Novel chalcone/aryl carboximidamide hybrids as potent anti-inflammatory via inhibition of prostaglandin E2 and inducible NO synthase activities: design,synthesis, molecular docking studies and ADMET prediction

Two series of chalcone/aryl carboximidamide hybrids 4a–f and 6a–f were synthesised and evaluated for their inhibitory activity against iNOS and PGE2. The most potent derivatives were further checked for their in vivo anti-inflammatory activity utilising carrageenan-induced rat paw oedema model. Compounds 4c, 4d, 6c and 6d were proved to be the most effective inhibitors of PGE2, LPS-induced NO production, iNOS activity. Moreover, 4c, 4d, 6c and 6d showed significant oedema inhibition ranging from 62.21% to 78.51%, compared to indomethacin (56.27 ± 2.14%) and celecoxib (12.32%). Additionally, 4c, 6a and 6e displayed good COX2 inhibitory activity while 4c, 6a and 6c exhibited the highest 5LOX inhibitory activity. Compounds 4c, 4d, 6c and 6d fit nicely into the pocket of iNOS protein (PDB ID: 1r35) via the important amino acid residues. Prediction of physicochemical parameters exhibited that 4c, 4d, 6c and 6d had acceptable physicochemical parameters and drug-likeness. The results indicated that chalcone/aryl carboximidamides 4c, 4d, 6c and 6d, in particular 4d and 6d, could be used as promising lead candidates as potent anti-inflammatory agents.     

A Peptide Bond from the Inter-lobe Segment in the Bilobal Lactoferrin Acts as a Preferred Site for Cleavage for Serine Proteases to Generate the Perfect C-lobe: Structure of the Pepsin Hydrolyzed Lactoferrin C-lobe at 2.28 Å Resolution

The Protein Journal - C-lobe represents the C-terminal half of lactoferrin which is a bilobal 80 kDa iron binding glycoprotein. The two lobes are designated as N-lobe (Ser1-Glu333) and...     

Therapeutic effects of Typha elephantina leave’s extract against paracetamol induced renal injury in rabbits

Present study focuses on ameliorative potential of Typha elephantina leave’s aqueous (TE.AQ) extract against Paracetamol (PCM) induced toxicity in rabbits. We fed the male rabbits with 300 mg PCM in alone and in combination with TE.AQ at different doses i.e. (100, 200 and 300 mg/kg body weight) or silymarin (100 mg/kg) daily for 21 days. PCM in alone significantly (P < 0.5) increased serum urea, uric acid, creatinine, total protein, albumin, globulin and blood urea nitrogen. Serum sodium, potassium and magnesium level were high. The glutathione, radical scavenging activity and Thiobarbituric acid reactive substances were significantly reduced. Treatment with TE.AQ at dose rate 300 mg/kg body weight and Silymarin significantly ameliorated all the parameters when compared with PCM administered group. The 100 and 200 mg of TE.AQ showed no significant effects. The histopathological examination confirmed the therapeutic potential of TE.AQ. These results established the presence of natural antioxidants in Typha elephantina leaves.     

Mating behaviour and behavioural ecology of a Predatory Wasp,Symmorphus allobrogus (de Saussure) (Hymenoptera: Eumeninae)

This paper represents an attempt to investigate the mating behaviour of Symmorphus allobrogus, explaining the willingness of male to mount and copulate. The male displays including mode and frequency of antennation and position while copulating, the displays further comprises of intensity and frequency of rejecting behaviour. The presence of the male’s copulatory and postcopulatory courtship studies, understands the maintenance of monandry. The wasp has numerous secondary sexual characters, and the mating behaviour follows a phyletic and the specific sexual mating characters in context of sexual selection. The duration of mating phases and the number of male antennation series during precopulatory, copulatory and postcopulatory phases of mounting, differs significantly. Mating success depends mostly on the activities of male in the premounting phase and the behaviour of both sexes has a roughly equal importance for it in precopulatory phase. While during copulation, activity of male has little influence on its duration; however, behaviour of female has crucial effect, inducing its earlier termination.     

Optimizing the Sensing Efficiency of Plasmonic Based Gas Sensor

Plasmonics - This paper investigates the behavior of the surface plasmon polaritons (SPPs) on dielectric-metal interface using Ag thin film on glass substrate. The Kretschman configuration, which...     

Reunderstanding Cairo through urban metabolism: Formal versus informal districts resource flow performance in fast urbanizing cities

Urban expansion can be seen as the most pervasive human impact on the environment where its high resource use contributes negatively to climate change and resource scarcity crises. Many experts call for decoupling resource use, economic development, and related urban development especially within cities of the Global South. This paper focuses on investigating resource efficiency through the lens of urban metabolism. It investigates current resource flows, through material flow analysis, from source to sink, in two diverse districts in Cairo: a formal district and an informal one, regarding materials (waste) and mobility. Consequently, the paper discusses locally responsive interventions that address local priorities as opposing to citywide one‐size fits all solution. The paper relies on parcel audits, which are embedded in an Urban Metabolism Information System developed by the Ecocity Builders and their partners, through a joint project with Cairo University. The methodology couples crowd‐sourced data, parcel audits, and experts’ knowledge to better understand resource flows based on a bottom‐up approach, given the unavailability of governmental data on the local level. The paper further correlates the perceived quality of life with the actual resource flows. It utilizes fieldwork investigations to argue against the local misconceptions regarding the inefficiency of informal areas/systems versus the higher efficiency of planned areas/systems. The paper concludes by proposing integrated solutions that respond to local needs and resources. It highlights the challenges and lessons of this tailored bottom‐up approach and its applicability in other cities worldwide.     

Production of bioethanol from four species of duckweeds (Landoltia punctata,Lemna aequinoctialis,Spirodela polyrrhiza,and Wolffia arrhiza) through optimization of saccharification process and fermentation with Saccharomyces cerevisiae

Duckweeds are promising potential sources for bioethanol production due to their high starch content and fast growth rate. We assessed the potential for four species, Landoltia punctata, Lemna aequinoctialis, Spirodela polyrrhiza, and Wolffia arrhiza, for bioethanol production. We also optimized a possible production procedure, which must include saccharification to convert starch to soluble sugars that can serve as a substrate for fermentation. Duckweeds were cultivated on 10% Hoagland solution for 12 days, harvested, dried, homogenized, and dissolved in solutions that were tested as substrates for bioethanol production by the yeast Saccharomyces cerevisiae. First, we optimized the saccharification process, including the ideal ratio of the enzyme used to convert starch into simple sugars. The greatest starch-to-sugar conversion was obtained when the α-amylase and amyloglucosidase was 2:1 (v/v) and with a 24 h incubation period at 50 °C. After saccharification, the solutions were incubated with the yeast, S. cerevisiae. The fermentation process was carried out for 48 h with 10% (v/v) yeast inoculum. The ethanol content was maximal approximately 24 h after the start of incubation, and the sugars and protein were minimal, with little change over the next 24 h. The final ethanol concentration obtained were 0.19, 0.17, 0.19, and 0.16 g ethanol/g dry biomass for L. punctata, L. aequinoctialis, S. polyrrhiza, and W. arrhiza respectively. We suggest that these four species of duckweed have the potential to serve sources of bioethanol and hope that the procedure we have optimized proves useful in the endeavour.     

Naringin inhibits the biofilms of metallo-β-lactamases (MβLs) producing Pseudomonas species isolated from camel meat

Food producing animals harbouring bacteria carrying drug resistance genes especially the metallo-beta-lactamase (MBL) pose high risk for the human population. In addition, formation of biofilm by these drug resistant pathogens represents major threat to food safety and public health. In this study, metallo-β-lactamases (MβLs) producing Pseudomonas spp. from camel meat were isolated and assessed for their biofilm formation. Further, in vitro and in silico studies were performed to study the effect of flavone naringin on biofilm formation against isolated Pseudomonas spp. A total of 55% isolates were found to produce metallo-β-lactamase enzyme. Naringin mitigated biofilm formation of Pseudomonas isolates up to 57%. Disturbed biofilm architecture and reduced the colonization of bacteria on glass was observed under scanning electron microscope (SEM) and confocal laser scanning microscope (CLSM). The biofilm related traits such as exopolysaccharides (EPS) and alginate production was also reduced remarkably in the presence of naringin. Eradication of preformed biofilms (32–60%) was also observed at the respective 0.50 × MICs. Molecular docking revealed that naringin showed strong affinity towards docked proteins with binding energy ranging from −8.6 to −8.8 kcal mol⁻¹. Presence of metallo-β-lactamase producers indicates that camel meat could be possible reservoir of drug-resistant Pseudomonas species of clinical importance. Naringin was successful in inhibiting biofilm formation as well as eradicating the preformed biofilms and demonstrated strong binding affinity towards biofilm associated protein. Thus, it is envisaged that naringin could be exploited as food preservative especially against the biofilm forming food-borne Pseudomonas species and is a promising prospect for the treatment of biofilm based infections.     

Characterization of the native honey bee (Apis mellifera jemenitica) in the south western region of Saudi Arabia using morphometric and genetic (mtDNA COI) characteristics

Apis mellifera jemenitica incorporates a few perceived subspecies that vary in their natural properties and farming qualities. Mitochondrial COI gene sequence (mtCOI) has not been used before for bee identification in the southwestern region of Saudi Arabia. The aim of this work was to study the morphometry and analyzing the mtCOI of all collected bees. The nucleotide sequence of the mtCOI gene was analyzed. Similarity searches and distances between each obtained DNA and sequences available in GenBank were made. Morphometric analysis revealed close similarities among the studied bees, but these similarities are different from those previously indicated in earlier studies of the same region. Molecular studies revealed that the collected bees are similar to each other and some other sequences found in GenBank, but these bees are a new hybrid or subspecies that are different from those previously reported in the same region, indicating the emergence of a new hybrid.     

6-Shogaol attenuated ethylene glycol and aluminium chloride induced urolithiasis and renal injuries in rodents

The 6-shogaol, is a flavanone type flavonoid that is abundant in citrus fruit and has a wide range of pharmacological effects. The present study attempted to evaluate the antiurolithic effect of 6-shogaol on ethylene glycol (EG) and ammonium chloride (AC)-induced experimental urolithiasis in rats. The efficacy of 6-shogaol 50 mg/kg and 100 mg/kg was studied in EG 0.75% (V/V) and AC 1% (W/V) experimentally induced urolithiasis in rats for 21 days. The weight difference, urine volume, the levels of calcium, phosphate, magnesium, oxalate and uric acid in urine was observed. The blood urea nitrogen, creatinine, uric acid in serum and levels of malondialdehyde (MDA) and glutathione (GSH) were also measured. Histopathological analyses in kidneys were also performed. The rats weights were higher in the 6-shogaol groups than the urolithiasis group. EG caused a significant increase in serum creatinine (p < 0.05), BUN (P < 0.001), and uric acid (p < 0.01) while treatment with Cystone (750 mg/kg), and 6-shogaol (50 and 100 mg/kg) showed the significant reduction in increased serum levels of creatinine (p < 0.001), uric acid (p < 0.01) and BUN (p < 0.001). Administration of EG and AC showed statistically significant (p < 0.001) elevated levels of MDA and reduction in GSH levels. Treatment of Cystone (750 mg/kg), and 6-shogaol (50 and 100 mg/kg) significantly (p < 0.001) reduced MDA levels and an increase GSH levels as compared to EG and AC-treated group. The histological findings further attested antiurolithiatic properties of 6-shogaol. The present study attributed clinical shreds of evidence first time that claiming the significant antiurolithic effect of 6-shogaol and could be a cost-effective candidate for the prevention and treatment of urolithiasis.