A new series of betulin derivatives containing one or two pharmacophores bearing an acetylenic and carbonyl function at the C-3 and/or C-28 positions has been synthesized and characterized by 1H- and 13C-NMR, IR, MS and elemental analyses. The crystal structure of 28-O-propynoylbetulin was determined by X-ray structural analysis. All new compounds, as well as betulin, were tested in vitro for their antiproliferative activity against human SW707 colorectal, CCRF/CEM leukemia, T47D breast cancer, and against murine P388 leukemia and Balb3T3 normal fibroblasts cell lines. Most of the compounds showed better cytotoxicity than betulin and cisplatin used as reference agent. 28-O-Propynoylbetulin was the most potent derivative, being over 500 times more potent than betulin and about 100 times more cytotoxic than cisplatin against the human leukemia (CCRF/CEM) cell line, with an ID50 value of 0.02 μg/mL.
For the first time, Raman spectroscopy has been employed to investigate formation of cross-links in collagen and porcine pericardium tissue upon glutaraldehyde (GA) treatment. GA treatment causes a very high fluorescence background, which overlaps Raman bands. It has been found that short fixation time, i.e. 2 h, reduces background radiation significantly, providing new possibilities for studying changes in molecular structure of collagen upon GA modification. The observed changes in position and intensity of Raman bands allowed us to recognize different types of GA-collagen interactions. Strong spectral evidence has been found for the peptide contribution to the formation of the GA-collagen cross-links and for the formation of secondary amines via Schiff base intermediates, and pyridinium-type cross-links. The results also revealed that different hydration levels and a more complex structure of intact tissue in comparison to collagen preparation strongly influence the formation of a GA cross-linking network, e.g. ether-type bond is preferred to form in a less hydrated collagen preparation. Our results have shown that GA treatment causes an increase in water content of pericardium tissue and collagen.
Jastrzębska, M, Kaczmarczyk, M, and Jastrzębski, Z. Effect of vitamin D supplementation on training adaptation in well-trained soccer players. J Strength Cond Res 30(9): 2648-2655, 2016-There is growing body of evidence implying that vitamin D may be associated with athletic performance, however, studies examining the effects of vitamin D on athletic performance are inconsistent. Moreover, very little literature exists about the vitamin D and training efficiency or adaptation, especially in high-level, well-trained athletes. The purpose of the current study was to investigate the effect of vitamin D supplementation on training adaptation in well-trained football players. The subjects were divided into 2 groups: the placebo group (PG) and the experimental group (SG, supplemented with vitamin D, 5,000 IU per day). Both groups were subjected to High Intensity Interval Training Program. The selection to the groups was based on peak power results attained before the experiment and position on the field. Blood samples for vitamin D level were taken from the players. In addition, total work, 5, 10, 20, and 30 m running speed, squat jump, and countermovement jump height were determined. There were no significant differences between SG and PG groups for any power-related characteristics at baseline. All power-related variables, except the 30 m sprint running time, improved significantly in response to interval training. However, the mean change scores (the differences between posttraining and pretraining values) did not differ significantly between SG and PG groups. In conclusion, an 8-week vitamin D supplementation in highly trained football players was not beneficial in terms of response to High Intensity Interval Training. Given the current level of evidence, the recommendation to use vitamin D supplements in all athletes to improve performance or training gains would be premature. To avoid a seasonal decrease in 25(OH)D level or to obtain optimal vitamin D levels, the combination of higher dietary intake and vitamin D supplementation may be necessary.
There is no clear evidence that vitamin D effectively improves physical capacity in high-level athletes. The aim of this study was to confirm that vitamin D supplementation of soccer players during eight-week high-intensity training would have a significant effect on their aerobic capacity. The subjects were divided into two groups: the experimental one that was supplemented with vitamin D (SG, n = 20), and the placebo group (PG, n = 16), not supplemented with vitamin D. All the players were subjected to the same soccer training described as High-Intensity Interval Training (HIIT). The data of the vitamin D level, PWC170, lactate threshold (LT) were collected just before and after the intervention. A significant increase in vitamin D concentration (119%) was observed in the supplemented group, while the non-supplemented group showed a decrease of 8.4%. The studied subjects improved VO2max results by 20% in the SG, and by 13% in the PG. The improvement in velocity at the LT was similar in both groups. Results of this study show that vitamin D can have a positive, though moderate, effect on aerobic performance in players subjected to high-intensity training in the form of small-sided games for 8 weeks.
In this paper we tested a group of 66 healthy volunteers in terms of the influence of circadian rhythm on selected parameters of the coagulation system and fibrinolytic system. Blood was collected at 6-hour intervals, at 8 am, 2 pm, 8 pm and 2 am. Circadian variability was observed in the coagulation system parameters as well as in the fibrinolytic system. We observed increased platelet aggregation, APTT prolongation, along with increased levels of factors (fibrinogen, PAI-1) and PAP and TAT complexes that influence coagulation and fibrinolysis systems, in the blood samples collected in the morning (8 am). We also demonstrated a circadian rhythm in the number of circulating platelets (PLT), with a peak in the afternoon (2 pm) accompanied by increased concentrations of t-PA, D-dimers and PT prolongation. Based on the obtained results it was possible to conclude that circadian rhythm had an influence on the activation of coagulation processes in the morning, with a progressive activation of fibrinolysis up to the afternoon. Our results may be helpful in determining the transient risk of cardiovascular events, including myocardial infarction and ischemic stroke, and hence, can contribute to the effective prevention of such events. Such observations may also become a starting point of departure for further studies aimed at determining the circadian effect of secretion of parameters in the hemostasis system on the other systems and parameters in the human body.
Objectives: The objective of the study was to reveal morphology, electrolyte and chosen biochemical parameters in terms of health risk in runners in reference to their age and running speed in the case of running a distance of 100 km, which occur after 12 h or 24 h of recovery. Material and Methods: Fourteen experienced, male, amateur, ultra-marathon runners, divided into two age and two speed groups took part in the 100-km run. Blood samples for analyses indexes were collected from the ulnar vein just before the run, after 25 km, 50 km, 75 km and 100 km, as well as 12 h and 24 h after termination of the run. Results: The sustained ultramarathon run along with the distance covered (p < 0.05) caused an increase in myoglobin (max 90-fold), bilirubin (max 2.8-fold) and total antioxidant status (max 1.15-fold), which also continued during the recovery. Significant changes in the number of white blood cells were observed with each sequential course and could be associated with muscle damage. The electrolyte showed changes towards slight hyperkalemia, but no changes in natrium and calcium concentrations. There were no significant differences between the age and speed groups for all the parameters after completing the 100-km run as well as after 12 h and 24 h of recovery. Conclusions: Considering changes in blood morphology and chosen biochemical parameters in ultra-marathon runners during a 100-km run it can be stated that such an exhausting effort may be dangerous for human health due to metabolic changes and large damage to the organs. Negative metabolic changes are independent of age of an ultramarathon runner and occur both in younger (32±5.33 years) and older participants (50.56±9.7 years). It can be concluded that organ damage and negative metabolic changes during a 100-km run occur similarly in participants less experienced as well as in well trained runners. Int J Occup Med Environ Health 2016;29(5):801-814
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