NEPHROPROTECTIVE ROLE OF ZINC AGAINST THE AMMONIUM SULFATE TOXICITY IN MALE ALBINO RATS

Objective: Intention of the present study is to investigate the protective role of zinc against ammonium sulfate (AS) toxicity in renal tissue by evaluating certain biochemical activities of albino rats. Methods: Rats were divided into four groups, namely control, ammonia, zinc, and ammonia + zinc. Rats were exposed to AS (18.3 mg/kg body weight) or zinc chloride (4 mg/kg body weight) or both through intraperitoneally for 7-day experimentation with 24-h time interval. Results: AS-administered rats showed significant increased levels of ammonia, urea, glutamine, glutamine synthetase, free amino acids, and lactate dehydrogenase and decreased levels of total proteins, pyruvate, succinate dehydrogenases, malate dehydrogenase, and biochemical activities when compared with control. Supplementation of zinc mitigated AS-induced oxidative stress and restored all the biochemical parameter activities. Zinc administered to normal rats did not exhibit any significant changes in any of the parameters studied. Conclusion: From the study, it concluded that zinc cotreatment with AS has effectively recovered the mitochondrial enzyme activities and ammonia metabolic biochemical parameters in renal tissue of rat treated with AS

Ligand-based virtual screening, molecular docking, QSAR and pharmacophore analysis of quercetin-associated potential novel analogs against epidermal growth factor receptor

<p>The present study was to explore expectation and examination of therapeutic potential quercetin analogs as efficient anticancer agents against human epidermal growth factor receptor (EGFR), which is a consistent hallmark for moderating the non-small-cell lung carcinoma (NSCLC). Here, ligand-based virtual screening, pharmacophore approach and molecular docking were established as rational strategies for recognition of small analogs against the ligand binding domain of EGFR (PDB code: 1XKK). Adverse effects, toxicogenomics and pharmacokinetics reported that 10 candidates showed reliable consequences with less side effects and more efficient for target receptor. Protein–ligand interaction profiles revealed that the probable H-bonds, atomic-π contacts, salt bridges and van der Waals interactions sustain the complexity and stability of receptor structure; thus, they could complicate to generate single alteration acquired for drug resistance. <i>In silico</i> anticancer properties explain the lead scaffolds which are assumed to be flexible and experimentally proved chemicals. The overall consequences indicated that recognized leads could be utilized as reference skeletons for new inhibitors envisaging toward EGFR to ameliorate NSCLC and other malignant disorders.</p

Functionalized 2-Amino-4<i>H</i>-1-Benzopyran-4-yl Phosphonate Scaffolds: Synthesis, Anticancer Evaluation and Computational Studies

Prostate, breast, and lung cancers are various human cancers that have been associated with SRC kinase mutations. Therefore, the development of potent and selective SRC kinase inhibitors is an exciting area of interest for researchers. In this study, we synthesized a series of 2-amino-4H-1-benzopyran-4-yl phosphonate derivatives through a one-pot reaction involving appropriately substituted salicylaldehydes, malononitrile, and diethyl phosphite, with meglumine as the catalyst. We conducted in vitro screening of these compounds for their anticancer activity against human prostate cancer (DU-145), breast cancer (MCF-7), and lung cancer (A549) cell lines using the MTT assay. Notably, compounds 4a, 4j, 4k, and 4l exhibited promising anticancer activity. Molecular docking studies of these compounds supported their potential as therapeutic agents for SRC kinase inhibition. Specifically, compounds 4a, 4b, 4c, 4d, and 4e demonstrated strong ΔG binding affinities ranging from −7.9 to −7.4 kcal/mol. These findings suggest that these molecules hold promise for cancer treatment.</p