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BACKGROUND: Leguminous Sophora moorcroftiana (SM) is a genuine medicinal material in Tibet. Many research results have reveal the Sophora moorcroftiana alkaloids (SMA), as the main active substance, have a wide range of effects, such as antibacterial, antitumor and antiparasitic effects. However, there are few reports on the inhibition of lung cancer (LC) and its inhibitory mechanism, and the pharmacological mechanism of SMA is still unclear, Therefore, exploring its mechanism of action is of great significance. METHODS: The SMA active components were obtained from the literature database. Whereas the corresponding targets were screened from the PubChem and PharmMapper database, UniProt database were conducted the correction and transformation of UniProt ID on the obtained targets. The GeneCards and OMIM databases identified targets associated with LC. Venny tools obtained the intersection targets of SMA and LC. R language and Cytoscape software constructed the visual of SMA - intersection targets - LC disease network. The intersection targets protein-protein interaction (PPI) network were built by the STRING database. The functions and pathways of the common targets of SMA and LC were enriched by gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG). Subsequently, molecular docking And A549 cells vitro experiment were performed to further validate our finding. RESULTS: We obtained six kinds of alkaloids in SM, 635 potential targets for these compounds, and 1,303 genes related to LC. SMA and LC intersection targets was 33, including ALB, CCND1, ESR1, NOTCH1 and AR. GO enrichment indicated that biological process of SMA was mainly involved in the positive regulation of transcription and nitric oxide biosynthetic process, and DNA-templated, etc. Biological functions were mainly involved in transcription factor binding and enzyme binding, etc. Cell components were mainly involved in protein complexes, extracellular exosome, cytoplasm and nuclear chromatin, etc., Which may be associated with its anti-LC effects. KEGG enrichment analysis showed that main pathways involved in the anti-LC effects of SMA, including pathway in cancer, non small-cell lung cancer, p53, PI3K-Akt and FOXO signaling pathways. Molecular docking analyses revealed that the six active compounds had a good binding activity with the main therapeutic targets 2W96, 2CCH and 1O96. Experiments in vitro proved that SMA inhibited the proliferation of LC A549 cells. CONCLUSIONS: Results of the present study, we have successfully revealed the SMA compounds had a multi-target and multi-channel regulatory mechanism in treatment LC, These findings provided a solid theoretical reference of SMA in the clinical treatment of LC.
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Alcaloides , Neoplasias Pulmonares , Sophora , Neoplasias Pulmonares/tratamento farmacológico , Simulação de Acoplamento Molecular , Farmacologia em Rede , Medicina Tradicional Tibetana , Fosfatidilinositol 3-Quinases , Alcaloides/farmacologiaRESUMO
Objective: A continuing care bundle can achieve a better outcome than a single implementation after discharge. This study aims to investigate the effect of this intervention in elderly patients with rectal cancer after radical resection with a permanent stoma. Methods: Elderly patients diagnosed with rectal cancer underwent radical resection with permanent stoma, they were divided into the control group (n = 42) and bundle group (n = 42). The control group received the conventional care, and the bundle group received the continuing care bundle in addition to the conventional care. At 1- and 3-month after discharge, self-efficacy, self-care knowledge, ability to change stoma appliances, negative emotions, quality of life, and patient satisfaction were observed. Results: The increased levels of self-efficacy, self-care knowledge, and ability to change stoma appliances were displayed in the bundle group after discharge as compared with that in the control group, along with the enhanced score of SF-36 subscales, including physical function (PF), role physical (RP), global health (GH) and vitality (V), social function (SF), and mental health (MH). Furthermore, patients showed alleviated depression and anxiety after the continuing care bundle as compared to those after conventional care. Besides, the bundle groups had higher patient satisfaction than the control group. Conclusions: Continuing care bundle can serve as an effectiveness intervention in elderly rectal cancer patients after radical resection with permanent stoma via increasing self-efficacy and self-care knowledge, enhancing the ability to change stoma appliance, reliving the negative emotion, and improving quality of life and patient satisfaction.
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This experiment is based on the principle of traditional Chinese medicine (TCM) pulse diagnosis, the human pulse signal collected by the sensor is organized into a dataset, and the algorithms are designed to apply feature extraction. After denoising, smoothing and eliminating baseline drift of the photoelectric sensors pulse data of several groups of subjects, we designed three algorithms to describe the difference between the two-dimensional images of the pulse data of normal people and patients with chronic diseases. Convert the calculated feature values into multi-dimensional arrays, enter the decision tree (DT) to balance the differences in human physiological conditions, then train in the support vector machine kernel method (SVM-KM) classifier. Experimental results show that the application of these feature mining algorithms to disease detection greatly improves the reliability of TCM diagnosis.
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Algoritmos , Máquina de Vetores de Suporte , Frequência Cardíaca , Humanos , Reprodutibilidade dos TestesRESUMO
Ginsenosides are the main active ingredients in ginseng. Studies have shown that ginsenosides have anti-virus, anti-tumor, anti-aging, nootropic, cardiovascular diseases-protecting, and other pharmacological activities. Thus, the development and utilization of ginsenosides have persistently attracted much attention. At present, the extraction of ginsenosides is mainly based on organic solvents, and there are relatively few studies on their green extraction. In this study, different deep eutectic solvents(DESs) were synthesized by heating and stirring method, combined with an emerging technology, mechanochemically-assisted extraction(MCAE), to extract ginsenosides in a green way. Six parameters that might affect the extraction effect were optimized to determine the optimal conditions, and the method validation was conducted. The new established method was compared with a commonly used extraction method(ultrasound-assisted extraction using 70% ethanol) to evaluate its extraction efficiency. The results revealed that the optimal extraction conditions of DES-MCAE were that the volume ratio of DES3(choline chlorideâ¶urea 1â¶2) and water in the extraction solvent was 6â¶4, and the liquid ratio and the linear vibration speed were 0.05 g·mL~(-1) and 4.0 m·s~(-1); the extraction was performed twice, 40 s each. With only 80 s extraction, the extraction rate of this method was 36.22% higher than that of ultrasoun-dassisted extraction using 70% ethanol. In this study, a DESs-based pretreatment method for ginsenosides was established and its rapid, green and efficient extraction was realized, which provided new ideas and methods for further research on green extraction of other active ingredients from Chinese medicine.
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Ginsenosídeos , Solventes Eutéticos Profundos , Solventes , Água , EtanolRESUMO
Three new paraconic acids, xylariacinics A-C (1-3), were isolated from the endophyte Xylariaceae sp. J4 harbored in the medicinal plant Blumea balsamifera. Their structures were elucidated on the basis of extensive spectroscopic data including HRMS, and NMR. The antibacterial efficacies of compounds 1-3 were evaluated against a panel of bacteria such as Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa. Their antifungal activities were also tested against Colletotrichum gloeosporioides. Unfortunately, all of them were inactive.
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Staphylococcus aureus , Xylariales , Antibacterianos/farmacologia , Bacillus subtilis , Endófitos , Testes de Sensibilidade MicrobianaRESUMO
Angelica sinensis (AS) is a common Traditional Chinese Medicine used for tonifying blood in China. Unprocessed AS and its four kinds of processed products (ASs) are used to treat blood deficiency syndrome in the country. The different blood-tonifying mechanisms of ASs remain unclear. In this work, a novel method integrating metabolomics and hematological and biochemical parameters was established to provide a complementary explanation of blood supplementation mechanism of ASs. Our results revealed that different ASs exhibited various blood supplementation effect, and that AS parched with alcohol demonstrated the best blood supplementation effect. Eight metabolites from liver tissue and 12 metabolites from spleen tissue were considered to be potential biomarkers. These biomarkers were involved in four metabolic pathways. Correlation analysis results showed that l-aspartic acid and l-alanine (spleen tissue), linoleic acid, and l-cystathionine (liver tissue) exhibited a high positive or negative correlation with the aforesaid biochemical indicators. The blood-supplementation effect mechanism of ASs were related to four metabolic pathways. l-Aspartic acid and l-alanine (spleen tissue), linoleic acid, and l-cystathionine (liver tissue) were the four key metabolites associated with the blood supplementation effect of ASs. This study gives a complementary explanation of the blood supplementation effect and mechanism of action of ASs.
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Angelica sinensis/química , Medicamentos de Ervas Chinesas/farmacologia , Medicina Tradicional Chinesa , Metaboloma/efeitos dos fármacos , Aminoácidos/metabolismo , Animais , Cromatografia Gasosa-Espectrometria de Massas , Ácido Linoleico/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Metabolômica/métodos , Camundongos , Baço/efeitos dos fármacos , Baço/metabolismoRESUMO
Gestational folic acid (FA) supplementation has been widely recognized for its benefits in preventing offspring defects, but its effect on postpartum females has not yet been adequately assessed. The occurrence of emotional and cognitive dysfunction is common in postpartum women, and its treatment remains limited. Considering the promising results of FA in various psychiatric disorders both in human and redents, we tested the effect of gestational FA administration on postpartum psychiatric behavioral phenotypes and the implicated brain-related mechanisms in a murine model. FA was administered orally in both the hormone-stimulated-pregnancy (HSP) model and pregnant mice at doses of 1 and 5 mg/kg. Postpartum behavioral results showed that the disorders of cognitive performance, depressive, and anxiety-related behaviors were all alleviated in the 5 mg/kg FA group. However, the general development of their offspring remained unaffected. Immunofluorescence and immunoblot results revealed that FA pretreatment significantly activated the maternal hippocampal BDNF-related pathway. Morphological studies have confirmed that FA promotes hippocampal neurogenesis. Moreover, synaptic plasticity and synaptic transmission are enhanced. All of these hippocampal changes play critical roles in rescuing neuronal function and behaviors. Thus, our data suggest that gestational FA administration has a therapeutic effect that improves cognition and reduces depression and anxiety in a murine postpartum model. This may be developed as a preventive and adjuvant therapeutic option for pregnant women.
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A pectinase-producing bacterial isolate, identified as Paenibacillus xylanexedens SZ 29, was screened by using the soil dilution plate with citrus pectin and congo red. A pectin methylesterase gene (Pxpme) was cloned and expressed in Escherichia coli. The gene coded for a protein with 334 amino acids and a calculated molecular mass of 36.76 kDa. PxPME showed the highest identity of 32.4% with the characterized carbohydrate esterase family 8 pectin methylesterase from Daucus carota. The recombined PxPME showed a specific activity with 39.38 U/mg against citrus pectin with >65% methylesterification. The optimal pH and temperature for PxPME activity were 5.0 and 45 °C. Its Km and Vmax value were determined to be 1.43 mg/mL and 71.5 µmol/mg·min, respectively. Moreover, PxPME could increase the firmness of pineapple cubes by 114% when combined with CaCl2. The acidic and mesophilic properties make PxPME a potential candidate for application in the fruit processing.
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Proteínas de Bactérias , Hidrolases de Éster Carboxílico , Paenibacillus , Pectinas/metabolismo , Proteínas Recombinantes , Proteínas de Bactérias/química , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Hidrolases de Éster Carboxílico/química , Hidrolases de Éster Carboxílico/genética , Hidrolases de Éster Carboxílico/metabolismo , Escherichia coli/genética , Manipulação de Alimentos , Frutas/química , Concentração de Íons de Hidrogênio , Paenibacillus/enzimologia , Paenibacillus/genética , Proteínas Recombinantes/química , Proteínas Recombinantes/genética , Proteínas Recombinantes/metabolismo , TemperaturaRESUMO
HIF-1α is an important factor regulating oxygen balance in mammals, and its expression is closely related to various physiological and pathological conditions of the body. Because HIF-1α plays an important role in the occurrence and development of cancer and other diseases, it has become an enduring research hotspot. At the same time, natural medicines and traditional Chinese medicine compounds have amazing curative effects in various diseases related to HIF-1 subtype due to their unique pharmacological effects and more effective ingredients. Therefore, in this article, we first outline the structure of HIF-1α and the regulation related to its expression, then introduce various diseases closely related to HIF-1α, and finally focus on the regulation of natural medicines and compound Chinese medicines through various pathways. This will help us understand HIF-1α systematically, and use HIF-1α as a target to discover more natural medicines and traditional Chinese medicines that can treat related diseases.
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Medicamentos de Ervas Chinesas/farmacologia , Subunidade alfa do Fator 1 Induzível por Hipóxia/antagonistas & inibidores , Neoplasias Hepáticas/tratamento farmacológico , Medicamentos de Ervas Chinesas/química , Humanos , Subunidade alfa do Fator 1 Induzível por Hipóxia/metabolismo , Neoplasias Hepáticas/metabolismo , Medicina Tradicional ChinesaRESUMO
The glycoprotein from Schisandra chinensis was obtained with alkali extraction and acid precipitation, purified with DEAE Sepharose Fast Flow and Superdex G-75 column. The molecular composition structure and antifatigue activities of glycoprotein were studied. SCGP's molecular weight was approximately 10 KDa, and it consisted of a carbohydrate component (52.94%) and protein component (47.06%). SCGP comprised mannose, galactoside, rhamnose, glucose, galactose, xylose, arabinose, and fucose, its molar ratio was 2.14 : 1.43 : 1.59 : 8.17 : 8.99 : 3.18 : 18.51 : 1, and it contained 16 kinds of amino acids. SCGP could obviously extend the swimming time in mice by increasing LDH, SOD level, GSH-Px activity, and liver glycogen and decreasing the contents of BUN and MDA. The antioxidant activity of SCGP is a potential mechanism of its antifatigue effect. In vitro antioxidant test showed that SCGP scavenged DPPH and OH radicals in a dose-dependent manner (IC50 was 0.91 mg/ml and 0.72 mg/ml).
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Alzheimer's disease (AD) is a progressive age-related neurodegenerative disease characterized by memory loss and cognitive impairment. The major characteristics of AD are amyloid ß plaques, apoptosis, autophagy dysfunction, neuroinflammation, oxidative stress, and mitochondrial dysfunction. These are mostly used as the significant indicators for selecting the effects of potential drugs. It is imperative to explain AD pathogenesis and realize productive treatments. Although the currently used chemical drugs for clinical applications of AD are effective in managing the symptoms, they are inadequate to achieve anticipated preventive or therapeutic outcomes. There are new strategies for treating AD. Traditional Chinese Medicine (TCM) has accumulated thousands of years of experience in treating dementia. Nowadays, numerous modern pharmacological studies have verified the efficacy of many bioactive ingredients isolated from TCM for AD treatment. In this review, representative TCM for the treatment of AD are discussed, and among these herbal medicines, the Lamiaceae family accounts for the highest proportion. It is concluded that monomers and extracts from TCM have potential therapeutic effect for AD treatment.
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As one of the most important components of the lake ecosystem, microorganisms from the freshwater and sediment play an important role in many ecological processes. However, the difference and correlation of bacterial community between these two niches were not clear. This study investigated the diversity of microbial community of freshwater and sediment samples from fifteen locations in Poyang Lake wetland. The correlation between the bacterial community and physicochemical property of Poyang Lake wetland was analyzed by artificial neural network (ANN). Our results demonstrated that the freshwater and sediment bacterial community were dominated by groups of the Bacteroidetes (23.33%) and ß-Proteobacteria (22.54%) separately, whereas, Canalipalpata, Bacillariophyta, Gemmatimonadetes, and Verrucomicrobia were detected in freshwater niches only. Phylogenetic analysis further indicated that bacterial composition in freshwater significantly differed with the sediment niches. There are 34 unique species accounted for 85% in fresh water samples and 28 unique species accounted for 82% in sediment samples. Cluster analysis further proved that all the samples from freshwater niches clustered closely together, far from the rest sediment samples. ANN analysis revealed that the freshwater with high N and P nutrients will greatly increase the diversity of the bacterial communities. In general, both environmental physicochemical properties, not each factor independently, contributed to the shift in the bacterial community structure. The five tributaries (Gan, Fu, Xin, Rao, Xiu Rivers) play a vital role in shaping the bacterial communities of Poyang Lake. This study provides new insights for understanding of microbial community compositions and structures of Poyang Lake wetland.
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Bactérias/isolamento & purificação , Sedimentos Geológicos/microbiologia , Lagos/microbiologia , Microbiota , Bactérias/classificação , Bactérias/genética , China , Sedimentos Geológicos/química , Lagos/química , Redes Neurais de Computação , Nitrogênio/análise , Nitrogênio/metabolismo , Fósforo/análise , Fósforo/metabolismo , Filogenia , Áreas AlagadasRESUMO
Bombyx Batryticatus (BB) is a known traditional Chinese medicine (TCM) utilized to treat convulsions, epilepsy, cough, asthma, headaches, etc. in China for thousands of years. This study is aimed at investigating optimum extraction of protein-rich extracts from BB (BBPs) using response surface methodology (RSM) and exploring the protective effects of BBPs against nerve growth factor (NGF)-induced PC12 cells injured by glutamate (Glu) and their underlying mechanisms. The results indicated optimum process of extraction was as follows: extraction time 1.00 h, ratio of liquid to the raw material 3.80 mL/g and ultrasonic power 230.0 W. The cell viability of PC12 cells stimulated by Glu was determined by CCK-8 assay. The levels of γ-aminobutyric (GABA), interleukin-1ß (IL-1ß), interleukin-4 (IL-4), tumor necrosis factor-α (TNF-α), 5-hydroxytryptamine (5-HT) and glucocorticoid receptor alpha (GR) in PC12 cells were assayed by ELISA. Furthermore, the Ca2+ levels in PC12 cells were determined by flow cytometry analysis. Protein and mRNA expressions of GABAA-Rα1, NMDAR1, GAD 65, GAD 67, GAT 1 and GAT 3 in PC12 cells were evaluated by real-time polymerase chain reaction (RT-PCR) and Western blotting assays. Results revealed that BBPs decreased toxic effects due to Glu treatment and decreased Ca2+ levels in PC12 cells. After BBPs treatments, levels of GABA and 5-HT were increased and contents of TNF-α, IL-4 and IL-1ß were decreased in NGF-induced PC12 cells injured by Glu. Moreover, BBPs up-regulated the expressions of GABAA-Rα1, GAD 65 and GAD 67, whereas down-regulated that of NMDAR1 GAT 1 and GAT 3. These findings suggested that BBPs possessed protective effects on NGF-induced PC12 cells injured by Glu via γ-Aminobutyric Acid (GABA) signaling pathways, which demonstrated that BBPs has potential anti-epileptic effect in vitro. These findings may be useful in the development of novel medicine for the treatment of epilepsy.
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Bombyx/metabolismo , Ácido Glutâmico/efeitos adversos , Proteínas de Insetos/farmacologia , Transdução de Sinais/efeitos dos fármacos , Ácido gama-Aminobutírico/metabolismo , Animais , Sobrevivência Celular/efeitos dos fármacos , Proteínas de Insetos/isolamento & purificação , Interleucina-1beta/metabolismo , Interleucina-4/metabolismo , Fator de Crescimento Neural/farmacologia , Células PC12 , Ratos , Receptores de Glucocorticoides/metabolismo , Serotonina/metabolismo , Fator de Necrose Tumoral alfa/metabolismoRESUMO
Liver fibrosis is involved in the progression of most chronic liver diseases. Even though we have made a huge progress in order to understand the pathogenesis of liver fibrosis, however, there is still a lack of productive treatments. Being a traditional Chinese medicine, Platycodin D (PD), an oleanane kind of triterpenoid saponin has been put to extensive use for treating different kinds of illnesses that include not just anti-nociceptive, but also antiviral, anti-inflammatory, and anti-cancer for thousands of years. Nonetheless, there has been no clarification made for its effects on the progression of liver fibrosis. In this manner, we carried out in vitro studies for the purpose of investigating the anti-fibrosis impact of PD. Activation of hepatic stellate cells was evaluated by means of the detection of the proliferation of HSCs and the expression of specific proteins. We discovered the fact that PD had the potential of activating HSCs. Thereafter, we detected the apoptosis and autophagy of the HSCs; as the results suggested, PD induced apoptosis and autophagy of the HSCs. It augmented the expression level of apoptotic proteins that included Bax, Cytochrome C (cyto-c), cleaved caspase3 and cleaved caspase9, in addition to the autophagy relevant proteins, for instance, LC3II, beclin1, Atg5 and Atg9. Further research was carried out for the investigation of the underlying molecular mechanism, and discovered that PD promoted the phosphorylation of JNK and c-Jun. Treating the JNK inhibitor P600125 inhibited the effect of PD, confirming the impact of PD on the regulation of JNK/c-Jun pathway. Thus, we speculated that PD alleviates liver fibrosis and activation of hepatic stellate via promoting phosphorylation of JNK and c-Jun and further altering the autophagy along with apoptosis of HSCs.
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Células Estreladas do Fígado/efeitos dos fármacos , Cirrose Hepática/prevenção & controle , Fígado/efeitos dos fármacos , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Saponinas/farmacologia , Triterpenos/farmacologia , Animais , Apoptose/efeitos dos fármacos , Proteínas Reguladoras de Apoptose/metabolismo , Autofagia/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Células Estreladas do Fígado/metabolismo , Células Estreladas do Fígado/patologia , Humanos , Fígado/metabolismo , Fígado/patologia , Cirrose Hepática/metabolismo , Cirrose Hepática/patologia , Camundongos , Camundongos Endogâmicos C57BL , Fosforilação , Saponinas/administração & dosagem , Saponinas/uso terapêutico , Triterpenos/administração & dosagem , Triterpenos/uso terapêuticoRESUMO
Objective:Analyze the composition of Tongzhifang,regularity of modified prescriptions based on outpatient medical records of national famous Chinese medicine practitioner Professor YU Ying-ao for the treatment of epilepsy as well as data mining, and summarize the clinical experience of Professor YU in diagnosis and treatment of epilepsy, in order to provide the reference basis for the traditional Chinese medicine treatment epilepsy. Method:Based on the data of outpatient medical records of Professor YU for epilepsy diagnosis and treatment,this study conducted standard patient follow-up,clinical data collection,pretreatment and mining analysis,and was confirmed through expert interviews. Liquorice 2.3 data mining platform and SPSS 17.0 were used for data management and statistical analysis. Result:A total of 1 219 medical records of 243 cases were completely collected. As a result, Professor YU Ying-ao's Tongzhifang for epilepsy was based on ancient prescription Baijinwan,in which Shenglongchi and Ostreae Concha enhance tranquilizing and hyperactivity-subduing effects,Citri Reticulatae Pericarpium,Armeniacae Semen Amarum,Arisaema Cum Bile and Bambusae Caulis in Taenias eliminate phlegm and free channels, Salviae Miltiorrhizae Radix et Rhizoma and Persicae Semen promote blood circulation to remove blood stasis, and the 10 herbs were meticulously composed and well compatible. According to the small sample data,the total effective rate of patients with tetany type epilepsy taking this prescription for 3 months and 6 months was 80% (P<0.01), with no adverse reactions. As for the dosage of Tongzhifang,the dosage for adult pills is generally 3-6 times that of decoction prescriptions,and the dosage for children's pills is generally 5-10 times that of decoction prescriptions. Under the guidance of the combination of disease differentiation and syndrome differentiation,epilepsy at the acute phase was treated with additionally Hupomo 1.5-3 g,the ratio of Curcumae Radix to Alumen is usually 4∶1, severe convulsion was treated with additionally Uncariae Ramulus Cum Uncis, Bombyx Batryticatus and Pheretima, epilepsy due to trauma was treated with additionally Typhae Pollen, Eupolyphaga Steleophaga, Carthami Flos and Radix Paeoniae Rubra; constipation was treated with additionally Cannabis Fructus; fatigue was treated with additionally Astragali Radix; dyspepsia was treated with additionally Galli Gigerii Endothelium Corneum; and irritability treated with additionally Gentiana scabra Bunge. Conclusion:The composition of Professor YU's Tongzhifang for treating epilepsy with Qianzhen Zhixian Huatan Tongluo method is relatively stable. Modified prescriptions are based on syndrome differentiation. Clinical experience and dosage range of decoction prescription and pill prescription for adults and children are available.
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A new xanthone glycoside, 3,5,7,8-tetramethoxyxanthone-1-O-ß-D-glucopyranoside (1), along with five known compounds, mangiferin (2), kaempferol (3), quercetin (4), chlorogenic acid (5) and diploptene (6), was isolated from the whole plants of Pyrrosia sheareri (Bak.) Ching. The structure of compound 1 was established on the basis of extensive spectroscopic analyses and chemical methods.
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Glicosídeos/isolamento & purificação , Polypodiaceae/química , Xantonas/isolamento & purificação , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Glicosídeos/química , Quempferóis/isolamento & purificação , Estrutura Molecular , Quercetina/isolamento & purificação , Análise Espectral , Triterpenos/isolamento & purificação , Xantonas/químicaRESUMO
Four new α-pyrones, hypotiens A-D (1-4), were isolated from a fungal endophyte, Hypoxylon investiens J2, harbored in the medicinal plant Blumea balsamifera. Their structures were determined through detailed HRMS and NMR spectroscopic data. Compounds 1-4 are new α-pyrone derivatives containing an unusual dimethyl substitution in the highly unsaturated side chain. Their plausible biosynthetic pathway was discussed. Biological assay indicated that compounds 1-4 showed no antimicrobial, quorum sensing inhibitory, and cytotoxic activities. The specific side chain in α-pyrone derivatives 1-4 might be responsible for the weak pharmacological activities.
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Owing to the unique advantages of high specificity and minimal invasiveness, photothermal therapy (PTT) has been evidenced with great potential in cancer treatment. However, most photothermal agents present a shortage of photobleaching and nonspecific biodistribution in clinical application. In this study, we conjugated a new Indocyanine Green Dye (IR820) with self-assembled polypeptide (ELP) via chemical bonding in an aqueous environment. This preparation method could effectively avoid damaging the polypeptide. ELP-IR820 was fabricated as nanoconjugates with diameters of approximately 50 nm. The use of ELP-IR820 notably enhanced photothermal-mediated cytotoxicity on CT-26 cancer cells. We demonstrate that the ELP-IR820 nanoparticles significantly improved drug accumulation in the tumor and photothermal effect in vivo compared to the free dye and monomer ELP-IR820. ELP-IR820 nanoparticle also exhibited outstanding ability to cause prominent tumor tissue growth inhibition via the photothermal effect. No noticeable toxicity was detected for all treatment groups. These investigations broaden the application of NIR dyes as a multimodal photothermal therapy platform.
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Verde de Indocianina/química , Peptídeos/química , Peptídeos/uso terapêutico , Fototerapia/métodos , Sequência de Aminoácidos , Animais , Linhagem Celular Tumoral , Transformação Celular Neoplásica , Feminino , Humanos , Hipertermia Induzida , Camundongos , Camundongos Endogâmicos BALB C , Nanopartículas/química , Peptídeos/farmacocinética , Temperatura , Distribuição TecidualRESUMO
PURPOSE: The National Comprehensive Cancer Network guidelines indicate that radiotherapy in gastric cancer shows limited effectiveness at reducing the growth of gastric cancer. Therefore, enhancing the sensitivity and effect of radiotherapy with propranolol, a ß-adrenoceptor antagonist, could reduce tumor growth. The role of propranolol as a radiosensitizer has not been adequately studied; therefore, the purpose of the present study is to evaluate the effect of propranolol as a radiosensitizer against gastric cancer in vivo. METHODS: Sixty-four male nude mice bearing tumor xenografts were randomly divided into four groups. Cell culture was performed using the human gastric adenocarcinoma cell line SGC-7901. Mice with tumor xenografts were treated with propranolol, isoproterenol, and radiation. The data for tumor weight and volume were obtained for statistical analyses. Furthermore, the expression levels of COX-2, NF-κB, VEGF, and EGFR were examined using immunohistochemical techniques and Western blotting. RESULTS: The growth in the volume and weight of the tumor was lower in mouse models treated with propranolol and radiation therapy compared to the other groups. Decreased expression of NF-κB was also observed in treatment groups where both propranolol and radiation were used, leading to the reduction of COX-2, EGFR, and VEGF expression compared to that in the other groups. CONCLUSION: The present study indicated that propranolol potentiates the antitumor effects of radiotherapy in gastric cancer by inhibiting NF-κB expression and its downstream genes: VEGF, EGFR, and COX-2.
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Propranolol/uso terapêutico , Radiossensibilizantes/uso terapêutico , Neoplasias Gástricas/tratamento farmacológico , Animais , Modelos Animais de Doenças , Humanos , Masculino , Camundongos Nus , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/patologia , Propranolol/administração & dosagem , Radiossensibilizantes/administração & dosagem , Neoplasias Gástricas/patologia , Células Tumorais CultivadasRESUMO
Depression is a common, dysthymic, and psychiatric disorder, resulting in enormous social and economic burden. Dammarane sapogenins (DS), an active fraction from oriental ginseng, has shown antidepressant-like effects in chronic restraint rats and sleep interruption-induced mice, and the present study aimed to further confirm the antidepressant effects of DS in a model of chronic unpredictable mild stress (CUMS) and to explore the underlying mechanism. Oral administration of DS (20, 40, and 80 mg/kg) markedly improved depressant-like behaviors, increasing the sucrose intake in the sucrose preference test and reducing the latency in the novelty-suppressed feeding test, and decreasing the immobility time in both the tail suspension and forced swimming tests, compared with the CUMS mice. Biochemical analysis of brain tissue and serum showed that DS treatment restored the decreased hippocampal neurotransmitter concentrations of serotonin, dopamine, norepinephrine (noradrenaline), and gamma-aminobutyric acid, and decreased the elevated of serum hormone levels (corticotrophin releasing factor, adrenocorticotrophic hormone, and corticosterone) induced by CUMS. Our findings confirm that DS exerts an antidepressant-like effect in the CUMS model of depression in mice, and suggest it may be mediated by regulation of neurotransmitters and hypothalamic-pituitary-adrenal axis.