Preliminary antifungal activity assay of selected chlorine-containing derivatives of xanthone and phenoxyethyl amines.

The aim of this study was to evaluate antifungal activity in a diverse group of chlorine-containing xanthone and phenoxyethyl amine derivatives - and to select the most promising compounds for further studies. The antifungal efficacy of 16 compounds was tested with qualitative and quantitative methods against both reference and clinical strains of dermatophytes, moulds and yeasts. The disc-diffusion method has demonstrated that from 16 tested compounds, 7 possess good antifungal activity against dermatophytes and/or moulds while none of them has shown good efficacy against yeasts or bacterial strains. The most active compounds (2, 4, 10, 11, 12, 15, 16) were tested quantitatively by broth dilution method to obtain MIC values. The MIC values against dermatophytes ranged from 8 to 64 µg/ml. Compound 2 was the most active one against dermatophytes (MIC 50 and MIC 90 were 8 µg/ml). The MIC values for moulds ranged from 16 to 256 µg/ml. Compound 4 was the most active one against moulds, with MIC 50 and MIC 90 values amounting to 32 µg/ml. Among the tested compounds, compound 4 (derivative of xanthone) was the most active one and expressed good antifungal efficacy against clinical strains of dermatophytes and moulds. However, another xanthone derivative (compound 2) was the most active and selective against dermatophytes.

ACTIVITY OF THYME OIL (OLEUM THYMI) AGAINST MULTIDRUG-RESISTANT ACINETOBACTER BAUMANNII AND PSEUDOMONAS AERUGINOSA.

Almost as soon as antibiotics were introduced to treat infectious diseases, it could be observed that bacteria were able to develop resistance against them. Currently, multidrug-resistant strains are being isolated mainly in the hospital environment. These are primarily non-fermenting Gram-negative bacilli, which exhibit both natural and acquired resistance to multiple antibiotics and disinfectants rendering them difficult to eradicate. The development of new, effective and safe substances that prevent troublesome infections is greatly needed to provide alternative therapeutic options for patients. There is increasing interest in drugs of natural origin, including essential oils. It is of particular interest that, although active against many bacterial strains, they do not contribute to antibacterial resistance against their components. The aim of our study was to evaluate the in vino antibacterial activity of thyme oil against multidrug-resistant strains of A. baumannii and P. aeriginosa using the disc diffusion and macrodilution methods. The strains were isolated from patients hospitalized in the years 2013-2014. The in vitto antibacterial activity of thyme oil was assessed by the disc diffusion method and the inhibition zones for the oil at different concentrations, produced against A. baumannii, ranged from 7 to 44 mm. Low level of activity of thyme oil was observed against P. aeruginosa strains. The results of serial dilution tests confirmed the high activity of thyme oil against A. baumannii isolates, expressed as MIC values ranging from 0.25 to 2 µL/mL. These results suggest the need for further studies of antibacterial activity of essential oils, especially against multidrug-resistant bacterial isolates.

Dermatophytes isolated from superficial fungal infections in Krakow, Poland, between 1995 and 2010.

Superficial fungal infections due to dermatophytes are common over the world and their frequency is constantly increasing. The aim of our study was to discuss fungal infections with frequency of occurrence, clinical stages and aetiology in patients admitted to dermatological ward and microbiological laboratory of the specialist hospital in Krakow. Investigations performed between 1995 and 2010 included the group of 5333 individuals. Dermatophyte infections, confirmed by culture, were revealed in 1007 subjects (18.9%), i.e. in 553 males and 454 females. The most frequent clinical forms of infections were tinea unguium and tinea pedis, caused mainly by Trichophyton rubrum and by Trichophyton mentagrophytes. Tinea corporis, tinea manuum, tinea capitis and tinea cruris constituted a small percentage of infections and the main aetiological factors of these dermatomycoses were also T. rubrum and T. mentagrophytes. Between 1995 and 2000 there were stated small differences in the number of isolated strains of dermatophytes in comparison with the number of examined patients. Since 2006 there has been observed a decrease in number of patients in our hospital with suspected fungal infections, but per cent of positive cultures has remained unchanged in comparison with earlier period.

The role of Candida in inflammatory bowel disease. Estimation of transmission of C. albicans fungi in gastrointestinal tract based on genetic affinity between strains.

BACKGROUND: The pathogenesis of inflammatory bowel disease (IBD), is related to the effect of fungal presence in the gastrointestinal tract (GI) on IBD development. MATERIAL/METHODS: One hundred twenty-six patients underwent mycological investigation. We analyzed of the occurrence of fungal infection in the clinical material collected from the GI tract of patients with IBD and control groups. We assessed fungal flora transmission from the oral cavity to further segments of the GI tract based on comparative studies of genotypes of fungal strains. The studies were carried out using conventional methods. The fungal genotypes were determined with the PCR-RAPD method. RESULTS: Of 407 samples, 220 of them had fungi. The most frequently isolated species was C. albicans in patients with IBD and in control group, respectively 84.4% and 81%. Analysis of the streak patterns of the products of the PCR-RAPD reaction carried out for C. albicans strains isolated from the material collected from 10 patients, showed 100% affinity between the strains cultivated from the same patient. Genetic affinity between the strains was confirmed in 3 primers used in the examination. CONCLUSIONS: The presence of fungi in the oral cavity of patients with IBD may affect more frequent colonization of the colonic mucosa in the active phase of disease. Genetic affinity of C. albicans strains indicates the possibility of fungal transmission from the oral cavity to further segments of the GI tract.

Antifungal and antibacterial activity of the newly synthesized 2-xanthone derivatives.

A series of 2-substituted xanthone derivatives 8-20 containing selected allyl, cinnamyl, morpholine, and imidazole moieties were synthesized and tested for their antifungal and antibacterial in-vitro properties. Of the newly synthesized derivatives, ten revealed antifungal activity especially against Trichophyton mentagrophytes (the biggest inhibition zones ranged 35 mm for 11 and 13). 2-(3-(Allylamino)propoxy)-9H-xanthen-9-one hydrochloride 9 inhibited growth of all of the examined fungal species. Significant efficacy against evaluated yeasts and dermatophytes was also observed for 6-chloro-2-methyl-9H-xanthen-9-one derivatives 11-13 containing encyclic amine moieties. Additionally, compounds 9, 11, and 12 hindered development of bacteria species but in a lesser degree. They were efficacious against Staphylococcus aureus, Escherichia coli, and Enterococcus faecalis.

[Studies on the influence of Candida fungal colonization on the healing process of inflammatory lesions in the colon in rat animal model]. / Wplyw kolonizacji grzybów Candida na gojenie zmian zapalnych blony sluzowej jelita grubego w modelu zwierzecym colitis ulcerosa.

Present-day methods of successful treatment of inflammatory bowel diseases (IBD) result from a better understanding of their pathophysiology due to advances in preclinical studies in this area of knowledge. Until recently microbiological studies have been focused on the bacterial aspects in pathogenesis of GI disorders, however in the last years an interest in the presence of fungi in the gastrointestinal tract has also increased. In this study using an animal model of ulcerative colitis, the impact of fungal colonization of the colon on the intensity of inflammatory changes in the colonic mucosa and the course of their healing was carried out. The macroscopic and microscopic criteria relating to the changes of weight of examined fragments of the colon were evaluated while assessing differences between groups tested. The intensity of intestinal inflammatory changes was determined by assessment of such parameters, as colonic blood flow (CBF), the level of MPO as a marker of colonic neutrophil infiltration intensity and the plasma levels of IL-1beta; and TNF-alpha concentrations. Results at the 3rd day after TNBS rectal administration revealed an increase of weight of isolated segments of inflammed colon, a decrease of CBF and the 4-5 fold increase of plasma MPO activity. Candida colonization of colon mucosa of rats delayed healing of colonic ulcers, induced by TNBS and this was associated with the increased expression of plasma IL-1beta and TNF-alpha levels. Administration of antifungal (fluconazole) or probiotic (Lacidofil) treatment to C. albicans infected rats exerted favorable effect on healing of inflammatory changes in the colon because the area of ulcerations in groups of rats treated with fluconazole or Lacidofil was significantly smaller in comparison with those inoculated with Candida solution only. Administration of fluconazole or Lacidofil significantly decreased the weight of colon segments, the MPO activity and the plasma IL-1beta and TNF-alpha levels, as compared with respective values in the group receiving Candida only. The results of our studies indicate the deteriorating influence of Candida on the healing process of inflamed colon in the animal model of ulcerative colitis. Concomitant therapy with probiotic or antifungal treatment improved healing of colonic lesions, decreased the weight of inflamed colonic tissue and also attenuated the MPO activity and plasma proinflammatory cytokines IL-1beta and TNF-alpha levels.

A triterpene saponin from Lysimachia thyrsiflora L.

A triterpene saponoside (LTS-4) isolated from the underground parts of Lysimachia thyrsiflora L. was defined as 3-O-{beta-D-xylopyranosyl-(1 --> 2)-beta-D-glucopyranosyl-(1 --> 4)-[beta-D-glucopyranosyl-(1 --> 2)]-alpha-L-arabinopyranosyl}-cyclamiretin A. Structure assignment was performed on the basis of spectroscopic data including homo- and heteronuclear 1D and 2D NMR (COSY, TOCSY, NOESY, HETCOR, HMBC and DEPT) and FAB-MS studies. The compound was tested in vitro for antimicrobial and cytotoxic activity.

[Candidiasis in the experimental model of ulcerative colitis]. / Kandydiaza w doswiadczalnym modelu zapalenia jelita grubego.

In the present study on animal model of ulcerative colitis the influence of fungal colonization on the severity of inflammatory lesions in the colon and the course of their healing was evaluated. The results of our studies revealed, that significant fungal colonization (over 10(4) CFU/ml) delayed ulcer healing in the colon. It corresponded with the decrease of colonic blood flow (CBF) in the region of lesions and increase of interleukin (IL)-1beta, tumor necrosis factor(TNF)-alpha level in the serum. Introduction of antifungal therapy (fluconazole) or probiotic in rats inoculated with Candida accelerated the process of ulcer healing in the colon, expressed through the reduction of macro- and microscopic lesions in the colon and decrease of MPO, IL-beta TNF-alpha serum level.

Steroidal glycosides from the underground parts of Allium ursinum L. and their cytostatic and antimicrobial activity.

The aim of this study was the isolation and structural elucidation of steroidal glycosides from the underground parts of ramson Allium ursinum L. The structures of the isolated compounds were established based upon chromatographic methods and 1D- and 2D-NMR, MS and IR analyses. The mixture of two steroidal saponins: (25R)-spirost-5-en-3b-ol tetrasaccharide and (25R)-spirost-5, 25(27)-dien-3b-ol tetrasaccharide, along with a 3-hydroxypregna-5,16-dien-20-one glycoside were identified. The results of in vitro cytotoxic activity of the mixture of spirostanol saponins against cell lines melanoma B16 and sarcoma XC and human fibroblasts HSF are also reported. The spirostanol saponins mixture was investigated to determine its in vitro antimicrobal activity against Trichophyton mentagrophytes and Microsporum canis.

[The influence of Candida albicans on the course of ulcerative colitis]. / Wplyw kolonizacji grzybów Candida na przebieg wrzodziejacego zapalenia jelita grubego.

UNLABELLED: The influence of microbiological factor is taken into consideration in the pathogenesis of ulcerative colitis (UC). The aim of studies was to: 1.evaluate the presence of significant fungal colonization, over 10(5) CFU/ml in patients with UC and the control group (irritable colon syndrome, IBS); 2. estimate the influence of antifungal treatment in the activity of UC. MATERIAL AND METHODS: We evaluated 72 patients aged from 18-72 years, 60 patients with UC, 12 with IBS. Clinical investigation: initially and after 4 weeks interview and colonoscopy with colon biopsies for histology and mycology were taken. Activity of UC was evaluated according to: clinical, endoscopic and histological IACH criteria. 13 patients with significant fungal colonization were given antifungal treatment. Biopsies for histology were stained with hematoxylin-epsin (H-E). Qualitative and quantitative mycolo-gical evaluation was performed according to Muller method. RESULTS: 1. Significant fungal colonization was more frequent in patients with UC history over 5 years, in comparison with shorter disease history and IBS, in 33.3%, 13.8% and 1.3% respectively. 2. Candida albicans was most often isolated in 91.7% of cases. 3. Initial analysis of the activity index of UC in patients with significant and non-significant fungal colonization did not revealed differences between these groups, 13.84 and 14.0 respectively. 3. After 4 weeks stronger decrease of the UC activity index was observed in patients with significant fungal colonization treated with antifungal treatment, in comparison with patients not given antifungal therapy: 8.0 and 10.41 respectively, p<0.01. Differences were significant according to clinical 2.23 (C) -3.33 (D), p<0.05 and endoscopic cryteria: 3.46 (C) -4.84 (D), p<0.01. CONCLUSIONS: 1. Significant fungal colonization of colon may influence the activation of UC. 2. Longer disease history may be the risk factor of significant fungal colonization in colon. 3. Antifungal treatment in patients with significant colonization caused clinical improvement of UC.