Nontoxic combretafuranone analogues with high in vitro antibacterial activity.

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.

Radio-telemetry shows differences in the behaviour of wild and hatchery-reared European grayling Thymallus thymallus in response to environmental variables.

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.

Diel dualism in the energy consumption of the European catfish Silurus glanis.

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.

Post-release growth and dispersal of pond and hatchery-reared European grayling Thymallus thymallus compared with their wild conspecifics in a small stream.

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.

Factors influencing movement behaviour and home range size in ide Leuciscus idus.

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.

[Gestational diabetes mellitus and disorders of glucose tolerance in pregnant women with essential hypertension]. / Gestacní diabetes mellitus a porucha tolerance glukózy u tehotných trpících esenciální hypertenzí.

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.

[The effect of self-monitoring on perinatal outcome in insulin therapy of diabetic women during pregnancy]. / Vliv selfmonitoringu na perinatální výsledky u inzulínem lécených diabeticek v tehotenství.

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.

[Prenatal preparation--a part of the care of young female diabetic patients]. / Prekoncepcní príprava--soucást péce o mladou diabeticku.

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.

[Prophylactic administration of Claforan in patients with premature loss of amniotic fluid]. / Profylaktická aplikace Claforanu u pacientek s predcasným odtokem plodové vody.

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.

[Viral hepatitis A in the catchment area of the Brno University Hospital 1983-1990]. / Virová hepatitis A ve spádové oblasti Fakultní nemocnice Brno v letech 1983-1990.

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.

[Delivery of neonates with a birth weight of less than 1500 grams. Perinatal results during a 6-year period and possibilities of affecting them]. / Porod novorozence s porodní hmotností pod 1500 gramu. Nase perinatální výsledky za sestileté období a moznosti jejich ovlivnení.

The authors evaluated the perinatal mortality and condition on delivery of 167 neonates with a birth weight under 1500 g who were delivered and hospitalized at the 2nd Department of Gynecology and Obstetrics in Brno between Jan. 1, 1985 and Dec. 31, 1990. The perinatal mortality of neonates with a birth weight below 1000 g was 73.1%, of those with a birth weight 1000 g-1500 g it was 25.9%. Early neonatal mortality was not influenced by the patient's age exceeding 30 years, occupation, environment, status, number of interrupted pregnancies, spontaneous abortions and previous spontaneous and induced deliveries, administration of tocolysis, corticoids, the position of the foetus, transport in utero, way of delivery, indication for Caesarean section and sex. Early neonatal mortality was influenced by the mother's age less than 20 years, administration of antibiotics, multiple pregnancy, grade of asphyxia, presence of RDS, necessity of respiratory support, incidence of intracerebral haemorrhage and birth trauma. In the discussion the authors mention possible ways of reducing the perinatal morbidity and early neonatal morbidity in the mentioned range of birth weights.

[Serologic diagnosis of infectious mononucleosis in children]. / Sérologická diagnostika infekcní mononukleózy u detí.

In 116 children admitted to hospital with tonsillitis of varying types and suspected infectious mononucleosis resp., antibodies, of the IgM class against the EB virus VCA were detected in 27%, a quadruple increase of IgG antibodies in 20% and a negative finding of IgG antibodies also in a second serum sample in 24%. In another group of 51 children admitted with suspected infectious mononucleosis IgM antibodies were found in 47%, a fourfold increase of IgG in 53% and a negative finding of IgG in 10%. In sub-groups of 25 and 30 children resp. from the above groups it was possible to compare the results of specific serology of the EB virus with tests for heterophil antibodies in two serum samples. IgM antibodies were detected in 40% and 50% of children resp., a fourfold rise of IgG in 20% and 67% of children resp., the absence of IgG in 20% and 7% of children resp. Paul-Bunnell reaction was positive in 64% and 60% resp., the OCH-test in 60% and 70% resp., Tomcsik reaction in 16% in the first sub-group and the IM-test in 60% in the second sub-group. In younger children (1-5 years) positive Paul-Bunnell and Tomcsik reactions were less frequent. The IM-test was not positive in any of the children in this age group. An EB-virus aetiology was proved in all types of tonsillitis, least frequently in angina streptococcia (11%), most frequently in angina pseudomembranosa (46%) and mononucleosis infectiosa susp. (54%).

[Clinical problems in non-A, non-B viral hepatitis. I. Diagnosis of non-A, non-B viral hepatitis and its role in the occurrence of acute viral hepatitis in the Czechoslovak population]. / Klinická problematika virových hepatitid non-A, non-B. I. Diagnostika virové hepatitidy non-A, non-B a její podíl na výskytu akutních virových hepatitid v nasí populaci.

Using RIA and ELISA methods the authors examined HBsAg, anti-HBc IgM and anti-HAV IgM antibodies in 830 adult patients and 101 children with acute viral hepatitis from the catchment area of the South Moravian region. In these groups also the most frequent hepatotropic infectious agent as the possible cause of hepatitis was examined. It was revealed that in adults viral hepatitis A accounted for 22%, viral hepatitis B for 48.5%, viral hepatitis non-A, non-B for 28.8% of the group. The percentage distribution of viral hepatitis in children is different: hepatitis A predominates (65%), hepatitis B is less frequent (22%) and viral hepatitis non-A, non-B is least frequent (13%). It was demonstrated that viral hepatitis non-A, non-B is under our conditions a very frequent disease, it accounts for one quarter of all cases of viral hepatitis and if we take into account that non-A, non-B hepatitis has frequently permanent serious sequelae, then proper attention must be paid to this disease. The authors demonstrate that differentiation of types of viral hepatitis by routine methods is possible which leads to a substantially more accurate differentiation of hepatitis.