Synthesis and antimycobacterial evaluation of various 7-substituted ciprofloxacin derivatives

Tuberculosis continues to be a major cause of morbidity and mortality all over the world. Various 7-substituted ciprofloxacin derivatives were synthesized and evaluated for antimycobacterial activity in vitro and in vivo against Mycobacterium tuberculosis and for inhibition of the supercoiling activity of DNA gyrase from Mycobacterium smegmatis. Preliminary results indicated that most of the compounds demonstrated better in vitro antimycobacterial activity against M. tuberculosis than ciprofloxacin. Compound 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-[[N4-[1'-(5-methylisatinyl-beta-semicarbazo)]methyl]N1-piperazinyl]-3-quinoline carboxylic acid (3h) decreased the bacterial load in spleen tissue with 0.76-log10 protections and was considered to be moderately active in reducing bacterial count in spleen. The results demonstrated the potential and importance of developing new quinolone derivatives against mycobacterial infections.     

Intermedilysin is essential for the invasion of hepatoma HepG2 cells by Streptococcus intermedius

Streptococcus intermedius causes endogenous infections leading to abscesses. This species produces intermedilysin (ILY), a human-specific cytolysin. Because of the significant correlation between higher ILY production levels by S. intermedius and deep-seated abscesses, we constructed ily knockout mutant UNS38 B3 and complementation strain UNS38 B3R1 in order to investigate the role of ILY in deep-seated infections. Strain UNS38 reduced the viability of human liver cell line HepG2 at infection but not of rat liver cell line BRL3A. Isogenic mutant strain UNS38 B3 was not cytotoxic in either cell line. Quantification of S. intermedius revealed that in infected HepG2 cells UNS38 but not UNS38 B3 increased intracellularly concomitantly with increasing cell damage. This difference between UNS38 and UNS38 B3 was not observed with UNS38 B3R1. Invasion and proliferation in BRL3A cells was not observed. Masking UNS38 or UNS38 B3R1 with ILY antibody drastically decreased adherence and invasion of HepG2. Moreover, coating strain UNS38 B3 with ILY partially restored adherence to HepG2 but without subsequent bacterial growth. At 1 day post-infection, many intact UNS38 were detected in the damaged phagosomes of HepG2 with bacterial proliferation observed in the cytoplasm of dead HepG2 after an additional 2 day incubation. These results indicate that surface-bound ILY on S. intermedius is an important factor for invasion of human cells by this bacterium and that secretion of ILY within host cells is essential for subsequent host cell death. These data strongly implicate ILY as an important factor in the pathogenesis of abscesses in vivo by this streptococcus.     

Reduction of diabetes-induced oxidative stress by phosphodiesterase inhibitors in rats

Increased oxidative stress has been suggested to be involved in the pathogenesis and progression of diabetic tissue damage. The aim of this study was to investigate the effect of different phosphodiesterase inhibitors on lipid peroxidation and total antioxidant capacity (TAC) of plasma in streptozotocin-induced diabetic rats (Rattus norvegicus). Rats became diabetic by a single administration of streptozotocin (STZ, 45 mg/kg). The effects of 15-days treatment by milrinone, sildenafil, and theophylline as cyclic-AMP and -GMP phosphodiesterase inhibitors (PDEIs) on diabetes-induced oxidative stress were studied. The levels of glucose, malonedialdehyde (MDA) the by product of lipid peroxides, and TAC (FRAP test) were estimated in plasma of control and experimental groups of rats. A significant increase in the levels of plasma glucose, and MDA and a concomitant decrease in the levels of TAC were observed in diabetic rats. These alterations were reverted back to near normal level after the treatment with PDEIs. Treatment of diabetic rats by PDEIs reduced MDA levels and increased TAC in the order of milrinone>sildenafil>theophylline. In conclusion, the present investigation show that PDIS possesses antioxidant activities, which may be attributed to their enhancing effect on cellular cyclic nucleotides contributing to the protection against oxidative stress in streptozotocin-induced diabetes. Exact mechanism of protective actions of cAMP- and cGMP-phosphodiesterase remains to be elucidated by further studies. This finding may suggest a place for PDEIs in maintaining health in diabetes.     

Nanoconfined polymers: modelling and simulation approaches

In this article, application of molecular simulation methods for studying molecular pictures of nanoconfined polymers is reviewed and discussed. The simulation methods, covering a range from atomistic to systematically parameterised coarse-grained models, employed in the literature to study nanoconfined polymers are reviewed and their results are compared together. The effect of polymer–surface interactions, surface curvature and surface area on the alteration of polymer structure and dynamics from the unperturbed (bulk) polymer properties are discussed. The length scales over which the surface influences the polymer structure and dynamics and the magnitude of surface effect on dynamics deceleration in the interphase are addressed in terms of different local and global chain properties.     

New and old adjuvants in allergen‐specific immunotherapy: With a focus on nanoparticles

Allergic diseases have remarkably increased in recent years. Nowadays, efforts for curing and management of these disorders are an important concern worldwide. Allergen‐specific immunotherapy (ASIT) has recently gained more attention as a means for the management of allergic diseases. Adjuvants or helper agents are materials applied for better stimulating and shifting of protective responses, and these belong to an extremely diverse collection of complexes. The main function of adjuvants includes acting as depot foundations, transferring vehicles, and immunostimulators. Immunostimulatory adjuvants have gained increasing attention for ASIT. In this regard, the present study provides a review of old and new adjuvants used in allergen immunotherapy.     

Performance evaluation of a machine vision system for insect pests identification of field crops using artificial neural networks

Feature extraction is a crucial part of advanced image recognition systems. In this research, an autonomous detection device was designed and developed for insect pest detection to improve the ability of intelligent systems in order to annihilate harmful insect pests in agricultural crop fields. Device included a dark chamber, a CCD digital camera, a LDR lightening module and a personal computer. The proposed programme for precise insect pest detection was based on an image processing algorithm and artificial neural networks (ANNs). After image acquisition, the insect pests’ images were extracted from original images with Canny filtration. Afterwards, four morphological and three textural features from the obtained images were measured and normalised. Performance of ANN model was tested successfully for Beet armyworm (Spodoptera exigua) recognition in images using back-propagation supervised learning method and inspection data. Results showed that proposed system was able to identify S. exigua in the images from other species. Such this machine vision system can be used in autonomous field robots to achieve a modern farmer’s assistant.     

An artificial neural network approach to identify fungal diseases of cucumber (Cucumis sativus L.) plants using digital image processing

Nowadays, artificial intelligence solutions such as digital image processing and artificial neural networks (ANN) have become important applicable techniques in phytomonitoring and plant health detection systems. In this research, an autonomous device was designed and developed for detecting two types of fungi (Pseudoperonospora cubensis, Sphaerotheca fuliginea) that infect the cucumber (Cucumis sativus L.) plant leaves. This device was able to recognise the fungal diseases of plants by detecting their symptoms on plant leaves (downy mildew and powdery mildew). For leaves of cucumber inoculated with different spores of the fungi, it was possible to estimate the amount of hour post inoculation (HPI) by extracting leaves’ image parameters. Device included a dark chamber, a CCD digital camera, a thermal camera, a light dependent resistor lightening module and a personal computer. The proposed programme for precise disease detection was based on an image processing algorithm and ANN. Three textural features and two thermal parameters from the obtained images were measured and normalised. Performance of ANN model was tested successfully for disease recognition and detecting HPI in images using back-propagation supervised learning method and inspection data. Such this machine vision system can be used in robotic intelligent systems to achieve a modern farmer’s assistant in agricultural crop fields.     

Selective bactericidal activity of nanopatterned superhydrophobic cicada Psaltoda claripennis wing surfaces

The nanopattern on the surface of Clanger cicada (Psaltoda claripennis) wings represents the first example of a new class of biomaterials that can kill bacteria on contact based solely on its physical surface structure. As such, they provide a model for the development of novel functional surfaces that possess an increased resistance to bacterial contamination and infection. Their effectiveness against a wide spectrum of bacteria, however, is yet to be established. Here, the bactericidal properties of the wings were tested against several bacterial species, possessing a range of combinations of morphology and cell wall type. The tested species were primarily pathogens, and included Bacillus subtilis, Branhamella catarrhalis, Escherichia coli, Planococcus maritimus, Pseudomonas aeruginosa, Pseudomonas fluorescens, and Staphylococcus aureus. The wings were found to consistently kill Gram-negative cells (i.e., B. catarrhalis, E. coli, P. aeruginosa, and P. fluorescens), while Gram-positive cells (B. subtilis, P. maritimus, and S. aureus) remained resistant. The morphology of the cells did not appear to play any role in determining cell susceptibility. The bactericidal activity of the wing was also found to be quite efficient; 6.1?±?1.5?×?10⁶ P. aeruginosa cells in suspension were inactivated per square centimeter of wing surface after 30-min incubation. These findings demonstrate the potential for the development of selective bactericidal surfaces incorporating cicada wing nanopatterns into the design.