Arylsulfonyl histamine derivatives as powerful and selective α-glucosidase inhibitors.

A series of simple N-arylbenzenesulfonyl histamine derivatives were prepared and screened against α-glucosidase. Inhibition was in the micromolar range for several N α,N τ-di-arylsulfonyl compounds, with N α,N τ-di-4-trifluorobenzenesulfonyl histamine (IId) being the best inhibitor. Compound IId is a reversible and competitive α-glucosidase inhibitor, and presented good selectivity with respect to other target enzymes, including ß-glucosidase and α-amylase, and interesting predicted physicochemical properties. Docking studies have been run to postulate ligand-enzyme interactions to account for the experimental results. In vivo, compound IId produced a similar hypoglycemic effect to acarbose with half of its dose.

School-based individualised lifestyle intervention decreases obesity and the metabolic syndrome in Mexican children.

BACKGROUND: Currently, there is limited evidence about effective strategies to manage childhood obesity and the metabolic syndrome in school settings. The present study aims to analyse changes in the prevalence of being overweight/obese and having the metabolic syndrome in relation to a 10-month lifestyle intervention based on individualised face-to-face sessions and parental education in school settings. METHODS: The study sample comprised a cross-sectional sample of 96 overweight/obese Mexican children aged 6-12 years from eight schools. Clinical, anthropometric measurements and 24-h recalls were obtained during each of 13 visits. Laboratory measurements were determined at the beginning and end. The energy-reduced diet was based on dietary recommended intakes. Individualised structured daily meals and a physical activity plan, tailored-made for each child, were provided every 3 weeks at the schools. Parental attendance was required. Student's t-test, McNemar and Shapiro-Wilk tests and simple linear regression were used for the statistical analysis. RESULTS: The prevalence of metabolic syndrome fell significantly from 44% to 16% (P < 0.01), high blood pressure fell from 19% to 0%, hypertrigliceridaemia fell from 64% to 35%, high-density lipoprotein-cholesterol ≤ 40 fell from 60% to 41%, hyperglycaemia fell from 1% to 0%, and waist circumference ≥90th percentile fell from 72% to 57%. There was a 2.84 [95% confidence interval (CI) = -4.10 to -1.58; P < 0.01] significant decrease in body mass index percentile and in body-fat percentage (95% CI = -3.31 to -1.55; P < 0.01). Of the overweight children, 32% achieved normal-weight, whereas 24% of the obese ones converted to overweight and 1% reached normal-weight. Physical activity increased 16 min/day(-1) (P = 0.02) and 2 days/week(-1) . CONCLUSIONS: A school-setting lifestyle intervention led to a decreased prevalence of being overweight/obese and to a striking reduction in the prevalence of the metabolic syndrome in a sample of Mexican children.

Buccodental pathology in patients with insulin-dependent diabetes mellitus: a clinical study.

OBJECTIVE: A study is made to determine whether patients with type 1 (insulin-dependent) diabetes mellitus (IDDM) suffer oral complications attributable to the disease, or whether some disorder of the oral cavity can be regarded as pathognomonic of diabetes. MATERIAL AND METHODS: Thirty juvenile diabetics and 30 healthy individuals were evaluated for dental caries and oral mucosal lesions, with the performance of basal and stimulated sialometry in all cases, to assess possible alterations in salivary flow. In addition, an study of periodontal variables was made such as the presence of bacterial plaque, gingival status and attachment losses. RESULTS AND CONCLUSIONS: The diabetics were found to have significantly greater periodontal attachment loss, even though oral hygiene was significantly better among these patients. There were no differences between the two groups in terms of the number of caries, the presence of mucosal lesions or salivary flow.

Estudio clínico sobre la patología bucodentaria en el paciente diabético tipo 1 / Buccodental pathology in patients with insulin-dependent diabetes mellitus: a clinical study

Objetivo: Comprobar si los pacientes diabéticos insulino-dependientes presentaban complicaciones a nivel bucal debidas a su enfermedad o si existía alguna patología patognomónica de la diabetes mellitus en la cavidad oral. Material y métodos: Se realizó una exploración de 30 individuos diabéticos juveniles (DM 1) y 30 individuos sanos en el que se consignó la existencia de caries dental y la posible existencia de lesiones en la mucosa oral, se realizó una sialometría basal y estimulada en la totalidad de los pacientes para estudiar posibles alteraciones en el flujo salival, y se realizó un estudio de variablesperiodontales tales como la presencia de placa bacteriana, estudio de las condiciones gingivales y de la pérdida de inserción. Resultados y conclusiones: Los diabéticos tenían una mayor pérdida de inserción en su periodonto, siendo esta diferencia significativa. Este hecho ocurría incluso cuando las condiciones de higiene oral eran significativamente mejores para el grupo diabético. No había diferencias en el número de caries encontradas, en la presencia de lesiones en la mucosa o en la tasa de flujo salival (AU)

Immunoradiometric assay of lipid A: a test for detecting and quantitating endotoxins of various origins.

The ability to measure circulating endotoxin in various disease states has been hampered by the lack of a specific and quantitative assay. The test most commonly used has been the Limulus gelation assay, which measures an enzymatic effect of endotoxin rather than the substance itself. Based on a solid-phase immunoradiometric assay previously developed to detect the specific lipopolysaccharide from Escherichia coli 026, a similar assay has been developed for the lipid A moiety of endotoxins. The assay uses rabbit antibodies to lipid A which do not react with ketodeoxyoctonate, myristic or beta-hydroxymyristic acids, and detects lipid A obtained from endotoxins of various origins after acid hydrolysis of lipopolysaccharide. Experiments in rats given exogenous endotoxin suggest that this assay can be useful for quantitation of bacterial endotoxins in serum and for studying the pathophysiology of experimental endotoxemia.