AbstractThe frequency of Bacillus subtilis infection such as pneumonia pan-opthalmitis, visceral abscess or musculoskeletal infection etc. complications following bacteremia, meningitis in children & the infection associated with majority of motor vehicle accidents associated with trauma & gun shoot injury. Antibiotics which appear especially useful in the treatment of Bacillus. infection are clindamycin and vancomycin to which vast majority of strains are susceptible in vitro. Our objective is to test the synthesized peptidomimetics with the efforts mainly directed towards the identification of antibacterial compounds against recurrent septicemia infection. Six peptidomimetics namely G-A-L-D (C60-soot Glu-ala-leu-Asp), D-P-F (C60-soot Asp-pro-Phe), I-R (C60-soot Ile-Arg), L-R (C60-soot leu-Arg), E-R (C60-soot Glu-Arg), D-E (C60-soot Asp-Glu), the column eluted compounds were tested for disc diffusion using gram positive Bacillus Subtilis strains at different concentrations predicted by pH and inhibitory concentrations. I-R (C60-soot Ile-Arg), & D-E (C60-soot Asp-Glu) was found to be very effective along with 5 compounds against Bacillus Subtilis strain tested. Maximum activity 100 µg/ml for synthesized peptidomimetics with the corresponding zonal inhibition diameter (11 mm; 11 mm; 14 mm; 11 mm; 11 mm; 14 mm) against Bacillus subtilis strain. This is the first evidence based report that proves I-R (C60-soot Ile-Arg) & D-E (C60-soot Asp-Glu) has shown antibacterial action against gram positive strains of Bacillus Subtilis against recurrent septicemia infection

01 Feb 2017·ChemistryOpenQ3 · CHEMISTRY

Insights into the Binding of Cyclic RGD Peptidomimetics to α₅β₁Integrin by using Live-Cell NMR And Computational Studies

Q3 · CHEMISTRY

ArticleOA

Author: Arosio, Daniela ; Piarulli, Umberto ; Tringali, Cristina ; Gennari, Cesare ; Potenza, Donatella ; Pignataro, Luca ; Guzzetti, Ileana ; Vasile, Francesca ; Belvisi, Laura ; Civera, Monica

The interaction of a small library of cyclic DKP-RGD peptidomimetics with α₅β₁ integrin has been investigated by means of an integrated experimental and computational approach. Bioaffinity NMR techniques, including saturation transfer difference (STD) and transferred NOESY, were applied to the ligands in a suspension of intact MDA-MB-231 breast cancer cells, in which integrin α₅β₁ is highly expressed. The NMR data were compared with the docking calculations of the RGD ligands in the crystal structure of the α₅β₁ binding site, and were integrated with competitive binding assays to the purified α₅β₁ integrin. Ligand binding epitopes involve protons of both the RGD moiety and the DKP scaffold, although the stereochemistry and the functionalization of the DKP scaffold as well as the macrocycle conformation determine a great variability in the interaction. The ligand showing the highest number of STD signals is also the most potent α₅β₁ ligand of the series, displaying a nanomolar IC₅₀ value.

04 Dec 2015·Current Medicinal ChemistryQ2 · MEDICINE

Current Advances in L-DOPA and DOPA-Peptidomimetics: Chemistry, Applications and Biological Activity

Q2 · MEDICINE

Review

Author: Rotelli, Luca ; Tortolini, Silvia ; Botta, Giorgia ; Saladino, Raffaele ; Bizzarri, Bruno Mattia

L-3,4-Dihydroxyphenylalanine [2-amino-3-(3,4-dihydroxyphenyl) propanoic acid (L-DOPA) is a natural constituent of animal and plant tissue derived from post-translational modification of the amino acid tyrosine. L-DOPA is modified during metabolism to catecholamine neurotransmitters, noradrenaline and adrenaline, which are characterized by different biological activities. L-DOPA has been the first drug of choice in the therapy of Parkinson's disease that is a progressive neurodegenerative disorder involving the loss of dopaminergic neurons of substantia nigra pars compacta. The social and economic impact of these diseases is very high due to the progressive aging of the population. This review focuses on the biological effect of LDOPA, as well as on the synthesis of L-DOPA derivatives and their application in central nervous system diseases. Among them, L-DOPA-containing peptides (L-DOPA-Pep) show important biological and pharmacological activities. For example, L-DOPA analogues of the alpha-factor interact with models of the G protein-coupled receptor, inhibit the oxidation of low-density lipoproteins, and are used for improving L-DOPA absorption in long-term treatment of Parkinson's disease and as skin moisturizer in cosmetic compositions. Moreover, L-DOPA residues in proteins provide reactive tools for the preparation of adhesives and coatings materials. Usually, L-DOPA-Pep is prepared by traditional liquid or solid state procedures starting from simple amino acids. Recently, selective side-chain modifications of pre-formed peptides have also been reported both for linear and branched peptides. Here, we describe the recent advances in the synthesis of L-DOPA and dopa-peptidomimetics and their biological and pharmacological activities, focusing the attention on new synthetic procedures and biological mechanism of actions.

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