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Synthesis of 2-Furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives as suitable antibacterial agents with mild cytotoxicity

2022-10-27T10:41:08Z

Title: Synthesis of 2-Furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives as suitable antibacterial agents with mild cytotoxicity Authors: Abbasi, Muhammad Athar; Nazeer, Muhammad Mubashar; Rehman, Aziz-ur-; Siddiqui, Sabahat Zahra; Hussain, Ghulam; Shah, Syed Adnan Ali; Ahmad, Irshad; Shahid, Muhammad; Sarwar, Muhammad Salman Abstract: The aim of the present research work was synthesis of some 2-furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives and to ascertain their antibacterial potential. The cytotoxicity of these molecules was also checked to find out their utility as possible therapeutic agents. The synthesis was initiated by reacting furyl(-1-piperazinyl)methanone (1) in N,N-dimethylformamide (DMF) and lithium hydride with different aralkyl halides (2a-j) to afford 2-furyl[(4-aralkyl)-1- piperazinyl]methanone derivatives (3a–j). The structural confirmation of all the synthesized compounds was done by IR, EI-MS, 1 H-NMR and 13C-NMR spectral techniques and through elemental analysis. The results of in vitro antibacterial activity of all the synthesized compounds were screened against Gram-negative (S. typhi, E. coli, P. aeruginosa) and Gram-positive (B. subtilis, S. aureus) bacteria and were found to be decent inhibitors. Amongst the synthesized molecules, 3e showed lowest minimum inhibitory concentration MIC = 7.52±0.µg/mL against S. Typhi, credibly due to the presence of 2-bromobenzyl group, relative to the reference standard, ciprofloxacin, having MIC = 7.45±0.58µg/mL.

The effect of ivermectin on secondary spermatocytes and serum total proteins

2022-10-27T10:40:35Z

Title: The effect of ivermectin on secondary spermatocytes and serum total proteins Authors: Sweify, Karima Mohammad; Darwish, Iman Abd El Moneim; Hafez, Dalia Demerdash Abd El Monem Abstract: Ivermectin, a broad-spectrum anti-parasitic agent first used in veterinary medicine, is active against numerous species of helminths and arthropods. In this study, we aimed to demonstrate the effects of administration of ivermectin on secondary meiotic division and serum total proteins. Male mice treated with single injections of 200ug/kg b.w. IVM. Meiotic chromosomes were prepared after 6 hours, 2, 5, 10 and 12 days to cover the different phases of meiotic division. Blood samples were collected after 1, 7 and 14 days of the last injection to determine total protein content. Euploidy (haploid no which equal 20 chromosomes) was recorded in 8.6 of the scored cells of secondary spermatocytes. Hyperhaploid (metaphases that include more than 20 and less than 23 chromosomes) was also considered. A total of 46 hyperhaploid metaphases were registered for 2100 examined cells. The hyper-haploidy index was 2.49% versus 0.8% for the control. Acentric fragments were occasionally occurred. After 1 and 7 days, single injections of IVM led to elevate the total protein content than that resulted after double treatment. However, the data obtained after 14 days were closed together. In conclusion, IVM is produced a considerable signs of chromosomal damage to germ cells. So, the cytogenetic studies revealed high clastogenicity of the drug. On the other hand, the differences in total protein concentration obtained between treated and control samples indicate genotoxic potential for IVM.

Protective effects of Butea frondosa leaves against stress induced immune impairment in sprague dawley rats

2022-10-27T10:39:35Z

Title: Protective effects of Butea frondosa leaves against stress induced immune impairment in sprague dawley rats Authors: Rizvi, Aleza; Mahdi, Abbas Ali; Wahab, Shadma; Mishra, Anuradha Abstract: Stress is thought to impair immune function through emotional or behavioral manifestations thus the present study was done to assessed the effect of ethanolic extract of Butea frondosa (BF) leaves on behaviour, immunomodulatory activity and brain acetyl cholinesterase activity in normal and stress induced male rats. Neuroprotective effects of BF, doses (100,200,400mg/kg p.o) were measured by assessing the changes in the behaviour and the immunity of the rats. In stress control, the results indicated that the retention transfer latency, time spent in a closed arm, agglutination , total leukocytes counts (TLC), total paw edema ,size of spleen , decreased significantly (p<0.01) while glucose level, size of the kidney and the liver, AChE activity increased significantly (p<0.01) in comparison with normal control. In BF (200mg/kg) treated rats, the results indicated that the time spent in a closed arm (p<0.01), agglutination (p<0.01), TLC (p<0.01), total paw edema (p<0.05), size of spleen(p<0.01) , increased significantly while glucose level (p<0.01), size of the kidney and the liver (p<0.01), AChE activity (p<0.01) decreased significantly in comparison with stress control. This study therefore concluded that the ethanolic extract of BF (200mg/kg) showed a protective effect against the stress induced impaired immune system and the psychological disorders.

Phytochemical analysis and antimicrobial activity of aqueous and methanolic extracts of the flowers of Nelumbium speciosum

2022-10-27T10:37:39Z

Title: Phytochemical analysis and antimicrobial activity of aqueous and methanolic extracts of the flowers of Nelumbium speciosum Authors: Bashir, Sajid; Sial, Rubina Naureen; Ashraf, Muhammad Umer; Mushtaq, Muhammad Naveed; Adnan, Muhammad Abdul Jabar; Erum, Alia Abstract: In present investigation aqueous and methanolic extracts of Nelumbium speciosum flowers were screened for phytochemical constituents and antibacterial activity to ascertain their traditional use. Antimicrobial activity of both extracts was tested by Kirby-Bauer disc diffusion method against four Gram positive strains, viz. Staphylococcus aureus (ATCC25923), Streptococcus agalactiae (13813), Bacillus subtilis (ATCC 6633), Staphylococcus epidermidis (ATCC 12228) and four Gram negative bacterial strains Escherichia coli (ATCC 8739), Pseudomonas aeruginosa (ATCC 27853), Proteus mirabilis (12453) and Klebsiella pneumoniae (10031). Phytochemical analysis showed the presence of tannins, saponins and alkaloids in both extracts while flavonoids and steroids were present only in methanolic extract. Methanolic extract of Nelumbium speciosum flower showed concentration dependent antibacterial activity against all tested strains with maximum zone of inhibition (17.3±0.3mm) against P. aeruginosa. Aqueous extract showed concentration dependent activity against S. aureus, E. coli, B. subtilis and S. epidermidis with maximum antibacterial activity against E. coli (14.3±0.3mm). MIC of methanolic and aqueous extracts was in the range of 0.015-0.251 and 0.0625-0.251 mg/mL, respectively. Results showed that methanolic extract of Nelumbium speciosum exhibits superior antibacterial activity than aqueous extract.