Synthesis,structure–activity relationship and molecular docking of 3-oxoaurones and 3-thioaurones as acetylcholinesterase and butyrylcholinesterase inhibitors

The present study describes efficient and facile syntheses of varyingly substituted 3-thioaurones from the corresponding 3-oxoaurones using Lawesson’s reagent and phosphorous pentasulfide. In comparison, the latter methodology was proved more convenient, giving higher yields and required short and simple methodology. The structures of synthetic compounds were unambiguously elucidated by IR, MS and NMR spectroscopy. All synthetic compounds were screened for their inhibitory potential against in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Molecular docking studies were also performed in order to examine their binding interactions with AChE and BChE human proteins. Both studies revealed that some of these compounds were found to be good inhibitors against AChE and BChE.     

Molecular factors regulating E-cadherin expression in urothelial bladder cancer and their correlations with the clinicopathological features

This study aimed to assess the expression of S100A4, Twist and E-cadherin (mRNA and protein) in urothelial bladder cancer, investigate the correlation between them and evaluate their association with the clinicopathological features of the disease. The study included 54 patients diagnosed as urothelial bladder cancer of different stages and grades. The expression levels of S100A4, Twist and E-cadherin (mRNA and protein) in tissue samples were determined by quantitative RT-PCR and immunohistochemistry. The expression of S100A4 and Twist was significantly upregulated while E- cadherin was significantly downregulated in urothelial bladder cancer tissues compared to the adjacent surrounding normal bladder tissues at both mRNA and protein levels (p?<?0.001). Expression levels of S100A4 and Twist were significantly higher in recurrent tumor than in non-recurrent tumors (p?<?0.001) while the expression level of E-cadherin was significantly lower in recurrent tumors than in non-recurrent tumors at both mRNA and protein levels (p?<?0.001). There was a significant positive correlation between S100A4 and Twist expressions (r?=?0.875, p?<?0.001) while significant negative correlations were found between E- cadherin and S100A4 expressions(r=- 0.803, p?<?0.001) and between E-cadherin and Twist (r?=??0.809, p?<?0.001). Up-regulation of S100A4 and Twist and down-regulation of E-cadherin in urothelial bladder cancer tissues compared to adjacent normal tissues were observed. There was a significant negative correlation between S100A4 and E- cadherin and between E- cadherin and Twist expression. However, there was a significant positive correlation between S100A4 and Twist expressions. Furthermore, the alterations in the gene expression were associated with disease stage and grade.     

Synthesis and activity against HBV of novel Tetra-seconucleoside analogues of dyphlline having the acyclic chains of ACV and HBG

Selective alkylation of dyphylline (1) with (2-acetoxyethoxy)methyl bromide (2a) or 4-acetoxybutyl bromide (2b) afforded 3'-O-[(acetoxyethoxy)methyl]dyphylline (3a) and 3'-O-(4-acetoxybutyl)-dyphylline (3b), respectively. A trans esterification process rather than alkylation of the dihydroxy-propyl side chain in 1 had taken place during the reaction with 2-p-toluoyloxy)ethyl chloride (5) to afford the respective 3'-toluoyloxy derivative 7 and not the anticipated 3'-O-[(p-toluoyloxy)ethyl]-dyphylline (6). Deacylation of 3a,b and 7 afforded 4a,b and 1, respectively. Viral screening of selected compounds against HBV has been investigated.     

Natural wool/cellulose acetate blends regenerated from the ionic liquid 1-butyl-3-methylimidazolium chloride

Dissolution and blending one of the most commonly used natural polymers, i.e., wool using a green solvent ionic liquid is described. The cleaned natural wool from merino sheep was directly dissolved and regenerated from 1-butyl-3-methylimidazolium chloride (BMIMCl) without any modifications. BMIMCl was subsequently used to develop wool/cellulose acetate (CA) blends. Blending modification of wool in this IL green solvent led to significant increase in glass transition temperature (T_g) and thermal stability compared to the pure components. It was found that there exist strong intermolecular hydrogen bonding interactions between regenerated wool and CA. Moreover homogeneous surface morphology was observed in the blends with higher CA concentrations. At the final stage of the blending process, the IL solvent was recycled completely. This work presents a green processing route for development of novel natural wool blended materials.     

Fixed-bed adsorption performance of oil palm shell-based activated carbon for removal of 2,4,6-trichlorophenol

This study investigated the adsorption potential of oil palm shell-based activated carbon to remove 2,4,6-trichlorophenol from aqueous solution using fixed-bed adsorption column. The effects of 2,4,6-trichlorophenol inlet concentration, feed flow rate and activated carbon bed height on the breakthrough characteristics of the adsorption system were determined. The regeneration efficiency of the oil palm shell-based activated carbon was evaluated using ethanol desorption technique. Through ethanol desorption, 96.25% of the adsorption sites could be recovered from the regenerated activated carbon.     

Alterations in sucrose metabolizing enzyme activities and total phenol content of Curcuma Ionga L. as affected by different triazole compounds

Changes in the sucrose metabolism of Cur-cuma longa L. plants were studied under treatment with different triazole compounds viz., triadimefon (TDM) and propiconazole (PCZ). Plants were treated with TDM at 15 mg/L and PCZ at 10 mg/L separately by soil drenching on 80, 110, and 140 days after planting (DAP). The plants were harvested randomly on 90, 120, and 150DAP to determine the effect of both the triazoles on sucrose metabolizing enzymes and phenol content. The sucrose metabolism was studied by analyzing sucrose metaboliz-ing enzymes like sucrose synthase and sucrose phosphate synthase. All the analyses were assayed in leaves and tubers of both control and treated plants. It was found that both of the triazole compounds had profound effects on these parameters.     

Molecular Confirmation of Intraspecific Tomato (<Emphasis Type="Italic">Solanum lycopersicum)</Emphasis> Hybrids and Their Evaluation Against Late Blight and Cucumber Mosaic Virus

Tomato is one of the most consumed vegetables in the world. Diseases are the number one concern in the development of high-yield and disease-resistant tomato hybrids which is the foremost priority of breeders. Present study was conducted (1) to develop DNA-based markers for genetic confirmation of tomato F₁ hybrids, (2) to utilize sequenced characterized amplified region (SCAR) marker linked to the Ph-3 gene for Phytophthora infestans resistance in tomato and (3) to evaluate male and female parental genotypes and their F₁ hybrids against late blight (LB) and cucumber mosaic virus (CMV). For molecular studies, 58 previously reported markers including RAPDs (10), SCAR (01), EST-SSR (01) and SSR (46) were applied. The SCAR marker clearly differentiated the LB3 and LB4 from Roma and T-1359 and provided evidence for Ph-3 gene. The SCAR marker was able to confirm the Ph-3 gene in the hybrids Roma × LB4, Roma × LB3, Riogrande × LB2, Riogrande × LB3 and Roma × LB7. Out of several tested primers, SSR-22 proved useful for genetic confirmation of F₁ hybrid TMS1 × Money Maker (MM). For LB, tested hybrids/genotypes were ranked as susceptible to highly susceptible with different infection percentage (IP). However, the pace of symptom development was slower in hybrid Rio × LB2, 45% IP after 10 days of inoculation compared with 85% disease in one of the parent genotypes (Riogrande). None of the tested genotypes was found resistant; however, TMS1 responded as tolerant against CMV using mechanical inoculation. Under natural field conditions, TMS1 was found resistant while hybrids TMS1 × Naqeeb and TMS1 × MM were tolerant where as others were found to be susceptible. In conclusion, all tomato hybrids were genetically confirmed using DNA-based markers. SCAR marker was useful for marker-assisted confirmation of the Ph-3 gene in parental lines and hybrids; however, this gene was unable to provide protection against the local population of P. infestans.     

Effects of nickel toxicity on morphological and physiological aspects of osmoregulation in <Emphasis Type="Italic">Typha domingensis</Emphasis> (<Emphasis Type="Italic">Typhaceae</Emphasis>) populations

The present work examined morphological and physiological aspects of osmoregulation in some differently adapted populations of Typha domingensis. Six populations of T. domingensis were grown in waterlogged conditions under four levels of nickel (0, 50, 100 and 1500 mg/kg of Ni). The Ni tolerance was explored on the basis of different characteristics of shoots. Along with the increasing level of Ni stress, all populations showed an increment of proline and glycinebetaine content, low photosynthetic and transpiration rates and decreased chlorophyll content. Analyzed morphological parameters revealed possible adaptations to deal with Ni stress. The less tolerant Sahianwala population produced more aerenchyma, less accumulation of osmolytes and reduced shoot fresh weight under Ni stress than the tolerant ones. Our results suggested that T. domingensis has the capacity to survive under Ni stress and could be used for the absorption of toxic metal ions from industrially polluted water.