Synthesis, in vitro biological screening and molecular docking studies of novel camphor-based thiazoles.

Synthesis, characterization and investigation of antibacterial and antifungal activities of twelve camphor based 2,4-disubstituted 1,3-thiazoles is presented. Their structures were determined using NMR, IR, FAB MS and HRMS analyses. Among the derivatives, 3i and 5 were found to exhibit antifungal and antibacterial activities comparable to that of fluconazole and ciprofloxacin against yeast belonging to Candida spp., MIC 0.12-0.98 µg/ml and Gram-positive bacteria including both pathogenic S. aureus and opportunistic S. epidermidis, MIC 0.98-7.81 µg/ml, B. subtilis and B. cereus, MIC 3.91-31.25 µg/ml, and M. luteus, MIC 0.98 µg/ml species, respectively. Molecular docking studies of all compounds into the active sites of microbial enzymes indicated a possible targets SAP and NMT, thiazoles 3a-j, 4, 5 showed more favourable affinity than the native ligand.

[Influence of slime production and adhesion of Candida sp. on biofilm formation]. / Wplyw adhezji i wytwarzania sluzu na zdolnosc tworzenia biofilmu przez Candida sp.

The increase of fungal infections in recent years is connected with the progress in medicine. The vast usage of biomaterials is an inseparable element of contemporary medicine but it also leads to development of infections. Yeast-like fungi Candida albicans are still the main pathogen of candidiasis. The ability to slime production and adhesion to polystyrene of Candida sp. on different surfaces can cause to form biofilm on surfaces of biomaterials used in production of catheters, drains and prosthesis. The aim of the study was to evaluate the influence of slime production and adhesion to polystyrene, of Candida sp. on biofilm formation on different biomaterials. 50 strains of Candida sp. were examined. They isolated from ill to Clinics of Anesthesiology and Intensive Therapy University Hospital No 1 of dr. A. Jurasza in Bydgoszcz. The ability to slime production was evaluated by Christensen method in modification Davenport and Branchini methods. The adhesion to polystyrene was evaluated by Richards et el method. The ability to produce biofilm biomaterials by the studied fungi was measured after 72 hours of incubation at 37 degrees C on different biomaterials. Yeast-like fungi Candida sp. fabricating slime and adhesion forming frequently biofilm on surface researched of biomaterials. Influence of chosen biological specificity ascertain on the ability to produce biofilm on surfaces of siliconized latex and polyvinylchloride.

[Susceptibility to antifungal agents of Candida sp. and biofilm formation]. / Lekowrazliwosc a zdolnosc tworzenia biofilmu przez Candida sp.

In recent years the increase in frequency of fungal infections with Candida sp. was noticed. These infections are connected with ability of Candida sp. to form biofilm on surfaces of biomaterials used in medicine. Furthermore fungal infections make serious therapeutic problems because ofbiofilm resistance to antifungal agents actually. The aim of the study was to evaluate the susceptibility to antifungal agents of Candida sp. and their ability to form biofilm on different biomaterials. 50 strains of Candida sp. isolated from patients of University Hospital No. 1 of dr A. Jurasz in Bydgoszcz were examined. API Candida (bioMérieux) tests were used to identify Candida sp. strains. The susceptibility of the yeast strains to antifungal agents was evaluated by ATB FUNGUS 2 INT (bioMérieux) tests. The susceptibility of examined strains to voriconazole, posaconazole, caspofungin and anidulafungin was assessed by means ofEtests (AB BIODISK) method employing drug concentrations from 0,002 to 32 microg/ml. All analysed strains were susceptible to amphotericin B and caspofungin. Biofilm formation on different biomaterials (silicon, latex, polychloride vinyl, polypropylene, nylon) was measured after 72 hour incubation at 37 degrees C. All examined yeasts formed biofilm on all analysed biomaterials. The highest number of strains formed biofilm on surface of polychloride vinyl: 23 (92,0%) by C. albicans strains and 24 (96,0%) Candida non-albicans strains. The lowest number of the strains formed biofilm on the surface of nylon: 12 (48,0%) of C. albicans strains and 9 (36,0%) of Candida non-albicans strains. The studied strains resistant to azoles and anidulafungin display stronger ability to form biofilm on surfaces of all analysed biomaterials.

[Evaluation of the API ZYM system and RPMI agar plates supplemented with Tween 40 for detection of lipolytic enzymes of Candida spp]. / Ocena przydatnosci testu API ZYM i podloza RPMI wzbogaconego w Tween 40 do wykrywania lipolitycznych enzymów Candida sp.

Lipolytic activity of 40 strains of Candida spp. was tested on API ZYM system and on RPMI agar plates supplemented with 1% Tween 40. Lipolytic activity was indicated by opaque zones around the inoculum cylindrical holes were punched in the medium. Clearing of the medium around the bacterial colonies indicated that an isolate produce lipase. Only 4 (21.1%) strains of C. albicans, and 3 (14.1%) strains of non-C. albicans which hydrolyzed 2-naftylomirystylan by use of the API ZYM system was observed. In contrast, 16 (78.9%) strains of C. albicans and 17 (80.7%) strains of non-C. albicans produced lipases on the agar plate using RPMI agar plates supplemented with 1.0% Tween 40. Determination oflipase activities with the API ZYM system were in no agreement with lipase tests in RPMI supplemented with Tween 40. Our study verify greater usefulness of RPMI supplemented with Tween 40 for detection of lipolytic enzymes of Candida species in comparison to the API ZYM.

[Comparison of three methods detection of slime production by Staphylococcus aureus and Staphylococcus epidermidis]. / Porównanie trzech metod oceny wytwarzania sluzu przez Staphylococcus aureus i Staphylococcus epidermidis.

In this article, slime production of Staphylococcus aureus and Staphylococcus epidermidis strains from infective skin lesions was evaluated by three different methods: Congo red agar method (CRA), Christensen tube method (CT) and spectrophotometric method (SC). All strains by CT method interpreted as negative (dark-claret or red colonies of the surface). 12 (37.5%) strains of S. aureus, 16 (50.0%) strains of S. epidermidis produced slime as shown by CT method, 6 (18.7%) strains of S. aureus, 8 (25,0%) strains of S. epidermidis by SC method. They also found a correlation of slime production by CT and SC method (p > 0.05).

[The species variety and drug susceptibility of fungi isolated from blood samples of patients of the Dr. A. Jurasz university hospital in Bydgoszcz in the years 2005-2008]. / Zróznicowanie gatunkowe i lekowrazliwosc grzybów wyosobnionych z krwi pacjentów szpitala uniwersyteckiego w Bydgoszczy w latach 2005-2008.

The aim of the study was retrospective analysis of the species variety and the drug susceptibility to antifungal drugs of fungal strains isolated form blood samples of patients of the dr. A. Jurasz University Hospital in Bydgoszcz, in the years 2005-2008. A total of 79 strains patients was isolated from 68 during these four years. Above 96% strains belong to Candida spp., while three strains--to Cryptococcus spp. Almost 56% strains were isolated from more than one blood sample. In the first three years of analysis gradual increase of the number of cultured strains was observed, but in 2008 the decrease was noticed. The majority of strains were obtained from patients of the Anesthesiology and Intensive Care Clinic (32,9%) and the Pediatrics, Hematology and Oncology Clinic (24,1%). Every year the same species were the most frequently cultered: C. albicans, C. parapsilosis i C. glabrata. C albicans was found as the dominant species each year. Almost 32% of strains were isolated from blood samples obtained by peripheral insertion of a needle and by catheter as well. C. parapsilosis was the most frequently isolated species from those cases (48,0%). Among non-C. albicans species there were higher percentages of strains resistant to flucytosine, amphotericin B and fluconazole observed.

[The influence of cell surface hydrophobicity Candida sp. on biofilm formation on different biomaterials]. / Wplyw wlasciwosci hydrofobowych Candida sp. na zdolnosc wytwarzania biofilmu na powierzchni wybranych biomaterialów.

The ability of yeasts to form biofilm is believed to play an important role in patomechanism of fungal infection. Candida sp. is considered to form biofilm on surfaces of biomaterials used in production of catheters, drains and prosthesis. Therefore this may lead to serious problems in patients with biomaterials used for diagnostic or therapeutic purposes. The aim of the study was to evaluate the influence of cell surface hydrophobicity (CSH) of Candida sp. on biofilm formation on different biomaterials. CSH was evaluated by two methods: Salt Aggregation Test (SAT) and Microbe Adhesion to Hydrocarbon Test (MATH). Biofilm formation on different biomaterials was measured by Richard's method after 72 hour incubation at 37 degrees C. Candida biofilm formation occurred more frequently in case of strains exhibiting hydrophobic than hydrophilic properties of cell surface. The statistically significant correlation between CSH and ability of biofilm formation on different biomaterials was observed (p < 0.05).

[The evaluation of relationship between the origin of Candida sp. and the ability of biofilm formation on surface of different biomaterials]. / Ocena zaleznosci miedzy pochodzeniem szczepów Candida sp., a ich zdolnoscia wytwarzania biofilmu na powierzchni róznych biomaterialów.

The increase of fungal infections in recent years is connected with the progress in medicine. The vast usage of biomaterials is an inseparable element of contemporary medicine but it also leads to development of infections. The ability to produce biofilm by those yeasts plays an important role in the pathogenesis of candidiasis. Candida biofilm can form on the surface of plastic materials (silicon, polychloride vinyl, polymethacrylate methyl) used to catheters, drains and dentures production that is why it is a serious problem in case of fungal infections in patients who during the diagnosis and treatment have contact with biomaterials. The aim of the study was the assessment of ability to form biofilm on the surface of different biomaterials (latex silicon, polychloride vinyl, polystyrene, nylon and polymethacrylate methyl). 150 strains of Candida sp. were examined: 85 (56.7%) C. albicans and 65 (43.3%) C. non-albicans. The examined yeasts produced biofilm on the surface of polymethacrylate methyl in 39.3%, latex silicone in 38.7%, polychloride vinyl in 38.0%, polystyrene in 35.3% and nylon in 30.7%. Biofilm was most frequently produced by the strains of C. albicans, C. tropicalis, C. glabrata, C. parapsilosis, C. krusei and C. lusitaniae species.

[Hydrophobic properties of Candida sp. comparing the two methods]. / Wlasciwosci hydrofobowe Candida sp.--analiza porównawcza dwóch metod.

Yeast-like fungi Candida albicans are still the main pathogen of candidiasis although in recent years the growth of infections caused by Candida non-albicans species such as C. glabrata, C. parapsilosis, C. tropicalis have been observed. The aim of the study was the assessment ofhydrophobic properties of Candida sp. on the basis of methods: salt aggregation test (SAT) and to p-xylene (MATH). 150 strains of Candida sp. were examined: 85 (56.7%) C. albicans and 65 (43.3%) C. non-albicans among which there were 14 (9.3%) strains of C. tropicalis, 13 (8.7%) of C. glabrata, 12 (8.0%) of C. parapsilosis, 8 (5.3%) strains of C. krusei and C. lusitaniae, 6 (4.0%) strains of C. famata, 2 strains of C. glabrata and 1 strains of C. kefyr and C. lipolytica. The assessment of hydrophobic properties was done in MATH method the higher percentage (38.7-53.3%) of the strains with hydrophobic properties was found in comparison with the method SAT--23.3-37.3%. Hydrophobic properties were more often observed in case of C. non-albicans strains than C. albicans depending on growth temperature.

[Evaluation of Agar Candida ID2 (bioMerieux) a chromogenic medium for yeasts differentiation]. / Ocena przydatnosci chromogennych podlozy Agar Candida ID 2 do identyfikacji grzybów rodzaju Candida.

Invasive diagnostic and therapeutic methods, widespread antibiotic therapy and rising percent of the immunocompromised patients cause incrementation of frequency of occurrence of the yeast infection. C. albicans is the most commonly isolated species of Candida from clinical samples. However, recently growth of frequency of isolation Candida non - albicans from clinical specimens have been observed. Yeast-like fungi different from C. albicans have become serious clinical problem. Conventional methods of identification of the yeast-like fungi carry away a lot time enough. Employment of chromogenic agar shortens latency on result. We decided to examine the usefulness ofAgar Candida ID2 (CAN2) (bioMérieux) in the identification of Candida species. The subjects within the study were 146 of Candida spp strains which were isolated from the clinical specimens of patients hospitalized at the University Hospital in Bydgoszcz. Germ tube test. Api 20C AUX test (bioMérieux) and Agar Candida ID2 (bioMérieux) were used. We have ascertained correspondence of identifying species amounted to 82.2% of analyzed Candida species between API 20C AUX test and kind of growth on CAN2 medium. Divergence of results received between CAN2 medium and API 20C AUX test suggests necessity of conducting of verification data with other methods. In conclusion, our study shows that Agar Candida ID2 is an effective medium for the isolation yeast-like fungi and in preliminary identification of Candida species direct from clinical materials.

[Influence of incubation conditions on cell surface hydrophobicity of Candida species fungi]. / Wplyw warunków hodowli na hydrofobowosc powierzchni komórek grzybów rodzaju Candida.

Cell surface hydrophobicity (CSH) is considered to be one of several virulence factors of Candida yeast-like fungi. The aim of the study was a measurment of hydrophobic properties of Candida sp. depending on growth conditions. A total of 139 strains of Candida (80 - C. albicans and 59 - C. non-albicans) were examined. The method of salt aggregation test (SAT) was used. The strains were cultured on three different media, in two variants of incubation temperature and time. The incubation temperature and microbiological medium affected CSH of just C. albicans strains. The influence of incubation time on CSH of examined species of Candida was not occurred. There was a strong correlation between CSH and species of Candida demonstrated in the study Hydrophobic properties were more frequent and stronger among strains of C. non-albicans than C. albicans species. The results of the study indicates that CSH of Candida spp. is a dynamic feature. The ability to change surface properties may play a role in pathogenesis of candidosis.

[Comparison of the antibiotic sensitivity of lipophilic Corynebacterium sp. isolated from patients on the day of admission and during hospitalization]. / Porównanie wrazliwosci na antybiotyki lipofilnych gatunków Corynebacterium sp. izolowanych od chorych w dniu przyjecia do szpitala i podczas hospitalizacji.

Lipophilic species of Corynebacterium are increasing problem in hospital infections. The aim of this study was to evaluate occurrence of these microorganisms in the materials taken from patients in the day of admission and during the hospitalization as well as comparison of their antibiotic sensitivity. The investigation included 65 strains isolated from hospitalized patients and 48 strains isolated from unchanged skin. Using Api Coryne test 5 species were identified. C. urealyticum dominated, the other were C. subsp. lipophilum and C. jeikeium. Among strains isolated from unchanged diseased skin the most C. jeikeium and C. accolens occurred. All strains were sensitive to glycopeptide, quinupristin/dalphopristin. The strains isolated from hospitalized patients were usually sensitive to fuside acid, doxycycline as well as tetracycline. Strains isolated from unchanged skin were sensitive to almost all tested antibiotics. In the group of 65 strains isolated from hospitalized patients 99.0% were multiresistant. In the group of strains isolated from unchanged skin only two strains were multiresistant. Differences in antibiotic sensitivity among analysed Corynebacterium sp. were confirmed. Majority of the "hospital strains" were characterized by multiresistance. Basing on these results it is possible to suppose, that multiresistance is main factor that favours lipophilic Corynebacterium species in the process of colonization of mucous membranes, skins as well as developing infections.