A library of thirty two 3,4-diphenylfuranones related to both combretastatin A-4 and antifungal 5-(acyloxymethyl)-3-(halophenyl)-2,5-dihydrofuran-2-ones was prepared. Cytotoxic effects on a panel of cancer and normal cell lines and antiinfective activity were evaluated, and the data were complemented with tests for the activation of caspase 3 and 7. High cytotoxicity was observed in some of the halogenated analogues, eg. 3-(3,4-dichlorophenyl)-4-(4-methylphenyl)-2,5-dihydrofuran-2-one with IC50 0.12-0.23 μM, but the compounds were also highly toxic against non-malignant control cells. More importantly, notable antibacterial activity indicating G+ selectivity has been found in the 3,4-diarylfuranone class of compounds for the first time. Hydroxymethylation of furanone C5 knocked out cytotoxic effects (up to 40 μM) while maintaining significant activity against Staphylococcus strains in some derivatives. MIC95 of the most promising compound, 3-(4-bromophenyl)-5,5-bis(hydroxymethyl)-4-(4-methylphenyl)-2,5-dihydrofuran-2-one against S. aureus strain ATCC 6538 was 0.98 μM (0.38 μg/mL) and 3.9 μM (1.52 μg/mL) after 24 and 48 h, respectively.
- Klíčová slova
- Antibacterial, Combretafuranone, Combretastatin analogue, Cytotoxic, Furanone, Synthesis,
- MeSH
- antibakteriální látky chemická syntéza chemie farmakologie MeSH
- antifungální látky chemická syntéza chemie farmakologie MeSH
- apoptóza účinky léků MeSH
- Bacteria účinky léků MeSH
- furany chemická syntéza chemie farmakologie MeSH
- houby účinky léků MeSH
- kultivované buňky MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- molekulární struktura MeSH
- proliferace buněk účinky léků MeSH
- viabilita buněk účinky léků MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- antibakteriální látky MeSH
- antifungální látky MeSH
- furany MeSH
Juvenile wild and hatchery-reared European grayling Thymallus thymallus were tagged with radio-transmitters and tracked in the Blanice River, River Elbe catchment, Czech Republic, to study their behavioural response to stocking and environmental variation. Both wild and hatchery-reared T. thymallus increased their diel movements and home range with increasing light intensity, flow, temperature and turbidity, but the characteristics of their responses differed. Environmental variables influenced the movement of wild T. thymallus up to a specific threshold, whereas no such threshold was observed in hatchery-reared T. thymallus. Hatchery-reared fish displayed greater total migration distance over the study period (total migration) than did wild fish, which was caused mainly by their dispersal in the downstream direction.
- Klíčová slova
- migration, movement behaviour, salmonids, stocking, threshold, turbidity,
- Publikační typ
- časopisecké články MeSH
Twenty individuals of the largest European freshwater predator, the European catfish Silurus glanis, were tagged with electromyogram (EMG) physiological telemetry sensors. The fish were observed during diel cycles during the spring and summer in the Elbe and Berounka Rivers, Czech Republic. The purpose of this study was to determine whether diel dualism in the activity of S. glanis occurs naturally or is induced by the laboratory environment and by the conditions occurring in aquaculture. The results obtained from the riverine environment tended to show dualism in the use of the light and dark phases of the day because 35% of the individuals varied from a site-specific common diel activity pattern. The EMG values increased in accordance with the mass (M) of the fish. To eliminate the influence of M on individual energy consumption, the EMG records were analysed in terms of the EMG:M ratios. High individual variability was found in these ratios. The diel activity pattern of the individuals with relatively high energy consumption differed from the common diel activity pattern. In contrast, the fish that adopted the common diel activity pattern displayed relatively low energy consumption. The results of this study indicated that dualism and energy consumption are related. The EMG values also varied with the values of the environmental variables. Increasing temperature was associated with high EMG values, whereas the EMG values decreased with increasing flow.
- MeSH
- cirkadiánní rytmus * MeSH
- energetický metabolismus * MeSH
- pohybová aktivita fyziologie MeSH
- sumci metabolismus MeSH
- telemetrie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Geografické názvy
- Česká republika MeSH
The growth, and dispersal of stocked European grayling Thymallus thymallus, reared in a hatchery (fed dry food pellets) or in a pond (fed natural food), compared with their wild conspecifics was assessed from the recapture of individually tagged fish 168 days after their release into the Blanice River, Czech Republic. Recapture rates and site fidelity were higher for wild T. thymallus than for artificially reared fish. Specific growth rate and upstream or downstream dispersal did not significantly differ between any of the groups of fish. An influence of rearing conditions (pond v. hatchery) on the overall performance of stocked fish was not demonstrated. Initially, lower condition factors of reared T. thymallus were equal to wild fish after recapture, suggesting adaptation of artificially reared fish that remained in the sections studied.
- MeSH
- chování zvířat * MeSH
- lineární modely MeSH
- řeky MeSH
- rybářství MeSH
- Salmonidae růst a vývoj fyziologie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- srovnávací studie MeSH
- Geografické názvy
- Česká republika MeSH
Seventeen individuals of ide Leuciscus idus were radio-tracked weekly from September 2003 to September 2004 in the River Elbe, Czech Republic, to examine migration patterns and the influence of environmental factors on their diurnal behaviour. Of the 10 environmental factors measured, L. idus were significantly influenced by turbidity, which increased diurnal movement and the home range size of the species. The peak of longitudinal movement occurred in the spring, indicating pre-spawning migration. Migrating fish moved downstream and later returned upstream to the vicinity of their original locations, displaying a homing behaviour.
- MeSH
- Cyprinidae fyziologie MeSH
- lineární modely MeSH
- migrace zvířat * MeSH
- nefelometrie a turbidimetrie MeSH
- řeky MeSH
- teritoriální chování * MeSH
- životní prostředí * MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Geografické názvy
- Česká republika MeSH
The authors compare perinatal results in insulin treated diabetic women who were followed up in the out-patient department of the Second Gynaecological and Obstetric Clinic of the Masaryk University in Brno. In 1980-1984 148 pregnant diabetic women were followed up and in 1985-1991 when self-monitoring has become part of comprehensive treatment of pregnant diabetics in our department, 279 women were followed up. The patients were monitored during pregnancy by a diabetologist and gynaecologist. Other members of the team are a paediatrician, geneticist, psychologist, dietitian, and educational nurse. As to laboratory parameters, short-term and long-term compensation of diabetes were monitored. Systematic preconception preparation of diabetic patients, with an attempt to achieve normal blood sugar levels and genetic examination of both partners from part of comprehensive care. The results achieved in our department revealed a statistically significant decline of the incidence of foetopathies in neonates at the 5% level of significance and a decline of hypoglycaemia in foetuses at the 0.1% level.
- MeSH
- dospělí MeSH
- glykosurie MeSH
- inzulin terapeutické užití MeSH
- lidé MeSH
- péče o sebe * MeSH
- selfmonitoring glykemie MeSH
- těhotenství při diabetu krev farmakoterapie moč MeSH
- těhotenství MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- Názvy látek
- inzulin MeSH
The authors revealed during dispensarization of pregnant women suffering from essential hypertension that the disease is relatively frequently associated with some metabolic disorders, i. e. obesity, gestational diabetes or impaired glucose tolerance. They draw attention to a similarity with Reaven's syndrome in non-pregnant women. The authors recommend to screen for diabetes all obese pregnant women and those with hypertension to detect an impaired glucose metabolism and prevent foetopathies in neonates of thus affected mothers. The authors consider obesity one of the subsidiary criteria in the differential diagnosis of essential hypertension and preeclampsia.
- MeSH
- gestační diabetes komplikace diagnóza MeSH
- glukosa metabolismus MeSH
- hypertenze komplikace diagnóza MeSH
- komplikace těhotenství diagnóza MeSH
- lidé MeSH
- novorozenec MeSH
- obezita komplikace MeSH
- preeklampsie komplikace diagnóza MeSH
- těhotenství MeSH
- Check Tag
- lidé MeSH
- novorozenec MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- Názvy látek
- glukosa MeSH
In the Second Gynaecological and Obstetric Clinic in Brno there has been for more than 15 years a specialized department for treatment of diabetes during pregnancy. The department monitors and treats pregnant diabetics from approximately two thirds of the former South Moravian region, i.e. patients with diabetes assessed before pregnancy as well as those where an impaired carbohydrate metabolism was detected during pregnancy. The authors submit an account of the organization of team work in their out-patient department.
- MeSH
- dospělí MeSH
- gestační diabetes terapie MeSH
- lidé MeSH
- mladiství MeSH
- poradenství * MeSH
- prenatální péče * MeSH
- těhotenství při diabetu * terapie MeSH
- těhotenství MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- mladiství MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
The authors compared two groups of pregnant women with early loss of amniotic fluid. In the first group Claforan was administered, 3 x 1 g by the i.m. route, and in the second group Ampicillin, 3 x 1 g by the i.m. route. The data were recorded in a special protocol and were divided into three groups: 1. patient before delivery, 2. patient during puerperium, 3. neonate. From the results two conclusions were drawn: 1. The authors did not detect any reasons why antibiotics should not be administered prophylactically in case of premature loss of amniotic fluid. 2. The main differences between the compared groups were found in neonates where after administration of Claforan there was a substantially lower incidence of positive bacterial cultures than after Ampicillin and there was also a lower incidence of RDS II and adnatal infections.
- MeSH
- ampicilin aplikace a dávkování MeSH
- bakteriální infekce etiologie prevence a kontrola MeSH
- cefotaxim aplikace a dávkování MeSH
- dospělí MeSH
- lidé MeSH
- nemoci plodu etiologie prevence a kontrola MeSH
- novorozenec MeSH
- předčasný odtok plodové vody komplikace MeSH
- těhotenství MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- novorozenec MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- srovnávací studie MeSH
- Názvy látek
- ampicilin MeSH
- cefotaxim MeSH
Introduction of assessment of specific anti-HAV IgM antibodies by the RIA method in 1983 and in 1989 also by the ELISA method made accurate aetiological diagnosis of viral hepatitis A (HA) possible. The authors evaluated the incidence of HA in 1983 to 1990 in the catchment area of the Clinic for Infectious Diseases of the University Hospital and Policlinic in Brno-Bohunice and the Clinic of Infectious Diseases in Children of the Paediatric University Hospital with Policlinic in Brno-Cerná Pole, i.e. in a catchment area with a population of cca 850,000. In 1990 the incidence of HA increased markedly to 126 cases. This increase was due to an epidemic of HA from September to December 1990 when in September 13, in October 45 and in November 17 patients contracted the disease. In December the number of HA declined to 8. Eighteen patients from this epidemic were from the municipal Brno area 3, i.e. the area of Husovice and Zidenice. Mostly patients of gypsy origin with mutual contacts were involved. The majority of cases of HA in this epidemic had a not quite typical course, very frequently the course was protracted.
- MeSH
- dítě MeSH
- dospělí MeSH
- ELISA MeSH
- hepatitida - protilátky analýza MeSH
- hepatitida A - protilátky MeSH
- hepatitida A epidemiologie MeSH
- imunoglobulin M analýza MeSH
- incidence MeSH
- lidé MeSH
- radioimunoanalýza MeSH
- Check Tag
- dítě MeSH
- dospělí MeSH
- lidé MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- Geografické názvy
- Československo epidemiologie MeSH
- Názvy látek
- hepatitida - protilátky MeSH
- hepatitida A - protilátky MeSH
- imunoglobulin M MeSH