RESUMO
Latent thermal energy storage (LTES) devices can efficiently store renewable energy in thermal form and guarantee a stable-temperature thermal energy supply. The gravity-driven motion melting (GDMM) process improves the overall melting rate for packaged phase-change material (PCM) by constructing an enhanced flow field in the liquid phase. However, due to the complex mechanisms involved in fluid-solid coupling and liquid-solid phase transition, numerical simulation studies that demonstrate physical details are necessary. In this study, a simplified numerical model based on the Eulerian method is proposed. We aimed to introduce a fluid deformation yield stress equation to the "solid phase" based on the Bingham fluid assumption. As a result, fluid-solid coupling and liquid-solid phase transition processes become continuously solvable. The proposed model is validated by the referenced experimental measurements. The enhanced performance of liquid-phase convection and the macroscopic settling of the "solid phase" are numerically analyzed. The results indicate that the enhanced liquid-phase fluidity allows for a stronger heat transfer process than natural convection for the pure liquid phase. The gravity-driven pressure difference is directly proportional to the vertical melting rate, which indicates the feasibility of controlling the pressure difference to improve the melting rate.
RESUMO
Chemome characterization is the prerequisite for either therapeutic mechanism clarification or quality control of traditional Chinese medicine prescriptions (TCMPs). Liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) currently serves as the most popular analytical tool; however, chemome characterization is still challenged by MS/MS spectral acquisition and post-acquisition data processing. Here, an integrated strategy was proposed for in-depth chemome clarification of Shengbai oral liquid (SBOL). Gas phase ion fractionation with staggered mass ranges was demonstrated to be the superior acquisition method regarding MS2 spectrum coverage in this study, and narrower mass range further advanced coverage. To facilitate information extraction, all ingredient materials were measured in parallel to form an in-house library, where each MS1 -MS2 item generated a square mass-to-charge ratio (m/z) frame to capture the tagged identity and each chemical family produced a pentagon frame for mass defect features to accomplish chemical analogs-targeted quasi-molecular ion extraction. Square m/z frame imprinting captured 355 identities, while mass defect frames extracted 275 compounds. Attributing to comprehensive MS2 spectrum acquisition and efficient data processing, 355 components were captured and tentatively identified, resulting in a clarified chemical composition for SBOL. Therefore, the proposed strategy should be meaningful for the chemome characterization of TCMPs.
Assuntos
Medicamentos de Ervas Chinesas , Medicina Tradicional Chinesa , Cromatografia Líquida , Espectrometria de Massas em Tandem , Medicamentos de Ervas Chinesas/análise , Cromatografia Líquida de Alta Pressão/métodosRESUMO
In order to provide scientific basics for exploitation and sufficient application of Polyporus umbellatus resources and study the monosaccharide composition of P. umbellatus polysaccharides,the anthrone-sulfuric acid method was applied to compare polysaccharide content of P. umbellatus from 17 producing areas. The monosaccharides were derived by 1-phenyl-3-methyl-5-pyrazolone( PMP) and the derivatives were identified by UPLC-MS/MS and the content of each monosaccharide component was determined simultaneously. The results demonstrated that there was a certain difference in total polysaccharide content of P. umbellatus from different regions,and the content of total P. umbellatus polysaccharide from Shaanxi province and Sichuan province( 1. 15% and 1. 90%) was relatively higher than that of others areas. Polysaccharides from P. umbellatus was mainly composed of eight monosaccharides,including glucose,glucuronic acid,galactose,ribose,xylose,arabinose,mannose and fucose. The contents of glucose( 17. 65 mg·g-1) was higher than others. The ribose was the lowest( 0. 13 mg·g-1). In addition,fructose,rhamnose and galacturonic acid were also detected in some samples. Furthermore,the results of cluster analysis( CA) and principal component analysis( PCA) indicated that totally 17 batches of P. umbellatus polysaccharide could be classified into three clusters,samples collected from Wuchang in Heilongjiang province were clustered into one group separately. The study can provide a basis for rational utilization of P. umbellatus resources,and also implies the sequence of monosaccharide linking and pharmacological activity of P. umbellatus polysaccharides.
Assuntos
Monossacarídeos/química , Polyporus/química , Polissacarídeos/química , China , Cromatografia Líquida de Alta Pressão , Geografia , Espectrometria de Massas em TandemRESUMO
Schisandrin B has received much attention owing to its various biological activities. The present study was aimed at the formulation development of schisandrin B and investigation of the pharmacokinetic profiles, distribution and excretion of schisandrin B in Sprague-Dawley rats. In this study, micronized schisandrin B particles with particle size of 10-20 µm were chosen as the research object. Chromatographic separation was carried out on a BDS Hypersil C18 column (50 × 2.1 mm, i.d. 3.5 µm). Schisandrin B and deoxyschizandrin (internal standard) were detected without interference in the multiple reaction monitoring mode with positive electrospray ionization. The pharmacokinetic parameters were calculated by a noncompartmental method. The area under concentration-time curve and the maximum concentration showed a significant difference in gender. The calculated absolute oral bioavailability of schisandrin B was ~55.0% for female rat and 19.3% for male rat. Schisandrin B exhibited linear pharmacokinetics properties within the range of the tested oral dose (10, 20 and 40 mg/kg). After oral administration of schisandrin B, it was extensively distributed in ovary and adipose tissue. The result also showed very low urinary, biliary and fecal excretion of schisandrin B implying that schisandrin B was excreted mainly in the forms of metabolites.
Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Lignanas/análise , Lignanas/farmacocinética , Compostos Policíclicos/análise , Compostos Policíclicos/farmacocinética , Espectrometria de Massas em Tandem/métodos , Animais , Ciclo-Octanos/análise , Ciclo-Octanos/química , Ciclo-Octanos/farmacocinética , Feminino , Lignanas/química , Modelos Lineares , Masculino , Compostos Policíclicos/química , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Distribuição TecidualRESUMO
In this study, it is to compare the effectiveness of prevention against and treatment of doxorubicin (DOX) induced cardiotoxicity by dexrazoxane and schisandrin B (Sch B) in rats. Sprague-Dawley (SD) rats were randomly divided into the following 6 groups: normal saline group, DOX group, DOX+DEX group, DOX+Sch B (80 mg x kg(-1)) group, DOX+Sch B (40 mg x kg(-1)) group and DOX+Sch B (20 mg x kg(-1)) group. The results showed that Sch B could combat the increase of myocardial enzymes in peripheral blood, decrease of the enzyme activity of myocardial tissue antioxidant enzymes and disorders of systolic and diastolic function of heart in rats intravenously injected with doxorubicin (15 mg x kg(-1)). Sch B was better than DEX in protecting rat against DOX-induced the symptoms. Sch B could protect rat against DOX-induced acute cardiomyopathy and has clinical potential applications.
Assuntos
Antibióticos Antineoplásicos/efeitos adversos , Cardiotoxicidade/tratamento farmacológico , Dexrazoxano/uso terapêutico , Doxorrubicina/efeitos adversos , Lignanas/uso terapêutico , Compostos Policíclicos/uso terapêutico , Animais , Antioxidantes/metabolismo , Cardiomiopatias/induzido quimicamente , Cardiomiopatias/tratamento farmacológico , Ciclo-Octanos/uso terapêutico , Coração/fisiopatologia , Miocárdio/enzimologia , Ratos , Ratos Sprague-DawleyRESUMO
Claudins, the integral tight junction proteins that regulate paracellular permeability and cell polarity, are frequently dysregulated in cancer; however, their roles in regulating EGFR tyrosine kinase inhibitors (EGFR-TKIs) resistance in non-small cell lung cancer (NSCLC) are unknown. To this end, we performed GEO dataset analysis and identified that claudin1 was a critical regulator of EGFR-TKI resistance in NSCLC cells. We also found that claudin1, which was highly induced by continuous gefitinib treatment, was significantly upregulated in EGFR-TKI-resistant NSCLC cells. By knocking down claudin1 in cell lines and xenograft models, we established that gefitinib resistance was decreased. Moreover, claudin1 knockdown suppressed the expression levels of pluripotency markers (Oct4, Nanog, Sox2, CD133, and ALDH1A1). Claudin1 loss inhibited phosphorylated AKT (p-AKT) expression and reduced cancer cell stemness by suppressing AKT activation. Furthermore, SKL2001, a ß-catenin agonist, upregulated the expression levels of claudin1, p-AKT, and pluripotency markers, and 1,25-dihydroxy-vitamin D3 (1,25(OH)2D3) reduced claudin1 expression, AKT activation, and cancer cell stemness by inhibiting ß-catenin, and suppressed claudin1/AKT pathway mediated cancer stem-like properties and gefitinib resistance. Collectively, inhibition of claudin1-mediated cancer stem-like properties by 1,25(OH)2D3 may decrease gefitinib resistance through the AKT pathway, which may be a promising therapeutic strategy for inhibiting gefitinib resistance in EGFR-mutant lung adenocarcinoma.
RESUMO
Colitis-associated cancer (CAC) has a close relationship with ulcerative colitis (UC). Therapeutic effect of Schisandrin B (SchB) on UC and CAC remains largely unknown. We investigated the preventative effect of SchB on the dextran sulphate sodium (DSS) model of UC and azoxymethane (AOM)/DSS model of CAC. Furthermore, focal adhesion kinase (FAK) activation and influence on commensal microbiota are important for UC treatment. Impact on FAK activation by SchB in UC development was evaluated in vivo and vitro. We also conducted 16S rRNA sequencing to detect regulation of gut microbiota by SchB. Enhanced protection of intestinal epithelial barrier by SchB through activating FAK contributed to protective effect on colon for the fact that protection of SchB can be reversed by inhibition of FAK phosphorylation. Furthermore, influence on gut microbiota by SchB also played a significant role in UC prevention. Our results revealed that SchB was potent to prevent UC by enhancing protection of intestinal epithelial barrier and influence on gut microbiota, which led to inhibition of CAC. SchB was potential to become a new treatment for UC and prevention of CAC.
Assuntos
Colite Ulcerativa/prevenção & controle , Neoplasias do Colo/patologia , Proteína-Tirosina Quinases de Adesão Focal/metabolismo , Microbioma Gastrointestinal/efeitos dos fármacos , Lignanas/farmacologia , Compostos Policíclicos/farmacologia , Animais , Células CACO-2 , Colite Ulcerativa/complicações , Colite Ulcerativa/microbiologia , Colite Ulcerativa/patologia , Neoplasias do Colo/complicações , Ciclo-Octanos/farmacologia , Citoproteção/efeitos dos fármacos , Ativação Enzimática/efeitos dos fármacos , Células HCT116 , Humanos , Mucosa Intestinal/efeitos dos fármacos , Mucosa Intestinal/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Permeabilidade/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacosRESUMO
Melittin is the main effective component of bee venom and has extensive biological functions; however, serious side effects have restricted its clinical application. Preclinical and clinical studies showed that the main adverse events were allergic reaction and pain at the administration site. To decrease the toxicity, we prepared melittin nano-liposomes by encapsulating melittin with poloxamer 188 and explored the inhibitory activities on liver cancer together with biological safety. Here, we showed that melittin nano-liposomes significantly inhibited the survival of hepatocellular carcinoma (HCC) cells in vitro and prominently suppressed the growth of subcutaneous and orthotopic HCC transplantation tumors in vivo. It was important that it induced less inflammation and allergy in mice compared with melittin. Overall, melittin nano-liposomes would have a better application in HCC therapy due to its significant anti-tumor activity and better biological safety.