The piperazine derivatives have been shown to inhibit human acetylcholinesterase. Virtual screening by molecular docking of piperazine derivatives 1-(1,4-benzodioxane-2-carbonyl) piperazine (K), 4-(4-methyl)-benzenesulfonyl-1-(1,4-benzodioxane-2-carbonyl) piperazine (S1), and 4-(4-chloro)-benzenesulfonyl-1-(1,4-benzodioxane-2-carbonyl) piperazine (S3) has been shown to bind at peripheral anionic site and catalytic sites, whereas 4-benzenesulfonyl-1-(1,4-benzodioxane-2-carbonyl) piperazine (S4) and 4-(2,5-dichloro)-benzenesulfonyl-1-(1,4-benzodioxane-2-carbonyl) piperazine (S7) do not bind either to peripheral anionic site or catalytic site with hydrogen bond. All the derivatives have differed in number of H-bonds and hydrophobic interactions. The peripheral anionic site interacting molecules have proven to be potential therapeutics in inhibiting amyloid peptides aggregation in Alzheimer’s disease. All the piperazine derivatives follow Lipinski’s rule of five. Among all the derivatives 1-(1,4-benzodioxane-2-carbonyl) piperazine (K) was found to have the lowest TPSA value.
Introduction: The use of plant extracts in the green synthesis of metallic nanoparticles is one of the simplest, most practical, economical, and ecologically friendly methods for avoiding the use of toxic chemicals.Method: Silver nanoparticles (AgNPs) were synthesized, employing a high-efficiency, non- toxic, cost-effective, green, and simple technique that included the use of Salacia oblonga root extract (SOR) as a capping agent compared to synthetic nanoparticles. The use of S. oblonga can be seen in traditional medicines for treating diabetes, obesity, rheumatism, gonorrhea, asthma, and hyperglycemia. The objectives of the current study were to green synthesize S. oblonga root extract silver nanoparticles (SOR-AgNPs), characterize them, and study their antioxidant, antibacterial, and antidiabetic activities.Result: The shape of SOR-AgNPs was spherical, at less than 99.8 nm in size, and exhibited a crystalline peak at XRD. The green synthesized SOR-AgNPs showed significant antioxidant properties like DPPH (80.64 μg/mL), reducing power capacity (81.09 ± SEM μg/mL), nitric oxide (96.58 μg/mL), and hydroxyl (58.38 μg/mL) radical scavenging activities. The MIC of SOR-AgNPs was lower in gram-positive bacteria. The SOR-AgNPs have displayed efficient inhibitory activity against α-amylase, with an EC50 of 58.38 μg/mL. Analysis of capping protein around the SOR-AgNPs showed a molecular weight of 30 kDa.Discussion: These SOR-AgNPs could be used as antibacterial and antidiabetic drugs in the future as it is cheap, non-toxic, and environmentally friendly. Bio-fabricated AgNPs had a significant impact on bacterial strains and could be used as a starting point for future antibacterial drug development.
In the present investigation, a metal-chelating bioactive peptide was derived from Citrullus lanatus seed milk fermented with Lactococcus lactis. The cationic fermented milk peptide (FMP) thus obtained was purified using the HiTrap-chelating column followed by rpHPLC. The FMP possessed the ability to chelate multiple divalent cations like Cu 2+ , Ca 2+ , and Fe 2+ with 86.81%, 61.04%, and 24.32% of chelation respectively and further it exhibited 78.03% of DPPH free radical scavenging activity. Interaction of FMP with metal ions was assessed by change in the absorption spectra and was analyzed by ultraviolet-visible and fluorescence spectroscopy. The FMP-metal complexes were found stable at simulated gastric conditions. In vitro analysis using intestinal Caco-2 cell lines revealed that there was an increase in metal bioavailability in the presence of the FMP and was least influenced by the addition of a dietary inhibitor, phytic acid. By LC-MS analysis the molecular mass of FMP was found to be 11.6 kD and it contains oxygen-rich and nitrogen-rich amino acids that favor the metal chelation. In our study, we have found that the fermented C. lanatus seed milk can serve as a potential functional food with bioenhancer peptides that increase metal bioavailability and enhance human health.
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