Tensile fatigue behaviour of articular cartilage

Although fatigue has been implicated in cartilage failure there are only two studies by the same author, and in both of which cartilage was tested in the direction parallel to the collagen orientation in the surface layer. In the present work articular cartilage was tested also along the perpendicular direction, being the direction in which cartilage possesses lower tensile strength.Specimens were tested under cyclic tensile load. Number of cycles at failure was recorded as well as elongation of the specimen. To date 72 specimens have been tested all from one knee joint.The number of cycles to failure ranged between two and 1.5 million. The surface and deep layers have better fatigue properties whether tested in the parallel or the perpendicular direction, while the middle layer was far weaker. Better fatigue behaviour was observed with specimens tested in parallel than in perpendicular direction to the fibres.     

Enzymatic hydrolysis of rice straw and corn stalks for monosugars production

Rice straw and corn stalks were used as fermentation substrate for the evaluation of cellulases activity secreted by different organisms. The substrates were pretreated with alkaline hydrogen peroxide (AHP) for 6 h at 30 and 60 °C. From the fermentation studies, rice straw and corn stalks substrates showed the highest cellulases activity after 96 h at 60 °C of pre-treatment.     

Assessment of the antimicrobial activity of the lipoidal and pigment extracts of Punica granatum L. leaves

Punica granatum L. is one of the famous and old species belonging to Family Punicaceae. The lipoidal and natural pigment extracts of the pomegranate were screened for their antimicrobial activity against nine different microbial pathogens. Three different doses of each extract (50, 100 and 150?μl) at three different contact times (15, 30 and 60?min) were examined. Results can be cleared that, all tested microbial pathogens were inhibited by 150?μl of both extracts at 60?min. Furthermore, the removal efficiency of n-hexane extract was powerful than the pigment extract. Also, the quantitative evaluation of the pigments in the leaves was performed using spectroscopical and HPLC analyses, carotenoids and chlorophylls content of P. granatum L. leaves were spectroscopically determined (mg/g) as 6.7?±?0.214 and 4.9?±?0.251, respectively. Chlorophyll a and b were 2.33?±?0.014 and 1.51?±?0.023, respectively. HPLC analysis of lutein and β-carotene were investigated as 3.652 and 1.915?mg/g. GC/MS analysis of the saponifiable and unsaponifiable fraction of n-hexane extract was carried out and α-amyrin acetate, ergosterol, and α-tocopherol were isolated, purified and identified using different spectroscopical methods. Toxicity assessment demonstrated their high biocompatibility since no toxic effect was recorded.     

The role of biofilm in the development and dissemination of ubiquitous pathogens in drinking water distribution systems: an overview of surveillance,outbreaks, and prevention

World Journal of Microbiology and Biotechnology - Biosurfactants can be widely used in industries as pharmaceutical agents, for microbial enhanced oil recovery, crop biostimulation, among others....     

Approved spectrofluorimetric strategies for assurance of three modern antineoplastic drugs: tepotinib,sotorasib, and darolutamide in their dose forms and biological liquids utilizing mercurochrome

An approved, straightforward, fast, and delicate spectrofluorimetric strategy was developed for the estimation of tepotinib (TEPO), sotorasib (SOTO), and darolutamide (DARO) as new antineoplastic drugs. The spectrofluorimetric strategy was based on quantitative fluorescence quenching of MER at 538 nm after being excited at 350 nm by the addition of the cited drugs in the presence of acetate buffer (pH 3.5). The degree of fluorescence quenching was directly proportional to the concentrations of the cited drugs within the concentration range of 0.5–10.0, 0.2–10, and 0.4–10.0 μg ml⁻¹ for TEPO, SOTO, and DARO, respectively. Mean ± standard deviation (SD) were calculated for the studied drugs as follows; 99.9 ± 0.87, 99.72 ± 1.08, and 100.21 ± 1.44, for TEPO, SOTO, and DARO, respectively. Limit of detection (LOD) values were 0.16, 0.05, and 0.11 μg ml⁻¹, whereas limit of quantitation (LOQ) values were 0.5, 0.15, and 0.36 μg ml⁻¹ for TEPO, SOTO, and DARO, respectively. Statistical comparison through detailed strategies produced greater understanding and found that there were no noteworthy contrasts in exactness and exactness between strategies. The proposed strategy was used effectively to analyze the measurement of different forms of the examined drugs. Moreover, the recommended fluorimetric strategy was used for examination of TEPO, SOTO, and DARO in human plasma and urine tests.     

Ligand-based design,synthesis, computational insights,and in vitro studies of novel N-(5-Nitrothiazol-2-yl)-carboxamido derivatives as potent inhibitors of SARS-CoV-2 main protease

The global outbreak of the COVID-19 pandemic provokes scientists to make a prompt development of new effective therapeutic interventions for the battle against SARS-CoV-2. A new series of N-(5-nitrothiazol-2-yl)-carboxamido derivatives were designed and synthesised based on the structural optimisation principle of the SARS-CoV Mpro co-crystallized WR1 inhibitor. Notably, compound 3b achieved the most promising anti-SARS-CoV-2 activity with an IC₅₀ value of 174.7 µg/mL. On the other hand, compounds 3a, 3b, and 3c showed very promising SARS-CoV-2 Mpro inhibitory effects with IC₅₀ values of 4.67, 5.12, and 11.90 µg/mL, respectively. Compound 3b docking score was very promising (−6.94 kcal/mol) and its binding mode was nearly similar to that of WR1. Besides, the molecular dynamics (MD) simulations of compound 3b showed its great stability inside the binding pocket until around 40 ns. Finally, a very promising SAR was concluded to help to design more powerful SARS-CoV-2 Mpro inhibitors shortly.     

Characterization of the 1,25-dihydroxycholecalciferol-stimulated calcium influx pathway in CaCo-2 cells

The present studies were conducted to investigate the mechanisms underlying the 1,25-dihydroxycholecalciferol (1,25(OH)₂D₃)-induced increase in intracellular Ca²⁺ ([Ca²⁺] _i ) in individual CaCo-2 cells. In the presence of 2mm Ca²⁺, 1,25(OH)₂D₃-induced a rapid transient rise in [Ca²⁺] _i in Fura-2-loaded cells in a concentration-dependent manner, which decreased, but did not return to baseline levels. In Ca²⁺-free buffer, this hormone still induced a transient rise in [Ca²⁺] _i , although of lower magnitude, but [Ca²⁺] _i then subsequently fell to baseline. In addition, 1,25(OH)₂D₃ also rapidly induced⁴⁵Ca uptake by these cells, indicating that the sustained rise in [Ca²⁺] _i was due to Ca²⁺ entry. In Mn²⁺-containing solutions, 1,25(OH)₂D₃ increased the rate of Mn²⁺ influx which was temporally preceded by an increase in [Ca²⁺] _i . The sustained rise in [Ca²⁺] _i was inhibited in the presence of external La³⁺ (0.5mm). 1,25(OH)₂D₃ did not increase Ba²⁺ entry into the cells. Moreover, neither high external K⁺ (75mm), nor the addition of Bay K 8644 (1 μm), an L-type, voltage-dependent Ca²⁺ channel agonist, alone or in combination, were found to increase [Ca²⁺] _i , 1,25(OH)₂D₃ did, however, increase intracellular Na⁺ in the absence, but not in the presence of 2mm Ca²⁺, as assessed by the sodium-sensitive dye, sodium-binding benzofuran isophthalate. These data, therefore, indicate that CaCo-2 cells do not express L-type, voltage-dependent Ca²⁺ channels. 1,25(OH)₂D₃ does appear to activate a La³⁺-inhibitable, cation influx pathway in CaCo-2 cells.     

24-Epibrassinolide alleviates salt-induced inhibition of productivity by increasing nutrients and compatible solutes accumulation and enhancing antioxidant system in wheat (Triticum aestivum L.)

Two wheat (Triticum aestivum L.) cultivars, Sids 1 and Giza 168, were grown under non-saline or saline conditions (4.7 and 9.4 dS m^?1) and were sprayed with 0.00, 0.05 and 0.10 mg l^?1 24-epibrassinolide (EBL). Salt stress markedly decreased plant productivity and N, P, and K uptake, particularly in Giza 168. A follow-up treatment with 0.1 mg l^?1 EBL detoxified the stress generated by salinity and considerably improved the above parameters, especially in Sids 1. Organic solutes (soluble sugars, free amino acids, proline and glycinebetaine), antioxidative enzymes (superoxide dismutase, peroxidase, catalase and glutathione reductase), antioxidant molecules (glutathione and ascorbate) and Ca and Mg levels were increased under saline condition, and these increases proved to be more significant in salt-stressed plants sprayed with EBL, particularly at 0.1 mg l^?1 EBL with Sids 1. Sodium concentration, lipid peroxidation, hydrogen peroxide content and electrolyte leakage were increased under salt stress and significantly decreased when 0.1 mg l^?1 EBL was sprayed. Clearly, EBL alleviates salt-induced inhibition of productivity by altering the physiological and biochemical properties of the plant.     

Effect of Different Selenium Supplementation Levels on Selenium Status in Camel

Twelve female camels divided into three groups received, after a 2-week adaptation period, an oral Se supplementation (0, 2, and 4 mg, respectively) under sodium selenite form for 3 months. Feed intake was assessed daily, blood samples and body weight were taken on a weekly basis, and feces and urine samples were collected every 2 weeks up to 1 month after the end of the supplementation period. The Se concentration in serum was increased significantly in supplemented groups. The maximum level was observed in the period of supplementation in the camel receiving 4 mg (492.5 ng/mL), which was fourfold higher than the value at the beginning of the trial (126 to 138.5 ng/mL according to the groups). The selenium concentration increased significantly in urine and feces but to a lesser extent. A similar trend was observed with glutathione-peroxidase (GSH-Px) values varying between 8.4 and 96.5 IU/g Hb. However, no difference occurred between the two groups receiving 2 or 4 mg Se at the supplementation period. Vitamin E (mean 1.13 +/- 0.61 microg/mL with range 0.27-3.09) did not change significantly. Significant correlations were reported between serum Se, GSH-Px, fecal, and urinary excretion or concentration.     

Development of novel liver X receptor modulators based on a 1,2,4-triazole scaffold

Liver?X?Receptor (LXR) agonists have been reported as a potential treatment for atherosclerosis, Alzheimer’s disease and hepatitis C virus (HCV) infection. We have designed and synthesized a series of potent compounds based on a 1,2,4-triazole scaffold as novel LXR modulators. In cell-based cotransfection assays these compounds generally functioned as LXR agonists and we observed compounds with selectivity towards LXRα (7-fold) and LXRβ (7-fold) in terms of potency. Assessment of the effects of selected compounds on LXR target gene expression in HepG2 cells revealed that compounds 6a-b and 8a-b behaved as inverse agonists on FASN expression even though they were agonists in the LXRα and LXRβ cotransfection assays. Interestingly, these compounds had no effect on the expression of SREBP-1c confirming a unique LXR modulator pharmacology. Molecular docking studies and evaluation of ADME properties in-silico show that active compounds possess favorable binding modes and ADME profiles. Thus, these compounds may be useful for in vivo characterization of LXR modulators with unique profiles and determination of their potential clinical utility.