Can physical activity influence the quality of sleep among the elderly?

Introduction: Research shows that over the half of people in the age of more than fifty have got problems with lowered quality of sleep. The cause of lowered quality of sleep is i.a. waking up early, lengthened sleep latency, increased number of waking during the night or shortened time of sleep. The aim of the study was to show how significant are sleep related problems which appear after the age of fifty and how regular physical activity can improve the quality of sleep and as a result functioning of the elderly. Physical activity delays involutional changes and the process of ageing, which lets the elderly stay independent and self-reliant in everyday activities. The aim of the study: The study was to mark the connection between physical activity intensity and the quality of sleep of the elderly. 290 Material and methods: Research for the study was made by means of anonymous survey which consisted of two questionnaires: The Pittsburgh Sleep Quality Index (PSQI) and The International Physical Activity Questionnaire. The survey was targeted at people in the age of over fifty. 100 people took part in the research. Results: Significant statistical correlation between early falling asleep, waking up at night or before dawn with the intensive or moderate physical effort has been obtained. Conclusions: The research has shown that people who performed intense or moderate physical activity woke up less frequently during the night, fell asleep faster and reported better quality of sleep. In addition, it has been noticed that the lowered quality of sleep has got a negative influence on i.a. energy levels and staying alert

4-[Bis(thiazol-2-ylamino)methyl]phenol

We have designed and synthesized novel bis-thiazole derivative. A 4-[bis(thiazol-2-ylamino)methyl]phenol was efficiently prepared in 71% yield by the reaction of 2-aminothiazole with 4-hydroxybenzaldehyde in ethanol for 24 h. The structure of newly obtained compound was characterized by 1H, 13C NMR and mass spectrometry. Bis-thiazole derivative exhibits high tyrosinase inhibitory activity with an IC50 value of 29.71 μM. This inhibitory activity is 2.4 times higher than that of activity of kojic acid (IC50 72.27 µM) and almost 13 times higher than that of ascorbic acid (IC50 385.6 µM). Obtained data suggest that the presented compound may be a leading candidate for a tyrosinase inhibitor

Triazene salts: Design, synthesis, ctDNA interaction, lipophilicity determination, DFT calculation, and antiproliferative activity against human cancer cell lines

Synthesis, characterization and investigation of antiproliferative activity of nine triazene salts against human cancer cells lines (MV-4-11, MCF-7, JURKAT, HT-29, Hep-G2, HeLa, Du-145 and DAUDI), and normal human mammary epithelial cell line (MCF7-10A) is presented. The structures of novel compounds were determined using 1H and 13C NMR, and GC-APCI-MS analyses. Among the derivatives, compound 2c, 2d, 2e and 2f has very strong activity against biphenotypic B myelomonocytic leukemia MV4-11, with IC50 values from 5.42 to 7.69 µg/ml. The cytotoxic activity of compounds 2c-2f against normal human mammary gland epithelial cells MCF-10A is 6–11 times lower than against cancer cell lines. Our results also show that compounds 2c and 2f have very strong activity against DAUDI and HT-29 with IC50 4.91 µg/ml and 5.59 µg/ml, respectively. Their lipophilicity was determined using reversed-phase ultra-performance liquid chromatography and correlated with antiproliferative activity. Our UV–Vis spectroscopic results indicate also that triazene salts tends to interact with negatively charged DNA phosphate chain. To support the experiment, theoretical calculations of the 1H NMR shifts were carried out within the Density Functional Theory. Keywords: Antiproliferative activity, Triazene, Nuclear Magnetic Resonance, Lipophilicity, DN

Tropinone-Derived Alkaloids as Potent Anticancer Agents: Synthesis, Tyrosinase Inhibition, Mechanism of Action, DFT Calculation, and Molecular Docking Studies

A new series of hybrid compounds with tropinone and thiazole rings in the structure was designed and synthesized as potential anticancer agents. They were tested against human multiple myeloma (RPMI 8226), lung carcinoma (A549), breast adenocarcinoma (MDA-MB-231), and mouse skin melanoma (B16-F10) cell lines. Toxicity was tested on human normal skin fibroblasts (HSF) and normal colon fibroblasts (CCD-18Co). The growth inhibition mechanism of the most active derivative was analyzed through investigation of its effect on the distribution of cell cycle phases and ability to induce apoptosis and necrosis in RPMI 8226 and A549 cancer cells. The tyrosinase inhibitory potential was assessed, followed by molecular docking studies. Compounds 3a–3h show high anticancer activity against MDA-MB-231 and B16-F10 cell lines with IC50 values of 1.51–3.03 µM. Moreover, the cytotoxic activity of the investigated compounds against HSF and CCD-18Co cells was 8–70 times lower than against the cancer cells or no toxicity was shown in our tests, with derivative 3a being particularly successful. The mechanism of action of compound 3a in RPMI 8226 cell was shown to be through induction of cell death through apoptosis. The derivatives show ability to inhibit the tyrosinase activity with a mixed mechanism of inhibition. The final molecular docking results showed for IC50 distinct correlation with experiment