Ultrasonic synthesis, characterization of ß-aminoketones by bismuth(III) triflate and determination of antigenotoxic properties.

Direct-type catalytic Mannich reaction for the synthesis of ß-aminoketones from cyclohexanone, substituted aromatic amines and aromatic or hetero-aromatic aldehydes has been applied in water with bismuth triflate under ultrasound. Good yields of the expected ß-aminoketones were obtained from available substrates, at room temperature in 1-2 hours. This study was designed to evaluate the mutagenic and antimutagenic potential of synthesized ß-aminoketones compounds using Ames/Salmonella and Escherichia coli WP2 bacterial reverse mutation assay systems.

One-pot synthesis of indenonaphthopyrans catalyzed by copper(II) triflate: a comparative study of reflux and ultrasound methods.

An effective and environment-friendly protocol for the synthesis of indenonaphthopyrans has been developed by one-pot reaction of 2-naphthol, various aromatic aldehydes and 1,3-indandione, in the presence of copper(II) triflate as the catalyst while using reflux (Method A) and ultrasound (Method B). The Method B approach offers the advantages of a simple reaction method, short reaction time, excellent yield, and showcases the economic importance of the catalysts for such processes.

Tumor-associated tissue eosinophilia as a prognostic factor in squamous cell carcinoma of the larynx.

Inflammatory infiltration with eosinophilia in or around the tumoral tissue varies among the cases with invasive squamous cell carcinoma of the larynx. The aim of this study was to investigate the possible role of the tumor-associated tissue eosinophilia (TATE) as a predictive factor for the metastatic status in laryngeal squamous cell carcinoma in patients who had neck dissections. One hundred consecutive specimens from the patients who had been treated surgically for invasive squamous cell carcinoma of the larynx were re-evaluated in terms of TATE. Based on the eosinophil counts per 10 high power field (HPF), the cases were grouped into three different categories (I, II, III) according to three different cut off values (A, B, C). The number of eosinophil cells per 10 HPF for the groups were defined as: IA: 0-10; IB: 11-29; IC: 30 and greater; IIA: 0-20; IIB: 21-39; IIC: 40 and greater; IIIA: 0-30; IIIB: 31-49; IIIC: 50 and greater. Statistical significance between tissue eosinophil counts of the metastatic and non-metastatic lymph node groups were evaluated. This study comprised 97 male and three female patients with squamous cell carcinoma of the larynx (mean age 59.9). Forty-five were well differentiated, 50 were moderately differentiated and five were poorly differentiated invasive squamous cell carcinoma. At least one lymph node metastasis was observed in 34 cases. Eosinophil counts varied between 1 and 138 per 10 HPF in the tumor and/or peritumoral areas. In the three distinct categories with three different cut off values of eosinophil cell counts among nonmetastatic cases and cases with lymph node metastasis, correlation of eosinophil counts with lymph node metastasis were statistically insignificant (Crosstabs, χ(2)). Although in the series, numerical values of the TATE seem to be increased in patients with laryngeal squamous cell carcinoma with lymph node metastasis, this fact has not been confirmed with statistical analysis.

Inhibition of the mutagenic effects of N-methyl-N'-nitro-N-nitrosoguanidine and 9-aminoacridine by indenopyridines in the Salmonella typhimurium tester strain 1537 and E. coli.

The goal of the present research was to determine the protective potential of five newly synthesized indenopyridine derivatives against N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) and 9-aminoacridine (9-AA) induced mutagenesis. MNNG sensitive Escherichia coli WP2uvrA and 9-AA sensitive Salmonella typhimurium TA1537 were chosen as the bacterial tester strains. All of the test compounds showed significant antimutagenic activity at various tested concentrations. The inhibition rates ranged from 25.6% (Compound 2 - 1 mM/plate) to 68.2% (Compound 1 - 2.5 mM/plate) for MNNG and from 25.7% (Compound 4 - 1 mM/plate) to 76.1% (Compound 3 - 2.5 mM/plate) for 9-AA genotoxicity. Moreover, the mutagenicity of the test compounds was investigated by using the same strains. None of the test compounds has mutagenic properties on the bacterial strains at the highest concentration of 2.5 mM. Thus, the findings of the present study give valuable clues to develop new strategies for chemical prevention from MNNG and 9-AA genotoxicity by using synthetic indenopyridine derivatives.

Genotoxic and antigenotoxic assessment of four newly synthesized dihydropyridine derivatives.

The current study aims to determine the genotoxic and antigenotoxic potential of four newly synthesized dihydropyridine derivatives using Escherichia coli WP2 and Ames/Salmonella bacterial reversion assay systems. The bacterial mutant tester strains, E. coli WP2uvrA with a point mutation and Salmonella typhimurium TA1537 with a frameshift mutation, were used to determine genotoxic potentials of the test compounds. To determine antigenotoxic potentials of the test compounds, the same strains were also used together with positive mutagens N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) for E. coli WP2uvrA and 9-aminoacridine (9-AA) for S. typhimurium TA1537. According to the results, neither of the test compounds showed significant genotoxic activity on both tester strains at the tested concentrations. However, except compound 4, all the test compounds showed significant antigenotoxic activity on MNNG- or/and 9-AA-induced mutations. The inhibition rates of mutagenesis ranged from 27.0% (compound 2: 2.5 mM/plate) to 65.0% (compound 2: 0.5 mM/plate) for MNNG and from 30.6% (compound 2: 2 mM/plate) to 58.5% (compound 1: 1 mM/plate) for 9-AA genotoxicity. According to these results, it is concluded that all the test compounds do not have a mutagenic potential on the bacterial strains at the tested concentrations, and some of them have antigenotoxic potentials against MNNG- and 9-AA-induced mutagenesis.

Antigenotoxic properties of two newly synthesized ß-aminoketones against N-methyl-N'-nitro-N-nitrosoguanidine and 9-aminoacridine-induced mutagenesis.

The aim of this study was to determine the antigenotoxic potential of two newly synthesized ß-aminoketones against N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) and 9-aminoacridine (9-AA)-induced mutagenesis. The mutant bacterial tester strains were MNNG-sensitive Escherichia coli WP2 uvrA and 9-AA-sensitive Salmonella typhimurium TA1537. Both test compounds showed significant antimutagenic activity at various tested concentrations. The inhibition rates ranged from 29.5% (compound 1: 2 mM/plate) to 47.5% (compound 2: 1.5 mM/plate) for MNNG and from 25.0% (compound 2: 1 mM/plate) to 52.1% (compound 2: 2.5 mM/plate) for 9-AA genotoxicity. Moreover, the mutagenicity of the test compounds was investigated by using the same strains. Neither test compound has mutagenic properties on the bacterial strains at the tested concentrations. Thus, the findings of the present study give valuable information about chemical prevention from MNNG and 9-AA genotoxicity by using synthetic ß-aminoketones.

Protective properties of five newly synthesized cyclic compounds against sodium azide and N-methyl-N'-nitro-N-nitrosoguanidine genotoxicity.

The current study aims to determine the antimutagenic potential of five newly synthesized cyclic compounds against the genotoxic agents sodium azide (NaN3) and N-methyl-N'-nitro-N-nitrosoguanidine (MNNG). The mutant bacterial tester strains were NaN3-sensitive Salmonella typhimurium TA1535 and MNNG-sensitive Escherichia coli WP2uvrA. According to the results, all the test compounds showed significant antimutagenic activity. The inhibition rates ranged from 26.05% (Compound 4-1 µg/plate) to 68.54% (Compound 5-0.01 µg/plate) for NaN3 and from 32.44% (Compound 3-1 µg/plate) to 60.77% (Compound 5-1 µg/plate) for MNNG genotoxicity. Moreover, the mutagenic potential of the test compounds was investigated using the same strains. The results showed that all the test compounds do not have mutagenic potential on the bacterial strains at the tested concentrations. Thus, the findings of the present study give valuable information about chemical prevention from NaN3 and MNNG genotoxicity.

Serum matrix metalloproteinases and tympanosclerosis.

AIM: To investigate levels of matrix metalloproteinases 2 and 9, and of their tissue inhibitor (i.e. tissue inhibitor matrix metalloproteinase 1), in the serum of patients with tympanosclerosis. MATERIALS AND METHOD: We included 40 patients (age range 13-63 years) who had undergone surgery in the ENT department of Izmir Atatürk Training and Research Hospital between 2002 and 2007. Twenty had uncomplicated chronic otitis media and 20 had tympanosclerosis. We also included as the control group 20 individuals with no history of previous otic complaints or systemic or infectious disease. Serum levels of serum matrix metalloproteinases 2 and 9 and of tissue inhibitor matrix metalloproteinase 1 were measured in all subjects and compared. RESULT: Significantly higher levels of serum matrix metalloproteinases 2 and 9 were found in the tympanosclerosis group, compared with the chronic otitis media and control groups. There was no statistically significant difference in tissue inhibitor matrix metalloproteinase 1 level between the three groups. CONCLUSION: Tympanosclerosis surgery has poor success rates, since the pathological process is still active. We suggest that high levels of matrix metalloproteinases may play a role in the continuation of the disease process.

Targetoid haemosiderotic haemangioma: dermoscopic monitoring of three cases and review of the literature.

Targetoid haemosiderotic haemangioma represents a new, rarely reported, distinctive, benign vascular tumour, characterized histopathologically by a biphasic growth pattern of dilated vascular structures in the superficial dermis lined by prominent hobnail endothelial cells and collagen dissecting, rather narrow neoplastic vessels in deeper parts of the lesion. In the initial stage, the lesion is seen as a small purple or violaceous papule, 2--3 mm in diameter. Over time, the ecchymotic ring expands peripherally until it disappears spontaneously. In the later stages, however, the central papule remains as a slightly raised dermal lesion with a purple to brownish discolouration. We report three cases whose repetitive cyclic morphological changes of targetoid haemosiderotic haemangiomas were monitored dermoscopically at 3-month follow-ups. Histopathological examination of each lesion identified the features of targetoid haemosiderotic haemangioma. To the best of our knowledge, our three cases are the first reported in the literature of targetoid haemosiderotic haemangiomas that were regularly monitored by dermoscopic examinations, enabling development of the different stages of the same lesion to be followed.

Ectodermal dysplasia showing clinical overlap between AEC, Rapp-Hodgkin and CHAND syndromes.

The ectodermal dysplasias represent a complex collection of congenital abnormalities of skin, hair, teeth, nail, and sweat gland development, many of which have overlapping clinical features. In this report, we describe a 7-year-old girl, born to clinically normal parents, with ankyloblepharon, cleft lip/palate and hair abnormalities, features resembling the autosomal dominant disorder, ankyloblepharon-ectodermal dysplasia-clefting (AEC) syndrome, which results from mutations in the sterile-alpha motif domain of the gene encoding the transcription factor, p63. However, direct sequencing of the p63 gene in this individual did not reveal any pathogenic sequence variants. Moreover, two of her paternal cousins were discovered to have similar congenital ectodermal anomalies, raising the alternative possibility of an autosomal recessive pattern of inheritance. Furthermore, all affected individuals lacked a history of erosive scalp dermatitis that is usually characteristic of AEC syndrome. Instead, the scalp hair was coarse and wiry. In addition, another atypical feature, hypohidrosis, was present. Collectively, the clinical features also resembled Rapp-Hodgkin syndrome, Bowen-Armstrong syndrome and CHAND syndrome, but did not appear to fit neatly with any one particular disorder. This case highlights the difficulties in trying to classify the ectodermal dysplasia syndromes on clinical features alone.

Malignant eccrine poroma in an unusual location.

Malignant eccrine poroma is a rare skin appendage tumour, originating from the intraepidermal and upper dermal eccrine ducts. The tumour either arises spontaneously or develops in a long-standing eccrine poroma, generally in elderly people over 60. Clinically, it tends to be a localized lesion, which manifests itself as a nodule or ulcerated tumour, favouring extremities. We report an 83-year-old female with an enlarging and bleeding tumour on her lumbosacral region. This lesion first appeared as a small pigmented papule and progressed to an erythematous patch with central papular portion and some peripheral pigmentation. Histopathology revealed malignant eccrine poroma. Also, immunohistochemically, diffuse and intense p53 staining was observed. Regular pigment pattern, brown globules and black dots were seen in dermoscopic examination. After performing a wide excision, 20 months of follow-up revealed no recurrence or metastasis of the tumour. This case represents an unusually located malignant eccrine poroma with some pigmentation.