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1.
Molecules ; 29(5)2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38474673

RESUMO

1,3,6-Trigalloylglucose is a natural compound that can be extracted from the aqueous extracts of ripe fruit of Terminalia chebula Retz, commonly known as "Haritaki". The potential anti-Helicobacter pylori (HP) activity of this compound has not been extensively studied or confirmed in scientific research. This compound was isolated using a semi-preparative liquid chromatography (LC) system and identified through Ultra-high-performance liquid chromatography-MS/MS (UPLC-MS/MS) and Nuclear Magnetic Resonance (NMR). Its role was evaluated using Minimum inhibitory concentration (MIC) assay and minimum bactericidal concentration (MBC) assay, scanning electron microscope (SEM), inhibiting kinetics curves, urea fast test, Cell Counting Kit-8 (CCK-8) assay, Western blot, and Griess Reagent System. Results showed that this compound effectively inhibits the growth of HP strain ATCC 700392, damages the HP structure, and suppresses the Cytotoxin-associated gene A (Cag A) protein, a crucial factor in HP infection. Importantly, it exhibits selective antimicrobial activity without impacting normal epithelial cells GES-1. In vitro studies have revealed that 1,3,6-Trigalloylglucose acts as an anti-adhesive agent, disrupting the adhesion of HP to host cells, a critical step in HP infection. These findings underscore the potential of 1,3,6-Trigalloylglucose as a targeted therapeutic agent against HP infections.


Assuntos
Helicobacter pylori , Terminalia , Extratos Vegetais/química , Terminalia/química , Cromatografia Líquida , Espectrometria de Massas em Tandem , Água
2.
Acta Pharmacol Sin ; 44(12): 2492-2503, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37468692

RESUMO

Endothelial dysfunction, a central hallmark of cardiovascular pathogenesis in diabetes mellitus, is characterized by impaired endothelial nitric oxide synthase (eNOS) and NO bioavailability. However, the underlying mechanisms remain unclear. Here in this study, we aimed to identify the role of calmodulin (CaM) in diabetic eNOS dysfunction. Human umbilical vein endothelial cells and murine endothelial progenitor cells (EPCs) treated with high glucose (HG) exhibited downregulated CaM mRNA/protein and vascular endothelial growth factor (VEGF) expression with impeded eNOS phosphorylation and cell migration/tube formation. These perturbations were reduplicated in CALM1-knockdown cells but prevented in CALM1-overexpressing cells. EPCs from type 2 diabetes animals behaved similarly to HG-treated normal EPCs, which could be rescued by CALM1-gene transduction. Consistently, diabetic animals displayed impaired eNOS phosphorylation, endothelium-dependent dilation, and CaM expression in the aorta, as well as deficient physical interaction of CaM and eNOS in the gastrocnemius. Local CALM1 gene delivery into a diabetic mouse ischemic hindlimb improved the blunted limb blood perfusion and gastrocnemius angiogenesis, and foot injuries. Diabetic patients showed insufficient foot microvascular autoregulation, eNOS phosphorylation, and NO production with downregulated CaM expression in the arterial endothelium, and abnormal CALM1 transcription in genome-wide sequencing analysis. Therefore, our findings demonstrated that downregulated CaM expression is responsible for endothelium dysfunction and angiogenesis impairment in diabetes, and provided a novel mechanism and target to protect against diabetic endothelial injury.


Assuntos
Diabetes Mellitus Tipo 2 , Humanos , Camundongos , Animais , Diabetes Mellitus Tipo 2/metabolismo , Calmodulina/genética , Calmodulina/metabolismo , Fator A de Crescimento do Endotélio Vascular/metabolismo , Células Endoteliais da Veia Umbilical Humana/metabolismo , Endotélio/metabolismo , Isquemia/metabolismo , Óxido Nítrico Sintase Tipo III/genética , Óxido Nítrico Sintase Tipo III/metabolismo , Neovascularização Fisiológica
3.
Artigo em Inglês | MEDLINE | ID: mdl-37045748

RESUMO

BACKGROUND: Adolescent idiopathic scoliosis (AIS) is the most prevalent spinal deformity, which may have long-term negative consequences on adolescents. The research on the etiology is of great importance for identifying high-risk population and formulate tailored prevention. This study aimed to evaluate the association between academic-related factors and daily lifestyle habits and AIS. METHODS: In this population-based case-control study, 491 AIS cases and 1,346 healthy controls that frequency-matched by age and sex were recruited in Shenzhen, Southern China. AIS was diagnosed as a Cobb angle ≥ 10° on standing posteroanterior radiographs of the whole spine. The academic-related factors (e.g., reading and writing posture) and daily lifestyle habits (e.g., intake of milk and dairy products) were collected by a self-reported questionnaire. The logistic regression analysis was performed. RESULTS: After adjusting for potential confounding factors, multivariable logistic regression models demonstrated that academic-related factors were associated with AIS. Individuals with poor reading and writing posture were more likely to have AIS (AOR: 2.06, 95%CI: 1.58-2.68). Moreover, there was a significant association between heavy school bags and AIS (AOR: 2.22, 95%CI: 1.50-3.31). Additionally, adolescents who reported daily screen time on weekdays over 2 hours were more likely to develop AIS (P < 0.001). Regarding daily lifestyle habits, individuals without the habit of taking milk and dairy products had a higher risk of developing AIS (AOR: 1.87, 95%CI: 1.29-2.71). CONCLUSIONS: Academic-related factors and daily lifestyle habits were associated with AIS among Chinese adolescents. Schools, families, and related facilities are recommended to take actions on developing effective prevention and management strategies that integrates "Student-Family-School-Education-Health-Sports" for AIS.


Assuntos
Escoliose , Esportes , Humanos , Adolescente , Escoliose/epidemiologia , Escoliose/etiologia , Estudos de Casos e Controles , Estilo de Vida , Fatores de Risco
4.
Artigo em Inglês | MEDLINE | ID: mdl-37766541

RESUMO

BACKGROUND: Adolescent idiopathic scoliosis (AIS) is the most common type of idiopathic scoliosis, affecting approximately 0.61%-6.15% adolescents worldwide. To date, the results on the relationship between moderate-to-vigorous physical activity (MVPA) and AIS were inconsistent, and the association between screen time (ST) and AIS remained unclear. This study aimed to describe MVPA and ST among adolescents, and to explore the independent and joint associations between PA, ST, and AIS. METHODS: A frequency-matched case-control study based on the 2021 Chinese School-based Scoliosis Screening Program in Shenzhen city, south China, was conducted. The research involved 494 AIS patients (aged 9-17 years) and 994 sex- and age-matched healthy controls. MVPA and ST were measured using a self-administered questionnaire. Logistic regression models estimated associations between PA, ST, and AIS. RESULTS: Compared to subjects meeting the recommended 60-min daily of MVPA, adolescents reporting daily MVPA time less than 60 min had 1.76 times higher odds of experiencing AIS (95% CI: 1.32-2.35) and adolescents reporting daily MVPA in inactive status had 2.14 times higher odds of experiencing AIS (95% CI: 1.51-3.03). Moreover, participants reporting ST for 2 hours or more had 3.40 times higher odds of AIS compared with those reporting ST less than 2 hours (95% CI: 2.35-4.93). When compared with the adolescents reporting both ST and MVPA meeting the guidelines recommended times (ST < 2 h and MVPA ≥ 60 min/day), those reporting both ST ≥ 2 h and MVPA in inactive status are 8.84 times more likely to develop AIS (95% CI: 3.99-19.61). CONCLUSIONS: This study reported that the insufficient MVPA, especially MVPA in inactive status, and excessive ST were risk factors for AIS. Additionally, the joint effects of insufficient MVPA and excessive ST probably increase the risk of AIS.


Assuntos
Exercício Físico , Escoliose , Tempo de Tela , Adolescente , Humanos , Estudos de Casos e Controles , Escoliose/epidemiologia , População do Leste Asiático
5.
Zhongguo Zhong Yao Za Zhi ; 48(10): 2803-2809, 2023 May.
Artigo em Zh | MEDLINE | ID: mdl-37282940

RESUMO

This study aimed to explore the potentiating effect and mechanism of the extract of Jingfang Granules(JFG) on the activation of macrophages. The RAW264.7 cells were treated with JFG extract and then stimulated by multiple agents. Subsequently, mRNA was extracted, and reverse transcription-polymerase chain reaction(RT-PCR) was used to measure the mRNA transcription of multiple cytokines in RAW264.7 cells. The levels of cytokines in the cell supernatant were detected by enzyme-linked immunosorbent assay(ELISA). In addition, the intracellular proteins were extracted and the activation of signaling pathways was determined by Western blot. The results showed that JFG extract alone could not promote or slightly promote the mRNA transcription of TNF-α, IL-6, IL-1ß, MIP-1α, MCP-1, CCL5, IP-10, and IFN-ß, and significantly enhance the mRNA transcription of these cytokines in RAW264.7 cells induced by R848 and CpG in a dose-dependent manner. Furthermore, JFG extract also potentiated the secretion of TNF-α, IL-6, MCP-1, and IFN-ß by RAW264.7 cells stimulated with R848 and CpG. As revealed by mechanism analysis, JFG extract enhanced the phosphorylation of p38, ERK1/2, IRF3, STAT1, and STAT3 in RAW264.7 cells induced by CpG. The findings of this study indicate that JFG extract can selectively potentiate the activation of macrophages induced by R848 and CpG, which may be attributed to the promotion of the activation of MAPKs, IRF3, and STAT1/3 signaling pathways.


Assuntos
Interleucina-6 , Fator de Necrose Tumoral alfa , Fator de Necrose Tumoral alfa/metabolismo , Interleucina-6/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/metabolismo , Lipopolissacarídeos/farmacologia , Macrófagos , Citocinas/genética , Citocinas/metabolismo , RNA Mensageiro/metabolismo
6.
Genomics ; 112(1): 55-64, 2020 01.
Artigo em Inglês | MEDLINE | ID: mdl-31404627

RESUMO

Coilia nasus (C. nasus) is an important anadromous fish species that resides in the Yangtze River in China. However, wild C. nasus have suffered serious damage as a result of overfishing and environmental pollution. We performed comparative liver and brain transcriptome analyses of C. nasus from the Jingjiang (JJ) and Dangtu (DT) sections of the Yangtze River. The results indicate that, during migration, most signal pathways in C. nasus livers were downregulated, indicating that the liver has a function in energy conservation. The brain assumes more of a regulatory role, and the signal transduction pathways and relevant genes were upregulated. This study provides genetic information for screening the key regulatory genes of gonad development of C. nasus, which can be applied in the artificial breeding of C. nasus, providing high-quality fish fry for proliferation and release and may also contribute to efforts towards the restoration of wild C. nasus.


Assuntos
Migração Animal , Peixes/genética , Transdução de Sinais/genética , Animais , Encéfalo/metabolismo , China , Metabolismo Energético/genética , Feminino , Peixes/metabolismo , Peixes/fisiologia , Perfilação da Expressão Gênica , Genoma , Fígado/metabolismo , Masculino
7.
Aesthetic Plast Surg ; 45(5): 2426-2436, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-33959783

RESUMO

BACKGROUND: Autologous fat grafts have been widely in use for reconstruction, contour abnormalities, and cosmetic surgeries. However, the grafted fat one-year survival rate is unpredictable and always low (20%-80%). Standardizing the existing transplantation technology is difficult due to the limiting conditions. Scaffold materials or drugs are unsuitable to employ because of legal restrictions, complex production, and undetermined hazards. Therefore, a simpler and more effective approach to improve grafted fat survival rate is using commercial products as additives. Earlier studies proved that porcine acellular dermal matrix (PADM), a biomaterial clinically used for wound repair, could work as a scaffold for lipo-implantation. This study aimed at investigating the hitherto unclear effect of PADM on transplanted fat survival. METHODS: Thirty-two 8-week-old female nude mice were divided into two groups. Control mice received a 300 µl fat injection, while the PADM group mice were injected with a 300 µl PADM-fat mixture. After a 4-week treatment, fat weight and liquefaction ratio were assessed. Histological changes were quantified via hematoxylin & eosin (H&E) staining. Macrophage infiltration and vascular regeneration were revealed using an anti-CD34 antibody. Mouse and human mRNA expression levels were gauged via RNA-sequencing. On the third day post implantation, the mRNA expression levels of inflammatory genes Mcp-1 and Tnf-α were measured by qRT-PCR. RESULTS: The weight of surviving grafted fat did not differ between the control and the PADM group. However, adding PADM significantly decreased fat liquefaction. H&E-stained sections showed that PADM decreased fat necrosis, increased fat tissue regeneration, and raised CD34 levels in the regenerated tissue. RNA-sequencing showed that, compared to controls, fats from PADM-added group expressed more mouse-related mRNA but less human-related mRNA. The following GO and KEGG analysis showed that added PADM increased extracellular matrix (ECM) genes expression levels. The qRT-PCR showed that adding PADM increased Mcp-1 and Tnf-α mRNA expression levels. CONCLUSIONS: In summary, PADM addition increased fat survival rate by reducing fat liquefaction through an increased macrophage infiltration, ECM regeneration, and revascularization. Therefore, PADM addition is a workable application in autologous fat grafting. NO LEVEL ASSIGNED: This journal requires that authors assign a level of evidence to each article. For a full description of these Evidence-Based Medicine ratings, please refer to the Table of Contents or the online Instructions to Authors www.springer.com/00266 .


Assuntos
Derme Acelular , Tecido Adiposo , Animais , Feminino , Camundongos , Camundongos Nus , Taxa de Sobrevida , Suínos , Cicatrização
8.
Zhongguo Zhong Yao Za Zhi ; 46(16): 4131-4138, 2021 Aug.
Artigo em Zh | MEDLINE | ID: mdl-34467724

RESUMO

Eleven condensed tannins were isolated from the roots of Indigofera stachyodes by various column chromatography techniques including silica gel, octadecyl silica(ODS), Sephadex LH-20, and semi-preparative high performance liquid chromatography(HPLC). These compounds were identified on the basis of physicochemical properties, nuclear magnetic resonance(NMR) and mass spectrometry(MS) data as stachyotannin A(1), epicatechin-(2ß→O→7,4ß→8)-epiafzelechin-(4ß→8)-catechin(2), cinnamtannin D1(3), cinnamtannin B1(4), epicatechin-(2ß→O→7,4ß→8)-epiafzelechin-(4α→8)-epicatechin(5), gambiriin C(6), proanthocyanidin A1(7), proanthocyanidin A2(8), aesculitannin B(9), proanthocyanidin A4(10), and procyanidin B5(11). Compound 1 is a new compound. Compounds 2-11 were isolated from Indigofera for the first time. Furthermore, compounds 1, 2, and 4-11 showed inhibitory effects on thrombin-induced ATP release in platelets.


Assuntos
Indigofera , Proantocianidinas , Cromatografia Líquida de Alta Pressão , Espectroscopia de Ressonância Magnética , Extratos Vegetais
9.
J Biol Chem ; 294(8): 2628-2641, 2019 02 22.
Artigo em Inglês | MEDLINE | ID: mdl-30602571

RESUMO

Trametes robiniophila Murr. (Huaier) is a mushroom with a long history of use as a medicinal ingredient in China and exhibits good clinical efficacy in cancer management. However, the antitumor components of Huaier and the underlying molecular mechanisms remain poorly understood. Here, we isolated a proteoglycan with a molecular mass of ∼5.59 × 104 Da from Huaier aqueous extract. We named this proteoglycan TPG-1, and using FTIR and additional biochemical analyses, we determined that its total carbohydrate and protein compositions are 43.9 and 41.2%, respectively. Using biochemical assays and immunoblotting, we found that exposing murine RAW264.7 macrophages to TPG-1 promotes the production of nitric oxide (NO), tumor necrosis factor α (TNFα), and interleukin-6 (IL-6) through Toll-like receptor 4 (TLR4)-dependent activation of NF-κB and mitogen-activated protein kinase (MAPK) signaling. Of note, the TPG-1 treatment significantly inhibited the tumorigenesis of human hepatoma HepG2 cells likely at least in part by increasing serum levels of TNFα and promoting leukocyte infiltration into tumors in nude mice. TPG-1 also exhibited good antitumor activity in hepatoma H22-bearing mice and had no obvious adverse effects in these mice. We conclude that TPG-1 exerts antitumor activity partially through an immune-potentiating effect due to activation of the TLR4-NF-κB/MAPK signaling cassette. Therefore, TPG-1 may be a promising candidate drug for cancer immunotherapy. This study has identified the TPG-1 proteoglycan as an antitumor agent and provided insights into TPG-1's molecular mechanism, suggesting a potential utility for applying this agent in cancer therapy.


Assuntos
Carcinoma Hepatocelular/tratamento farmacológico , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Neoplasias Hepáticas/tratamento farmacológico , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , NF-kappa B/metabolismo , Proteínas de Neoplasias/metabolismo , Receptor 4 Toll-Like/metabolismo , Trametes/química , Regulação para Cima/efeitos dos fármacos , Animais , Antineoplásicos , Carcinoma Hepatocelular/genética , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Citocinas/biossíntese , Citocinas/genética , Células Hep G2 , Humanos , Neoplasias Hepáticas/genética , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Sistema de Sinalização das MAP Quinases/genética , Camundongos Nus , NF-kappa B/genética , Proteínas de Neoplasias/genética , Óxido Nítrico/genética , Óxido Nítrico/metabolismo , Proteoglicanas/química , Proteoglicanas/farmacologia , Receptor 4 Toll-Like/genética , Ensaios Antitumorais Modelo de Xenoenxerto
10.
Pharmacogenomics J ; 20(2): 169-178, 2020 04.
Artigo em Inglês | MEDLINE | ID: mdl-31796890

RESUMO

Many medical centers in the United States have implemented pharmacogenomics (PGx) programs to integrate PGx into clinical practice. The roles of pharmacists in optimizing medication use based on genetic testing results are emergently evolving. A literature search was conducted to assess pharmacists' roles in pharmacogenetics/pharmacogenomics or precision/personalized medicine programs. Fifteen PGx pharmacy practice models implemented in eleven hospitals and one community pharmacy in the U.S. were selected for evaluation. Pharmacists perform results interpretation, genotype-guided medication selection and adjustment, medication acquisition, adverse reactions monitoring, and patient education. Institutions that are interested in implementing a PGx program should plan the strategies to overcome the challenges, such as educational knowledge gaps, informatics, and reimbursement issues. Strong institutional support, well-defined goals, standardized procedures, and strategies to educate clinicians and patients are the prerequisites to comprehensively deliver genomic data for individualized drug therapy.


Assuntos
Serviços Comunitários de Farmácia/organização & administração , Conduta do Tratamento Medicamentoso/organização & administração , Farmacêuticos/organização & administração , Farmacogenética/métodos , Medicina de Precisão/métodos , Conhecimentos, Atitudes e Prática em Saúde , Humanos , Educação de Pacientes como Assunto , Papel Profissional , Estados Unidos
11.
J Nat Prod ; 81(3): 543-553, 2018 03 23.
Artigo em Inglês | MEDLINE | ID: mdl-29227647

RESUMO

Sixteen new 2-(2-phenylethyl)chromone dimers, including four pairs of enantiomers (1a/1b, 3a/3b, 6a/6b, and 8a/8b), along with eight optically pure analogues (2, 4, 5, 7, and 9-12) were isolated from the resinous wood of Aquilaria sinensis. Their structures were determined by extensive spectroscopic analysis (1D and 2D NMR, UV, IR, and HRMS) and experimental and computed ECD data. Compounds 1-10 feature an unusual 3,4-dihydro-2 H-pyran ring linkage connecting two 2-(2-phenylethyl)chromone monomeric units, while compounds 11 and 12 possess an unprecedented 6,7-dihydro-5 H-1,4-dioxepine moiety in their structures. A putative biosynthetic pathway of the representative structures via a diepoxy derivative of a chromone with a nonoxygenated A-ring is also proposed. Compounds 1a/1b, 2, 3a/3b, 5, 7, 8a/8b, and 10-12 exhibited significant inhibition of nitric oxide production in lipopolysaccharide-stimulated RAW264.7 cells with IC50 values in the range 7.0-12.0 µM.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Thymelaeaceae/química , Madeira/química , Animais , Linhagem Celular , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Lipopolissacarídeos/farmacologia , Espectroscopia de Ressonância Magnética/métodos , Camundongos , Óxido Nítrico/metabolismo , Células RAW 264.7 , Resinas Vegetais/química , Resinas Vegetais/farmacologia
12.
Planta Med ; 84(1): 20-25, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-28651290

RESUMO

The anti-inflammatory effects of boldine and reticuline isolated from Litsea cubeba were evaluated by using xylene-induced ear edema and carrageenan-induced paw edema in mice and rats. Our results demonstrated that intragastric administration with boldine and reticuline significantly mitigated ear weight in mice and decreased paw volume in rats. A combination administration of boldine (0.5 mg/kg) + reticuline (0.25 mg/kg) resulted in a potentiated inhibition in these two models. In parallel, boldine or reticuline reduce the infiltration of neutrophil leukocytes in rat paw tissue, respectively, and the combination of the two groups performed a better anti-inflammatory activity as shown in histopathologies. Boldine, reticuline, and their combination notably inhibited mRNA expressions of TNF-α, and IL-6 and reduced the phosphorylation levels of Janus kinase 2 (JAK2) and signal transducer and activator of transcription 3 (STAT3). Beyond that, their combination also can reduce the phosphorylation levels of p65 and IκBα in the pathological tissues of animals, as observed by real-time PCR and western blot analyses, respectively. These findings indicate for the first time that boldine and reticuline have not only anti-inflammatory activity but also potential synergistic effects in vivo. The underlying mechanism may relate to the inhibition on the expression of pro-inflammatory cytokines, such as TNF-α and IL-6, which may be a consequence of JAK2/STAT3 and NF-κB pathway involvements. This study provides useful data for further exploration and application of boldine and reticuline as potential anti-inflammatory medicines.


Assuntos
Anti-Inflamatórios/farmacologia , Aporfinas/farmacologia , Janus Quinase 2/antagonistas & inibidores , Litsea , NF-kappa B/antagonistas & inibidores , Extratos Vegetais/farmacologia , Fator de Transcrição STAT3/antagonistas & inibidores , Transdução de Sinais/efeitos dos fármacos , Animais , Benzilisoquinolinas/farmacologia , Western Blotting , Edema/tratamento farmacológico , Interleucina-6/metabolismo , Janus Quinase 2/fisiologia , Litsea/química , Masculino , Camundongos , Camundongos Endogâmicos ICR , NF-kappa B/fisiologia , Ratos , Ratos Sprague-Dawley , Reação em Cadeia da Polimerase em Tempo Real , Fator de Transcrição STAT3/fisiologia , Fator de Necrose Tumoral alfa/metabolismo
13.
J Nat Prod ; 80(10): 2699-2707, 2017 10 27.
Artigo em Inglês | MEDLINE | ID: mdl-28960979

RESUMO

Eight new chrysogenolides (A-H (1-8)) and seven known (9-15) 3,5-dimethylorsellinic acid derived meroterpenoids were isolated from the solid substrate fermentation cultures of a Huperzia serrata endophytic fungus, Penicillium chrysogenum MT-12. The structures of the new compounds were elucidated by interpretation of spectroscopic and spectrometric data (1D and 2D NMR, IR, and HRESIMS). The absolute configurations of 1-4 were determined by single-crystal X-ray crystallographic analysis, and those of 5-8 were assigned on the basis of experimental and calculated electronic circular dichroism spectra. Compounds 3, 4, 6, 11, and 12 showed inhibition of nitric oxide production in lipopolysaccharide-activated RAW 264.7 macrophage cells with IC50 values in the range of 4.3-78.2 µM (positive control, indomethacin, IC50 = 33.6 ± 1.4 µM).


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Huperzia/microbiologia , Penicillium chrysogenum/química , Resorcinóis/isolamento & purificação , Animais , Cristalografia por Raios X , Medicamentos de Ervas Chinesas/química , Concentração Inibidora 50 , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Camundongos , Conformação Molecular , Estrutura Molecular , Óxido Nítrico/biossíntese , Ressonância Magnética Nuclear Biomolecular , Resorcinóis/química
14.
J Nat Prod ; 79(5): 1415-22, 2016 05 27.
Artigo em Inglês | MEDLINE | ID: mdl-27120704

RESUMO

Five new meroterpenoids, purpurogenolides A-E (1-5), and four known metabolites (6-9) were isolated from the solid substrate fermentation cultures of the fungus Penicillium purpurogenum MHz 111. The structures of the new meroterpenoids were elucidated by analysis of spectroscopic and spectrometric data (1D and 2D NMR, IR, and HRESIMS). The absolute configurations of 1 and 5 were determined by single-crystal X-ray crystallographic analysis, and those of 2-4 were elucidated on the basis of experimental and calculated electronic circular dichroism spectra. Compounds 2-4 and 6 showed inhibition of nitric oxide production in lipopolysaccharide-activated BV-2 microglial cells with IC50 values of 0.8-30.0 µM.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Óxido Nítrico/biossíntese , Penicillium/química , Terpenos/isolamento & purificação , Terpenos/farmacologia , China , Cristalografia por Raios X , Medicamentos de Ervas Chinesas/química , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Conformação Molecular , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Microbiologia do Solo , Talaromyces , Terpenos/química
15.
Acta Radiol ; 57(10): 1201-4, 2016 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26671306

RESUMO

BACKGROUND: Partial splenic artery embolization (PSE) is an effective treatment modality for patients with hypersplenism. It is less invasive and has a quicker recovery compared with surgical procedures. PSE is usually performed using a femoral artery approach that requires bedrest for a few hours, which is rarely the case for transradial PSE. PURPOSE: To compare the transradial and transfemoral approaches for embolization of spleen in patients with hypersplenism. MATERIAL AND METHODS: In all, 84 patients with hypersplenism who required PSE were recruited. They were randomly divided into two groups on the basis of the procedure followed: the transradial approach (R-PSE, n = 39) or transfemoral approach (F-PSE, n = 45). Technical success, puncture rate, total procedure time, X-ray exposure time, length of stay in hospital (LOS), and complications of the two groups were recorded. RESULTS: The procedure time, X-ray exposure time, and LOS were found to be lower in the R-PSE group than in the F-PSE. However, this difference was not statistically significant. CONCLUSION: The transradial artery approach for PSE in patients with hypersplenism is feasible with no major complications as compared to the femoral approach.


Assuntos
Embolização Terapêutica/métodos , Hiperesplenismo/terapia , Adulto , Idoso , Diagnóstico por Imagem , Feminino , Artéria Femoral , Humanos , Hiperesplenismo/diagnóstico por imagem , Hiperesplenismo/etiologia , Tempo de Internação/estatística & dados numéricos , Cirrose Hepática/complicações , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Artéria Radial , Radiografia Intervencionista , Fatores de Tempo , Resultado do Tratamento
16.
J Asian Nat Prod Res ; 18(1): 51-8, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26651866

RESUMO

A new monoterpene and a new lignan, named litsecols A and B (1 and 2), respectively, together with nine known compounds (3-11), were isolated in a continuous investigation on the roots and stems of Litsea cubeba. Their structures were elucidated on the basis of extensive spectroscopic data analysis, and the absolute configuration of 1 was resolved by X-ray diffraction analysis. Compounds 2-5 and 7-9 showed significant inhibitory activity against nitric oxide (NO) production in lipopolysaccharide (LPS)-induced murine microglial (Bv-2) cell line. Compounds 10 and 11 exhibited significant neuroprotective effect against hydrogen peroxide-induced oxidative damage in rat adrenal pheochromocytoma (PC12) cell line.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Lignanas/isolamento & purificação , Monoterpenos/isolamento & purificação , Fármacos Neuroprotetores/isolamento & purificação , Animais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Peróxido de Hidrogênio/farmacologia , Lignanas/química , Lignanas/farmacologia , Lipopolissacarídeos/farmacologia , Litsea/química , Camundongos , Estrutura Molecular , Monoterpenos/química , Monoterpenos/farmacologia , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacologia , Óxido Nítrico/biossíntese , Ressonância Magnética Nuclear Biomolecular , Células PC12 , Raízes de Plantas/química , Caules de Planta/química , Ratos
17.
Zhongguo Zhong Yao Za Zhi ; 41(22): 4197-4203, 2016 Nov.
Artigo em Zh | MEDLINE | ID: mdl-28933089

RESUMO

Chemical constituents from the fruits of Vitex negundo var. cannabifolia and their nitric oxide (NO) inhibitory and cytotoxic activities were investigated. The compounds were isolated and purified by various column chromatography, and their structures were identified by physiochemical properties and spectroscopic data. Thirteen lignans and six phenolic compounds were isolated from the CH2Cl2 extract of the fruits of V. negundo var. cannabifolia, respectively. Their structures were elucidated as 6-hydroxy-4-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-3,4-dihydro-2-naphthaldehyde (1), vitedoin A (2), vitexdoin F (3), detetrahydroconidendrin (4), vitexdoin E (5), 4-oxosesamin (6), L-sesamin (7), (+)-beechenol (8), ligballinol (9), 2-(4-hydroxyphenyl)-6-(3-methoxy-4-hydroxyphenyl)-3,7-dioxabicyclo[3.3.0]octane (10), (-)-pinoresinol (11), balanophonin (12), thero-guaiacylglycerol-ß-coniferyl aldehyde ether (13), trans-p-coumaryl aldehyde (14), coniferyl aldehyde (15), 5,7-dihydroxychromone (16), trans-3,5-dimethoxy-4-hydroxy-cinnamic aldehyde (17), frambinone (18), and alternariol 4-methyl ether (19). Compounds 8-10,14,18,19 were firstly isolated from Verbenaceae family, compound 13 was obtained from Vitex species, and 6,7,12,15-17 from V. negundo var. cannabifolia for the first time, respectively. The isolated compounds were evaluated for their anti-inflammatory and cytotoxic effects in vitro. Eight compounds (3,5,7,10,11,14,15,17) showed inhibition against NO production in LPS-stimulated RAW 267.4 cells (IC50 in the range of 7.8-81.1 µmol•L⁻¹) and four compounds (1-4) showed cytotoxicity on HepG-2 cells (IC50 in the range of 5.2-24.2 µmol•L⁻¹).


Assuntos
Frutas/química , Compostos Fitoquímicos/isolamento & purificação , Vitex/química , Animais , Células Hep G2 , Humanos , Camundongos , Óxido Nítrico/metabolismo , Compostos Fitoquímicos/farmacologia , Células RAW 264.7
18.
Bioorg Med Chem ; 23(4): 681-93, 2015 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-25614115

RESUMO

Poly(ADP-ribose)polymerase-1 (PARP-1) has emerged as a promising anticancer drug target due to its key role in the DNA repair process. In this work, a novel series of 1-benzyl-quinazoline-2,4(1H,3H)-dione derivatives were designed and synthesized as human PARP-1 inhibitors, structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values of single or double digit nanomolar level. Compound 7j was a potent PARP-1 and PARP-2 inhibitor and it could selectively kill the breast cancer cells MX-1 and MDA-MB-468 with mutated BRCA1/2 and PTEN, respectively, in comparison with homologous recombination proficient cell types such as breast cancer cells MDA-MB-231. In addition, compound 7j displayed the strongest potentiation effect on temozolomide in MX-1 cells (PF50=3.77) in this series of PARP-1 inhibitors.


Assuntos
Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores de Poli(ADP-Ribose) Polimerases , Quinazolinas/química , Quinazolinas/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Mama/efeitos dos fármacos , Mama/enzimologia , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/enzimologia , Linhagem Celular Tumoral , Feminino , Humanos , Simulação de Acoplamento Molecular , Poli(ADP-Ribose) Polimerase-1 , Poli(ADP-Ribose) Polimerases/metabolismo , Relação Estrutura-Atividade
19.
Phys Chem Chem Phys ; 17(10): 6809-18, 2015 Mar 14.
Artigo em Inglês | MEDLINE | ID: mdl-25669900

RESUMO

The refrigeration capability of a thermoelectric device is dictated by interfacial effects and the figure of merit ZT, which govern the contact resistance and the Carnot efficiency for heat conversion. Here we report a controllable (110) oriented Bi0.5Sb1.5Te3 film grown on a Cu film electrode. The hierarchical Bi0.5Sb1.5Te3 film is composed of tens of cactus like flakes that have a (110) oriented backbone and abundant 50-80 nm branches in the (015) direction. The lattice mismatch of the (110) oriented Bi0.5Sb1.5Te3 to the Cu electrode is estimated to be approximately 2.4%, which implies a decreased interfacial dislocation density and formation of fewer interfacial defects leading to low contact resistance (1.0 × 10(-9) Ω m(2)). The enhanced out plane ZT ≈ 0.73 is calculated from the in plane properties. Hence a maximum heat-flux pumping capability of 138 W cm(-2) can be obtained for Tc = 400 K and the corresponding temperature difference is 6 K. Our work indicates that the control of the metal-semiconductor interfacial structure is an efficient approach to improve the refrigeration capability.

20.
J Nat Prod ; 78(9): 2276-85, 2015 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-26348503

RESUMO

Twenty new polyoxygenated labdane diterpenoids (1-20) were isolated from the aerial parts of Leonurus macranthus. Their structures were elucidated on the basis of spectroscopic and spectrometric data (1D and 2D NMR, IR, and HRESIMS). The absolute configurations of macranthin A (1) and 6-O-deacetylmacranthin A (2) were determined by single-crystal X-ray crystallographic analysis and a modified Mosher's method, respectively. Compounds 1-9, 12, 14, and 19 showed inhibition of nitric oxide production in lipopolysaccharide-activated BV-2 microglial cells with IC50 values of 10.0-63.7 µM.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Leonurus/química , Animais , Anti-Inflamatórios/química , Diterpenos/química , Medicamentos de Ervas Chinesas/química , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico/biossíntese , Ressonância Magnética Nuclear Biomolecular , Componentes Aéreos da Planta/química
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