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Isatidis Radix is the dried root of the Isatis indigotica, with pharmacological effects such as heat-clearing and detoxification, cooling blood and pharyngeal relief, antibacterial and anti-inflammatory effects. It is often used clinically to prevent and treat influenza and other diseases. In this paper, relevant domestic and foreign literatures in recent years were summarized, and it was found that Isatidis Radix lignans, indole alkaloids, polysaccharides, etc. were the main active components against influenza virus. Then its pharmacological effects and the mechanism of action were reviewed, providing a basis for in-depth research on the antiviral effect of Isatidis Radix.
Subject(s)
Antiviral Agents/pharmacology , Drugs, Chinese Herbal , Isatis , Orthomyxoviridae , Plant Roots , PolysaccharidesABSTRACT
Trading volume in Chinese medicinal materials market has gradually declined, and origin market trade has become a trend. Studying the degree of market integration is helpful to understand the operation of origin market of Chinese medicinal materials, which is of great significance for rational planning of the production of Chinese medicinal materials and improving market efficiency. In this study, four varieties (Lonicerae Japonicae Flos, Lycii Fructus, Isatidis Radix and Pseudostellariae Radix) were selected to study the market integration degree of Chinese medicinal materials. Based on the price index data from 2013 to 2019, this paper makes an empirical analysis by using co-integration test, error correction model and Granger causality test. The results showed that the long-term integration of Chinese medicinal materials market was relatively high, but the short-term integration was far lower than the long-term integration. Finally, the author puts forward four policy suggestions: improving the price information platform conduction of Chinese medicinal materials, building high-quality brand of Chinese medicinal materials in non-authentic producing areas, speeding up the establishment quality traceability system and building modern logistics system of Chinese medicinal materials.
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Objective: To establish a method for the determination of fractal dimension of ethanol precipitation flocs in two kinds of root medicinal herbs (Astragali Radix and Isatidis Radix). Method: The ethanol-precipitated flocs of Astragali Radix and Isatidis Radix were taken as the research objects. Firstly, the original microscopic images of the ethanol precipitation flocs were binarized by Ostu algorithm. Secondly, the influence of sampling volume, dilution multiple, image magnification ratio and number of image acquisition sites on fractal dimension was investigated using perimeter-area method. Result: The ethanol precipitation flocs of Astragali Radix and Isatidis Radix had fractal characteristics. At the same time, the stable and reliable fractal dimension of the flocs could be obtained when the sampling volume was 600-800 μL, the sample was diluted to 5-20 times, the microscopic image was enlarged to 200 times or 400 times, and four different image acquisition sites were selected. Conclusion: The established method is stable and feasible, which can provide reference for the fractal theory of ethanol precipitation flocs of root medicinal herbs.
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OBJECTIVE@#To investigate anti-inflammatory and immunomodulation effects of different ecotype from Isatidis Radix growing in Gansu province.@*METHODS@#Mice were randomly divided into 6 groups (=11)and used the auricular swelling and paw edema to observe the anti-inflammatory effects of Isatidis Radix; Mice were randomly divided into 7 groups (=11) and through the gasbag synovitis model to observe the anti-inflammatory effects of Isatidis Radix; Mice were randomly divided into 6 groups (=11), the immunosuppressed model were established by injection of cyclophosphamide (CTX) to study the effects of Isatidis Radix on index of thymus, blood routine and cytokines.@*RESULTS@#Gansu different ecotype from Isatidis Radix could reduce the swelling of the mice auricle, paw edema and total protein, leukotriene B(LTB)and malonaldehyde(MDA) in airbag synovitis exudates, and upgrade serum levels of superoxide dismutase (SOD); Degrade the tumor necrosis factor-α (TNF-α) and upgrade the index of thymus, the number of red and white corpuscles, the level of interferon-γ (IFN-γ), interleukin-4 (IL-4) (<0.05, 0.01) of mice immunosuppressed model; Above the research of anti-inflammatory and immunomodulation, there were no significant differences between Isatidis Radix of Gansu different ecotype and tetraploid.@*CONCLUSIONS@#Different ecotype of Isatidis Radix has obvious functions in anti-inflammatory and immunomodulation, but there are no significant differences between Gansu different ecotype and tetraploid.
Subject(s)
Animals , Mice , Anti-Inflammatory Agents , Pharmacology , China , Cytokines , Allergy and Immunology , Drugs, Chinese Herbal , Pharmacology , Ecotype , Immunomodulation , Isatis , Chemistry , Plant Extracts , Pharmacology , Random AllocationABSTRACT
Objective:To optimize the flash extraction process of Isatidis Radix by Box-Behnken experimental design. Methods:A flash extraction method was used with the extraction voltage, material-liquid ratio and extraction time as the independent variables. A Hassan’s method was used to calculate the normalized value(OD) of comprehensive evaluation of the dry extract yield and the epi-goitrin extraction rate in order to establish the mathematical relationship between the comprehensive evaluation OD and the independent variables, and the response surface method was used to predict the best process conditions. Results:The optimum process conditions were as follows:voltage of 88 V, material-liquid ratio of 19. 62, and extraction time of 2. 03 min. The rate of dry extract and epigoitrin extraction was 37. 902% and 0. 1887%, respectively. Conclusion:The measured value is close to the predicted one,which indicates the comprehensive flash extraction parameters optimized by Box-Behnken experimental design can be used for the extraction for Isatidis Radix.
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Objective To investigate the antiviral activity and chemical composition of n-butanol extract of Isatidis Radix. Methods Each component of total n-butanol extracts was detected by solvent and chromatogram, the anti-HSV-1 activities of each component were detected by MTT assay in vitro, each component of total n-butanol extracts was analyzed by CUPLC-Q-TOF-MS, and the data were analyzed by Markview and Excel software to find the difference among different components. According to statistics, the components related to antivirus activities were obtained. Results According to the similarity of chemical composition, 20 components were extracted and separated from n-butanol extract of Isatidis Radix by chromatography, and 10 components had antiviral activity. Forty-four chemical components were detected by UPLC-Q-TOF-MS from n-butanol extracts and their chemical structures were confirmed. Difference analysis of chemical components discovered 15 chemical components such as alkaloids, organic acids, sugars and amino acid derivatives associated with antiviral activity, especially 1-methoxy-3-carbaldehyde, 3-(3’,5’-dimethoxy- 4’-hydroxy)-2-indolinone, 1-methoxy-3-indolinone, 3-(methylsulfinyl) propylglucosinolate, and glucosamine-6-phosphatee in higher levels of the active components, which was worth further study. Conclusion The n-butanol extract of Isatidis Radix mainly contains indole alkaloids, organic acids, nucleosides and amino acids, wherein the single-indole, a sulfur glycosides and sugars and amino acid derivatives are closely related to the antiviral activity.
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Objective To evaluate the quality of Isatidis Radix from different ecotypes by using projection pursuit model. Methods Totally 11 batches of Isatidis Radix from different ecotypes in Gansu Province were used as evaluation samples. With the contents of epigoitrin, uridine, guanosine, adenosine, benzoic acid, salicylic acid, indigo, indirubin, and alcohol extract as evaluating indexes, combined with projection pursuit model established by DPS V 9.50 statistics software, the quality of Isatidis Radix was evaluated. Results Based on the evalution of nine main indexes, quality order of the 11 batches of Isatidis Radix was acquired: S2>S1>S9>S7>S8>S3>S5>S10>S11>S4>S6. Conclusion The projection pursuit model was available for the quality evaluation of different ecotype Isatidis Radix. The quality of Isatidis Radix from different ecotypes is different significantly, and the quality of tetraploid Isatidis Radix of Shijiazhuang is the best.
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AIM To observe the effects of aqueous extract of Isatidis Radix (AEIR) on formation of hyperlipidemia in rats.METHODS Seventy-two male SD rats were randomly divided into six groups,normal control group,model group,AEIR low-dose (20 mg/kg),middle-dose (40 mg/kg),high-dose (80 mg/kg)groups and fenofibrate (20 mg/kg) group.Drugs were intragastrically administered for 40 days,body weights were recorded every five days.The rats in the normal control group were fed with ordinary diet,those in the other five groups were fed with high fat diet.At the end of experiment,the rats were killed,then ratio of fat weight to body weight,serum lipid level,LPL,HL,MDA and SOD were detected.The pathological changes of liver tissue were observed by light microscope.RESULTS AEIR significantly decreased body weight,fat weight and ratio of fat weight to body weight;significantly reduced the levels of TC,TG and LDL;significantly enhanced the activities of LPL and HL;significantly decreased MDA content and increased SOD activity in serum and liver tissue.Compared with the model group,the adipose degeneration of liver tissue in the various AEIR groups and fenofibrate group was improved.CONCLUSION AEIR can prevent the formation of hyperlipidemia in rats by regulating lipid metabolism.
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Isatidis Radix,the root of Isatis indigotica Fort.(Cruciferae),is a representitive herb widely used for clearing away heat-toxin in traditional Chinese medicine (TCM).Lariciresinol is a representitive component of lignans and an important efficacious substance with the antiviral effect.This review elucidated the progress on its biosynthetic pathways,the screening of key regulatory genes and metabolic engineering of lignans components in Isatidis Radix,providing a favorable reference for the full understanding of biosynthesis of antiviral active components,the quality improvement of Isatidis Radix and the sustainable utilization of TCM resources.
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Objective: To explore the bidirectional solid fermentation transformation of 25 different edible fungal strains with Isatidis Radix (IR) and Isatidis Folium (IF) to get the synergism antibacterial effect of fermentation substance. Methods: The dominant strains grown on IR and IF were obtained through initial screening and repeated screening. The antibacterial effect of fermentation product substance were determined by antibacterial test and TLC. Results: The results showed that repeated screening got three strains which could grow fast in IR (G-11, G-13, and G-7) and IF (G-2, G-11, and G-3). The G-3 strain and G-11 strain fermentation substance had better antibacterial effect than IR and IF respectively. The methanol extract of G-2 fermented IF substance appeared a new spot by TCL, it should be an additional component after fermentation. Conclusion: The bidirectional solid fermentation could improved antibacterial effect of IR and IF, and the new active ingredients can be produced.
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Objective To observe the effects ofTrametes robiniophila Murr and Isatidis Radix bidirectional fermentation products on the migration and invasion of human breast cancer MCF-7 cells and relevant factors; To discuss relevant mechanism of action.Methods Breast carcinoma cell line MCF-7 was used as research subject in this experiment. Control group, Isatidis Radix group,Trametes robiniophila Murr group, andTrametes robiniophila Murr and Isatidis Radix group were included in the experiment. The effects ofTrametes robiniophila Murr and Isatidis Radix bidirectional fermentation products on MCF-7 cell proliferation were measured by MTT method. Cell scratch assay, transwell assay and adhesion assay were used to measure the effects ofTrametes robiniophila Murrand Isatidis Radix bidirectional fermentation products on the migration, invasion and adhesion capability of MCF-7 cells, respectively. The effects ofTrametes robiniophila Murrand Isatidis Radix bidirectional fermentation products on the mRNA expression of MMP-9 and Vimentin were measured by RT-PCR.Results Compared with Isatidis Radix group andTrametes robiniophila Murrgroup, Trametes robiniophila Murr and Isatidis Radix bidirectional fermentation products could significantly inhibit the proliferation, migration, invasion and adhesion capability of MCF-7 cells (P<0.05). Similarly,Trametes robiniophila Murr and Isatidis Radix bidirectional fermentation products reduced the mRNA expression of MMP-9 and Vimentin (P<0.05).ConclusionTrametes robiniophila Murrand Isatidis Radix bidirectional fermentation products may down-regulate the expression of MMP-9 and Vimentin to inhibit the migration, invasion and adhesion capabilities of MCF-7 cells.
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Objective Currently, powdered Chinese herbal medicines (CHMs) were mainly evaluated through physical property, chemical dissolution, and bioactivity independently. It could not reflect the quality comprehensively. This paper was to explore and establish a comprehensive evaluation method for powdered CHMs. Methods Isatidis Radix was chosen as an exemple. Firstly, powdered Isatidis Radix in different particle size was prepared. Then, their physical properties were characterized. The dissolution of index component epigoitrin was determined, and their antiviral activities were evaluated by neuraminidase-based bioassay. Results As the particle size decreased, powder distribution tended to be uniform, and the dissolution of epigoitrin increased, antiviral activity enhanced. According to cluster analysis of above results, the sequence of evaluation consequence was ultrafine powder S2 (D90: 32.80 ± 0.29) > ultrafine powder S1 (D90: 52.08 ± 0.53) > fine powder S0 (D90: 118.16 ± 0.76) (from the superior to the inferior). Conclusion Overall, the comprehensive evaluation for powdered CHMs based on the physical characterization, chemical dissolution, and bioassay could not only be used to evaluate powdered herbs, but also guide the screening and optimization of the particle size of powder.
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Objective To identify Isatidis Radix in different areas by SDS-PAGE;To provide the basis for the identification and quality evaluation of Isatidis Radix. Methods By using SDS-PAGE technology, the protein profiles of Isatidis Radix in Heilongjiang and Hebei regions were established. Results Isatidis Radix protein in Heilongjiang contained about 13 protein subunits, and the major subunits were 10.5 kD, 23.0 kD, 24.9 kD, and 44.1 kD. Isatidis Radix protein in Hebei contained about 12 subunits, and the major subunits were 55.6 kD, 45.9 kD, 34.3 kD, 18.9 kD, 12.4 kD, and 10.5 kD. Conclusion SDS-PAGE technology can be used as one of the references to identify Isatidis Radix in different areas.
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OBJECTIVE: To establish a high performance capillary electrophoresis( HPCE) method for simultaneous determination of seven nucleosides, including epigoitrin, uracil, thymine, adenosine, hypoxanthine, guanosine and uridine in Isatidis Radix. METHODS: The chromatographic separation was performed on an uncoated fused silica capillary(75 μm × 64.5 cm, 56 cm of effective length) with separation voltage of 20 kV. 60 mmol · L-1 Na2B4O7-15 mmol · L-1 β-CD was selected as the running buffer solution(pH 9.6). The detection wavelength was set at 254 nm. The sample was injected at 5 kPa × 5 s and column temperature was maintained at 25°C. RESULTS: The calibration curves of the seven nucleosides showed good linearity (r > 0.9994). The average recoveries of the method were between 97.15%-100.40%. The contents of the seven nucleosides in Isatidis Radix samples of different batches were different. CONCLUSION: The established method is simple, accurate and can be used for the quality control of Isatidis Radix.
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Objective: To observe the anti-inflammatory and analgesic activities of the different fractions from Isatidis Radix. Methods: The anti-inflammatory effects were observed by a in vitro model of LPS-stimulated RAW264.7 macrophages, and the analgesic effects were evaluated by the writhing test and the tail-immersion test in mice. Results: The water extract, 30%, 50%, and 70% ethanol extracts of Isatidis Radix all had anti-inflammatory and analgesic activities. The 50% and 70% ethanol extracts were the main anti-inflammatory effective fractions. The water extract and 70% ethanol extract were the main analgesic effective fractions. Conclusion: Different fractions of Isatidis Radix all have anti-inflammatory and analgesic activities, and the 70% ethanol extract has stronger activities. The mechanism of the anti-inflammatory and analgesic activities of the 70% ethanol extract may be related to the inhibition of the release of TNF-α and PGE2 from macrophages.
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Objective To establish a HPLC method for simultaneous determination of uracil,hypoxanthine,guanosine, thymine,and( R,S)-goitrin in Isatidis Radix. Methods The determination was performed on a Hanbon Hedera C18 column (4. 6 mm×250 mm,5 μm). The mobile phase consisted of acetonitrile( A)and water( B)with linear gradient elution at the flow rate of 1.0 mL·min-1. The column temperature was 30 ℃. Detection wavelength was 254 nm. Results The linear range of uracil,hypoxanthine,guanosine,thymine,and(R,S)-goitrin was 1.97-39.40 mg·L-1(r=0.999 9),1.25-50.00 mg·L-1(r=0.999 9),0.25-10.40 mg·L-1(r=0. 999 6),2. 84-56. 70 mg·L-1(r=0. 999 9),and 0. 72-28.80 mg·L-1(r=0.999 8), respectively. The average recovery was 99. 36%(RSD=0. 91%),99. 79%(RSD=1. 12%),100. 90%(RSD=1. 71%),98. 67%(RSD=1. 50%),and 99. 33%(RSD=0. 94%),respectively. Conclusion The method is simple,accurate,reliable,reproducible and sensitive,which can be used as an effective method for quality control of Isatidis Radix.
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Objective: To study the active components with anti-bacterial effect in Isatidis Radix. Methods: Using cylinder-plate method with bacteriostatic coefficient as the index, the anti-Escherichia coli AG100A effects of five extracts (total extract, tatal organic acid extract, total alkaloids extract, tatal nudeoside extract, and total anthraquinone extract) from Isatidis Radix were studied. After the determination of the most active extract, HPLC fingerprints on 10 batches of Isatidis Radix from different habitats were established. The correlations between areas of common peaks and bacteriostatic coefficients were analyzed by principal component analysis (PCA). Results: The total organic acid extract showed the best anti-bacterial effect, with 21 common peaks in HPLC fingerprint. The results of the PCA demonstrated that the common peaks 2, 10, 16, 18, 20, and 21 were connected closely with the antibacterial activity, among which the common peaks 10 and 18 were proved to be salicylic acid and benzoic acid, respectively. Conclusion: The total organic acid extract from Isatidis Radix shows the significant antibacterial effect, in which salicylic acid and benzoic acid are the active chemical constituents with the antibacterial activity.
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Objective: To study the chemical constituents in the antiviral fraction of Isatidis Radix and the activity of the monomer components. Methods: The water extract of Isatidis Radix was adsorbed by macroporous resin, and the antiviral fraction was eluted with 10% and 50% ethanol, repeatedly separated and purificated by silica gel column chromatography, reverse phase silica gel column chromatography, and Sephadex LH-20. The chemical structures were identificated using physicochemical constants and spectral data. Results: Ten compounds were isolated from the active fraction of water extract, and they were respectively identified as syringin (1), 4-(1, 2, 3-trihydroxypropyl)-2, 6-dimethoxyphenyl-1-O-β-D-glucopyranoside (2), isolariciresino (3), isolariciresinol 4-O-β-D-glucopyranoside (4), lariciresinol-4-O-β-D-glucopyranoside (5), lariciresinol-4, 4'-bis-O-β-D-glucopyranoside (6), 2-hydroxy-1, 4-benzenedi carboxylic acid (7), D-mannitol (8), indole-3-acetonitrile6-O-β-D-glucopyranoside (9), and 3-[2'-(5'-hydroxymethyl) furyl]-1(2H)-isoquinoline-7-O-β-D-glucopyranoside (10). Conclusion: Compounds 2, 4, 7, 8, and 10 are isolated from Isatidis Radix for the first time. Compound 10 has the significant effect of anti-HSV-2 virus. Therapeutic index (TI) is 6.07. Compounds 1, 5, and 6 also show some inhibition to HSV virus.
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Objective To study the active components in Isatidis Radix with agglutination effect on red blood cells. Methods The different extracts from Isatidis Radix were obtained by the means of systematic solvent extraction and their antivirus activity was studied by hemagglutination test. The HPLC fingerprints of the most active extracts from Isatidis Radix were established and also the extracts were bioassayed. The spectrum-activity relationship of the extracts was studied by mathematical statistics method. Results The n-butanol extracts had the best agglutination effect on red blood cells of the rabbit. The study on the spectrum-activity relationship of the extracts found that the greater the proportional area of common peaks 2 and 11 (retention time were 7.23 and 43.00 min) of the extracts had, the stronger the agglutination effect of the extracts had. Conclusion Common peaks 2 and 11 could be characteristic peak for anti-virus activity of Isatidis Radix. The spectrum-activity relationship of Isatidis Radix established could provide the theoretical basis and the data support for the pattern of quality control of Chinese materia medica.
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Objective: To establish and optimize a bio-evaluation method based on antiviral activity detection for Isatidis Radix quality control. Methods: According to the fact that antivirus activity is the main pharmacological effect of Isatidis Radix, the means of hemagglutination activity detection and the means of influenza virus neuraminidase (NA) activity detection were used for establishing two antiviral activity detection methods for the bio-evaluation of Isatidis Radix. In addition, contrastive analyzation and optimization of the two methods were carried out in this study. Results: The two methods could be used to evaluate and distinct the biological activities of different batches of Isatidis Radix samples and both methods have good repeatabilities (RSD = 7.0% and 5.78%). The result shows a good correlation (P<0.01, r = -0.81) between the neuraminidase inhibitory activity and the hemagglutination activity of Isatidis Radix. The relationship between agglutination activity and antiviral effect of Isatidis Radix was further verified. Agglutination detection method has the superiority to its safety, inexpensiveness, easiness, and practicality. Conclusion: This novel method could reflect the pharmacodynamic activity of Isatidis Radix on anti-influenza virus and be helpful for the quality control of Isatidis Radix. This study provides reference for the bio-evaluation on the quality control of Chinese materia medica.