A new vinyl selenone-based domino approach to spirocyclopropyl oxindoles endowed with anti-HIV RT activity.

Herein, we disclose a general and flexible access to spirocyclopropyl oxindoles by a domino Michael/intramolecular nucleophilic substitution pathway with variously substituted vinyl selenones and enolizable oxindoles in aqueous sodium hydroxide solution. The spirocyclopropyl oxindole being a privileged scaffold, some of the synthesized compounds were selected for biological evaluation. Compound showed selective anti-HIV-1 activity thanks to its ability to inhibit the reverse transcriptase.

Physical exercise for late-life major depression.

BACKGROUND: Interventions including physical exercise may help improve the outcomes of late-life major depression, but few studies are available. AIMS: To investigate whether augmenting sertraline therapy with physical exercise leads to better outcomes of late-life major depression. METHOD: Primary care patients (465 years) with major depression were randomised to 24 weeks of higher-intensity, progressive aerobic exercise plus sertraline (S+PAE), lower-intensity, non-progressive exercise plus sertraline (S+NPE) and sertraline alone. The primary outcome was remission (a score of ≤10 on the Hamilton Rating Scale for Depression). RESULTS: A total of 121 patients were included. At study end, 45% of participants in the sertraline group, 73% of those in the S+NPE group and 81% of those in the S+PAE group achieved remission (P = 0.001). A shorter time to remission was observed in the S+PAE group than in the sertraline-only group. CONCLUSIONS: Physical exercise may be a safe and effective augmentation to antidepressant therapy in late-life major depression.

Physical Exercise for Late-Life Major Depression.

(Reprinted with permission from Br J Psychiatry 2005; 207: 235-242).

[The risk factors of atherosclerotic disease. Life style and primary prevention]. / Fattori di rischio della malattia aterosclerotica. Stile di vita e prevenzione primaria.

Atherosclerosis brings about cardiovascular diseases and is the world's largest cause of death. Risk factors are to be considered in their incidence and correlation to various pathologies. Cholesterolaemia, smoking, physical inactivity, alcohol are held to be the most important risk factors. Hypercholesterolaemia involves a greater incidence of coronary heart disease; studies on cholesterol reduction however did not give evidence of any reduction in overall mortality. Alcohol displays an u-shaped relation between levels of assumption and associated mortality, depending on the fact that moderate drinkers show decreasing mortality scores and even a decreasing incidence of cardiovascular diseases (while the curve inflects upwards for serious drinkers). A direct correlation appears instead between both smoking and sedentary life on the one hand and both cardiovascular pathologies and mortality on the other. In order to reduce the risk factors' influence, on the ground of available studies and published trials do the authors offer practical indications. Fats in diet should be less than 30% of total calories (where of 10% saturated, 10% monounsaturated, 10% polyunsaturated); abstention from smoking must be absolute; alcohol should not exceed 15 g/die; some physical activity should be practised for 40-60 minutes, twice a week.

Basal and stimulated serum immunoreactive trypsin in normal subjects.

Fasting serum immunoreactive trypsin (IRT) concentrations were measured in 35 healthy subjects. In 10 of them serum IRT levels were also evaluated after administration of secretin (GIH, 75 CU i.v. over 2 minutes); in 7 after a Lundh meal; in 12 after a standard protein meal (Liebig meat extract, 15 g in 150 ml of water) and in 13 after a glucose (1 g/Kg) oral load. Serum IRT was measured by radioimmunoassay (Trypsik kit, CIS, Sorin-Biomedica, Saluggia, Vercelli, Italy). Fasting serum IRT was 25.8 +/- 9 ng/ml (mean +/- SD). No correlation was found between age and serum IRT levels, nor were any statistical differrences observed in IRT concentration between the two sexes. A standard protein meal, Lundh meal or oral load of glucose did not provoke a significant increase in serum IRT levels. Only rapid i.v. injection of secretin was able to induce a significant rise of IRT over basal levels in healthy subjects. This behaviour is probably due more to an engorgement of the pancreatic ductal system with regurgitation of trypsinogen into the blood steam rather than to a direct effect of secretin on the synthesis and secretion of trypsin or to intestinal reabsorption of this enzyme.

Human heart rate variability and sleep stages.

With the aim of better understanding the dynamic changes in sympatho-vagal tone occurring during the night, human heart rate variability (HRV) during the various sleep stages was evaluated by means of autoregressive spectral analysis. Each recording consisted of an electroencephalogram, an electrooculogram, and electromyogram, and electrocardiogram, and a spirometry trace. All of the data were sampled and stored in digital form. Sleep was analysed visually, but HRV was analysed off-line by means of original software using Burg's algorithm to calculate the LF/HF ratio (LF: 0.04-0.12 Hz; HF: 0.15-0.35 Hz) for each sleep stage. Seven healthy subjects (four males; mean age 35 years) were enrolled in the study. Our findings show a progressive and significant reduction in the LF/HF ratio through sleep stages S1-S4, as a result of an increase in the HF component; this indicates the prevalence of parasympathetic activity during slow-wave sleep. During wakefulness, S1 and REM, the LF/HF values were similar and close to 1.