Synthesis of Hydroxybenzofuranyl-pyrazolyl and Hydroxyphenyl-pyrazolyl Chalcones and Their Corresponding Pyrazoline Derivatives as COX Inhibitors, Anti-inflammatory and Gastroprotective Agents.

Five new series of hydroxybenzofuranyl-pyrazolyl chalcones 3a,b, hydroxyphenyl-pyrazolyl chalcones 6a-c and their corresponding pyrazolylpyrazolines 4a, d, 7a-c and 8a-f have been synthesized and evaluated for their in vitro cyclooxygenase (COX)-1 and COX-2 inhibitory activity. All the synthesized compounds exhibited dual COX-1 and COX-2 inhibitory activity with obvious selectivity against COX-2. The pyrazolylpyrazolines 4a-d and 8a-f bearing two vicinal aryl moieties in the pyrazoline nucleus showed more selectivity towards COX-2. Within these two series, derivatives 4c, d and 8d-f bearing the benzenesulfonamide group were the most selective. Compounds 4a-d and 8a-f were further subjected to in vivo anti-inflammatory screening, ulcerogenic liability and showed good anti-inflammatory activity with no ulcerogenic effect. In addition compounds 4c and 8d as examples showed prostaglandin (PG)E2 inhibition % 44.23 and 51.4 respectively, tumor necrosis factor α (TNFα) inhibition % 33.48 and 41.41 respectively and gastroprotective effect in ethanol induced rodent gastric ulcer model. In addition, to explore the binding mode and selectivity of our compounds, 8d and celecoxib were docked into the active site of COX-1 and COX-2. It was found that compound 8d exhibited a binding pattern and interactions similar to that of celecoxib with COX-2 active site, while bitter manner of interaction than celecoxib to COX-1 active site.

Numerical analysis of three-dimensional echo decorrelation imaging.

A numerical model for three-dimensional echo decorrelation imaging, a pulse-echo ultrasound method applicable to thermal ablation monitoring, is presented. Beam patterns for steered transmit and receive array apertures are combined with a three-dimensional numerical tissue model to yield beamformed scan lines in a pyramidal configuration, volumetric B-mode images, and spatial maps of normalized decorrelation between sequential image volumes. Simulated three-dimensional echo decorrelation images of random media are analyzed as estimators of local tissue reflectivity decoherence, mimicking thermal ablation effects. The estimation error is analyzed as a function of correlation window size, scan line density, and ensemble averaging of decorrelation maps.

Radiofrequency ablation for liver: Comparison between expert eye and hyperspectral imaging assessment.

Liver/hepatic cancer (HC) is a disease that roughly afflicts 10% of cancer patients worldwide. HC is in charge of the death of 0.8 million patients on the earth. Multiple approaches, including thermal ablation, target the treatment of HC. In this study, we investigated radiofrequency (RF) ablation. Expert clinicians' visual assessment (VA) dominantly evaluated the outcome of ablation. Inattentively, the disfavors of VA are being subjective and eye-acuity dependent. In support, we propose hyperspectral imaging (HSI) for objective assessment of liver ablation. To verify our proposal, we computed the ablated liver area using VA and HSI. Unfortunately, HSI is a time-intensive technique. To make it less intensive, we present a way of reducing data analysis time. Saving time permits medical decisions, likewise continue or stop RF ablation, to be taken safer and faster. The way to reduce the time for HSI data analysis depends on narrowing the spectral bands of interest to only the most relevant ones to liver chromophores. Liver chromophores change in concentration because of thermal ablation. VA hardly senses these changes, however, HSI does it. Ultimately, the spectral band centered at 630 nm is optimal for objectively support RF ablation decision-makers.

Non-ulcerogenic pyrazolyl 2-hydroxychalcones and pyrazolylpyrazolines derived from naturally existing furochromone (khellin): semi-synthesis, docking study and anti-inflammatory activity.

Novel pyrazolyl 2-hydroxychalcone derivatives 3a-e and pyrazolylpyrazoline derivatives 4a-e and 5a-j derived from the naturally existing furochromone (Khellin) were synthesized and evaluated for their in vivo anti-inflammatory activity. Most of the synthesized compounds showed better or comparable activity to that of Diclofenac as reference drug. Twelve compounds were evaluated for their ulcerogenic potential and exhibited no ulcerogenic effect. In addition compounds 3c, 5c and 5h as examples showed PGE2 inhibition % 88.86, 65.87 and 44.06, respectively and TNFα inhibition % 48.62, 31.11 and 16.02, respectively in rat serum samples. Compounds 3c, 5c, 5h and Celecoxib were subjected to in vitro COX-1 and COX-2 inhibition assay, showed selectivity index 45.04, 102.04, 131.58 and 185.18, respectively. The computational finding supported those of in vitro, where the pyrazolylpyrazolines interacted with the COX-2 enzyme in a similar orientation to that of Celecoxib, while chlacones were found to exhibit similar orientation to that of Diclofenac.

Efficient anomaly detection from medical signals and images with convolutional neural networks for Internet of medical things (IoMT) systems.

Deep learning is one of the most promising machine learning techniques that revolutionalized the artificial intelligence field. The known traditional and convolutional neural networks (CNNs) have been utilized in medical pattern recognition applications that depend on deep learning concepts. This is attributed to the importance of anomaly detection (AD) in automatic diagnosis systems. In this paper, the AD is performed on medical electroencephalography (EEG) signal spectrograms and medical corneal images for Internet of medical things (IoMT) systems. Deep learning based on the CNN models is employed for this task with training and testing phases. Each input image passes through a series of convolution layers with different kernel filters. For the classification task, pooling and fully-connected layers are utilized. Computer simulation experiments reveal the success and superiority of the proposed models for automated medical diagnosis in IoMT systems.

High Precision Monitoring of Radiofrequency Ablation for Liver Using Hyperspectral Imaging.

Minimally invasive procedures are achieving better satisfaction for treating liver cancers. Energy-based techniques were studied as prospective alternatives to the gold standard of liver transplantation. Among these techniques, radiofrequency (RF) was investigated for the selective ablation of liver tissue. In addition to optimizing the RF settings for the purpose of overcoming tissue perforation or inadequate ablation, an instrument collecting quantitative data regarding the intraoperative tissue status can aid the treatment procedure. This study demonstrates an innovative noninvasive technique using hyperspectral imaging (HSI) for monitoring RF ablative therapy in ex-vivo liver tissue. The cubic data generated by HSI provides spectral as well as spatial properties of the liver tissue included in each pixel of the field of view. In our study, the applied statistical analysis saves the computational burdens of multivariate analysis techniques. For this purpose, spectral angle mapper, logistic regression algorithm, and principal component analysis were applied. Of all spectral bands captured by the HSI camera, bands centered at 760 and 960 nm were identified for predicting the ablated area. Based on statistical analysis, the threshold for predicting the ablated area of the liver samples was determined, provided that the specificity is kept at 90%.

The Impact of Illegal Waste Sites on the Transmission of Zoonotic Cutaneous Leishmaniasis in Central Tunisia.

Illegal waste disposal represents a risk health factor for vector-borne diseases by providing shelter for rodents and their ectoparasites. The presence of the Phlebotomus papatasi vector of Leishmania major, an etiologic agent of zoonotic cutaneous leishmaniasis (ZCL), was assessed at illegal waste sites located at the vicinity of villages in endemic areas of Central Tunisia. The study was performed over a two-year period over three nights from July to September 2017, and over three nights in September 2018. Household waste is deposited illegally forming dumpsites at the vicinity of each village and contains several rodent burrows of Psammomys obesus, the main reservoir host of L. major. Sandflies were collected from rodent burrows in the natural environment and in dumpsites using sticky traps and were identified at species level. Female sandflies were tested for the presence of L. major by PCR. Our entomological survey showed that Phlebotomus papatasi is the most abundant sandfly species associated with rodent burrows in these waste sites. The densities of P. papatasi in dumpsites are significantly higher compared to the natural environment. The minimum infection rate of P. papatasi with L. major in these illegal waste sites is not significantly different compared to the natural environment. Considering the short flight range of P. papatasi, increases in its densities, associated with burrows of P. obesus in illegal waste sites located at the edge of villages, expands the overlap of infected ZCL vectors with communities. Thus, illegal waste sites pose a high risk of spreading ZCL to neighboring home ranges. Waste management is an environmentally friendly method of controlling sandfly populations and should be included in an integrated management program for controlling ZCL in endemic countries.

In vivo ultrasound thermal ablation control using echo decorrelation imaging in rabbit liver and VX2 tumor.

The utility of echo decorrelation imaging feedback for real-time control of in vivo ultrasound thermal ablation was assessed in rabbit liver with VX2 tumor. High-intensity focused ultrasound (HIFU) and unfocused (bulk) ablation were performed using 5 MHz linear image-ablate arrays. Treatments comprised up to nine lower-power sonications, followed by up to nine higher-power sonications, ceasing when the average cumulative echo decorrelation within a control region of interest exceeded a predefined threshold (- 2.3, log10-scaled echo decorrelation per millisecond, corresponding to 90% specificity for tumor ablation prediction in previous in vivo experiments). This threshold was exceeded in all cases for both HIFU (N = 12) and bulk (N = 8) ablation. Controlled HIFU trials achieved a significantly higher average ablation rate compared to comparable ablation trials without image-based control, reported previously. Both controlled HIFU and bulk ablation trials required significantly less treatment time than these previous uncontrolled trials. Prediction of local liver and VX2 tumor ablation using echo decorrelation was tested using receiver operator characteristic curve analysis, showing prediction capability statistically equivalent to uncontrolled trials. Compared to uncontrolled trials, controlled trials resulted in smaller thermal ablation regions and higher contrast between echo decorrelation in treated vs. untreated regions. These results indicate that control using echo decorrelation imaging may reduce treatment duration and increase treatment reliability for in vivo thermal ablation.

Optimized Echo Decorrelation Imaging Feedback for Bulk Ultrasound Ablation Control.

Feasibility of controlling bulk ultrasound (US) thermal ablation using echo decorrelation imaging was investigated in ex vivo bovine liver. The first of two ablation and control procedures used a sequence of constant-intensity sonication cycles, ceased when the minimum echo decorrelation within a control region of interest (ROI) exceeded a predetermined threshold. The second procedure used a variable-intensity sonication sequence, with spatially averaged decorrelation as the stopping criterion. US exposures and echo decorrelation imaging were performed by a linear image-ablate array. Based on preliminary experiments, control ROIs and thresholds for the minimum-decorrelation and average-decorrelation criteria were specified. Controlled trials for the minimum-decorrelation and average-decorrelation criteria were compared with uncontrolled trials employing 9 or 18 cycles of matching sonication sequences. Lesion dimensions, treatment times, ablation rates, and areas under receiver operating characteristic curves were statistically compared. Successfully controlled trials using both criteria required significantly shorter treatment times than corresponding 18-cycle treatments, with better ablation prediction performance than uncontrolled 9-cycle and 18-cycle treatments. Either control approach resulted in greater ablation rate than corresponding 9-cycle or 18-cycle uncontrolled approaches. A post hoc analysis studied the effect of exchanging control criteria between the two series of controlled experiments. For either group, the average time needed to exceed the alternative decorrelation threshold approximately matched the average duration of successfully controlled experimental trials. These results indicate that either approach, using minimum-decorrelation or average-decorrelation criteria, is feasible for control of bulk US ablation. In addition, use of a variable-intensity sonication sequence for bulk US thermal ablation can result in larger ablated regions compared to constant-intensity sonication sequences.

Real-Time Spatiotemporal Control of High-Intensity Focused Ultrasound Thermal Ablation Using Echo Decorrelation Imaging in ex Vivo Bovine Liver.

The ability to control high-intensity focused ultrasound (HIFU) thermal ablation using echo decorrelation imaging feedback was evaluated in ex vivo bovine liver. Sonications were automatically ceased when the minimum cumulative echo decorrelation within the region of interest exceeded an ablation control threshold, determined from preliminary experiments as -2.7 (log-scaled decorrelation per millisecond), corresponding to 90% specificity for local ablation prediction. Controlled HIFU thermal ablation experiments were compared with uncontrolled experiments employing two, five or nine sonication cycles. Means and standard errors of the lesion width, area and depth, as well as receiver operating characteristic curves testing ablation prediction performance, were computed for each group. Controlled trials exhibited significantly smaller average lesion area, width and treatment time than five-cycle or nine-cycle uncontrolled trials and also had significantly greater prediction capability than two-cycle uncontrolled trials. These results suggest echo decorrelation imaging is an effective approach to real-time HIFU ablation control.

Lures for red palm weevil trapping systems: aggregation pheromone and synthetic kairomone.

BACKGROUND: The optimisation of the lure is essential for the implementation of trapping systems to control insect pests. In this work, the response of the red palm weevil (RPW), Rhynchophorus ferrugineus Olivier, to increasing emission rates of its aggregation pheromone (ferrugineol) and the efficacy of a convenient synthetic kairomone based on fermentation odours (ethyl acetate and ethanol) have been evaluated in different years and locations along the Mediterranean basin. RESULTS: In general, although capture data and emission had noticeable variability among locations, significantly fewer RPW were captured in pyramidal Picusan® traps with the lowest ferrugineol emission rates tested (0.6-3.8 mg day-1 ). Captures increased rapidly with ferrugineol emission up to 4-5 mg day-1 ; then, higher emission rates did not improve or reduce captures, up to the highest emission rate tested of 50.9 mg day-1 . Thus, there is no evidence of an optimum release rate corresponding to a maximum of RPW catches. Traps baited with the synthetic kairomone (1:3 ethyl acetate/ethanol) captured 1.4-2.2 times more total weevils than traps baited only with ferrugineol. Moreover, in most of the locations, the synthetic blend was at least as effective as the local coattractants used (plant material + molasses). CONCLUSIONS: Ferrugineol emission rate can vary in a wide range without significantly affecting RPW response. Coattractants based on fermenting compounds, ethyl acetate and ethanol, are able to improve the attractant level of ferrugineol and could be employed to replace non-standardised natural kairomones in RPW trapping systems after further optimisation of their proportions and doses. © 2016 Society of Chemical Industry.

Community-based epidemiological study of epilepsy in the Qena governorate in Upper Egypt, a door-to-door survey.

BACKGROUND: The aim of this study is to estimate the epidemiological features of epilepsy in a representative governorate of Upper Egypt. MATERIALS AND METHODS: A door-to-door community-based survey study was performed using a sample of 10 areas among various districts of the Qena governorate in Upper Egypt. Six were classified as rural areas, and the remaining four were classified as urban areas, with a total population of 8027 inhabitants. The population was screened using an epilepsy-screening questionnaire. Positive cases with suspected epilepsy were referred to Qena University Hospital to be further evaluated by a qualified neurologist and for further investigations, such as neuroimaging and electroencephalography. RESULTS: One hundred patients had a confirmed diagnosis of epilepsy, with a lifetime prevalence of 12.46/1000. The active prevalence rate of epilepsy was 2.12/1000, while the incidence rate was 123/100000. Seventy-six percent of the patients had idiopathic epilepsies, while 24% had symptomatic epilepsy. Generalized epilepsies were more common (70.1%) than partial epilepsy (26.3%), meanwhile epilepsies with mixed seizure types were 2.6%. The most common seizure type was generalized tonic clonic seizures (51.8%). The age-specific prevalence rate of epilepsy was much higher in infancy and early childhood (62.5 and 37.04/1000, respectively), which regressed steadily with age. Idiopathic epilepsies were significantly more common in urban areas than in rural areas (P=0.01), while symptomatic epilepsies were more common in rural areas than in urban areas (P<0.005). CONCLUSION: Upper Egypt is characterized by a relatively high incidence and prevalence of epilepsy and epilepsy-related medical service, and more cultural education should be directed to those areas in Egypt.