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ObjectiveTo explore the mechanism of Xueniao capsule in the treatment of acute pyelonephritis (APN) by network pharmacology and experimental verification. MethodThe effect of Xueniao capsule on APN was investigated based on the APN model in rats. The Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), Chemistryl Database, and SymMap were searched for the chemical components of Smilacis Chinae Rhizoma,Coicis Semen, and Trachycarpi Petiolus. The target information of the components was collected from PharmMapper and SwissTargetPrediction, and disease target information from Therapeutic Target Database (TTD), DrugBank, DisGeNET, GeneCards, and Online Mendelian Inheritance in Man(OMIM). The key genes of Xueniao capsule for APN underwent Gene Ontology(GO) and Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway enrichment analyses by Metascap. Real-time quantitative polymerase chain reaction (PCR) and Western blot were employed to verify the prediction results. ResultCompared with the blank group and the sham operation group, the model group showed an increased ratio of the left kidney to the right kidney and organ index(P<0.05, P<0.01),up-regulated white blood cells (WBC),neutrophils (NEUT),monocytes (MONO), and lymphocytes (LY)(P<0.05, P<0.01), and elevated levels of nuclear factor-κB(NF-κB), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α)(P<0.05, P<0.01). Compared with the model group, the norfloxacin group, the low- and high-dose Xueniao capsule groups showed a decreased ratio of the left kidney to the right kidney and organ index(P<0.05, P<0.01), dwindled levels of WBC, NEUT, MONO, and LY(P<0.05, P<0.01), and reduced levels of NF-κB, IL-6, and TNF-α(P<0.05, P<0.01). The medium-dose Xueniao capsule group showed a decreased ratio of the left kidney to the right kidney and organ index(P<0.05, P<0.01), reduced levels of WBC, NEUT, MONO, and LY(P<0.05, P<0.01), and dwindled levels of IL-6 and TNF-α(P<0.05, P<0.01). Network pharmacological analysis revealed 17 active compounds from Smilacis Chinae Rhizoma, 18 active compounds from Coicis Semen, six active compounds from Trachycarpi Petiolus, and 39 key genes for the treatment of APN in Xueniao capsule. GO enrichment analysis demonstrated 704 biological processes, 22 cellular components, and 59 molecular functions. Sixty-two pathways were enriched in KEGG enrichment analysis. The experimental verification results showed that compared with the blank group, the model group showed increased mRNA expression of prostaglandin-endoperoxide synthase 2 (PTGS2), mitogen-activated protein kinase 1 (MAPK1)/extracellular signal-regulated protein kinase 2 (ERK2),phosphoinositide 3 kinase (PI3K),protein kinase B2(Akt2),Janus kinase 2 (JAK2),and signal transducer and activator of transcription 3 (STAT3)and protein expression of PI3K, Akt2, JAK2, and STAT3 (P<0.05, P<0.01). Compared with the model group, the low-dose Xueniao capsule group showed decreased mRNA expression of MAPK1, PI3K, JAK2, and STAT3 and protein expression of PI3K, JAK2, and STAT3 (P<0.05, P<0.01). The medium-dose Xueniao capsule group showed decreased mRNA expression of MAPK1, PTGS2, PI3K, JAK2, and STAT3, and protein expression of PI3K, JAK2, and STAT3 (P<0.05, P<0.01). The high-dose Xueniao capsule group showed reduced mRNA expression of PTGS2, MAPK1, PI3K, Akt2, JAK2, and STAT3 and protein expression of PI3K, Akt2, JAK2, and STAT3 (P<0.05, P<0.01). ConclusionXueniao capsule has a certain curative effect on APN via multiple targets and multiple pathways. The mechanism may be related to the inhibition of the PI3K/Akt signaling pathway and the JAK2/STAT3 signaling pathway.
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With the ultra high performance liquid chromatography-quadruple-electrostatic field orbitrap high resolution mass spectrometry(UHPLC-Q Exactive Orbitrap-MS)-based metabonomics technology, this study aims to analyze the effect of Chaiqin Ningshen Granules(CNG) on endogenous metabolites in insomnia rats of liver depression syndrome and explore the sleep-improving mechanism of this prescription. Parachlorophenylalanine(PCPA, ip) and chronic stimulation were combined to induce insomnia of liver depression pattern in rats, and the effect of CNG on the macroscopic signs, hemorheology, and neurotransmitters in the hippocampus of insomnia rats of liver depression syndrome was observed. After the administration, rat hippocampus was collected for liquid chromatography-mass spectrometry(LC-MS) analysis of the metabolomics. Principal component analysis(PCA), partial least squares discriminant analysis(PLS-DA), and orthogonal partial least squares discriminant analysis(OPLS-DA) were employed for analyzing the metabolites in rat hippocampus and screening potential biomarkers. MetPA was used to yield the related metabolic pathways and metabolic networks. The results show that the drugs can significantly improve the mental state, liver depression, and blood stasis of rats, significantly increase the content of 5-hydroxytryptamine(5-HT) and gamma aminobutyric acid(GABA) in hippocampus(except low-dose CNG), and significantly reduce the content of glucose(Glu)(except low-dose CNG). Among them, estazolam and high-dose CNG had better effect than others. Metabolomics analysis yielded 27 potential biomarkers related to insomnia. MetPA analysis showed 4 metabolic pathways of estazolam in intervening insomnia and 3 metabolic pathways of high-dose CNG in intervening insomnia, involving purine metabolism, glycerophospholipid metabolism, histidine metabolism, and caffeine metabolism. CNG can alleviate insomnia by regulating endogenous differential metabolites and further related metabolic pathways. The result lays a basis for further elucidating the mechanism of CNG in improving sleep.
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Animais , Ratos , Biomarcadores , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/farmacologia , Estazolam , Hipocampo/metabolismo , Metabolômica/métodos , Sono , Distúrbios do Início e da Manutenção do Sono/tratamento farmacológicoRESUMO
Twenty-six compounds, including sixteen meroterpenoids(1-16), a triterpenoid(17), four terpenoid derivatives(18-21), and five aromatic compounds(22-26), were isolated from the leaves of Psidium guajava. Their structures were identified by spectroscopic analyses including NMR and MS. Compounds 21-26 were obtained from plants of Psidium for the first time. Based on the structure,(R)-2-ethylhexyl 2H-1,2,3-triazole-4-carboxylate(24 a), an α-glucosidase inhibitor recently isolated from Paramignya trimera, should be revised as compound 24. Meroterpenoids 1-16 were evaluated for their antitumor and antifungal activities. Meroterpenoids psiguajadial D(4), guapsidial A(5), 4,5-diepipsidial A(7), guadial A(14), and guadial B(15) showed cytotoxicities against five human tumor cell lines(HL-60, A-549, SMMC-7721, MCF-7, and SW-480), among which 5 was the most effective with an IC_(50) of 3.21-9.94 μmol·L~(-1).
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Humanos , Antifúngicos/farmacologia , Espectroscopia de Ressonância Magnética , Extratos Vegetais , Folhas de Planta , Psidium , TerpenosRESUMO
Chronic obstructive pulmonary disease (COPD) complicated with pulmonary tuberculosis (PTB) is becoming more and more common. The coexistence of two diseases brings difficulty to the control of the disease. Smoking, biofuel exposure, vitamin D deficiency and diabetes may be common risk factors for both diseases. Complementary prevention and control strategies can be designed for the above risk factors. This article contains review with tuberculosis as a risk factor for COPD, COPD combined with tuberculosis, and the prevention strategies for both diseases.
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Parthenocarpy, the productions of seedless fruit without pollination or fertilization, is a potentially desirable trait in many commercially grown fruits, especially in pear, which is self-incompatible. Phytohormones play important roles in fruit set, a process crucial for parthenocarpy. In this study, 2,4-dichlorophenoxyacetic acid (2,4-D), an artificially synthesized plant growth regulator with functions similar to auxin, was found to induce parthenocarpy in pear. Histological observations revealed that 2,4-D promoted cell division and expansion, which increased cortex thickness, but the effect was weakened by paclobutrazol (PAC), a gibberellin (GA) biosynthesis inhibitor. Phenotypic differences in pear may therefore be due to different GA contents. Hormone testing indicated that 2,4-D mainly induced the production of bioactive GA4 , rather than GA3. Three key oxidase genes function in the GA biosynthetic pathway: GA20ox, GA3ox and GA2ox. In a pear group treated with only 2,4-D, PbGA20ox2-like and PbGA3ox-1 were significantly upregulated. When treated with 2,4-D supplemented with PAC, however, expression levels of these genes were significantly downregulated. Additionally, PbGA2ox1-like and PbGA2ox2-like expression levels were significantly downregulated in pear treated with either 2,4-D only or 2,4-D supplemented with PAC. We thus hypothesize that 2,4-D can induce parthenocarpy by enhancing GA4 biosynthesis.
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Ácido 2,4-Diclorofenoxiacético/farmacologia , Giberelinas/metabolismo , Pyrus/efeitos dos fármacos , Pyrus/fisiologia , Frutas/efeitos dos fármacos , Frutas/fisiologia , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Triazóis/farmacologiaRESUMO
Objective:To establish HPLC-UV fingerprints of Ilex pubescens pieces,and simultaneously determine two components in 46 batches of I. pubescens in pieces of I. pubescens saponin A1 and B1,in order to provide a reference for the quality standard of I. pubescens slices. Method:Methanol was used to extract the I. pubescens saponin samples,and the extracts were measured by HPLC-UV with the absorption wavelength at 210 nm. Kromasil C18 column (4.6 mm×250 mm,5 μm) was used for determining the extracts at a flow rate of 1.0 mL·min-1. The mobile phase condition was acetonitrile-0.1% phosphoric acid aqueous solution with gradient mode. The chromatographic fingerprint similarity evaluation system of traditional Chinese medicine (2012 edition) was used to analyze I. pubescens fingerprints. SPSS 20.0 software was used to cluster the peak area of common peaks. Principal component analysis was performed to reduce the dimension of common peaks. Result:There were great differences between the root and stem parts in I. pubescens fingerprints. The fingerprints of roots and stems of I. pubescens were established respectively,cluster results assorted the roots of I. pubescens into three categories andthe branches of I. pubescens into two categories. The integrity and difference of I. pubescens decoction pieces from different parts and places of origin were compared,and the principal component analysis was performed to screen out the common components that played a decisive role in fingerprint of I. pubescens pieces. And the common peaks were determined. The content of saponin A1 and saponin B1 in Radix I. pubescens were determined. Conclusion:The established I. pubescens fingerprints and content determination methods are simple and suitable. Cluster analysis and principal component analysis are used to screen out the key components of quality control of I. pubescens. The results can provide references for quality control of I. pubescens.
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Serum pharmacochemistry of traditional Chinese medicine(TCM) is a new subject based on the identification of migrating components in serum after oral administration of TCM.After more than 20 years of development,serum pharmacochemistry of TCM has been widely recognized and applied by researchers.Based on the references related with the serum pharmacochemistry from these years,the research summarized the methods of serum pharmacochemistry of TCM,for example,selection of experimental animals,preparation of gastric irrigation,design of drug administration scheme,method and time of adoption blood,pretreatment of serum containing drug,as well as analysis of serum sample.In addition,the paper will emphatically introduce the application of serum pharmacochemistryof TCM,which includes clarifying the substance basis of Chinese medicine,establishing the quality standard of TCM,and clarifying the compatibility of compound Chinese medicine.At the same time,we will through some existing problems to look forward to the future of serum pharmacochemistryof TCM,so that people can have a comprehensive understanding of serum pharmacochemistryof TCM,hoping to lay a foundation for the further application of this method in TCM research.
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Objective To compare the efficacy difference of Green Forsythiae Fructus and Ripe Forsythiae Fructusby using Lianqiao powder and Yinqiao powder in the classic formula; To provide experimental evidence for the guidance of one for dual-use of the Forsythiae Fructus. Methods The guinea pig sore model was made with Staphylococcus aureus. 40 guinea pigs were randomly divided into blank group, model group, Lianqiao powder Green Forsythiae Fructus group and Lianqiao powder Ripe Forsythiae Fructus group. The blank group and the model group were fed with normal saline, while Lianqiao powder Green Forsythiae Fructus group and Lianqiao powder Ripe Forsythiae Fructus group were treated with 1.2 g raw medicine/kg liquid Lianqiao powder Green Forsythiae Fructus and Lianqiao powder Ripe Forsythiae Fructus for 7 d. The symptom score, blood and pathological changes of guinea pig soreness were observed. The model of acute lung injury was induced by 10% LPS aerosol inhalation. 40 rats were randomly divided into blank group, model group, Yinqiao powder Green Forsythiae Fructus group and Yinqiao powder Ripe Forsythiae Fructus group. The blank group and the model group were fed with normal saline, while Yinqiao powder Green Forsythiae Fructus group and Yinqiao powder Ripe Forsythiae Fructus group were treated with 4 g raw medicine/kg liquid Yinqiao powder Green Forsythiae Fructus and Yinqiao powder Ripe Forsythiae Fructus for 10 d. The levels of IL-6, TNF-α and IL-1β in the lung lavage fluid were detected. Results The effect of Lianqiao powder Green Forsythiae Fructus on the wound healing of guinea pig sore wound was faster than that of Lianqiao powder Ripe Forsythiae Fructus, but there was no significant difference between Lianqiao powder Green Forsythiae Fructus group and Lianqiao powder Ripe Forsythiae Fructus group in inhibiting the secretion and pathological changes of guinea pig sore wound. The levels of IL-6, TNF-α and IL-1β in Yinqiao powder Green Forsythiae Fructus group was lower than that in Yinqiao powder Green Forsythiae Fructus group, without statistical significance. Conclusion It is verified that there is efficacy differences between Green Forsythiae Fructus and Ripe Forsythiae Fructus in the different Chinese herbal compound.
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Objective Cancer, a disease induced by abnormally regulated cell growth and apoptosis, is imposing a global threat to human health.This study was to explore the effects of Chinese herbal extracts ( CHE) in inducing the apoptosis and inhibiting the proliferation of human lung cancer cells. Methods Human lung cancer A549 cells were divided into a negative control, a high-dose CHE (680 ng/mL), a medium-dose CHE (340 ng/mL), and a low-dose CHE (170 ng/mL) group.The inhibitory effect of CHE on the proliferation of the lung cancer cells was detected by CCK8 and LDH assays, the apoptosis of the cells was assessed by fluorescence microscopy and flow cytometry, and the expressions of hTERT mRNA, cleaved caspase-3 and cleaved PARP were deter-mined by RT-PCR and Western blot. Results CHE inhibited the proliferation of the A549 cells with an IC50 value of 510 ng/mL. Treatment with high-dose CHE for 48 hours significantly suppressed the proliferation of the cells, induced the release of LDH, and promo-ted the apoptosis of the cells by 72.3%.RT-PCR and Western blot showed that 24-hour treatment with medium-dose CHE reduced the expression of hTERT mRNA by 4 times that of the negative control and up-regulated the expressions of cleaved caspase-3 and cleaved PARP. Conclusion Chinese herbal extracts can induce cell apoptosis by decreasing the expression of hTERT mRNA and increasing those of the cleaved caspase 3 and cleaved PARP proteins.
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The certified reference materials (CRMs) of emodin in rhubarb and its alcohol extract, water extract were developed by using quantity transfer technology from single chemical composition to the complex systems. The CRM of emodin was used for quantity transfer, and high performance liquid chromatography (HPLC) method was used to determine the contents of emodin in different matrix composition. By establishing mathematical model and calculating the parts of uncertainty, the uncertainty values were finally gotten. CRMs of emodin in rhubarb, alcohol extract and water extract were accomplished. The content values of emodin were 0.40% ±0.03%, 1.15%±0.18%, 0.16%±0.08% (k=2,P=0.95), respectively. The established method for quantity transfer has successfully solved the technical problems that the value of active ingredient of traditional Chinese medicine can't be traced to SI units. The series of CRMs are assigned as grade primary reference materials, which are useful for quality control of the emodin content, also provide the accurate and reliable CRM, materials standard and standard methods.
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The research aimed to evaluate the intestinal absorption of alkaloids extracted by decoction and alcohol extraction proces- ses from Rhizoma Coptidis-Rheum rhabarum herbal pair via everted gut sacs. Berberine, palmatine, coptisine and epiberberine were the main alkaloids in this herbal pair and taken as the standard indexes in the quantitative analysis with multi-components by single marker (QAMS) method, in order to calculate absorption rate constant (Ka) and evaluate intestinal absorption characteristics of these four alkaloids extracted by different extraction methods in different intestinal segments in rats. The results showed that the four alkaloids extracted by two different processes in high, medium and low doses had linear absorption properties in the small intestine segment, which conformed to zero-order absorption rate, intestinal segment than 0.99. The absorption rate constant (Ka) of decoction group was higher than that of alcohol extraction group.
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Animais , Masculino , Ratos , Alcaloides , Farmacocinética , Coptis , Química , Absorção Intestinal , Ratos Sprague-Dawley , Rheum , QuímicaRESUMO
It is the most important mission that preserving and developing advancement of TCM theory and practice.We need defi nitive medical standard to standardize the development.Whether there was any standards in the history of traditional Chinese medicine is a hot question.Though the history research,we found that TCM classic literature was the medical standard in ancient China,which was confirmed by Tang-song government though official action.The standard teaching materials promoted the communication and development of TCM.After Song dynastythe standard position and function was strengthened continuouslywhich had a profound effect.
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<p><b>OBJECTIVES</b>To observe the influence of wen-yang herbs on the hemodynamics in liver fibrotic rats.</p><p><b>METHODS</b>Wistar rats with liver fibrosis, induced by carbon tetrachloride and alcohol, were randomly divided into a treatment group and a control group. The treatment group was administered wen-yang herbs and the control group saline. At the end of the experiment, the hemodynamic markers of the liver and the mesentery, the liver function and hydroxyproline content of liver tissues between the two groups were compared. Blood volume of the livers and hydroxyproline content of liver tissues were also determined.</p><p><b>RESULTS</b>Blood volume of the liver and mesentery (P < 0.01) and blood flow velocity of small vein of mesentery (P < 0.05) of the treatment group were distinctly higher than the control group. The hydroxyproline content (P < 0.01) of the treatment group was remarkably reduced and liver function was improved.</p><p><b>CONCLUSION</b>Wen-yang herbs can activate microcirculation of the liver and mesentery, decrease the deposit of collagen in the liver and improve liver function.</p>