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Gentamicin is an aminoglycoside antibiotic which accumulates by endocytosis in the lysosomes of the proximal tubular cells of the kidney and induces apoptosis (El Mouedden et al. 2000, Antimicrob. Chemother Agents; 44:6665-675). This process, depending on the gentamicin concentration, was reproduced on renal cells like LL-C PK1 (El Mouedden et al. 2000, Toxicol. Sci. 56:229-239).
Inside lysosomes, iron could form with gentamicin a complex able to oxydise the lipids or to take part involved in the formation of free radicals. These processes could be responsible for the permeabilisation of the lysosomal membrane, an event susceptible to activate mitochondria and pro-caspase 3 (Servais et al submitted).
The objective of this work was to determine if deferoxamine, a chelator of iron which accumulates preferentially in the lysosomes, could decrease the cellular toxicity induced by gentalin on LLC-PK1 cells as well as the number of cells in apoptosis
These two parameters have been investigated by following the release of lactase deshydrogenase and by counting the number of apoptotic cells after coloration with the DAPI, a known fluorescent marker which intercales in the DNA.
The results indicate a partial protective effect of the deferoxamine when cells are preincubated for 1h or 3h with deferoxamine 25μM and when the iron chelator is maintained for all the duration of incubation with gentamicin (2mM). This partial protective effect probably does not result from a modification of the accumulation of gentamicin. The conditions of use of the deferoxamine must however be strictly controlled due to its own cytotoxic and apoptotic effect.
The mechanisms involved in the protective effect of the deferoxamine apoptosis induced by gentamicin have to be further explored. The deferoxamine would prevent the destabilization of the lysosomial membrane following the formation of the gentamicin/iron-complex or the direct generation of oxygenated radicals, then preventing the release within the cytosol of lysosomal proteases and/or gentamicin, that would then activate mitochondria and the cascade of caspases

Gentamicins --- Deferoxamine --- Aminoglycosides --- Apoptosis

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Iron Overload --- Iron Chelating Agents --- Deferoxamine --- Blood Transfusion --- Chelation Therapy --- Anemia --- diagnosis --- therapeutic use --- therapeutic use --- adverse effects --- etiology

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The book starts with the editors’ preface summarizing the contributions of each of the following thirteen articles dealing with chemical and pharmacological aspects of the molecular modulators of the oxidative stress in regard to various therapeutic approaches in cardiovascular and neurodegenerative diseases, cancer, and diabetes. The seven articles present data from original research studies enlightening the roles and mechanisms of action of small molecular weight compounds (natural and synthetic; ascorbic acid/vitamin C, deferoxamine, N-acetylcysteine, MitoVitE, α-tocopherol, trolox, and ezetimibe) or proteins (SIRT3) in modulation of oxidative stress. In the six review papers, the authors present and discuss the possible therapeutic potential of novel approaches and compounds that are promising and deserve further investigation, in modulation of oxidative stress.

Research & information: general --- Biology, life sciences --- ascorbic acid --- deferoxamine --- N-acetylcysteine --- ischemia/reperfusion --- cardiac fibroblasts --- reactive oxygen species --- photobiomodulation --- reactive oxygen species (ROS) --- nuclear factor kappa-light-chain-enhancer of activated B cells (NF-кB) --- cancer --- diabetes --- wound healing --- glucose --- pentose phosphate pathway --- NADPH --- redox balance --- glycogen --- glycolysis --- stress resistance --- insulin resistance --- immunomodulation --- inflammation --- olive tree --- oxidative stress --- secoirioids --- sirtuin 3 --- high fat diet --- sex differences --- mice --- metabolic stress --- antioxidants --- ADHD --- Nrf2 --- NRF2-KEAP1 --- ROS --- cancer metabolism --- antioxidant --- cancer therapy --- chemoresistance --- radioresistance --- sepsis --- MitoVitE --- mitochondria --- gene expression --- cytokines --- mRNA --- vitamin C --- folic acid --- one-carbon metabolism --- C2C12 cells --- metabolomics --- mass spectrometry --- type 2 diabetes --- dipeptidyl peptidase-4 inhibitors --- biomarkers --- ER stress --- Ezetimibe --- ischemia-reperfusion --- ionizing radiation --- liver --- hydroperoxide --- epigenetics --- miR7/MAFG/Nrf2 axe --- ascorbic acid --- deferoxamine --- N-acetylcysteine --- ischemia/reperfusion --- cardiac fibroblasts --- reactive oxygen species --- photobiomodulation --- reactive oxygen species (ROS) --- nuclear factor kappa-light-chain-enhancer of activated B cells (NF-кB) --- cancer --- diabetes --- wound healing --- glucose --- pentose phosphate pathway --- NADPH --- redox balance --- glycogen --- glycolysis --- stress resistance --- insulin resistance --- immunomodulation --- inflammation --- olive tree --- oxidative stress --- secoirioids --- sirtuin 3 --- high fat diet --- sex differences --- mice --- metabolic stress --- antioxidants --- ADHD --- Nrf2 --- NRF2-KEAP1 --- ROS --- cancer metabolism --- antioxidant --- cancer therapy --- chemoresistance --- radioresistance --- sepsis --- MitoVitE --- mitochondria --- gene expression --- cytokines --- mRNA --- vitamin C --- folic acid --- one-carbon metabolism --- C2C12 cells --- metabolomics --- mass spectrometry --- type 2 diabetes --- dipeptidyl peptidase-4 inhibitors --- biomarkers --- ER stress --- Ezetimibe --- ischemia-reperfusion --- ionizing radiation --- liver --- hydroperoxide --- epigenetics --- miR7/MAFG/Nrf2 axe

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This Special Issue, entitled "Synthetic Peptides and Peptidomimetics: From Basic Science to Biomedical Applications", has included both reviews and original research contributions focused on the chemical design and biomedical applications of structurally modified bioactive peptides. The papers collected show how successful this class of molecules still is, both as model molecules for studying the structure of proteins and as potential therapeutics and diagnostics, and also as laboratory tools for advanced basic and applied studies. The large scientific community working in this field is in fact very active and productive, and is making the most of the potential and versatility of these molecules to generate increasingly interesting and innovative molecules of therapeutic interest and to understand the fundamental molecular mechanisms of life.

Research & information: general --- Biology, life sciences --- polymers --- peptidomimetics --- AFM --- transfection --- molecular modelling --- peptide --- α-helix --- hydrocarbon stapling --- ring-closing metathesis --- i,i + 1 staple --- X-ray structure --- deferoxamine --- RGD peptides --- integrins --- radiodiagnostics --- PET imaging --- retro-inverso peptides --- anticancer peptides --- drug delivery --- peptide antigens --- Aβ --- IAPP --- antimicrobial peptides --- peptides --- diagnostic --- ELISA --- microarray --- PET --- SPECT --- imaging diagnostic --- non-imaging diagnostic --- amphiphilic peptides --- non-viral gene delivery --- nanocarrier --- peptide self-assemblies --- stimuli responsive --- SARS-CoV-2 --- FRET --- molecular docking --- molecular dynamics --- MM-GBSA --- drug repurposing --- antiviral --- cancer --- cyclic peptide --- integrin --- αvβ3 --- ALOS4 --- melanoma --- fluorescent peptide --- environment-sensitive fluorophore --- peptide labeling --- luciferin --- membrane-binding peptide --- antimicrobial peptide --- antitumor peptide --- RGD peptide --- antiproliferative activity --- chirality --- conformational analysis --- density functional theory (DFT) --- ferrocene --- hydrogen bonds --- peptidomimetic --- X-ray --- protein–protein interactions (PPIs) --- voltage-gated Na+ (Nav) channels --- fibroblast growth factor 14 (FGF14) --- medium spiny neurons (MSNs) --- nucleus accumbens (NAc) --- neurotherapeutics --- cyclophilin A (CypA) --- apoptosis-inducing factor (AIF) --- human neuroblastoma SH-SY5Y cells --- staurosporine-mediated cell death --- AIF(370-394) peptide --- caspase-3 --- PARP --- antifungal --- antibacterial --- peptide-based therapies --- synthetic peptides --- polymers --- peptidomimetics --- AFM --- transfection --- molecular modelling --- peptide --- α-helix --- hydrocarbon stapling --- ring-closing metathesis --- i,i + 1 staple --- X-ray structure --- deferoxamine --- RGD peptides --- integrins --- radiodiagnostics --- PET imaging --- retro-inverso peptides --- anticancer peptides --- drug delivery --- peptide antigens --- Aβ --- IAPP --- antimicrobial peptides --- peptides --- diagnostic --- ELISA --- microarray --- PET --- SPECT --- imaging diagnostic --- non-imaging diagnostic --- amphiphilic peptides --- non-viral gene delivery --- nanocarrier --- peptide self-assemblies --- stimuli responsive --- SARS-CoV-2 --- FRET --- molecular docking --- molecular dynamics --- MM-GBSA --- drug repurposing --- antiviral --- cancer --- cyclic peptide --- integrin --- αvβ3 --- ALOS4 --- melanoma --- fluorescent peptide --- environment-sensitive fluorophore --- peptide labeling --- luciferin --- membrane-binding peptide --- antimicrobial peptide --- antitumor peptide --- RGD peptide --- antiproliferative activity --- chirality --- conformational analysis --- density functional theory (DFT) --- ferrocene --- hydrogen bonds --- peptidomimetic --- X-ray --- protein–protein interactions (PPIs) --- voltage-gated Na+ (Nav) channels --- fibroblast growth factor 14 (FGF14) --- medium spiny neurons (MSNs) --- nucleus accumbens (NAc) --- neurotherapeutics --- cyclophilin A (CypA) --- apoptosis-inducing factor (AIF) --- human neuroblastoma SH-SY5Y cells --- staurosporine-mediated cell death --- AIF(370-394) peptide --- caspase-3 --- PARP --- antifungal --- antibacterial --- peptide-based therapies --- synthetic peptides

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This Special Issue, entitled "Synthetic Peptides and Peptidomimetics: From Basic Science to Biomedical Applications", has included both reviews and original research contributions focused on the chemical design and biomedical applications of structurally modified bioactive peptides. The papers collected show how successful this class of molecules still is, both as model molecules for studying the structure of proteins and as potential therapeutics and diagnostics, and also as laboratory tools for advanced basic and applied studies. The large scientific community working in this field is in fact very active and productive, and is making the most of the potential and versatility of these molecules to generate increasingly interesting and innovative molecules of therapeutic interest and to understand the fundamental molecular mechanisms of life.

polymers --- peptidomimetics --- AFM --- transfection --- molecular modelling --- peptide --- α-helix --- hydrocarbon stapling --- ring-closing metathesis --- i,i + 1 staple --- X-ray structure --- deferoxamine --- RGD peptides --- integrins --- radiodiagnostics --- PET imaging --- retro-inverso peptides --- anticancer peptides --- drug delivery --- peptide antigens --- Aβ --- IAPP --- antimicrobial peptides --- peptides --- diagnostic --- ELISA --- microarray --- PET --- SPECT --- imaging diagnostic --- non-imaging diagnostic --- amphiphilic peptides --- non-viral gene delivery --- nanocarrier --- peptide self-assemblies --- stimuli responsive --- SARS-CoV-2 --- FRET --- molecular docking --- molecular dynamics --- MM-GBSA --- drug repurposing --- antiviral --- cancer --- cyclic peptide --- integrin --- αvβ3 --- ALOS4 --- melanoma --- fluorescent peptide --- environment-sensitive fluorophore --- peptide labeling --- luciferin --- membrane-binding peptide --- antimicrobial peptide --- antitumor peptide --- RGD peptide --- antiproliferative activity --- chirality --- conformational analysis --- density functional theory (DFT) --- ferrocene --- hydrogen bonds --- peptidomimetic --- X-ray --- protein–protein interactions (PPIs) --- voltage-gated Na+ (Nav) channels --- fibroblast growth factor 14 (FGF14) --- medium spiny neurons (MSNs) --- nucleus accumbens (NAc) --- neurotherapeutics --- cyclophilin A (CypA) --- apoptosis-inducing factor (AIF) --- human neuroblastoma SH-SY5Y cells --- staurosporine-mediated cell death --- AIF(370-394) peptide --- caspase-3 --- PARP --- antifungal --- antibacterial --- peptide-based therapies --- synthetic peptides