstract:
    Callicarpa Linn. (beautyberry) is one of the major genera in Verbenaceous, about 20 of which are medicinal plants. Beautyberry, called Zizhu in China, is a generic name of those species and largely used as hemostatic medicine. The Chinese Pharmacopoeia 2010 has admitted three new crude drugs from the genus of Callicarpa Linn. including Callicarpae Macrophyllae Folium, Callicarpae Caulis et Folium, and Callicarpae Formosanae Folium for the first time since the 1977 version of the Chinese Pharmacopoeia. In order to better understand these new crude drugs, we systematically described their bibliography, admission reasons, botanical identification, chemistry, and pharmacology. Several other species, out of national regulations but intensively studied and widely used, are also covered in this review.
    2012,4(3):245-251, DOI: 10.3969/j.issn.1674-6384.2012.03.012
    [Abstract] (2347) [HTML] (0) [PDF 221.06 K] (10442)
    Abstract:
    Objective Establishing a ?ngerprint method to identify the characteristic chemicals in the roots of Gentiana macrophylla and evaluate their quality. Methods RP-HPLC was developed for ?ngerprint analysis and determination of four ingredients in G. macrophylla roots from different sources. LC-ESI-TOF-MS was employed to identify the chromatographic peaks of the ?ngerprint. Results Five common peaks were identified by comparing their retention time with reference secoiridoid glucosides. Eight major peaks in chromatographic fingerprint were analyzed by on-line LC-ESI-TOF-MS. Four secoiridoid glucosides were identified based on their MS data. Conclusion The method is specific and could be served for the quality identi?cation and comprehensive evaluation of G. macrophylla.
    2015,7(), DOI:
    [Abstract] (2191) [HTML] (0) [PDF 503.58 K] (10067)
    Abstract:
    Traditional Chinese medicine (TCM) has developed over thousands of years and has accumulated abundant clinical experience, forming a comprehensive and unique medical system. Emerging evidence has begun to illustrate TCM as an area of important medical rediscoveries. This paper briefly introduced the concept, significance, and technology of network pharmacology based on network biology and systems biology. It focused on the theoretical system and potential prospect of TCM network applied in TCM research and development including predicting new drug targets, action mechanism, new drug discovery; evaluating pharmacodynamics, pharmacokinetics, safety, toxicology, quality control, and bioinformatics of drugs. We also discussed the opportunities and challenges in the development and application of network pharmacology in the modernization of TCM research.
    [Abstract] (2155) [HTML] (0) [PDF 583.26 K] (9692)
    Abstract:
    Rhubarb is a perennial herb belonging to the genus Rheum L. (Polygonaceae). Rhei Radix et Rhizoma (rhubarb roots and rhizomes) is one of the most popular Chinese materia medica and has been widely used for strong laxative function. About 200 compounds with six different types of skeletons (anthraquinone, anthrone, stilbene, flavonoids, acylglucoside, and pyrone) have so far been isolated from eighteen species of the genus Rheum L. These constituents showed extensive pharmacological activities including cathartic, diuretic, anticancer, hepatoprotective, anti-inflammatory, and analgesic effects, as well as toxicological effects. Chemical fingerprint, LC-MS, and other analytical techniques have been used for the quality control of rhubarb. This comprehensive review summarizes the researches into the isolation, pharmacological activities, and phytochemical analysis reported since investigations began in the late 1940s. In addition, pharmacokinetic studies and clinical application of rhubarb are also discussed in present paper.
    2016,8(3):196-208, DOI: 10.1016/S1674-6384(16)60043-6
    Abstract:
    Chinese Pharmacopoeia is updated every five years, of which traditional Chinese medicine (TCM) is the most important part. The 2015 version completed by the 10th Pharmacopoeia Commission has come into operation since December 1, 2015. Here we introduced the revision and improvement of quality evaluation and control standards of TCMs in Chinese Pharmacopoeia 2015.
    2010,2(4):250-261, DOI: 10.3969/j.issn.1674-6384.2010.04.003
    [Abstract] (2928) [HTML] (0) [PDF 401.07 K] (8713)
    Abstract:
    For the protection of consumers and developments of relevant industry, authentication of medicinal plants is a critical issue. This review covers various aspects of authentication methods and techniques based on molecular biology and genomics with special emphasis on molecular biology techniques including genome-based authentication, microchip-based authentication, DNA barcoding, and their applications.
    2010,2(2):148-152, DOI: 10.3969/j.issn.1674-6384.2010.02.010
    [Abstract] (3369) [HTML] (0) [PDF 215.71 K] (8619)
    Abstract:
    Objective To develop an efficient method to isolate and purify the main components isoaloeresin D and aloin from Aloe vera for its industrial production. Methods High-speed counter-current chromatography was used to isolate isoaloeresin D and aloin in a one-step separation from dried crude extract of A. vera. The biphasic solvent system composed of hexane-ethyl acetate-acetone-water (0.2︰5︰1.5︰5) was used at a flow rate of 1.0 mL/min, while the lipophilic phase was selected as the mobile phase and the apparatus was rotated at 840 r/min. The effluent was detected at 254 nm. Results Isoaloeresin D (53.1 mg) and aloin (106.9 mg) were separated from the crude extract (384.7 mg) with the purities of 98.6% and 99.5%, respectively. Conclusion HSCCC is a powerful technique for isolation and separation of chemical composition from aloe.
    2011,3(2):150-155, DOI: 10.3969/j.issn.1674-6384.2011.02.011
    [Abstract] (2540) [HTML] (0) [PDF 157.86 K] (8008)
    Abstract:
    Objective Ginger (Zingiber officinale) is widely used as a spice in cooking and as a medicinal herb in traditional herbal medicine. The present study was to investigate the analgesic and anti-inflammatory activities of ginger oil in experimental animal models. Methods The analgesic effect of the oils was evaluated by the “acetic acid” and “hot-plate” test models of pain in mice. The anti-inflammatory effect of the oil was investigated in rats, using rat paw edema induced by carrageenan, adjuvant arthritis, and vascular permeability induced by bradykinin, arachidonic acid, and histamine. Indomethacin (1 mg/kg), Aspirin (0.5 g/kg) and Dexamethasone (2.5 mg/kg) were used respectively as reference drugs for comparison. Results The ginger oil (0.25-1.0 g/kg) produced significant analgesic effect against chemically- and thermally-induced nociceptive pain stimuli in mice (P < 0.05, 0.01). And the ginger oil (0.25-1.0 g/kg) also significantly inhibited carrageenan-induced paw edema, adjuvant arthritis, and inflammatory mediators-induced vascular permeability in rats (P < 0.05, 0.001). Conclusion These findings confirm that the ginger oil can be used to treat pain and chronic inflammation such as rheumatic arthritis.
    2015,7(), DOI:
    [Abstract] (1782) [HTML] (0) [PDF 273.72 K] (7839)
    Abstract:
    Cistanches Herba, a famous traditional Chinese materia medica, has a laudatory title “desert ginseng”. According to Chinese Pharmacopoeia 2000, Cistanches Herba is the dry fleshy stem with scale-like leaves of Cistanche deserticola. In order to expand the drug source, Chinese Pharmacopoeia 2005 increased the plants in Cistanche Hoffmg. et Link (Orobanchaceae), C. tubulosa, and dry scaly leaf succulent stems were as genuine Cistanches Herba and still in use. In order to have more comprehensive understanding on Cistanches Herba, this paper focuses the reviews on the biological characteristics, chemical constituents, and pharmacological activities of Cistanches Herba, and its development prospects are looked forward. It provides the relative theoretical basis for the subsequent research work of Cistanches Herba and can be conducive to the development and utilization of Cistanches Herba.
    2015,7(), DOI:
    [Abstract] (1772) [HTML] (0) [PDF 324.52 K] (7728)
    Abstract:
    Objective To predict the total flavonoids concentration of Aurantii Fructus fried with bran in its extraction process. Methods Ultraviolet spectrophotometry was used to determine the concentration of total flavonoids in different extraction time (t ) and solvent load (M ). Then the predicted procedure was carried out using the following data: 1) based on Ficks second law, the parameters of the kinetic model could be deduced and the equation was established; 2) Locally weighted regression (LWR) code was developed in the WEKA software environment to predict the concentration. And then we used both methods to predict the concentration of total flavonoids in new experiments. Results After comparing the predicted results with the experimental data, the LWR model had better accuracy and performance in the prediction. Conclusion LWR is applied to analyze the extraction process of Chinese herb for the first time, and it is totally fit for the extraction. LWR-based system is a more simple and accurate way to predict than the established equation. It is a good choice especially for a process which exists no clearly rules, and can be used in the real-time control during the process.
    2010,2(2):81-105, DOI: 10.3969/j.issn.1674-6384.2010.02.001
    [Abstract] (2851) [HTML] (0) [PDF 822.05 K] (7490)
    Abstract:
    Objective The 1-aminocyclopropanecarboxylic acid (ACPC) is a natural micromolecule non-protein amino acid that exists only in plants. Despite the determination of its regulating effects on plants, several bioactivities and effects on animals or humans are still unclear. This review focuses the pharmaceutical effects,above all, the neuroprotective effects of ACPC on the cerebro- and cardiovascular system. Methods Two hundred and seventy nine studies were selected and identified from a total of 2457 references in Medline and Chemical Abstracts from 1957 to 2008. Only 38 articles on neuroprotective effects of ACPC from seven different countries qualified to be included in the analysis. Results ACPC has altogether following six general neuroprotective effects on the brain and nervous system: anti-neurotoxicity induced by NMDA, dynorphin-A, glutamate, and morphine; protection from cerebral neurological injury induced by ischemia; antidepressant and anxiolytic effects; anti-convulsion and -seizures and control of epilepsy; facilitation of spatial learning and memory; and the effect of reducing alcohol consumption. Conclusion ACPC has shown a variety of effects on plants and animals. The bioactivities and pharmaceutical effects on animals are of great significance to medical research and public health. Further clinical trials or epidemiological studies are needed to determine its effect in humans. Food intervention with ACPC-rich vegetables and fruits may be a suitable therapy for cerebro- and cardiovascular system diseases. Administration of trace exogenous ACPC could produce vegetables and fruits of rich endogenous ACPC.
    2015,7(), DOI:
    [Abstract] (1960) [HTML] (0) [PDF 488.37 K] (7262)
    Abstract:
    Bentysrepinine (Y101), a derivative of repensine, is a novel di-peptide structure isolated from Dichondra repens. In vitro and in vivo tests exhibited that bentysrepinine markedly inhibited DNA-HBV and cccDNA activities. The binding mode of Y101 and repensine with DNA polymerase was driven by hydrophobic interactions. This might provide novel recognition of inhibitory effect of Y101 against HBV, though its inhibition mechanism needs to be validated by bio-assay at cellular level and of polymerase activity. Preliminary docking study suggested that Y101 might be able to inhibit HIV inverse transcriptase, also have the potential to interact with DNA polymerase and HCV NS5B polymerase.
    2011,3(2):117-126, DOI: 10.3969/j.issn.1674-6384.2011.02.006
    [Abstract] (3110) [HTML] (0) [PDF 211.05 K] (7194)
    Abstract:
    The reports on chemical constituents of Hyoscyamus niger were summarized. The compounds include alkaloids, saponins, lignans, coumarinolignans, flavonoids, and some other nonalkaloidal compounds. TLC, HPLC, and GC were used for the qualitative and quantitative analyses of some chemical constituents in H. niger. Modern pharmacological experiments showed that H. niger had the analgesic, anti-inflammatory, antipyretic, anticonvulsant, spasmolytic, antidiarrhoeal, antisecretory, bronchodilatory, urinary bladder relaxant, hypotensive, cardiosuppressant, vasodilator, antitumor, and feeding deterrent properties. In addition, the toxicities of this medicinal plant were also described.
    2015,7(), DOI:
    [Abstract] (1861) [HTML] (0) [PDF 299.63 K] (6986)
    Abstract:
    The inception of network pharmacology comes from the advance in “multi-target, multi-drug” paradigm and opens up a new field for pharmaceutical science. Traditional Chinese medicine (TCM) is well-known for its use of medicinal herb combinations to treat the functional disorders induced by diseases through a holistic view, which naturally followed the principal of network pharmacology. In this review, the methodologies of network pharmacology in TCM studies were summarized. Specifically, the methodologies for network construction and network analysis were detailed by following several TCM study cases followed. The perspectives for TCM network pharmacology were also provided.
    2015,7(), DOI:
    [Abstract] (1779) [HTML] (0) [PDF 360.32 K] (6926)
    Abstract:
    Objective A reversed-phase HPLC method was established for the simultaneous determination of five hydrophilic and lipophilic components in the roots of Salvia miltiorrhiza. Methods Hydrophilic components including danshensu, protocatechuic aldehyde, and salvianolic acid B, and lipophilic components such as cryptotanshinone and tanshinone IIA, were successfully separated on a Waters Symmetry C18 reverse- phase column (250 mm × 4.6 mm, 5 μm), with acetonitrile-0.5% phosphoric acid (gradient elution) as mobile phase, the detection wavelength was set at 281 nm with flow rate of 1.0 mL/min, and the column temperature was maintained at 30 °C. Results The recovery of the method was in the range of 95.1%–102.5% and the precision was less than 3% for all five analytes. All the compounds showed good linearity (R2 > 0.9990) in a relatively wide concentration range. Therefore, this HPLC method demonstrated good reproducibility, stability, and accuracy in validation studies. Conclusion Simultaneous quanti?cation of the multiple components by HPLC would be a better strategy for the quality evaluation on the roots of S. miltiorrhiza.
    [Abstract] (3365) [HTML] (0) [PDF 469.82 K] (6799)
    Abstract:
    This review is briefly to recall the history of research and development (R&D) of Chinese materia medica (CMM) and to discuss the challenges of Chinese traditional and herbal medicines (CTHM) facing the modern science and technology. The R&D of CTHM is thought to be an important pathway for new drug discovery. Since1949, about 140 approved new drugs have been developed, among which about 80 originated directly or indirectly from medicinal plants. CTHM has gained interest from the international medical, biomedical, and pharmaceutical institutions as a valuable source of potential medicines. For the modernization of CMM and innovative research of CTHM, there are following challenges to be faced: (1) to evaluate the efficacy, pharmacological properties, action mechanism, and active chemical constituents; (2) to develop new methodologies for the quality and safety of CTHM; (3) to apply new “-omics” techniques to accelerate drug discoveries developed from CTHM; and (4) to apply international practices including good agricultural practice, good manufacturing practice, good laboratory practice, and good clinical practice in the R&D of CTHM.
    2010,2(3):180-188, DOI: 10.3969/j.issn.1674-6384.2010.03.004
    [Abstract] (2023) [HTML] (0) [PDF 265.22 K] (6620)
    Abstract:
    The publications on the journal of Chinese Traditional and Herbal Drugs in Vol.40, 2009 are briefly reviewed in the categories of chemical constituents, preparations and technologies, analysis and quality control, pharmacological and clinical studies, reviews, and finally healthy principles. Some comments, especially for hot topics have been personally provided.

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