Design,synthesis, antimicrobial,and DNA gyrase inhibitory properties of fluoroquinolone–dichloroacetic acid hybrids

A series of new fluoroquinolone conjugates 8a–g and 9a–f were synthesized via benzotriazole‐mediated synthetic approach with good yield and purity. Some of the synthesized analogs exhibited significant antibacterial properties against Escherichia coli and Staphylococcus aureus with potency higher than that of the parent drugs through in vitro standard bioassay procedure (conjugates 8c and 8d reveal antimicrobial properties with potency 1.9, 61.9, 20.7 and 2.4, 37.1, 8.3 folds relative to the parent antibiotic 6 against E. coli, S. aureus, and Enterococcus faecalis, respectively). The observed experimental data were supported by enzymatic DNA gyrase inhibitory property. Developed BMLR‐QSAR model validates the observed experimental data and recognizes the parameters responsible for the enhanced antibacterial properties.     

Expanding the clinical spectrum of STIP1 homology and U-box containing protein 1-associated ataxia

Journal of Neurology - STUB1 has been first associated with autosomal recessive (SCAR16, MIM# 615768) and later with dominant forms of ataxia (SCA48, MIM# 618093). Pathogenic variations in STUB1...     

Diffuse calvarial cavernoma: case report and review of the literature

Introduction

Cavernous hemangiomas of the skull are very infrequent lesions. They arise from intrinsic vasculature of skull bones and manifest at the fourth to fifth decades of life. Calvarial cavernomas are very rare among lesions of the skull. These lesions are usually focal and confined to one calvarial bone.

Discussion

In this report, we are describing a child with diffuse calvarial cavernoma, a very rare lesion with distinctive clinical and radiological manifestations. This is the first case of such morphology described in the literature.     

Judo Practice in Early Age Promotes High Level of Bone Mass Acquisition of Growing Boys' Skeleton

The current study aimed to exhibit effects of judo training for at least 2 yr on bone mass parameters in growing boys. Our population was composed of one hundred and thirty boys in tanner stage 1 and aged 10.52 ± 0.86 yr. Eleven judo players were therefore, excluded from the study because they do not have participate regularly to the judo training sessions during the last 2 yr. The resting sample was divided into two groups: 50 judo players (JU group) and 69 controls (C group). Bone mineral density (BMD), bone mineral content (BMC), and bone area (BA) were evaluated by using dual-photon X-ray absorptiometry on weight-bearing sites: the whole body, lumbar spine (L2-L4), legs, femoral necks and hips and on the non-weight bearing sites: arms and radiuses. Our findings displayed that judo participation was markedly associated with greater values of bone mass parameters in young judo players than control group. Accordingly, the BMD and BA results exhibited significant differences in the whole body, legs, dominant total hip, arms and both whole radiuses in addition to the dominant femoral neck, the non-dominant total hip and except the non-dominant whole radius for the BMC parameter. Additionally, data of the subject within t test has shown significant differences of bone mass parameters only in the non weight-bearing sites in the judo players without any obvious variation in the controls. Differences of BMD observed on the dominant arm and whole radius in addition to the increased BMC values showed in the dominant whole radius compared with their contra-lateral sites in judo players without any marked variation of BA parameters in all sites in both groups. In growing boys, judo practice was obviously associated with osteogenic effects in specific sites.     

Association of the insertion/deletion gene polymorphism of the apolipoprotein B signal peptide with myocardial infarction in Tunisian patients

BACKGROUND: Numerous polymorphisms of the apolipoprotein B (APOB) gene have been described. Particularly, the insertion/deletion (Ins/Del) polymorphism located in the coding part of the signal peptide of apoB, associated with modification of lipid concentrations and the risk of coronary artery disease and/or myocardial infarction (MI), has been reported in the general population. Moreover, conflicting results emerge from the literature and suggest that the effect is context-dependent. In the present study, the first investigation of the Ins/Del polymorphism of the APOB gene in Tunisian patients with MI, we examined a possible association between this polymorphism and MI in a subgroup of the Tunisian population. METHODS: A total of 318 Tunisian patients with MI and 368 healthy controls were included in the study. Genomic DNA was extracted from white blood cells, and the Ins/Del polymorphism was determined by electrophoresis in polyacrylamide gels after PCR amplification. A binary logistic regression analysis was performed to test how the association between MI and Ins/Del polymorphism is independent from confounding factors. RESULTS: A significant difference in genotype distribution and allele frequency was observed between patients and controls. Patients with MI had a frequency of 7.2% for the Del/Del genotype, 39.6% for the Ins/Del genotype, and 53.1% for the Ins/Ins genotype. Controls had a frequency of 3.0% for the Del/Del, 32.1% for the Ins/Del and 64.9% for the Ins/Ins genotype (chi2=12.93, p=0.002). The MI patient group showed a significantly higher frequency of the Del allele compared to controls (27.1% vs. 19.1%; chi2=12.50, p=0.0004). In comparison to the Ins/Ins homozygotes, the odds ratio (95% confidence interval) for MI was 1.51 (1.09-2.07) for Ins/Del heterozygotes and 2.95 (1.40-6.22) for Del/Del homozygotes. In multivariate analysis, age (p=0.001), smoking (p<0.001), hypertension (p=0.001), diabetes mellitus (p<0.001), and dyslipidemia (p=0.01) were independent correlates of the presence of MI, whereas the Ins/Del polymorphism (p=0.330) was not an independent predictor of MI. CONCLUSIONS: The present study shows a significant but not independent association between the Ins/Del polymorphism of the APOB gene and MI in the Tunisian population.     

Study of lipid profile and parieto-temporal lipid peroxidation in AlCl<Subscript>3</Subscript> mediated neurotoxicity. modulatory effect of fenugreek seeds

Background  

Peroxidation of lipid (LPO) membrane and cholesterol metabolism have been involved in the physiopathology of many diseases of aging brain. Therefore, this prospective animal study was carried firstly to find out the correlation between LPO in posterior brain and plasmatic cholesterol along with lipoprotein levels after chronic intoxication by aluminium chloride (AlCl₃). Chronic aluminum-induced neurotoxicity has been in fact related to enhanced brain lipid peroxidation together with hypercholesterolemia and hypertriglyceridemia, despite its controversial etiological role in neurodegenerative diseases. Secondly an evaluation of the effectiveness of fenugreek seeds in alleviating the engendered toxicity through these biochemical parameters was made.     

Effects of diabetes and/or hypercholesterolemia on skin development of rat fetuses

ObjectiveTo investigate the effects of diabetes and/or hypercholesterolemia on skin development during in utero life at 15, 17 &; 19 days old.MethodsSixty pregnant female albino Wistar rats were arranged into three groups: control, diabetic (single i.p. 60 mg streptozotocin/kg B.wt) and hypercholesterolemic (diet supplement 3% cholesterol 6 week prior to conception and throughout gestation). Pregnant rats were sacrificed at 15, 17 &; 19 days prenatal). Vibrissae skin biopsies were removed and allowed for scanning (SEM), light, and transmission electron microscopic (TEM) investigation. Also, DNA fragmentation and sodium dodecyl polyacrylamides gel electrophoresis (SDS-PAGE) were carried out.ResultsScanning electron microscopic observations revealed retarded hair follicle growth and deformations of their pattern structure. At light microscopic level, skin exhibited decreased epidermal cornification, as well as degeneration of hair follicles in fetuses of both diabetic and hypercholesterolemic groups. Transmission electron microscopy revealed abundant vacuolar spaces in the epidermis. Degenerative phases become more abundant in keratinocytes as well as in stratum germinativum cells. Fetal skin possessed altered protein expression and missing bands as well as separation of genomic DNA to several degraded bands in skin of 15-, 17-, and 19-day-old, maternally diabetic and/or hypercholesterolemic fetuses.ConclusionThese findings showed that maternal diabetes and/or hypercholesterolemia increased average deformation of hair follicles, vacuolation, and degeneration of epidermal cell layers. The observed findings resulted from altered protein expression and increased DNA fragmentation, which, in turn, disrupt epidermal cell differentiation.