In pharmaceutical science and drug design the versatility of the pyrrolidine scaffold relating to spatial arrangement, synthetic accessibility and pharmacological profile is a largely explored and most likely interesting one. Nonetheless, few evidences suggest the pivotal role of pyrrolidine as scaffold for multipotent agents in neurodegenerative diseases. We then challenged the enrolling in the field of Alzheimer disease of so far not ravelled targets of this chemical cliché with a structure based and computer-aided design strategy focusing on multi-target action, versatile synthesis as well as pharmacological safeness.
View Article and Find Full Text PDFThe benzothiazole nucleus is a major heterocyclic scaffold whose therapeutic potential has been thoroughly explored due to its structural simplicity and ease of synthesis. In fact, several benzothiazole derivatives have been synthesized over time, demonstrating numerous pharmacological properties such as anticancer, antimicrobial, anti-inflammatory, and antioxidant activities. Herein, we propose a new series of benzothiazole-phthalimide hybrids obtained by linking the phthalimide moiety to differently substituted benzothiazole nuclei through the N atom.
View Article and Find Full Text PDFNowadays, there has been considerable attention paid toward the recovery of waste plant matrices as possible sources of functional compounds with healthy properties. In this regard, we focus our attention on Salicornia, a halophyte plant that grows abundantly on the coasts of the Mediterranean area. Salicornia is used not only as a seasoned vegetable but also in traditional medicine for its beneficial effects in protecting against diseases such as obesity, diabetes, and cancer.
View Article and Find Full Text PDFAlzheimer's disease (AD) is a complex multi-factorial neurodegenerative disorder for which only few drugs (including donepezil, DPZ) are available as symptomatic treatments; thus, researchers are focusing on the development of innovative multi-target directed ligands (MTDLs), which could also alter the course of the disease. Among other pathological factors, oxidative stress has emerged as an important factor in AD that could affect several pathways involved in the onset and progression of the pathology. Herein, we propose a new series of hybrid molecules obtained by linking a phenothiazine moiety, known for its antioxidant properties, with -benzylpiperidine or -benzylpiperazine fragments, mimicking the core substructure of DPZ.
View Article and Find Full Text PDFBackground: Experimental studies suggest that mineral waters with high concentrations of calcium and bicarbonate can impact acid-base balance. The purpose of this study was to test the effect on acid-base balance and specific urine gravity, of a bicarbonate calcic mineral water (Acqua Lete®) compared to a minimally mineralized water.
Methods: 88 amateur male athletes underwent two experimental trials with a modified Wingate test: the first was carried out without hydration (Control Test, Test C, n = 88); the second was carried out after one week of controlled hydration (Test with hydration, Test H, n = 88), with 1.
Objectives: The aim of this study was to determine cardio-respiratory changes after endothoracic sympathetic denervation and their correlation with the extent of denervation.
Methods: A total of 45 patients with essential palmar hyperhidrosis were randomized into two groups: the conventional group (CG; 23 patients) and the simplified group (SG; 22 patients). In the CG, excision of T2 and T3 ganglia was performed, whereas in the SG only separation of the sympathetic chain was performed at the same level.
Purpose: Exercise training is a nonpharmacological intervention that improves cardiovascular function and enhances endothelial homeostasis in patients with cardiovascular diseases. However, the amount of benefit achieved varies widely depending on the type and duration of exercise. Moreover, data about the long-term effects of physical activity are scarce.
View Article and Find Full Text PDFUnlabelled: We compared the effects of exercise on serum levels of creatin kinase (CK) in athletes with persistent hyperCKemia at rest (CK group) and in healthy athletes (control group). Prospective controlled study. Eighteen male Caucasian athletes with high serum CK levels at rest (CK between 80 and 150 U/L) and 25 male Caucasian athletes with normal serum CK levels at rest (CK between 10 and 80 U/L).
View Article and Find Full Text PDFBackground: There is a growing body of evidence that physical training exerts its potential benefits on the individual health status by modulating the immune system and the whole body metabolism. A better knowledge of the physiologic immune response to exercise may help to understand the benefits of physical exercise in healthy individuals and elite athletes.
Aims: This study aims to analyse cardiotrophin-1 (CT-1) and Tumor Necrosis Factor-alpha (TNF-alpha) plasma levels at rest and during exercise in elite athletes and healthy controls.
Total creatin kinase (CK) and lactate dehydrogenase (LDH) serum levels depend on age, gender, race, muscle mass, physical activity, and climatic conditions. High CK serum levels in athletes following rest and without any further predisposing factors should prompt a full diagnostic workup, with special regards to signs of muscle weakness or other signs not always evident. In subjects who have silent myopathy, repeated intense prolonged exercise may produce negative effects, because given the continuous loss of muscle proteins, it does not induce the physiological muscle adaptations to physical training.
View Article and Find Full Text PDFWe determined whether a short-term exhaustive dynamic exercise (cycling) for about 18min induces changes in the intramuscular architecture of the quadriceps in trained athletes. Thirty-five male athletes (age 28.8+/-9.
View Article and Find Full Text PDFUnlabelled: AREAS OF GENERAL AGREEMENT: Total creatine kinase (CK) levels depend on age, gender, race, muscle mass, physical activity and climatic condition. High levels of serum CK in apparently healthy subjects may be correlated with physical training status, as they depend on sarcomeric damage: strenuous exercise that damages skeletal muscle cells results in increased total serum CK. The highest post-exercise serum enzyme activities are found after prolonged exercise such as ultradistance marathon running or weight-bearing exercises and downhill running, which include eccentric muscular contractions.
View Article and Find Full Text PDFAim: To study, by conventional echocardiography, left ventricular remodelling and function in master athletes, hypertension and hypertrophic cardiomyopathy.
Methods: We studied 30 master athletes (MA; soccer players; mean age 43.9+/-5.
CD39/ATP diphosphohydrolase is expressed on B lymphocytes, cytotoxic T lymphocytes, monocytes, platelets, and endothelial cells, and it has a critical role in the inhibition of platelet responsiveness. To determine whether strenuous exercise could acutely change expression of CD39 in platelets and lymphocytes, eight healthy sedentary men, 34 yr old (SD 7), and eight physically active men, 34 yr old (SD 6), performed graded upright cycle ergometry to volitional exhaustion. Blood samples collected both at baseline and after exercise test were employed to measure CD39 expression in platelets and lymphocytes.
View Article and Find Full Text PDFAim: The aim of the study was to evaluate in 263 competitive athletes possible correlations between changes induced by different sport activities in left ventricular (LV) structure and cardiac response during maximal physical effort.
Methods: A total of 160 top-level endurance athletes (ATE; swimmers, runners; 28+/-4 years; 98 male) and 103 strength-trained athletes (ATS; weight-lifters, body-builders; 27+/-5 years; male), selected on the basis of training protocol (dynamic vs. static exercise), underwent standard Doppler echocardiography, heart rate variability analysis and maximal exercise stress test by bicycle ergometry.