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1.
J Hum Nutr Diet ; 22(1): 40-9, 2009 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-18759957

RESUMEN

BACKGROUND: Overweight and obesity as well as weight dissatisfaction have been increasing in prevalence worldwide. Body weight dissatisfaction and fear of fatness are potential contributors to disordered eating. The present study aimed to investigate the prevalence of self-reported overweight and weight dissatisfaction along with associations with socio-demographic characteristics, body image, health complaints, risk behaviours, physical activity and television viewing in adolescents in Palestine. METHODS: The 2003/04 Palestinian Health Behaviour in School-aged Children (HBSC) is a cross-sectional survey of 17,817 adolescents from 405 randomly selected schools. Students from a representative sample of grades 6, 8, 10 and 12 (aged 12-18 years) self-completed a modified version of the international World Health Organization collaborative Health Behaviour in School-aged Children (HBSC-2002) questionnaire. RESULTS: Although 16.5% of the adolescents were overweight, almost twice that number (32.1%) were dissatisfied with their weight (i.e. dieting or perceiving a need to diet). Of those adolescents, two-thirds were not actually overweight (56.4% boys; 73.5% girls). One-fifth of the total number of adolescents (16.0% boys; 24.0% girls) were not overweight but were dissatisfied with their weight. Boys reporting overweight or weight dissatisfaction were more likely to have mothers with higher education or to be from more affluent families. Among both genders, but especially among girls, weight dissatisfaction was positively associated with most of the outcome variables (body image, health complaints, risk behaviours, and television viewing) regardless of weight status, whereas weight status was associated with only a few of the outcome variables. CONCLUSIONS: Weight dissatisfaction, independent of weight status, is associated with body image, health complaints, risk behaviours and television viewing, and represents a potential health risk factor for adolescents. Preventive interventions should focus not only on weight status, but also on body weight dissatisfaction.


Asunto(s)
Conducta del Adolescente/psicología , Árabes/estadística & datos numéricos , Imagen Corporal , Sobrepeso/psicología , Estudiantes/psicología , Adolescente , Fenómenos Fisiológicos Nutricionales de los Adolescentes , Peso Corporal/fisiología , Niño , Estudios Transversales , Escolaridad , Femenino , Conductas Relacionadas con la Salud , Humanos , Israel , Estilo de Vida , Masculino , Psicología del Adolescente , Instituciones Académicas , Autoimagen , Distribución por Sexo , Televisión
2.
J Med Chem ; 20(8): 1001-6, 1977 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-894670

RESUMEN

Fifteen 7-substituted 4-hydroxyquinoline-3-carboxylic acids have been designed to minimize covariance between the physicochemical substituent parameters: pi, MR, and sigmap. The molecules have been synthesized and evaluated for their ability to inhibit the respiration of Ehrlich ascites cells as a whole cell model and for their ability to inhibit malate dehydrogenase as an intracellular target enzyme model. Correlation analysis indicates that ascites cell inhibition is linearly related to pi and that malate dehydrogenase inhibition is linearly related to MR.


Asunto(s)
Hidroxiquinolinas/síntesis química , Consumo de Oxígeno/efectos de los fármacos , Animales , Carcinoma de Ehrlich/enzimología , Carcinoma de Ehrlich/metabolismo , Células Cultivadas , Depresión Química , Hidroxiquinolinas/farmacología , Técnicas In Vitro , Malato Deshidrogenasa/antagonistas & inhibidores , Análisis de Regresión , Relación Estructura-Actividad
3.
J Med Chem ; 28(4): 447-51, 1985 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-3981536

RESUMEN

The inhibitory activities of a set of nine 7-substituted-4-hydroxyquinoline-3-carboxylic acids against three dehydrogenase enzymes and one whole cell system (Ehrlich ascites tumor cells) have been subjected to principal component analysis. The results clearly indicate that activity against the whole cell test system cannot directly be attributed to inhibition of the enzymes evaluated. The enzyme systems are reflected by the first component that can be identified with polar and steric parameters while hydrophobic effects are absent. The second component is entirely due to the inhibition of ascites cell respiration that depends primarily on hydrophobicity.


Asunto(s)
Carcinoma de Ehrlich/metabolismo , Hidroxiquinolinas/farmacología , L-Lactato Deshidrogenasa/antagonistas & inhibidores , Malato Deshidrogenasa/antagonistas & inhibidores , Consumo de Oxígeno/efectos de los fármacos , Análisis de Varianza , Animales , Ácidos Carboxílicos/farmacología , Solubilidad , Relación Estructura-Actividad
4.
J Med Chem ; 24(12): 1422-9, 1981 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-6796688

RESUMEN

The inhibitory action of a set of 4,5-diamino-1,2-dihydro-2,2-dimethyl-1-(3-substituted-phenyl)-s-triazines on Lactobacillus casei dihydrofolate reductase is compared with their action on methotrexate-resistant and methotrexate-sensitive cell cultures by means of quantitative structure-selectivity analysis. The analysis uncovers major differences in the steric and hydrophobic interactions of the substituents X with the three different systems. Correlation analysis is used to define the hydrophobic binding site for 3-X in the isolated enzyme. This is shown to be similar to that of the sensitive cells but different from that in the resistant cells, which have a larger hydrophobic binding site. When X has the general structure 3-CH2ZC6H4-Y (Z = O or NH), it is shown that Y does not interact with the isolated enzyme, but in the living cells, Y interacts with a molecular barrier in a way that can be quantitatively related to the molar refractivity of X. The methotrexate-resistant cells are resistant to highly hydrophilic inhibitors such as methotrexate but are not able to resist hydrophobic inhibitors. The results with the inhibition of L. casei dihydrofolate reductase are compared with the inhibition of enzyme from bovine liver.


Asunto(s)
Antagonistas del Ácido Fólico , Lacticaseibacillus casei/enzimología , Triazinas/farmacología , Resistencia a Medicamentos , Lacticaseibacillus casei/crecimiento & desarrollo , Metotrexato/farmacología , Relación Estructura-Actividad
5.
J Med Chem ; 19(1): 131-5, 1976 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-1246035

RESUMEN

Seven para-substituted [phenylglyoxal bis(4-methyl-3-thiosemicarbazone)]copper (II) chelates (12-18) have been designed, synthesized, and tested for their ability to inhibit the respiration of rat liver slices as a normal cell model and Ehrlich ascites cells as a tumor cell model. Relationships between chemical structure and respiratory inhibition are described on a quantitative basis using substituent contants (pi, Es, and sigmap) by computerized multiparameter regression analyses. The correlations indicate that changes in Es have the largest effect on liver slice toxicity of chelates while pi and sigmap account for most of the variation in toxicity to ascites cells. A comparative analysis strongly suggests that electron-donating substituents with greater water solubility should increase cytotoxicity to ascites cells at the expense of cytotoxicity to the rat liver cells. The predictions of the equations were checked by synthesizing and testing an additional derivative. The results strengthen the initial predictions.


Asunto(s)
Antineoplásicos/síntesis química , Cobre , Tiosemicarbazonas/síntesis química , Animales , Antineoplásicos/farmacología , Carcinoma de Ehrlich/metabolismo , Quelantes , Cobre/farmacología , Técnicas In Vitro , Hígado/metabolismo , Ratones , Consumo de Oxígeno/efectos de los fármacos , Ratas , Análisis de Regresión , Espectrofotometría Ultravioleta , Relación Estructura-Actividad , Tiosemicarbazonas/farmacología
6.
J Med Chem ; 21(8): 804-9, 1978 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-691005

RESUMEN

The synthesis of an extended series of para-substituted [phenylglyoxal bis(4-methyl-3-thiosemicarbazone)] copper(II) chelates is reported. Subsequent biological evaluation and regression analysis have been performed, correlating pI50 with extrathermodynamic substituent parameters. Parabolic correlations with pi have resulted which predict optimum lipophilic character of the para substituent with respect to Ehrlich ascites cytotoxicity (pi0 = -2.13) and with respect to ascites vs. liver slice cytotoxicity (pi0 = -1.31). Results indicated clearly that the chelate most toxic to the tumor cell model may not be the most selective.


Asunto(s)
Antineoplásicos/síntesis química , Quelantes/síntesis química , Cobre/farmacología , Compuestos Organometálicos/síntesis química , Tiosemicarbazonas/síntesis química , Animales , Antineoplásicos/farmacología , Carcinoma de Ehrlich/metabolismo , Células Cultivadas , Quelantes/farmacología , Técnicas In Vitro , Cinética , Hígado/metabolismo , Ratones , Compuestos Organometálicos/farmacología , Consumo de Oxígeno/efectos de los fármacos , Ratas , Relación Estructura-Actividad , Tiosemicarbazonas/farmacología
7.
J Med Chem ; 28(12): 1910-6, 1985 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-3934385

RESUMEN

Sets of 5-(substituted benzyl)-2,4-diaminopyrimidines and 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(3-substituted phenyl)-s-triazines as well as several other antifolates were tested as inhibitors of Escherichia coli dihydrofolate reductase and E. coli cell cultures both sensitive and resistant to methotrexate. From the results quantitative structure-activity relationships (QSAR) were formulated. The triazines were found to inhibit sensitive and resistant cell cultures to the same degree, but the benzylpyrimidines showed marked differences against the two types of cells. Increased hydrophobicity produced benzylpyrimidines more active against the resistant E. coli cell. Metroprine did not discriminate between the two types of cells cultures, but pyrimethamine and 2,4-diamino-6-(2,5-dimethoxybenzyl)-5-methylpyrido[2,3-d]pyrimidin e (BW 301U) did. The results are compared with triazines and benzylpyrimidines acting on Lactobacillus casei and murine tumor cells sensitive and resistant to methotrexate. QSAR is shown to be an effective means for detecting receptor differences.


Asunto(s)
Metotrexato/farmacología , Pirimidinas/farmacología , Triazinas/farmacología , Transporte Biológico Activo , Fenómenos Químicos , Química , Farmacorresistencia Microbiana , Escherichia coli/efectos de los fármacos , Antagonistas del Ácido Fólico/farmacología , Lacticaseibacillus casei/efectos de los fármacos , Matemática , Pirimetamina/análogos & derivados , Pirimetamina/farmacología , Relación Estructura-Actividad
8.
J Med Chem ; 37(19): 3016-22, 1994 Sep 16.
Artículo en Inglés | MEDLINE | ID: mdl-7932523

RESUMEN

The synthesis of 2,3,6-triaminopyridine derivatives, representing a unique chemical structure for anticonvulsants, is described. The synthetic program was performed (a) to identify more potent analogs, (b) to determine structural properties controlling potency as well as neurotoxicity, and (c) to reduce the requirements for animal testing. As a result, besides other structural properties, the overall molecular lipophilicity (log k', octanol-coated column) explained changes in anticonvulsant potency and neurotoxicity. Mimicking the interaction of the amphiphilic triaminopyridines with biological membranes, NMR experiments in the presence of lecithin vesicles were conducted in order to measure the phospholipid-binding parameter log delta (1/T2). Replacement of log k' with log delta (1/T2) in the correlation analysis afforded a more significant equation describing the anticonvulsant activity of 21 derivatives.


Asunto(s)
Aminopiridinas/síntesis química , Aminopiridinas/farmacología , Anticonvulsivantes/síntesis química , Anticonvulsivantes/farmacología , Aminopiridinas/química , Analgésicos/síntesis química , Analgésicos/química , Analgésicos/farmacología , Animales , Anticonvulsivantes/química , Fenómenos Químicos , Química Física , Espectroscopía de Resonancia Magnética , Masculino , Ratones , Conformación Molecular , Estructura Molecular , Relación Estructura-Actividad
9.
J Med Chem ; 25(1): 57-63, 1982 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-7086823

RESUMEN

Studies on dehydrogenase enzyme inhibition have been extended with the design, synthesis, and correlation analysis of 7-[(substituted-benzyl)oxy]-, 7-[(substituted-phenethyl)oxy]-, and 7([substituted-phenoxy)ethoxy]-4-hydroxyquinoline-3-carboxylic acids. Sixteen new congeners and the fifteen molecules previously synthesized have been tested against cytoplasmic malate dehydrogenase and lactate dehydrogenase, as well as against mitochondrial malate dehydrogenase. The lipophilic congeners show a clear specificity for inhibition of the mitochondrial enzyme. Correlation analysis of the data on the three enzymes allows a comparison of the binding sites in quantitative terms, while examination of the data on inhibition of ascites tumor cell respiration affords an indication of membrane transport. A newly developed high-pressure liquid chromatography based retention index is compared to the octanol-water pi constant as a model for hydrophobic interactions.


Asunto(s)
Antineoplásicos/farmacología , Carcinoma de Ehrlich/metabolismo , Hidroxiquinolinas/farmacología , L-Lactato Deshidrogenasa/antagonistas & inhibidores , Malato Deshidrogenasa/antagonistas & inhibidores , Consumo de Oxígeno/efectos de los fármacos , Animales , Carcinoma de Ehrlich/tratamiento farmacológico , Conejos , Relación Estructura-Actividad
10.
J Appl Physiol (1985) ; 95(5): 1901-7, 2003 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-12857763

RESUMEN

The quantification of maximum oxygen uptake (V(O2 max)), a parameter characterizing the effective integration of the neural, cardiopulmonary, and metabolic systems, requires oxygen uptake (VO2) to attain a plateau. We were interested in whether a VO2 plateau was consistently manifest during maximal incremental ramp cycle ergometry and also in ascertaining the relationship between this peak VO2 (V(O2 peak)) and that determined from one, or several, maximal constant-load tests. Ventilatory and pulmonary gas-exchange variables were measured breath by breath with a turbine and mass spectrometer. On average, V(O2 peak) [3.51 +/- 0.8 (SD) l/min] for the ramp test did not differ from that extrapolated from the linear phase of the response in 71 subjects. In 12 of these subjects, the V(O2 peak) was less than the extrapolated value by 0.1-0.4 l/min (i.e., a "plateau"), and in 19 subjects, V(O2 peak) was higher by 0.05-0.4 l/min. In the remaining 40 subjects, we could not discriminate a difference. The V(O2 peak) from the incremental test also did not differ from that of a single maximum constant-load test in 38 subjects or from the V(O2 max) in 6 subjects who undertook a range of progressively greater discontinuous constant-load tests. A plateau in the actual VO2 response is therefore not an obligatory consequence of incremental exercise. Because the peak value attained was not different from the plateau in the plot of VO2 vs. work rate (for the constant-load tests), the V(O2 peak) attained on a maximum-effort incremental test is likely to be a valid index of V(O2 max), despite no evidence of a plateau in the data themselves. However, without additional tests, one cannot be certain.


Asunto(s)
Ejercicio Físico/fisiología , Pulmón/fisiología , Consumo de Oxígeno/fisiología , Adulto , Prueba de Esfuerzo/métodos , Humanos , Masculino , Persona de Mediana Edad , Distribución Normal , Intercambio Gaseoso Pulmonar/fisiología
12.
J Microbiol Methods ; 92(2): 183-8, 2013 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-23220059

RESUMEN

Microbial populations, especially those of viruses, are poorly studied in dairy wastewater treatment operations. Here we report signature nucleic acid metagenomic sequences obtained by pyrosequencing viromes of virus-like particles that were extracted from two dairy waste treatment lagoons. The lagoons are operated in series, with Lagoon I being used as the primary stage and Lagoon II as the secondary stage of wastewater treatment. An average of 2000 sequences was obtained from each lagoon. More than 300 signatures from each lagoon matched sequences in the virus database of the National Center for Biotechnology Information (NCBI). We utilized a bioinformatics approach and transmission electron microscopy (TEM) to characterize the viral diversity and presence of potential viral pathogens within the lagoons. Our results showed differences in viral community compositions between Lagoon I and Lagoon II, suggesting that the viral community changes significantly in the transition of water between the two lagoons. Furthermore, the diverse viral community in the lagoon samples contained signature sequences of a variety of bacterial, plant, and animal viruses. Bacteriophage sequences dominated the viral community metagenomes in both lagoons. Ultimately these results can be used to identify viral bioindicators to rapidly assess wastewater treatment quality and the potential impacts of dairy operations on watersheds. Our viral metagenomic sequences have been submitted to GenBank (GPID 65805) and can provide insight into the composition and structure of viral communities within wastewaters of dairy lagoon systems.


Asunto(s)
Biodiversidad , Industria de Alimentos , Metagenómica/métodos , Virus/clasificación , Virus/genética , Aguas Residuales/virología , Animales , Biología Computacional , Microscopía Electrónica de Transmisión , Virus/ultraestructura
20.
J Enzyme Inhib ; 1(4): 259-66, 1987.
Artículo en Inglés | MEDLINE | ID: mdl-3334246

RESUMEN

Growth inhibition of E. coli cell culture has been determined for a series of 4-substituted-N1-phenylsulfonilamides tested in the presence and absence of synergistic concentrations of trimethoprim. Quantitative structure-activity relationships, established by regression analysis, exhibit an identical dependence of bacterial growth inhibition on sulfonamide pKa irrespective of the presence or absence of trimethoprim. Examination of a small series of benzylpyrimidines in the presence or absence of 4-dimethylamino-N1-phenylsulfanilamide gave similar results. Since the presence of a synergistic agent affords no change in structure-activity relationships, it is concluded that no direct interaction between sulfonamides and benzylpyrimidines occurs and that the synergism observed is solely the result of the kinetic consequences of sequential blockade of the folate biosynthetic pathway.


Asunto(s)
Compuestos de Bencilo/farmacología , Escherichia coli/crecimiento & desarrollo , Pirimidinas/farmacología , Sulfanilamidas/farmacología , Sinergismo Farmacológico , Escherichia coli/efectos de los fármacos , Relación Estructura-Actividad , Sulfonamidas/farmacología
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