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Dioscoreae Rhizoma formula granules are made from decoction pieces by decocting， extracting， separating， concentrating， drying and granulating， which have the advantages of simple dispensing， convenient use and easy to take without decoction. However， because Dioscoreae Rhizoma is rich in starch and mucus components， its extract powder and formula granules are poorly soluble and difficult to dissolve or disperse completely within 5 min， and the insoluble material is difficult to dissolve completely even after 24 h in water， which affects the quality evaluation of the formula granules and medication psychology of patients. Therefore， by studying the dissolution process and mechanism of Dioscoreae Rhizoma extract and its formula granules， it was found that the special chemical composition of Dioscoreae Rhizoma， the denaturation of starch and its compounding with protein and other substances during the high temperature extraction process， and the contraction of coating membrane during the spray drying process were combined to form the special microstructure of coating membrane covering starch granules， and it is the root cause of poor solubility of Dioscoreae Rhizoma formula granules. Based on the research on the structure， property and function of the powder， this paper proposed a technical strategy to improve the solubility of Dioscoreae Rhizoma formula granules by powder modification process， and experimentally demonstrated that the modified Dioscoreae Rhizoma formula granules could completely dissolve within 2 min， which solved the technical problem and could provide reference for the improvement of solubility of other similar varieties， and promote the high-quality development of traditional Chinese medicine formula granule industry.
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ABSTRACT Introduction: Joint strength of the lower limbs plays a decisive role in the competitive ability of long jumpers. Special strength training based on science and targeted at the strength of the lower limb joints is an essential topic for long jumpers. Objective: To analyze isokinetic muscle strength characteristics of lower limb joints in long jumpers. Methods: Voluntary jumpers were submitted to isokinetic concentric contraction tests of the lower limbs and hip joints. We also analyzed the effect of strength training on lower limb joint injury. Results: The knee muscles of the athletes have reduced eccentric contractility. The ankle of the athlete has the most vulnerable joint to injuries in the sport. Conclusion: The explosive force and eccentric contractility of long jumpers' lower limb extensor muscles have the most significant impact on joint thrust and extension speed. Athletes need muscle strength training to develop isokinetic muscle strength. This can effectively prevent injury to lower extremity joint movements. The research findings of this paper can provide a specific theoretical basis for formulating scientific training for long jumpers. Level of evidence II; Therapeutic studies - investigation of treatment outcomes.
RESUMO Introdução: A força conjunta dos membros inferiores desempenha um papel decisivo na capacidade competitiva nos saltadores de salto em distância. O treinamento de força especial baseado na ciência e direcionado para a força das articulações dos membros inferiores é um tópico essencial para os saltadores. Objetivo: Analisar as características de força muscular isocinética das articulações dos membros inferiores em saltadores de salto em distância. Métodos: Saltadores voluntários foram submetidos à testes de contração concêntrica isocinética dos membros inferiores e articulação do quadril. Efetuou-se também a análise do efeito do treinamento de força na lesão das articulações dos membros inferiores. Resultados: Os músculos dos joelhos dos atletas têm uma contratilidade excêntrica reduzida. O tornozelo dos atletas possui a articulação mais vulnerável a lesões no esporte. Conclusão: A força de explosão e a capacidade de contração excêntrica dos músculos extensores dos membros inferiores dos saltadores de salto longo têm o impacto mais significativo no empuxo das articulações e na velocidade de extensão. Os atletas precisam de treinamento de força muscular para desenvolver a força muscular isocinética. Isto pode efetivamente evitar lesões nos movimentos das extremidades inferiores das articulações. Os resultados da pesquisa deste trabalho podem fornecer uma base teórica específica para a formulação do treinamento científico para os saltadores de salto longo. Nível de evidência II; Estudos terapêuticos - investigação dos resultados do tratamento.
RESUMEN Introducción: La fuerza articular de los miembros inferiores desempeña un papel decisivo en la capacidad competitiva de los saltadores de longitud. El entrenamiento de fuerza especial basado en la ciencia y dirigido a la fuerza de las articulaciones de los miembros inferiores es un tema esencial para los saltadores. Objetivo: Analizar las características de la fuerza muscular isocinética de las articulaciones de los miembros inferiores en saltadores de longitud. Métodos: Los saltadores voluntarios fueron sometidos a pruebas de contracción concéntrica isocinética de los miembros inferiores y de las articulaciones de la cadera. También se realizó un análisis del efecto del entrenamiento de fuerza en las lesiones de las articulaciones de los miembros inferiores. Resultados: Los músculos de la rodilla de los atletas tienen una contractilidad excéntrica reducida. El tobillo de los atletas tiene la articulación más vulnerable a las lesiones en el deporte. Conclusión: La fuerza de explosión y la contractilidad excéntrica de los músculos extensores de las extremidades inferiores de los saltadores de longitud tienen el impacto más significativo en el empuje articular y la velocidad de extensión. Los atletas necesitan entrenar la fuerza muscular para desarrollar la fuerza muscular isocinética. Esto puede prevenir eficazmente las lesiones en los movimientos de las articulaciones de las extremidades inferiores. Los resultados de la investigación de este trabajo pueden proporcionar una base teórica específica para la formulación del entrenamiento científico de los saltadores de longitud. Nivel de evidencia II; Estudios terapéuticos - investigación de los resultados del tratamiento.
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TGR5 is a bile acid-activated G protein-coupled receptor and plays an important role in the physiological and pathological processes of the biliary system. This article describes the normal expression of TGR5 in the liver and bile duct under normal physiological conditions and its functions including the regulation of bile acid secretion and metabolism and cytoprotection. This article also summarizes the changes in the expression and function of TGR5 under pathophysiological conditions and the mechanism of TGR5 in affecting the development and progression of biliary tract diseases through inflammatory response and cell proliferation and apoptosis. TGR5 may be a potential target for the treatment of biliary tract diseases in the future.
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ObjectiveTo explore the pharmacodynamic ingredients of Zhenqi Fuzheng granules （ZFG） for immunomodulatory through spectrum-effect relationship analysis， which provides experimental basis for improving the quality standard of ZFG. MethodEighteen batches of ZFG from six manufacturers were collected for analysis. The fingerprints were established by high performance liquid chromatography （HPLC）. Acetonitrile （A）-0.1% formic acid aqueous solution （B） were adopted as the mobile phase with gradient elution （0-15 min， 5%A； 15-23 min， 5%-8%A； 23-30 min， 8%-11%A； 30-45 min， 11%-18%A； 45-60 min， 18%-21%A； 60-67 min， 21%-23%A； 67-90 min， 23%-37%A）， the detection wavelength was 220 nm. Chemometric analysis such as similarity analysis and hierarchical cluster analysis （HCA） were subsequently used to analyze the similarities and chemical differences among these samples. A cyclophosphamide-induced immunodeficiency mouse model was used to evaluate the immune-enhancing effects of the products from different manufacturers. The spectrum-effect relationship between HPLC fingerprints and the immunomodulatory effects was examined using Spearman bivariate correlation analysis. HPLC coupled with mass spectrometry （HPLC-MSn） was used to identify the spectrum-effect related peaks with electrospray ionization， positive and negative ion modes， and scanning range of m/z 100-1 500. ResultThe HPLC fingerprint of ZFG was established， and twenty peaks with good resolution were selected as common peaks. The results of quality analysis and pharmacodynamic test showed there were significant differences in both ingredients content and immune-enhancing effects of ZFG from different manufacturers. Through spectrum-effect relationship study， twelve peaks were screened as bioactive ingredients peaks. Thereafter， eight peaks among them were subsequently identified by HPLC-MSn. They were salidroside （peak 2）， echinacoside （peak 5）， calycosin-7-glucoside （peak 6）， isomer of specnuezhenide （peak 7）， isonuezhenide （peak 9）， calycosin （peak 11）， nuezhenide G13 or oleonuezhenide （peak 14）， and formononetin （peak 18）， respectively. ConclusionThere are differences in quality and efficacy of ZFG produced by different manufacturers. Through spectrum-effect relationship analysis， the medicinal ingredients of ZFG for immune-enhancing effects are screened， which can provide reference for the improvement of its quality standard.
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OBJECTIVE To study the effects of Wenyang huazhuo tongluo formula conta ined serum on the expression and methylation of retinoic acid related nuclear orphan receptor （RORγt），and to explore the mechanism of its regulation of Th 17 cell proliferation in the treatment of scleroderma. METHODS Wistar rats were given 15，30，60 g/（kg·d）Wenyang huazhuo tongluo formula intragastrically to prepare different doses of drug-contained serum ，and peripheral blood of scleroderma patients were collected to sort Th 17 cells. Using blank serum as blank control ，methyltransferase inhibitor decitabine （DCA）as positive control ， Th17 cells were treated with different concentrations of drug-contained serum ，and then the proliferation of Th 17 cells was detected by CCK- 8；mRNA expressions of RORγt and IL-17 were detected by qRT-PCR ，and the protein expression of RORγt was detected by Western blot assay ；the protein expression of IL- 17 in the cell supernatant was detected by ELISA ，and the methylation level of RORγt gene promoter was detected by methylation-specific PCR. The transcriptional activity of RORγt gene promoter was detected by dual-luciferase assay. RESULTS Compared with blank control ，Wenyang huazhuo tongluo formula contained serum and DCA could inhibit the proliferation of Th 17 cells（P＜0.05），reduced the mRNA and protein expressions of RORγt and IL-17，enhanced the methylation level of RORγt gene promoter and attenuated ， the transcription activity of RORγt gene promoter. Except for mRNA expression of Th 17 and the methylation level of RORγt gene promoter in drug-contained serum low-dose group ，there were statistical significance in above indexes of other groups（P＜0.05）. CONCLUSIONS Wenyang huazhuo tongluo formula can promote the methylation lev el of RORγt gene，and inhibit the expression of RORγt and the secretion of IL-17，so as to inhibit the proliferation of Th 17 cells.
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Objective: To assess the incidence of symptomatic torus tubarius hypertrophy (TTH) in recurred OSA in children, and to explore the preliminary experience of partial resection of TTH assisted with radiofrequency ablation. Methods: From January 2004 to February 2020, 4 922 children, who diagnosed as OSA and received adenotonsillectomy at the Department of Otolaryngology, The 4th Medical Center of the PLA General Hospital, were retrospectively reviewed. There were 3 266 males and 1 656 females, the age ranged from 1 to 14 years old(median age of 5.0 years). Twenty-two cases were identified with recurrence of OSA syndrome, and the clinical data, including sex, age of primary operation, age of recurrence and presentation, and opertation methods were analyzed. Follow-up was carried out by outpatient visit or telephone. Graphpad prism 5.0 software was used for statistical analysis. Results: Twenty-two cases were identified as recurred OSA and received revised surgery in 4 922 cases. Among these 22 cases, 11 cases were diagnosed as TTH resulting in an incidence of 2.23‰(11/4 922), 1 case was cicatricial adhesion on tubal torus (0.20‰, 1/4 922), 10 cases were residual adenoid combined with tubal tonsil hypertrophy (2.03‰, 10/4 922). Median age of primary operation was 3.0 years (range:2.4 to 6.0 years) in 11 TTH cases. Recurrent interval varied from 2 months to 5.5 years (2.4±1.9 years) after first operation. Age of revised partial resection of TTH was 7.0±2.7 years (range: 4.0 to 12.0 years). Average time interval between primary operation and revised operation was 3.5±2.1 years (range: 0.5 to 6.0 years). Individualized treatments were carried out based on partial resection of TTH assisted with radiofrequency ablation. All of 11 cases received satisfied therapeutic results without nasopharyngeal stenosis occured. Twenty-two cases were followed up for 1.6 to 13 years (median follow-up time was 6.2 years). Conclusions: TTH contributed to recurred OSA in child. TTH might be misdiagnosed as tubal tonsil hypertrophy. Partial resection of TTH assisted with radiofrequency ablation was a safty and effective treatment.
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Adolescent , Child , Child, Preschool , Female , Humans , Infant , Male , Adenoidectomy , Adenoids/surgery , Hypertrophy/surgery , Retrospective Studies , Sleep Apnea, Obstructive/surgeryABSTRACT
Phyllanthi Fructus, a unique Chinese and Tibetan medicinal plant with both edible and medical values, has high potential of cultivation and development. The resources of Phyllanthi Fructus in China are rich, mainly distributed in Yunnan, Sichuan, Fujian, Guangdong, Guangxi, etc. Phyllanthi Fructus is widely used in the clinical practice of Chinese medicine and plays an important role in Tibetan medicine, Uyghur medicine, Yi medicine, and Mongolian medicine. Phyllanthi Fructus mainly contains phenolic acids,tannins, terpenes, sterols, fatty acids, flavonoids, amino acids and other compounds. Modern pharmacological studies show that Phyllanthi Fructus has antioxidant, anticancer, blood lipid-lowering, liver protective, antimicrobial, anti-inflammatory, and immune regulatory activities. In this paper, the research status of Phyllanthi Fructus was reviewed from the aspects of herbal textual research,chemical composition, and pharmacological action. The quality markers(Q-markers) of Phyllanthi Fructus were predicted and analyzed from the aspects of biogenic pathway, specificity and measurability of chemical components, efficacy, properties, new clinical uses, drug-food homology, and transformation of polyphenols. The results will provide a scientific basis for the quality control, quality evaluation, and standard formulation of Phyllanthi Fructus.
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China , Drugs, Chinese Herbal , Fruit , Medicine, Tibetan Traditional , Quality ControlABSTRACT
Phyllanthus emblica is a kind of traditional medicine and medicinal and edible plant, with rich variety resources and high development value. It is a key poverty alleviation variety in China at present. As P. emblica processing industry is rising gradually in recent years, in order to fully develop and utilize its industrial resources, this paper systematically introduces current comprehensive development and utilization of P. emblica, discusses the problems in P. emblica processing industry, and puts forward comprehensive development and utilization strategies and industrial models in terms of cultivation, breeding, grading, quality evaluation and waste recycling, so as to provide a certain reference for promoting the high-quality development of P. emblica industry in China.
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China , Medicine , Medicine, Traditional , Phyllanthus emblica , Plant Breeding , Plant ExtractsABSTRACT
Objective:Through the establishment and application of the biosafety autopsy pathology platform in Huoshenshan Hospital, the feasibility and application effect of the biosafety autopsy pathology platform were analyzed.Methods:The feasibility and application effect of the biosafety autopsy pathology platform were analyzed by layout design, instruments and equipment preparation, testing methods examination, and effect evaluation.Results:A total number of 26 cases of systematic autopsy and 8 cases of minimally invasive autopsy (puncture) were performed on the biosafety autopsy pathology platform, and no one was infected. Some pathology original findings were identified, including COVID-19 and pathological characteristics of identification, SARS respiratory failure mechanism and treatment significance, systemic distribution and spreading mechanism of the new coronavirus, the " storm" of inflammation pathological basis, some tumor markers rise in pulmonary pathological cell source and the overcast with fibrosis characteristics, such findings play important roles in the clinical diagnosis and treatment of COVID-19.Conclusions:The study of autopsy pathology is of great significance for the prevention and control of emerging infectious disease, which calls for early intervention. To promote the standard construction of biosafety autopsy platform is the key to the pathological study of emerging infectious diseases. Pathological research and clinical diagnosis and treatment should be combined to inform each other.
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Objective:To compare the embedding anastomosis with the intermittent eversion anastomosis on the pancreatic fistula rates after laparoscopic pancreaticoduodenectomy (LPD).Methods:The clinical data of 116 patients who underwent LPD at the Center Hospital of Xianyang City affiliated to Xi' an Jiaotong University Health Science Center from March 2016 to March 2020 were retrospectively studied. According to the method of pancreaticojejunostomy used, these patients were divided into the following two groups: the embedding anastomosis group ( n=55) and the intermittent eversion anastomosis group ( n=61). The duration of pancreaticojejunostomy, bilioenterostomy and gastrointestinal anastomoses, and the amounts of intraoperative blood loss and postoperative complication rates were compared between the two groups. Results:Of 116 patients in this study, there were 67 males and 49 females, with a median age of 61.5 years. No perioperative death occurred in the 2 groups. The operation time, digestive tract reconstruction time and pancreaticojejunostomy time in the embedded anastomosis group were (260±20), (65±15) and (35±15) min, respectively, which were significantly lower than those in the intermittent eversion anastomosis group (305±25), (81±25) and (45±12) min, (all P<0.05). The grade A and B pancreatic fistula rates in the embedded anastomosis group were 27.3%(15/55) and 21.8%(12/55), respectively, which were significantly higher than those in the intermittent eversion anastomosis group [8.2%(5/61) and 6.6%(4/61)], (all P<0.05). The postoperative hospital stay in the intermittent eversion anastomosis group (10.3±1.1) d was significantly lower than that in the embedding anastomosis group [(15.2±3.2) d, P<0.05]. Conclusion:In LPD, when compared with embedded pancreaticojejunostomy, intermittent eversion pancreaticojejunostomy reduced the postoperative pancreatic fistula rate and shortened the postoperative hospital stay.
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Objective@#To explore the impairments of the left visual field (LVF) superiority among children with autism spectrum disorder (ASD), for further understanding of the attentional mechanism of social disturbance in ASD.@*Methods@#The mixed design for repeated measured data was used. The case group was consisted of 105 ASD children enrolled from the rehabilitation agencies in Tianjin from Sept. 2016 to Dec. 2019; and 105 typically developed children were enrolled from Tianjin as the control group by matching the chronological age and gender distribution. The preferential looking paradigm was used to explore the LVF superiority by eye tracking system. Fixation count (FC), total fixation duration (TFD) and the proportion of left hemiface were analyzed by the Mixed design ANOVA, in which the main effect of "group", visual field (left vs. right) and gender of the faces was evaluated in addition to the interactions.@*Results@#All the participants in both the ASD group and TD group completed the experiments. For the whole face in LVF or RVF, the main effect of group showed the statistical significance on both FC and TFD [FC： F (1，206) =26.27, P <0.01; TFD： F (1，206) =51.23, P <0.01]. The interaction of group×visual field on FC also was statistically significant [ F (1，206) =4.619， P =0.03], and the case group showed the difference between LVF and RVF (0.33±0.02，0.54±0.03， P < 0.01 ) by further simple effect analysis, none of the rest was statistically significant. Both the left hemiface of FC & TFD showed the main effect of group [FC： F (1，206) =13.77， P ＜0.01；TFD： F (1，206) =12.89， P ＜0.01] and interaction of group×visual field [FC： F (1，206) = 36.99， P ＜0.01；TFD： F (1，206) =38.62， P ＜0.01), similarly, there was higher left hemiface proportion of both FC & TFD in RVF than that in LVF (FC：0.36±0.03，0.56±0.03， P <0.01; TFD：0.36±0.03，0.57±0.03， P <0.01).@*Conclusion@#LVF superiority is not presented among children with ASD in this study, while the fixation in RVF remained relatively unaffected. The finding indicates the involvement of the fusiform face area of right hemisphere in the pathogenesis of ASD in addition to the weak central coherence account.
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Objective:The differences of chemical compositions and pharmacological activities between the core and pulp of Phyllanthi Fructus were investigated by chemical analysis and <italic>in vitro</italic> test to explore the effect of the core on the quality of this medicinal material. Method:Literature， medicinal material standards and market research on the appearance of Phyllanthi Fructus were conducted based on existing databases. Ultra-high performance liquid chromatography-quadrupole-electrostatic field orbital trap high resolution mass spectrometry （UPLC-Q-Orbitrap HRMS） was used to identify the constituents of the core and pulp. The analysis was performed on Thermo Scientific Accucore C<sub>18</sub> column （2.1 mm×100 mm， 2.6 μm） with the mobile phase of 0.1% formic acid aqueous solution （A）-methanol （B） for gradient elution （0-25 min， 5%B； 25-30 min， 5%-95%B； 30-35 min， 95%-5%B）， the flow rate was 0.2 mL·min<sup>-1</sup>， heating electrospray ionization （HESI） was adopted with positive and negative ion modes， and the scanning range was <italic>m</italic>/<italic>z</italic> 100-1 500. High performance liquid chromatography （HPLC） was used to determine the contents of gallic acid， corilagin， chebulagic acid and ellagic acid in the core and pulp of Phyllanthi Fructus. Analysis was performed on Welchrom C<sub>18</sub> column （4.6 mm×250 mm， 5 μm） with mobile phase of methanol （A）-0.05% phosphoric acid aqueous solution （B） for gradient elution （0-6 min， 5%A； 6-15 min， 5%-7%A； 15-20 min， 7%-15%A； 20-25 min， 15%-21%A； 25-31 min， 21%-22%A； 31-41 min， 22%A； 41-47 min， 22%-28%A； 47-51 min， 28%-32%A； 51-57 min， 32%-38%A； 57-70 min， 38%-45%A； 70-80 min， 45%-65%A； 80-85 min， 65%-5%A）， the detection wavelength was set at 270 nm. The antibacterial effects of the core and pulp of Phyllanthi Fructus on <italic>Escherichia coli</italic> and <italic>Staphylococcus aureus</italic> were investigated by filter paper method， and their antioxidant activities were compared by 1，1-diphenyl-2-picrylhydrazyl （DPPH） free radical scavenging assay. Result:A total of 47 compounds were identified in the core and pulp of Phyllanthi Fructus， mainly including tannins， flavonoids， phenolic acids， fatty acids， amino acids， organic acids， saccharides and glycosides， most of which were concentrated in the pulp， and the fatty acids in the core accounted for a higher proportion. The contents of gallic acid， corilagin， chebulagic acid， ellagic acid and other phenolic compounds in the pulp of 20 batches of Phyllanthi Fructus were much higher than those in the core. The results of antibacterial test showed that the core of Phyllanthi Fructus with different concentrations had no antimicrobial effect. The DPPH radical scavenging test showed that the antioxidant activity of the core ［half-inhibitory concentration （IC<sub>50</sub>）=199.632 mg·L<sup>-1</sup>］ was much less than that of the pulp （IC<sub>50</sub>=12.688 mg·L<sup>-1</sup>）. Conclusion:From the perspectives of polyphenol content， antibacterial and antioxidant activities， it is scientific to use Phyllanthi Fructus pulp in ancient and modern times， which may be to remove the secondary parts of Phyllanthi Fructus， so as to enhance the actual utilization rate and therapeutic effect of medicinal materials. In view of the large proportion of the core of Phyllanthi Fructus and its high content of fatty acids and other components， whether or not to use it remains to be further studied in clinical application.
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Objective:To provide a scientific basis for the classification of Phyllanthi Fructus product grades. Method:A total of 30 batches of Phyllanthi Fructus currently available in the market were collected for quantification based on such appearance indexes as diameter， thickness， grain weight， and crust colour （<italic>L</italic><sup>*</sup>， <italic>a</italic><sup>*</sup>， and <italic>b</italic><sup>*</sup> values）. The contents of gallic acid， corilagin， chebulagic acid， and ellagic acid were measured by high performance liquid chromatography （HPLC）， followed by descriptive statistical analysis （DSA）， analysis of variance （ANOVA）， and principal component analysis （PCA） to determine the importance of each main index and explore the correlations between the appearance indexes and internal components. The classification standard of Phyllanthi Fructus product grades was formulated， and its scientificity was verified in hepatocelular carcinoma HepG2 cells. Result:The correlation analysis revealed that the crust colour <italic>L</italic><sup>*</sup>， <italic>a</italic><sup>*</sup>， and <italic>b</italic><sup>*</sup> values were significantly negatively correlated with corilagin， chebulagic acid， and ellagic acid （<italic>|r|</italic>>0.5， <italic>P</italic><0.01）， but irrelevant to gallic acid （<italic>|r|</italic><0.1）. Considering the variable coefficient of each index， PCA results， and the requirement of gallic acid as quality indicator for Phyllanthi Fructus in <italic>Chinese Pharmacopoeia</italic>， the crust colour <italic>L</italic><sup>*</sup>， <italic>a</italic><sup>*</sup>， and <italic>b</italic><sup>*</sup> values and gallic acid content were determined to be the classification indexes. The K-means cluster analysis confirmed that products with crust colour <italic>L</italic><sup>*</sup><44， <italic>a</italic><sup>*</sup><7， and <italic>b</italic><sup>*</sup><10 and gallic acid content >1.6% could be classified into the first class， and those failing to meet the above requirements into the second class. The cell experiment demonstrated that the half-maximal inhibitory concentration （IC<sub>50</sub>） of the first-class product against hepatocelular carcinoma HepG2 cells was lower than that of the second-class product. A colourimetric card was developed based on crust colour <italic>L</italic><sup>*</sup>， <italic>a</italic><sup>*</sup>， and <italic>b</italic><sup>*</sup> values to provide a visual tool for on-site evaluation of Phyllanthi Fructus products. Conclusion:This study has initially established the classification standard of Phyllanthi Fructus product grades， which contributes to guiding price negotiation of Phyllanthi Fructus products based on quality grade and thus ensuring high quality and high price.
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Polyethylene glycol (PEG) surface film-forming method was used to prepare hydrophilic Indigo Naturalis decoction pieces with stable effect.The preparation process of modified Indigo Naturalis was optimized and its microscopic properties,hydrophilicity,antipyretic efficacy,and safety were systematically evaluated.With equilibrium contact angle as assessment index,the influence of modifier type,modifier dosage,dispersant dosage,and co-grinding time on water solubility of Indigo Naturalis was investigated by single factor test.The results showed that the optimal preparation process was as follows.The 6%PEG6000 is dissolved in 10%anhydrous ethanol solution by sonification and then the mixture is ground with Indigo Naturalis for 2 min.The resultant product is dried on a square tray in an oven at 60℃to remove ethanol and thereby the PEG-modified hydrophilic Indigo Naturalis decoction pieces are yielded.The morphological observation under scanning electron microscope (SEM) indicated that the modified Indigo Naturalis had smoother surface than Indigo Naturalis,and energy spectrometer measurement showed that the nitrogen (N),calcium(Ca),oxygen (O),and silicon (Si) on the surface of modified Indigo Naturalis powder were less than those of Indigo Naturalis powder.Modified Indigo Naturalis had the equilibrium contact angle 18.96°smaller,polar component 22.222 m J·m~(-2)more,and nonpolar component 7.277 m J·m~(-2)smaller than the Indigo Naturalis powder.Multiple light scattering technique was employed to evaluate the dispersion in water and the result demonstrated that the transmittance of Indigo Naturalis and modified Indigo Naturalis was about85%and 75%,respectively,suggesting the higher dispersity of modified Indigo Naturalis.The suspension rate of modified Indigo Naturalis in water was determined by reflux treatment.The result showed that 57%of Indigo Naturalis was not wetted after refluxing for1 h,while the modified Indigo Naturalis was all wetted and dispersed into water.The dissolution of indigo and indirubin of modified Indigo Naturalis increased and the process was more stable.Then,rats were randomized into the blank group,model group,acetaminophen group,Indigo Naturalis group,and hydrophilic Indigo Naturalis group.The temperature changes of rats were observed after administration and the concentration of IL-1βand TNF-αin serum and IL-1βand PGE_2in hypothalamus was measured.The results indicated that the temperature of Indigo Naturalis group and hydrophilic Indigo Naturalis group dropped and the IL-1βlevel of the hydrophilic Indigo Naturalis group decreased (P<0.05) as compared with those in the model group.Thus,both Indigo Naturalis and hydrophilic Indigo Naturalis had antipyretic effect,particularly the hydrophilic Indigo Naturalis.The acute toxicity test of hydrophilic Indigo Naturalis verified that it had no toxicity to rats.In this study,the hydrophilic Indigo Naturalis decoction pieces were prepared with the PEG surface film-forming method,and the antipyretic efficacy and safety were evaluated,which expanded the technological means of powder modification for Chinese medicine and provided a method for clinical use of Chinese medicine.
Subject(s)
Animals , Rats , Drugs, Chinese Herbal , Hydrophobic and Hydrophilic Interactions , Indigo Carmine , Indigofera , Polyethylene GlycolsABSTRACT
As an effective antipyretic medicine,Indigo Naturalis has a long history of application in the field of Chinese medicine.The content of organics,mainly indigo and indirubin,is about 10%. However,the active ingredients and mechanism of its antipyretic effect have not yet been fully elucidated. In view of this,they were investigated in this study with the rectal temperature change as an indicator and 2,4-dinitrophenol-induced fever rats as subjects. The content of PGE2 and c AMP in the hypothalamus and the serum levels of TNF-α,IL-1β and IL-6 were determined by ELISA. Moreover,the plasma samples of fever rats were analyzed by metabonomics in combination with UPLC-Q-TOF-MS for the exploration of potential biomarkers and the discussion on the antipyretic mechanism of Indigo Naturalis and its active ingredients. The results showed that the rising trend of rectal temperature in rats was suppressed 0. 5 h after the treatment with Indigo Naturalis,organic matter,indigo or indirubin as compared with the rats of model group( P < 0. 05),among which Indigo Naturalis and organic matter had better antipyretic effect. ELISA results showed that organic matter and indigo can inhibit the expression of PGE2 and c AMP( P<0. 01),while Indigo Naturalis and organic matter were effective in curbing the increase in TNF-α( P<0. 05). A total of 21 endogenous metabolites were identified from the plasma samples of the Indigo Naturalis,organic matter,indigo and indirubin groups,which were mainly involved in glycerophospholipid metabolism.
Subject(s)
Animals , Rats , 2,4-Dinitrophenol , Antipyretics , Drugs, Chinese Herbal , Indigo Carmine , IndigoferaABSTRACT
Indigo Naturalis( IN) is mainly composed of 10% organic matter and 90% inorganic matter,with a poor wettability and strong hydrophobicity. Indigo,indirubin and effective ingredients are almost insoluble in water. And how it exerts its effect after oral administration still needs to be revealed. For this reason,this study put forward the hypothesis that " Indigo Naturalis forms a slightly soluble calcium carbonate carrier in a strong acid environment of gastric fluid,and organic substances are solubilized in the bile environment of intestinal fluid",and then verified the hypothesis. First,the dissolution apparatus was used to simulate the change process of IN in different digestive fluid,and the effects of low-dose and normal bile on the dissolution of inorganic substances and the release of organic substances were compared. After the surface morphology and element changes of IN in different digestive fluid were observed,it was found that bile is the key to promoting the dissolution of organic and inorganic substances in IN. Furthermore,the rat fever model induced by 2,4-dinitrophenol was used to study the antipyretic effect of IN in normal rats and bile duct ligation rats. It was found that the antipyretic effect of IN on normal rats was better than that of bile duct ligation rats. The above results indicated that after oral administration of IN,the calcium carbonate carrier was transformed into a slightly soluble state in acidic gastric fluid,and a small amount of organic matter was released. When IN entered the intestinal fluid mixed with bile,the carrier dissolved in a large amount,and indigo and indirubin were dissolved in a large amount,so as to absorb the blood and exert the effect. This study has a certain significance for guiding clinical application of IN. For patients with insufficient bile secretion( such as bile duct resection),oral administration with IN may not be effective and shall be paid attention.
Subject(s)
Animals , Humans , Rats , Bile , Hydrophobic and Hydrophilic Interactions , Indigo Carmine , Indigofera , Plant ExtractsABSTRACT
Indigo Naturalis has a long history of medicinal use with particularity and complexity in its processing. Before the Ming dynasty,Indigo Naturalis was extracted from the top layer of zymotic fluid,called " purified Indigo Naturalis". In modern processing,the precipitate " crude Indigo Naturalis" is dried to produce Indigo Naturalis after impurity removal. The form of Indigo Naturalis slices has undergone significant changes in ancient and modern times. In view of this,the quality comparison between crude Indigo Naturalis and purified Indigo Naturalis was conducted in this study with modern analytical techniques. Firstly,chemical composition was analyzed with UPLC-Q-TOF-MS,and the chemical composition of scent with HS-SPME/GC-MS/MS. The content of indigo,indirubin,total ash,and water-soluble extract was determined as well as the inorganic composition in crude Indigo Naturalis and purified Indigo Naturalis. Then,their microscopic morphology was observed and the surface element composition was investigated. Finally,the antipyretic activities of crude Indigo Naturalis and purified Indigo Naturalis were compared in the fever rat model induced by lipopolysaccharide and 2,4-dinitrophenol. The results demonstrated that the purified Indigo Naturalis had a faster and more lasting antipyretic effect,while the crude Indigo Naturalis had almost no antipyretic effect. This study is of great significance to the research on processing technology of Indigo Naturalis and provides reference for the formulation of its quality standards,production specifications and calibration procedures.
Subject(s)
Animals , Rats , Indigo Carmine , Indigofera , Plant Extracts , Tandem Mass SpectrometryABSTRACT
The soaking and fermentation of Baphicacanthus cusia( Nees),the important intermediate link of Indigo Naturalis processing,facilitates the synthesis of indigo and indirubin precursors and the dissolution of endogenous enzymes and other effective components,while the role of microorganisms in the fermentation is ignored. The present study investigated the changes of microbial community structure in Indigo Naturalis processing based on 16 S amplicon sequencing and bioinformatics. Meanwhile,the contents of indigo,indirubin,isatin,tryptanthrin,indole glycoside,etc. were determined to explore the correlation between the microorganisms and the alterations of the main components. As demonstrated by the results,the microbial diversity decreased gradually with the fermentation,which bottomed out after the addition of lime. Proteobacteria,Bacteroidetes,and Firmicutes were the main dominant communities in the fermentation. The relative abundance of Proteobacteria declined gradually with the prolongation of fermentation time,and to the lowest level after the addition of lime. The relative abundance of Firmicutes increased,and that of Bacteroidetes decreased first and then increased. The contents of effective substances in Indigo Naturalis also showed different variation tendencies. As fermentation went on,indole glycoside decreased gradually; indigo first increased and then decreased; indirubin and isatin first decreased and then increased; tryptanthrin gradually increased. Those changes were presumedly related to the roles of microorganisms in the synthesis of different components. This study preliminarily clarified the important role of microorganisms in the soaking and fermentation and provided a scientific basis for the control of Indigo Naturalis processing and the preparation of high-quality Indigo Naturalis.
Subject(s)
Fermentation , Indigo Carmine , Indigofera , Indoles , MicrobiotaABSTRACT
Traditional Chinese medicine( TCM) processing is a traditional pharmaceutical technology unique to China,which is an important means to ensure the safety and effectiveness of clinical medication. As China' s intangible cultural heritage,it contains a wealth of wisdom. With the evolution and optimization of processing methods,Indigo Naturalis,an ancient dye,has gradually become an effective medicine for the treatment of high fever in children,colitis,psoriasis,and leukemia. However,the quality of Indigo Naturalis pieces is difficult to be fundamentally improved due to the unique traditional processing method,complex technology,unclear principle,and outdated equipment. After spending 20 years in exploring the inheritance,innovation,and transformation of ancient lawtheory-principle-technology-equipment-quality control in Indigo Naturalis processing,our research group has basically expounded the processing principle and realized the modern expression and industrial transformation of traditional technology. As China enters a new era,the TCM industry has begun to undergo the high-quality transformation. It is urgent to carry out new excavations and improve the processing,quality,and clinical application of Indigo Naturalis pieces,to better inherit and innovate traditional processing technologies and meet people's demand for high-quality TCM health services.