Preferencje help
Widoczny [Schowaj] Abstrakt
Liczba wyników

Znaleziono wyników: 19

Liczba wyników na stronie
Pierwsza strona wyników Pięć stron wyników wstecz Poprzednia strona wyników Strona / 1 Następna strona wyników Pięć stron wyników wprzód Ostatnia strona wyników

Wyniki wyszukiwania

help Sortuj według:

help Ogranicz wyniki do:
Pierwsza strona wyników Pięć stron wyników wstecz Poprzednia strona wyników Strona / 1 Następna strona wyników Pięć stron wyników wprzód Ostatnia strona wyników
Fungicidal properties of 4-(1,3,4-thiadiazol-2-yl)benzene-1,3-diols set under in vitro conditions against five phytopathogenic fungi have been evaluated. The substitution panel includes amino-, alkyl-, alkoxyl-, aryl- and heteroarylderivatives. The most active compound with the benzyl substituent exhibits fungistatic effects amounting to 90-100% with the concentration of 20 μg mL-1 against R. solani, similar to the standard fungicides. The derivatives with amine moiety generally display lower activity than other analogues. F. culmorum seems to be the most refractory fungus compared to studied compounds. The influence of substitution of C-5 at the constant fragment at C-2 of 1,3,4-thiadiazole ring on the antifungal effect is discussed. To explain differences in the activity the quantum-chemical calculations were made.
In laboratory plate studies on the effect of L-histidine on the fungistatic action of 2,4,6- trihydroxybenzencarboditioic acid (TBKD) was recorded. A gradual increase of concentration of L-histidine in the mineral medium at first weakens and then increases inhibitory properties of the system. The mechanism of the molecular co-operation of the amino acid was also discussed.
Studies were the effect of 2,4,6-trihydroxybenzenocarboditioic acid (TBCD) on unpurified enzymatic extract of aconitate hydratase from Aspergillus niger fungi. The inhibition of aconitate hydratase functions, by means of estimation of regulation extent of equilibrium isomerization reactions of citrates under influence of TBCD, was found.
The retention behaviour of eighteen new antifungal dihydroxythiobenzanilides in a reversed-phase high performance thin-layer chromatographic system has been examined. Using water-acetone as the mobile phase, a linear relationship between the volume fraction of the organic solvent and the log k' values over a limited range was established for every solute. The physico-chemical parameters of these compounds were characterized by their hydrophobicity parameters log k'w, determined by extrapolation of the linear relationships for retention data in binary solvent systems to pure water. The good correlation obtained between log k' and S values of TLC equation supports the validity of the extrapolation technique. It was found that log k'w values of examined substances were correlated to their antimicrobial activity. The results suggest that log k'w might be an accurate model for assessment of the hydrophobicity of studied fungicides in biological systems.
Bee venom is a complex mixture of substances of natural origin, whose therapeutic properties are used in many areas of medicine. Generally accepted procedures applied in the process of developing new drugs include tests that examine interactions between the new drug and the enzymes of the cytochrome P450 group (CYP450), which play a key role in the metabolism of xenobiotics and endogenous substances in mammals. The use of bee venom in the treatment of various diseases and in immunotherapy makes it necessary to test this material for its effect on the enzymes of the CYP450 group in order to prevent health-threatening interactions. The purpose of this paper was to investigate the effect of bee venom and its main component, melittin, on CYP1A2 enzyme activity. This enzyme plays an important role in the metabolism of many pharmaceuticals and toxins. This is the first study on the effect of bee venom on the activity of an enzyme of the CYP450 family. The CYP1A2/CEC High Throughput Inhibitor Screening Kit (BD Biosciences) was used in the study. The method was based on the measurement of fluorescence of the enzymatic reaction product (3-cyano-7- -hydroksycoumarin) formed by the action of the CYP1A2 on the substrate (3-cyano-7-ethoxycoumarin) in the presence of a potential inhibitor in various concentrations. Furafylline was used as a model inhibitor. Twenty samples of bee venom from different years and of different origin, as well as melittin, were analyzed. The tests were performed at 37°C in 96-well microplates with an Infinite M200 Pro (Tecan) microplate reader. Fluorescence measurement parameters were as follows: excitation – 410 nm, emission – 460 nm. On the basis on the results obtained, IC₅₀ values were calculated, which are equal to the concentrations of particular inhibitors causing the inhibition of enzyme activity by 50%. The IC₅₀ values against CYP1A2 for different samples of bee venom ranged from 0.13 µg/ml to 2.38 µg/ml (mean = 0.74 µg/ml). Comparison of the IC₅₀ values for bee venom and furafylline (1.53 µg/ml) demonstrates potent inhibitor properties of bee venom against CYP1A2. The fact that IC₅₀ values for different bee venom samples show a relatively high variability may be caused by composition differences between particular bee venom samples. The data obtained also indicate that melittin is a relatively weak inhibitor of CYP1A2 activity compared to bee venom (IC₅₀ for melittin is 41.04 μg/ml). It can therefore be assumed that the inhibition of CYP1A2 by bee venom is caused by its other components. The results obtained highlight the problem of potential interactions between bee venom and therapy.
4BrABT (2-(4-Bromophenylamino)-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole) is a compound known for its interesting in vitro anticancer profile. 4BrABT inhibited proliferation and motility of several cancer cell lines in concentrations which were not toxic to normal cells. A major problem associated with cancer chemotherapy, but also caused by environmental factors such as pesticides, is neurotoxicity. Therefore, the aim of the presented study was an in vitro evaluation of the neuroprotective activity of this compound. 4BrABT activity (1–100 μM) was tested in cultures of mouse neurons, rat astrocytes and rat oligodendrocytes. A possible protective action of the compound in different neurodegenerative models, as serum deprivation (SD), excitotoxicity (presence of 500 μM glutamate in culture medium), as well as cisplatin toxicity (astroglia – 50 μM and oligodendroglia – 100 μM) was investigated. Cell viability in the tested cultures was assessed with the use of LDH and MTT methods. Moreover, 4BrABT ability to prevent the cisplatin-induced apoptosis in astrocyte and oligodendrocyte cultures was analysed after Hoechst 33342 fluorostaining. The obtained results indicate that 4BrABT was not toxic to neurons, astrocytes and oligodendrocytes. Moreover, a decrease in the neuronal LDH level was observed, which may suggest the ability of 4BrABT to act as a trophic agent. Furthermore, the protective action of the studied compound was shown in neuronal cultures exposed to neurotoxic conditions (presence of glutamate and trophic stress) and in cisplatin-treated astrocytes and oligodendrocytes. The expression of anticancer and neuroprotective activity raises hopes for the potential use of 4BrABT as a safe anticancer drug, or neuroprotective agent in chemotherapy-associated neurotoxicity.
Celem pracy była ocena różnic stężeń cholesterolu (TC), jego frakcji (LDL-C) i triacyloglicerydów (TG) w osoczu badanych pacjentów w okresie jesienno zimowym stosujących dietę hipolipemiczną. Badaniem objęto 47 osób ( 25 kobiet i 22 mężczyzn) w wieku 37-64 lata w związku z leczeniem nadwagi (BMI 27,5±3,9). Wszyscy pacjenci uczestniczący w badaniu od kilu miesięcy stosowali dietę opartą na ograniczeniu zawartości tłuszczów. U 22 osób z tej grupy stwierdzono hiperlipidemię typu II. U pacjentów u których stwierdzono wartości stężeń TC, LDL-C, i TG przekraczające podane zakresy referencyjne zalecono kontrolną wizytę po upływie 12 tygodni. Badanych podzielono na 2 grupy: I: grupa kontrolna: 22 osoby zdrowe (13 kobiet i 9 mężczyzn) z prawidłowymi stężeniami lipidów, w wielu 56,90±6,3 lat. II: 25 chorych z hiperlipidemią typu II (12 kobiet i 13 mężczyzn) w wieku 49,3 lat ±12,3 Po zakończeniu badań u pacjentów z hiperlipidemią typu II stwierdzono znamienny wzrost: 1. TC i LDL-C porównując grupę przed badaniem do grupy po 12 tygodniach obserwacji. 2. LDL-C i TG porównując grupę przed badaniem do grupy kontrolnej. 3. TG porównując grupę po 12 tygodniach obserwacji do grupy kontrolnej.
We determined CA1 hippocampal field to be involved in self‑exposure, a type of novelty‑seeking behaviour that has also been associated with short 22 kHz and flat 50 kHz ultrasonic vocalizations (USV) in adult male Long‑Evans rats. Rats were habituated for three days to a self‑exposure cage with two nose‑poke holes. On day four, the animals from the experimental group were allowed to turn the cage light off for 5 s with a nose‑poke (test/self‑exposure session), while rats from control‑yoked group had changing light conditions coupled and identical to the experimental animals. The experimental rats performed more nose‑pokes during self‑exposure session than animals from the control group. This effect was accompanied by a higher density of c‑Fos‑positive nuclei in the hippocampal CA1. There were no significant group differences in c‑Fos expression in other brain regions analysed. However, possible involvement of several other structures in self‑exposure (i.e., CA3, the dentate gyrus, amygdala, prefrontal cortex, and nucleus accumbens) is also discussed, as their correlational activity, reflected by c‑Fos immunoactivity, was observed in the experimental rats. During test sessions, there were more nose‑pokes accompanied by short 22 kHz calls and 50 kHz calls performed by the rats of the experimental group than of the control group. The CA1 region has previously been associated with novelty; short 22 kHz USV and flat 50 kHz USV could be associated with self‑exposure, also they appear to be emitted correlatively.
Pierwsza strona wyników Pięć stron wyników wstecz Poprzednia strona wyników Strona / 1 Następna strona wyników Pięć stron wyników wprzód Ostatnia strona wyników
JavaScript jest wyłączony w Twojej przeglądarce internetowej. Włącz go, a następnie odśwież stronę, aby móc w pełni z niej korzystać.