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1.
J Dairy Sci ; 105(3): 2011-2024, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34955261

RESUMO

Multidrug-resistant (MDR) Staphylococcus aureus and its biofilm formation have been challenging to control in milk and dairy industries. Biofilms formed by Staph. aureus may result in the failure of antibacterial agents and disinfectants to penetrate the biofilm in an attempt to control contamination. Novel natural antibacterial agents are required to combat MDR bacteria and biofilms. In this study, we evaluated the bactericidal, antibiofilm, and antimotility effects of Rumex japonicus Houtt. (RJH) extract on MDR Staph. aureus isolated from milk. The RJH extract exhibited good antibacterial activity against MDR strains with minimum inhibitory concentrations (MIC) ranging from 0.78 to 6.25 mg/mL and minimum bactericidal concentrations ranging from 3.125 to 12.5 mg/mL. The extract showed strong inhibition of biofilm formation (81.9%) at sub-MIC value and eradication of biofilm at higher concentrations. The motility of Staph. aureus was effectively blocked by the extract. Major compounds emodin, chrysophanol, and physcion were identified in RJH extract using HPLC-linear trap quadrupole (LTQ)/Orbitrap-mass spectrometry. The extract was nontoxic to human epithelial cell lines such as Caco-2 and HT-29 cell lines at concentrations ranging from 0.1 to 0.5 mg/mL, and from 0.1 to 0.75 mg/mL, respectively. These findings suggest that RJH extract could be an alternative to synthetic preservatives in milk and dairy products.


Assuntos
Staphylococcus aureus Resistente à Meticilina , Rumex , Animais , Antibacterianos/farmacologia , Biofilmes , Células CACO-2 , Humanos , Testes de Sensibilidade Microbiana/veterinária , Leite , Extratos Vegetais/farmacologia , Staphylococcus aureus
2.
J Biol Regul Homeost Agents ; 33(2): 439-445, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30971068

RESUMO

In this study, phosphorylation levels of vasodilator stimulated phosphoprotein (VASP) were detected by flow cytometry (FCM) to investigate the effects of ticagrelor and clopidogrel on platelet aggregation function (PAF) after percutaneous coronary intervention (PCI) in patients with acute coronary syndrome (ACS).


Assuntos
Síndrome Coronariana Aguda/terapia , Moléculas de Adesão Celular/metabolismo , Clopidogrel/uso terapêutico , Proteínas dos Microfilamentos/metabolismo , Intervenção Coronária Percutânea , Fosfoproteínas/metabolismo , Agregação Plaquetária/efeitos dos fármacos , Ticagrelor/uso terapêutico , Humanos , Fosforilação , Inibidores da Agregação Plaquetária/uso terapêutico , Resultado do Tratamento
3.
BMC Pregnancy Childbirth ; 18(1): 204, 2018 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-29859056

RESUMO

BACKGROUND: Misreporting of energy intake is common and can contribute to biased estimates of the relationship between diet and disease. Energy intake misreporting is poorly understood in pregnancy and there is limited research assessing characteristics of women who misreport energy intake or changes in misreporting of energy intake across pregnancy. METHODS: An observational study in n = 945 overweight or obese pregnant women receiving standard antenatal care who participated in the LIMIT randomised trial. Diet, physical activity, psychological factors, body image satisfaction and dieting behaviour were assessed at trial entry (10-20 weeks gestation) and 36 weeks gestation. Energy misreporting status was assessed through the ratio of daily energy intake over basal metabolic rate. Logistic regression analyses were conducted with the dependent variable of under reporting of energy intake at study entry or 36 weeks in separate analysis. RESULTS: At study entry and 36 weeks, women were classified as under reporters (38 vs 49.4%), adequate reporters (59.7 vs 49.8%) or over reporters of energy intake (2.3 vs 0.8%) respectively. The prevalence of under reporting energy intake at 36 weeks was higher than at study entry (early pregnancy). Body mass index (BMI) at study entry and 36 weeks and socioeconomic status, dieting behaviour and risk of depression at 36 weeks were independent predictors of under reporting of energy intake. CONCLUSIONS: Under reporting of energy intake was present in over a third of overweight and obese pregnant women and was higher in late compared to early pregnancy. Characteristics such as BMI, socioeconomic status, past dieting behaviour and risk of depression may aid in identifying women who either require support in accurate recording of food intake or attention for improving diet quality. Results were unable to distinguish whether under reporting reflects misreporting or a true restriction of dietary intake. TRIAL REGISTRATION: Australian and New Zealand Clinical Trials Registry ACTRN12607000161426 , registered 9/3/2007.


Assuntos
Inquéritos sobre Dietas/normas , Sobrepeso/psicologia , Complicações na Gravidez/psicologia , Gestantes/psicologia , Autorrelato/normas , Adulto , Confiabilidade dos Dados , Ingestão de Energia , Feminino , Humanos , Obesidade/psicologia , Gravidez , Adulto Jovem
4.
Genet Mol Res ; 15(2)2016 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-27323017

RESUMO

Hepatocellular carcinoma (HCC) is a complex polygenic disease whose development is dependent on many genetic factors. The let-7 family, an important and widely studied microRNA family, has been shown to play an important role in the initiation and progression of HCC. In this study, we examined the possible associations between single-nucleotide polymorphisms in the promoter region of the let-7 family (rs10877887) and the susceptibility and prognosis of HCC, using a case-control research model. Eighty-nine HCC patients and 95 healthy controls were genotypes by direct sequencing, and the correlation between rs10877887 genotypes and HCC susceptibility was evaluated using an unconditional logistic regression model. Populations with the CT + CC genotype were at a significantly higher risk of HCC compared to those with the TT genotype (CT + CC vs TT: odds ratio = 3.52, 95% confidence interval = 1.90-6.52; P < 0.05). Furthermore, we discovered that the genetic variant of rs10877887 might serve as a prognostic marker for survival in HCC patients, as the CT + CC genotype was associated with poor prognosis.


Assuntos
Carcinoma Hepatocelular/genética , Neoplasias Hepáticas/genética , MicroRNAs/genética , Idoso , Povo Asiático/genética , Carcinoma Hepatocelular/metabolismo , Estudos de Casos e Controles , China , Feminino , Predisposição Genética para Doença , Variação Genética , Humanos , Neoplasias Hepáticas/metabolismo , Masculino , MicroRNAs/metabolismo , Pessoa de Meia-Idade , Polimorfismo de Nucleotídeo Único , Prognóstico , Regiões Promotoras Genéticas
5.
Appl Opt ; 54(19): 5976-82, 2015 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-26193141

RESUMO

Ho(3+)-doped and Ho(3+)/Yb(3+)-codoped multicomponent germanium tellurite (MGT) glasses with multifarious emission channels in the near-infrared wavelength region have been fabricated and characterized. Judd-Ofelt intensity parameters of Ho(3+)-doped MGT glasses are solved to be Ω2=5.32×10(-20) cm(2), Ω(4)=2.73×10(-20) cm(2), and Ω(6)=1.12×10(-20) cm(2), indicating a higher asymmetric and stronger covalent environment around Ho(3+) ions in MGT glasses. Efficient infrared fluorescences have been observed in MGT glasses, and spontaneous emission probabilities are derived to be 230.4, 79.9, and 138.3 s(-1) for the (5)I(6)→(5)I(8), ((5)F(4),(5)S(2))→(5)I(5), and (5)I(7)→(5)I(8) radiative transitions, respectively. In Ho(3+)/Yb(3+)-codoped MGT glasses, the maximum stimulated emission cross-section of 2.0 µm emission is calculated to be 4.93×10(-21) cm(2), and the corresponding gain cross-section is derived to be 3.62×10(-21) cm(2) when the excited state population fraction P reaches 0.8. Multifarious infrared emissions show that Ho(3+) in MGT glasses is a good candidate for optical amplifiers and optoelectronic devices.


Assuntos
Germânio/química , Hólmio/química , Raios Infravermelhos , Telúrio/química , Desenho de Equipamento , Fluorescência , Vidro , Temperatura Alta , Luminescência , Dispositivos Ópticos , Óptica e Fotônica , Probabilidade , Espectrofotometria/métodos , Espectroscopia de Infravermelho com Transformada de Fourier , Temperatura , Itérbio/química
6.
Int J Obes (Lond) ; 37(5): 704-11, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-22868828

RESUMO

BACKGROUND: Ensuring adequate dietary intake during pregnancy has important implications for optimising maternal and fetal health. It is not known whether diet quality is altered over pregnancy and the post-partum period. OBJECTIVE: The aim of this study was to perform a comprehensive assessment of diet quality in overweight and obese women during pregnancy and early post-partum. DESIGN: In a prospective cohort study, n=301 overweight or obese pregnant women completed a food frequency questionnaire at study entry (10-20 weeks gestation), 28 weeks gestation, 36 weeks gestation and 4 months post-partum for assessment of macronutrient and micronutrient intake and diet quality by the Healthy Eating Index (HEI). RESULTS: Energy, macronutrient and dietary sources of micronutrients did not alter across pregnancy or post-partum. The HEI was of below average quality in 31.0% of women at baseline. This decreased from week 28 (P<0.001) and was maintained at a lower level post-partum such that HEI levels were lower compared with study entry (53.3±12.7 versus 56.7±10.1, P<0.001). The HEI decrease occurred in association with decreases in the milk, meat and unsaturated oil components, and increases in the proportion of energy from solid fats, alcohol and added sugars (P<0.001), and was independently predicted by the socioeconomic index for areas score (ß=-0.011, s.e.=0.011, P=0.031). CONCLUSION: We report for the first time that dietary quality decreases across pregnancy and is maintained at this reduced level in the early post-partum period in overweight and obese women. Dietary interventions aimed at improving diet quality should be targeted to early pregnancy and post-partum.


Assuntos
Dieta/estatística & dados numéricos , Comportamento Alimentar , Comportamentos Relacionados com a Saúde , Obesidade/epidemiologia , Período Pós-Parto , Adulto , Austrália/epidemiologia , Estudos de Coortes , Dieta/normas , Ingestão de Energia , Feminino , Conhecimentos, Atitudes e Prática em Saúde , Promoção da Saúde , Humanos , Micronutrientes , Obesidade/prevenção & controle , Gravidez , Cuidado Pré-Natal , Estudos Prospectivos , Fatores Socioeconômicos , Inquéritos e Questionários
7.
Matern Child Health J ; 17(10): 1879-87, 2013 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23263891

RESUMO

Overweight and obesity during pregnancy is associated with risk of a range of adverse health outcomes. While intervention studies aim to promote behavioral change, little is known about the underlying psychological mechanisms facilitating and hindering change. The aim of this study was to evaluate overweight and obese women's perceptions of making behavior change during pregnancy. We explored beliefs through self-administrated questionnaires (n = 464) and semi-structured face-to-face interviews (n = 26). Questions were designed according to the Health Belief Model. A triangulation protocol was followed to combine quantitative and qualitative data. A total of 269 women (58 %) indicated that high gestational weight gain is a concern, with 348 (75 %) indicating excessive weight gain is associated with complications during pregnancy or child birth. Women were aware of maternal complications associated with high gestational weight gain, but had more limited awareness of neonatal complications. While most women indicated in questionnaires that healthy eating and physical activity were associated with improved health during pregnancy, they were unable to identify specific benefits at interview. Barriers to making healthy behavior changes were highly individualized, the main barrier being lack of time. While the majority (91 %) of women indicated that they would make behavior changes if the change made them feel better, only half felt confident in their ability to do so. Interventions for overweight and obese pregnant women should incorporate education about neonatal health consequences and benefits of healthy behavior change in addition to incorporating strategies to enhance self-efficacy.


Assuntos
Comportamentos Relacionados com a Saúde , Conhecimentos, Atitudes e Prática em Saúde , Obesidade/psicologia , Sobrepeso/psicologia , Complicações na Gravidez/psicologia , Adulto , Índice de Massa Corporal , Cultura , Feminino , Humanos , Gravidez , Austrália do Sul , Inquéritos e Questionários , Aumento de Peso , Adulto Jovem
8.
Artigo em Zh | MEDLINE | ID: mdl-36992642

RESUMO

Objective: To analyze the difference of application methods and effects of local flap in small and medium-sized defects of different aesthetic subunits of nose, in order to provide reference for clinical work. Methods: A retrospective analysis was made on 59 patients with external nasal masses and scars who underwent surgical treatment in the Department of Aesthetic Plastic Surgery of the Affiliated Hospital of Qingdao University from July 1, 2021 to January 30, 2022, including 27 females and 32 males, aged 15 to 69 years. Using Likert scale, the repair methods and effects of local flap for nasal soft tissue defects were evaluated and summarized from three aspects of texture, flatness and scar concealment. GraphPad Prism 5.0 software was used for data statistics and analysis. Results: The use of skin flaps to repair small and medium-sized areas of the nose could achieve satisfactory results. For patients with different subunits, in terms of skin flatness and scar concealment degree in the operation area, patients' satisfaction with the dorsal and lateral nasal areas was higher than that of the alar and tip areas, respectively (F=6.40, P=0.001; F=10.57, P<0.001). For patients with different skin flap repair methods, the satisfaction of patients with Z-plasty and Dufourmentel skin flap was higher than that of other skin flap repair methods (F=4.38, P=0.002), and the satisfaction of patients with Dufourmentel skin flap was the highest in the degree of scar concealment (F=2.57, P=0.038). Conclusions: In the small and medium-sized defects of the nose, the use of multiple local flaps can achieve good cosmetic effects and functional recovery. The operator should select the appropriate flap repair method according to the characteristics of different aesthetic subunits of the nose.

9.
Zhonghua Shao Shang Za Zhi ; 38(11): 1034-1039, 2022 Nov 20.
Artigo em Zh | MEDLINE | ID: mdl-36418260

RESUMO

Objective: To investigate the application and clinical efficacy of ultrasound debridement method in residual burn wounds. Methods: A retrospective cohort study was conducted. From August 2017 to August 2021, 64 patients with residual burn wounds who met the inclusion criteria were admitted to the 980th Hospital of the Joint Logistic Support Force of PLA. According to the debridement method adopted for the residual wounds, the patients were divided into ultrasound debridement group (34 cases, 22 males and 12 females, aged (31±13) years) and traditional debridement group (30 cases, 19 males and 11 females, aged (32±13) years). After the corresponding debridement, the wounds of patients in the two groups were selected for stamp skin grafting or large skin grafting according to the wound site and skin donor status. For unhealed wounds after stage Ⅰ surgery, secondary debridement and skin grafting were be performed, with the wound debridement methods in the 2 groups being the same as those of stage Ⅰ, respectively. On postoperative day 3, drug-sensitive test was used to detect the bacteria in the wound and the positive rate of bacteria was calculate. On postoperative day 7, the survival rate of skin slices in wound and the incidence of subcutaneous hematoma were calculated. At discharge, wound healing time and debridement times of patients were counted, and the secondary debridement rate was calculated. Data were statistically analyzed with independent sample t test or chi-square test. Results: On postoperative day 3, the wounds in ultrasound debridement group were infected with Staphylococcus aureus in 2 cases and Pseudomonas aeruginosa in 2 cases, and the wounds in traditional debridement group were infected with Staphylococcus aureus in 5 cases, Pseudomonas aeruginosa in 3 cases, Acinetobacter baumannii in 1 cases, Klebsiella pneumoniae in 1 cases, and Enterobacter cloacae in 1 cases. The positive rate of bacteria of wound in ultrasound debridement group was significantly lower than that in traditional debridement group (χ2=5.51, P<0.05). On postoperative day 7, the survival rate of skin grafts in ultrasound debridement group was (92±5) %, which was significantly higher than (84±10) % in traditional debridement group (χ2=6.78, P<0.01); the incidence of subcutaneous hematoma in ultrasound debridement group was 17.6% (6/34), which was significantly lower than 40.0%( 12/30) in traditional debridement group, χ2=3.94, P<0.05. At discharge, the wound healing time in ultrasound debridement group was (11.0±2.0) d, which was significantly shorter than (13.0±3.1) d in traditional debridement group (t=3.81, P<0.01); the secondary debridement rate of wounds in ultrasound debridement group was 2.9% (1/34), which was significantly lower than 20.0% (6/30) in traditional debridement group (χ2=4.76, P<0.05). Conclusions: Ultrasound debridement method can significantly reduce the bacterial load of residual burn wounds, reduce postoperative hematoma formation, and promote the survival of skin grafts to shorten the course of disease of patients.


Assuntos
Bactérias , Queimaduras , Masculino , Feminino , Humanos , Desbridamento/métodos , Estudos Retrospectivos , Resultado do Tratamento , Queimaduras/cirurgia , Queimaduras/microbiologia , Hematoma
10.
Clin Transl Oncol ; 23(4): 820-826, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32857338

RESUMO

PURPOSE: To investigate the magnetic resonance imaging (MRI) images of brain glioma before postoperative radiotherapy, and to provide reference for the delineation of postoperative radiotherapy target area. METHODS: Retrospective analysis was performed on 106 cases of brain glioma confirmed by surgery and pathology in our hospital, including 70 cases of high-grade glioma (HGG) and 36 cases of low-grade glioma (LGG). The MRI images of the lesions within 1 month before and after surgery were analyzed, the apparent diffusion coefficient (ADC) values in the near and far tumor areas were measured, respectively, and the corresponding rADC values were calculated. RESULTS: The incidence of residual tumors of postoperative HGG and LGG was 0, 15.7% (0/36, 11/70), respectively. The incidence of postoperative reactive enhancement was 11.0% and 52.9% (4/36 and 37/70), respectively. About 30.6% and 81.4% (11/36 and 57/70) of patients with adjacent meningeal enhancement were found in the operative area. CONCLUSIONS: The MRI images of HGG and LGG before postoperative radiotherapy had certain characteristics, providing a favorable guidance for the delineation of the target area of radiotherapy and the formulation of treatment plan.


Assuntos
Neoplasias Encefálicas/diagnóstico por imagem , Glioma/diagnóstico por imagem , Imageamento por Ressonância Magnética/métodos , Adolescente , Adulto , Idoso , Edema Encefálico/diagnóstico por imagem , Neoplasias Encefálicas/patologia , Neoplasias Encefálicas/radioterapia , Neoplasias Encefálicas/cirurgia , Criança , Imagem de Tensor de Difusão , Feminino , Glioma/patologia , Glioma/radioterapia , Glioma/cirurgia , Humanos , Masculino , Meninges/diagnóstico por imagem , Pessoa de Meia-Idade , Gradação de Tumores , Recidiva Local de Neoplasia/diagnóstico por imagem , Neoplasia Residual/diagnóstico por imagem , Cuidados Pós-Operatórios , Complicações Pós-Operatórias/diagnóstico por imagem , Estudos Retrospectivos , Adulto Jovem
11.
Eur Rev Med Pharmacol Sci ; 23(3 Suppl): 24-30, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31389567

RESUMO

OBJECTIVE: To explore the association between human leukocyte antigen (HLA)-DPA1 gene polymorphism and primary glaucoma. PATIENTS AND METHODS: Six single nucleotide polymorphisms (SNPs) were genotyped in 51 patients and 51 healthy controls through Polymerase Chain Reaction (PCR). The possible association between HLA-DPA1 gene mutation and primary glaucoma was detected using the t-test and the Chi-square test. RESULTS: Rs1676486 genotype had a significant genetic correlation. Rs3753841 and rs12138977 genotypes had a higher minor-allele frequency in control group. The CT + CC genotype frequency of rs12138977 showed a significant genetic correlation in both case group and control group. Moreover, the rs12138977 polymorphism and corneal thickness had little influence on the occurrence of primary angle-closure glaucoma (PACG). Also, the main risk factors for PACG were intraocular hypertension and short axial length. CONCLUSIONS: The HLA-DPA1 gene polymorphism may be related to the severity of PACG.


Assuntos
Glaucoma de Ângulo Fechado/genética , Cadeias alfa de HLA-DP/genética , Polimorfismo de Nucleotídeo Único , Idoso , Estudos de Casos e Controles , Feminino , Estudos de Associação Genética , Predisposição Genética para Doença , Humanos , Masculino , Pessoa de Meia-Idade
12.
Int J Impot Res ; 18(5): 477-83, 2006.
Artigo em Inglês | MEDLINE | ID: mdl-16528290

RESUMO

Phosphodiesterase 5 (PDE5) inhibitors are efficacious in treating patients with erectile dysfunction. New PDE5 inhibitors with different selectivity and pharmacokinetic profiles have been vigorously pursued. Here we report two novel, potent, and selective PDE5 inhibitors, JNJ-10280205 and JNJ-10287069, with Ki values of 0.05 and 0.12 nM, respectively. Both compounds displayed superior selectivity against PDE1-4 and -6 when compared to sildenafil. In the anesthetized dogs, JNJ-10280205 and JNJ-10287069 exhibited similar efficacy as sildenafil in enhancing erectile functions, with no significant effect on cardiovascular parameters. Pharmacokinetic studies showed that JNJ-10287069 had better oral bioavailability than JNJ-10280205 in several animal species. In vitro study suggested that cytochrome P450 (CYP) 3A4 played a major role in the metabolism of both compounds. The compounds inhibited some of the CYP450 enzymes and the human ether-a-go-go (HERG) channel at much higher concentrations than that required to inhibit PDE5, thus, no cross inhibition would be expected at therapeutic doses. Both compounds are suitable clinical candidates.


Assuntos
3',5'-GMP Cíclico Fosfodiesterases/antagonistas & inibidores , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/uso terapêutico , Disfunção Erétil/tratamento farmacológico , Disfunção Erétil/enzimologia , Quinolonas/uso terapêutico , 3',5'-GMP Cíclico Fosfodiesterases/metabolismo , Animais , Nucleotídeo Cíclico Fosfodiesterase do Tipo 5 , Sistema Enzimático do Citocromo P-450/metabolismo , Cães , Inibidores Enzimáticos/farmacocinética , Canais de Potássio Éter-A-Go-Go/metabolismo , Haplorrinos , Humanos , Masculino , Quinolonas/farmacocinética , Ratos
13.
Mini Rev Med Chem ; 5(8): 701-8, 2005 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-16101406

RESUMO

The nuclear receptor for progesterone is a target for contraception and for several therapeutic indications. Progestin agonists and antagonists in clinical use mimic the steroidal backbone of the cognate ligand, progesterone. Thus, they have significant cross-reactivity with other steroid receptors. Recently, non-steroidal progesterone receptor ligands have begun to appear in the literature. This review will describe the current status of research into these promising new chemical entities.


Assuntos
Progestinas/farmacologia , Receptores de Progesterona/agonistas , Receptores de Progesterona/antagonistas & inibidores , Animais , Ligação Competitiva , Anticoncepção , Endometriose/tratamento farmacológico , Feminino , Terapia de Reposição Hormonal , Humanos , Ligantes , Receptores de Progesterona/classificação , Relação Estrutura-Atividade
14.
J Med Chem ; 37(5): 665-73, 1994 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-8126707

RESUMO

The proteases expressed by the HIV-1 and HIV-2 viruses process the polyproteins encoded by the viral genomes into the mature proteins required for virion replication and assembly. Eight analogs of haloperidol have been synthesized that cause time-dependent inactivation of the HIV-1 protease and, in six cases, HIV-2 protease. The IC50 values for the analogues are comparable to that of haloperidol itself. Enzyme inactivation is due to the presence of an epoxide in two of the analogues and carbonyl-conjugated double or triple bonds in the others. Irreversible inactivation is confirmed by the failure to recover activity when one of the inhibitors is removed from the medium. At pH 8.0, the agents inactivate the HIV-1 protease 4-80 times more rapidly than the HIV-2 protease. Faster inactivation of the HIV-1 protease is consistent with alkylation of cysteine residues because the HIV-1 protease has four such residues whereas the HIV-2 protease has none. Inactivation of the HIV-2 protease requires modification of non-cysteine residues. The similarities in the rates of inactivation of the HIV-2 protease by six agents that have intrinsically different reactivities toward nucleophiles suggest that the rate-limiting step in the inactivation process is not the alkylation reaction itself. At least five of the agents inhibit polyprotein processing in an ex vivo cell assay system, but they are also toxic to the cells.


Assuntos
Inibidores da Protease de HIV/síntese química , HIV-1/enzimologia , HIV-2/enzimologia , Haloperidol/análogos & derivados , Acetatos/química , Ácido Acético , Alquilação , Sítios de Ligação , Linhagem Celular , Compostos de Epóxi/síntese química , Glutationa/química , Protease de HIV/química , Protease de HIV/metabolismo , Inibidores da Protease de HIV/farmacologia , Células HeLa , Humanos , Concentração de Íons de Hidrogênio , Cetonas/síntese química , Cinética , Modelos Moleculares
15.
J Med Chem ; 41(16): 2939-45, 1998 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-9685233

RESUMO

A new class of inhibitors of the two-component regulatory systems (TCS) of bacteria was discovered based on the salicylanilide screening hits, closantel (1) and tetrachlorosalicylanilide (9). A systematic SAR study versus a model TCS, KinA/Spo0F, demonstrated the importance of electron-attracting substituents in the salicyloyl ring and hydrophobic groups in the anilide moiety for optimal activity. In addition, derivatives 8 and 16, containing the 2, 3-dihydroxybenzanilide structural motif, were potent inhibitors of the autophosphorylation of the KinA kinase, with IC50s of 2.8 and 6. 3 µM, respectively. Compound 8 also inhibited the TCS mediating vancomycin resistance (VanS/VanR) in a genetically engineered Enterococcus faecalis cell line at concentrations subinhibitory for growth. Closantel (1), tetrachlorosalicylanilide (9), and several related derivatives (2, 7, 10, 11, 20) had antibacterial activity against the drug-resistant organisms, methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VREF).


Assuntos
Antibacterianos/síntese química , Proteínas de Bactérias/antagonistas & inibidores , Inibidores Enzimáticos/síntese química , Bactérias Gram-Positivas/efeitos dos fármacos , Inibidores de Proteínas Quinases , Salicilanilidas/síntese química , Antibacterianos/química , Antibacterianos/farmacologia , Bacillus subtilis/enzimologia , Bacillus subtilis/metabolismo , Bacillus subtilis/fisiologia , Avaliação Pré-Clínica de Medicamentos , Resistência Microbiana a Medicamentos , Enterococcus faecium/efeitos dos fármacos , Enterococcus faecium/enzimologia , Enterococcus faecium/genética , Enterococcus faecium/metabolismo , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Bactérias Gram-Positivas/enzimologia , Bactérias Gram-Positivas/fisiologia , Luciferases/genética , Luciferases/metabolismo , Resistência a Meticilina , Testes de Sensibilidade Microbiana , Fosforilação , Proteínas Quinases/genética , Salicilanilidas/química , Salicilanilidas/farmacologia , Esporos Bacterianos/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-Atividade , Fatores de Transcrição/antagonistas & inibidores , Fatores de Transcrição/genética , Vancomicina/farmacologia
16.
Laryngoscope ; 110(9): 1563-6, 2000 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-10983963

RESUMO

OBJECTIVES/HYPOTHESIS: Deterioration of aerodigestive tract reflexes such as the esophagoglottal and pharyngoglottal closure reflexes and pharyngeal swallow has been documented in the elderly. However, the effect of aging on the contractile response of the upper esophageal sphincter (UES) to pharyngeal water stimulation has not been studied. The aim of this study was to characterize the pharyngo-UES reflex in the healthy elderly. METHODS: We studied nine healthy elderly (77 +/- 1 y [SD]; four men, five women) and nine healthy young volunteers (26 +/- 2 y [SD]; four men, five women). AUES sleeve sensor was used to measure the pressure. We tested pharyngeal stimulation induced by rapid pulse and slow continuous injection of water. RESULTS: The volume of water required to stimulate the pharyngo-UES contractile reflex by rapid pulse injection in the elderly (0.5 +/- 34 0.1 mL) was significantly higher than that in the young (0.1 +/- 0.02 mL) (P < .05). In contrast to young subjects, there was no pressure increase in resting UES pressure observed in the elderly for continuous pharyngeal water infusion. In both young and elderly, the threshold volume for the pharyngo-UES contractile reflex was significantly lower than that for pharyngeal swallows. CONCLUSIONS: The pharyngo-UES contractile reflex deteriorates with aging. This deterioration is primarily due to abnormalities of the afferent limb of the reflex.


Assuntos
Junção Esofagogástrica/fisiopatologia , Contração Muscular/fisiologia , Músculos Faríngeos/fisiopatologia , Reflexo Anormal/fisiologia , Idoso , Feminino , Humanos , Masculino , Manometria/métodos , Fatores de Tempo , Água
17.
Chin Med J (Engl) ; 108(7): 522-7, 1995 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-7555271

RESUMO

Two continuous cell lines derived from the neoplastic urothelium had been maintained in culture for more than two years. The first cell line derived from the urothelium of a fusion papillocarcinoma on the left lateral wall of the bladder was designated as TBC-1 and grown in vitro for more than 150 generations. The second cell line derived from the urothelium of a papillocarcinoma in the left renal pelvis was designated as TPC-1 and grown in vitro for more than 100 generations. Characterization studies made on both cell lines showed that the cells had a rapid doubling time, exhibited multilayering and produced tumors in sc of BALB/c. Tumor nodules that produced sc of BALB/c kept similar cellular and pathological features to those of the primary biopsy specimens under light and electron microscopes. TPC-1 cell line exhibited a three-dimensional structure of transitional epithelium on the nylon-mesh disk which was coated with a layer of rat tail collagen. Both TBC-1 and TPC-1 cell lines formed colonies in soft agar. Their forming rates were 35% and 28%, respectively. The chromosome number of TBC-1 cells ranged from 17 to 84, with a modal number of 54; whereas that of TPC-1 cells ranged from 28 to 139, with a modal number of 49. The TBC-1 cells showed mutant p53 and ras p21 protein expression and expressed weakly ABH blood group isoantigens. Analysis of lactic dehydrogenase (LDH) isozymes showed the highest levels of LDH isozyme 4 sonicated cell lysates of TBC-1 and TPC-1 respectively.


Assuntos
Carcinoma de Células de Transição/patologia , Neoplasias Renais/patologia , Células Tumorais Cultivadas , Neoplasias da Bexiga Urinária/patologia , Adulto , Idoso , Animais , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Ratos
18.
Zhonghua Zhong Liu Za Zhi ; 9(6): 427-9, 21, 1987 Nov.
Artigo em Zh | MEDLINE | ID: mdl-3452540

RESUMO

The cell line TBC-27, from a human bladder transitional cell carcinoma Grade II, was established and maintained for 8 months through 27 passages. TBC-27 cells have the epithelioid cell morphology during culture. The population doubling time of the 14th generation cells was 27 hours by growth curve. The chromosome karyotype of the 12th generation cells consisted mainly of hypodiploid (mode 40-45). Ultrastructurally, there was a great deal of freeribosome and vesicle in the cytoplasm and a great number of atypical microvilli on the surface of the 21st generation cells. The heterotransplantation test revealed that the xenografted tumor in the immunosuppressed suckling rats was similar to the initial bladder carcinoma in histology.


Assuntos
Carcinoma de Células de Transição/patologia , Neoplasias da Bexiga Urinária/patologia , Animais , Carcinoma de Células de Transição/ultraestrutura , Linhagem Celular , Feminino , Humanos , Pessoa de Meia-Idade , Transplante de Neoplasias , Ratos , Ratos Endogâmicos , Neoplasias da Bexiga Urinária/ultraestrutura
19.
Zhonghua Yu Fang Yi Xue Za Zhi ; 23(1): 9-12, 1989 Jan.
Artigo em Zh | MEDLINE | ID: mdl-2731456

RESUMO

This article analysis the meteorological data during the outbreaks of carbon monoxide poisoning and the conditions of 108 poisoned people in Baishan District from Oct., 1980 to Feb., 1985. The results showed that most of the poisoning cases happened in the months of the lowest air temperature. The main factors affecting poisoning were season, wind direction, raifall and atmospheric pressure, of secondary importance were air temperature and humidity. The time when CO poisoning most easily took place when the night was without wind, accompanied by snowfall or rainfall. The atmospheric pressure value was lower than average month value, and the humidity higher than average month value. The writer proposes to use the "average month value" method for forecasting "similar date" method.


Assuntos
Intoxicação por Monóxido de Carbono/epidemiologia , Conceitos Meteorológicos , Adolescente , Adulto , Criança , Pré-Escolar , China , Feminino , Humanos , Lactente , Masculino , Pessoa de Meia-Idade , Estações do Ano
20.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 21(11): 813-5, 2001 Nov.
Artigo em Zh | MEDLINE | ID: mdl-12575371

RESUMO

OBJECTIVE: To study the clinical effect and mechanism of Xuelong Granule (XLG) in antiliver fibrosis. METHODS: Ninety-eight patients with liver cirrhosis were divided into 2 groups randomly. The 58 Patients in the treated group were treated by XLG and the 40 patients in the control group were treated by Shenchai Granule for 3 months. Levels of serum hyaluronic acid (HA) and laminin (LN), and pathological changes of liver tissues were observed before and after treatment. In experimental study on model rats, the liver tissue content of hydroxyproline and pathological changes under light and electron microscope were observed. RESULTS: The total effective rate in the treated group was 72.4%, that in the control group was 40.0%, there was significant difference between the two groups (P < 0.01). The level of serum HA and LN in the treated group declined markedly after treatment, and pathological examination of 8 cases showed the fibrous tissues reduced obviously. Experimental study showed marked reduction of hydroxyproline content and significant lowering of fibrous tissue proliferation, both under light and electron microscope, in liver of model rats after XLG treatment. CONCLUSION: XLG has a definite effect in anti-liver fibrosis.


Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Ácido Hialurônico/sangue , Cirrose Hepática/tratamento farmacológico , Fitoterapia , Adulto , Idoso , Animais , Medicamentos de Ervas Chinesas/farmacologia , Feminino , Hepatite B/sangue , Humanos , Hidroxiprolina/metabolismo , Laminina/sangue , Fígado/patologia , Cirrose Hepática/sangue , Cirrose Hepática/virologia , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Ratos , Ratos Wistar
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