Nicola Borbone

Nicola Borbone
University of Naples Federico II | UNINA · Department of Pharmacy

Pharmaceutical Chemistry

About

167
Publications
17,781
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2,146
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Introduction
My research interests are in the field of nucleic acids chemistry and biology. The scientific work is focused on DNA quadruplexes formed by aptamers, telomeres, and synthetic G-rich oligonucleotides. The biological role played by these structures, as well as the potential application as biosensors or electronic nanodevices is currently investigated.
Additional affiliations
October 2019 - present
University of Naples Federico II
Position
  • Professor (Associate)
March 2006 - October 2019
University of Naples Federico II
Position
  • Researcher
January 2002 - December 2012
University of Naples Federico II
Education
November 1999 - November 2002
University of Naples Federico II
Field of study
  • Isolation and Structural Elucidation of Natural Compounds

Publications

Publications (167)
Article
Full-text available
Redox‐responsive silica drug delivery systems are synthesized by aeco‐friendly diatomite source to achieve on‐demand release of peptide nucleic acid (PNA) in tumor reducing microenvironment, aiming to inhibit the immune checkpoint programmed cell death 1 receptor/programmed cell death receptor ligand 1 (PD‐1/PD‐L1) in cancer cells. The nanoparticle...
Article
Full-text available
1,3-diaryl-2-propanone derivatives are synthetic compounds used as building blocks for the realization not only of antimicrobial drugs but also of new nanomaterials thanks to their ability to self-assemble in solution and interact with nucleopeptides. However, their ability to interact with proteins is a scarcely investigated theme considering the...
Article
i-Motifs, also known as i-tetraplexes, are secondary structures of DNA occurring in cytosine-rich oligonucleotides (CROs) that recall increasing interest in the scientific community for their relevance in various biological processes and DNA nanotechnology. This study reports the design of new structurally modified CROs, named Double-Ended-Linker-C...
Article
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Trans-polydatin (tPD), the 3-β-D-glucoside of the well-known nutraceutical trans-resveratrol, is a natural polyphenol with documented anti-cancer, anti-inflammatory, cardioprotective, and immunoregulatory effects. Considering the anticancer activity of tPD, in this work, we aimed to explore the binding properties of this natural compound with the G...
Article
Full-text available
The recent development of mRNA vaccines against the SARS-CoV-2 infection has turned the spotlight on the potential of nucleic acids as innovative prophylactic agents and as diagnostic and therapeutic tools. Until now, their use has been severely limited by their reduced half-life in the biological environment and the difficulties related to their t...
Article
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We herein report an innovative antisense approach based on Peptide Nucleic Acids (PNAs) to down-modulate CD5 expression levels in chronic lymphocytic leukemia (CLL). Using bioinformatics tools, we selected a 12-mer tract of the CD5 mRNA as the molecular target and synthesized the complementary and control PNA strands bearing a serine phosphate dipe...
Article
Full-text available
Three-dimensional chitosan-gallic acid complexes were proposed and prepared for the first time by a simple adsorption process of gallic acid (GA) on three-dimensional chitosan structures (3D chitosan). Highly porous 3D devices facilitate a high GA load, up to 2015 mmol/kg at pH 4.0. The preservation of the redox state of GA released from 3D chitosa...
Article
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Digital drug design reveals DNA aptamers binding SARS‐CoV‐2: A hybrid in silico et vitro approach, structure and interaction‐based drug design, has been developed to create highly specific DNA aptamers for the receptor‐binding domain of the SARS‐CoV‐2 spike protein. The structure and binding affinity of the aptamers were validated by small‐angle X‐...
Article
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Aptamer selection against novel infections is a complicated and time-consuming approach. Synergy can be achieved by using computational methods together with experimental procedures. This study aims to develop a reliable methodology for a rational aptamer in silico et vitro design. The new approach combines multiple steps: (1) Molecular design, bas...
Article
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Cyanobacteria require iron for growth and often inhabit iron-limited habitats, yet only a few siderophores are known to be produced by them. We report that cyanobacterial genomes frequently encode PKS/NRPS biosynthetic pathways for synthesis of lipopeptides featuring β -hydroxyaspartate ( β -OH-Asp), a residue known to be involved in iron chelation...
Chapter
In this paper, different nanostructured semiconductors with advanced properties are explored for the realization of both optical and electrical biosensors for DNA detection. A hybrid sensor constituted by graphene oxide (GO) covalently grafted on a porous silicon (PSi) matrix is realized. A peptide nucleic acid (PNA) probe, able to recognize its co...
Article
Full-text available
Cystic fibrosis (CF) is characterized by an airway obstruction caused by a thick mucus due to a malfunctioning Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) protein. The sticky mucus restricts drugs in reaching target cells limiting the efficiency of treatments. The development of new approaches to enhance drug delivery to the lungs re...
Article
Full-text available
Zinc oxide nanowires (ZnONWs) are largely used in biosensing applications due to their large specific surface area, photoluminescence emission and electron mobility. In this work, the surfaces of ZnONWs are modified by covalent bioconjugation of a peptidic nucleic acid (PNA) probe whose sequence is properly chosen to recognize a complementary DNA (...
Article
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Coronaviruses (CoVs) are positive-sense RNA enveloped viruses, members of the family Coronaviridae, that cause infections in a broad range of mammals including humans. Several CoV species lead to mild upper respiratory infections typically associated with common colds. However, three human CoV (HCoV) species: Severe Acute Respiratory Syndrome (SARS...
Chapter
Full-text available
Proteins are a class of intriguing biomolecules since they are involved in major biological and vital processes. As a result of their variety and complexity, proteins are widely used in biotechnological applications and they are the most used macromolecules in the biosensing field. Proteins orientation on the transducer's substrate is crucial for b...
Conference Paper
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Cyclic ADP-ribose (cADPR, 1, Figure 1) is a naturally occurring metabolite of NAD+capable of mobilizing Ca2+ ions from intracellular stores. [...]
Preprint
Full-text available
Cystic Fibrosis (CF) is characterized by an airway obstruction caused by a thick mucus due to a malfunctioning Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) protein. The sticky mucus restricts drugs in reaching target cells limiting the efficiency of treatments. The development of new approaches to enhance drug delivery to the lungs re...
Article
Full-text available
Peptide nucleic acid (PNA) is a synthetic DNA mimic that outperforms the properties of traditional oligonucleotides (ONs). On account of its outstanding features, such as remarkable binding affinity towards complementary DNA or RNA as well as high thermal and chemical stability, PNA has been proposed as a valuable alternative to the ON probe in gen...
Preprint
Peptide nucleic acid (PNA) is a synthetic DNA mimic that outperforms the properties of traditional oligonucleotides (ONs). On account of its outstanding features, such as remarkable binding affinity towards complementary DNA or RNA as well as high thermal and chemical stability, PNA has been proposed as a valuable alternative to the ON probe in gen...
Article
Full-text available
Mycalin A, a polybrominated C15 acetogenin isolated from the encrusting sponge Mycale rotalis, displays an antiproliferative activity on human melanoma (A375) and cervical adenocarcinoma (HeLa) cells and induces cell death by an apoptotic mechanism. Various analogues and degraded derivatives of the natural substance have been prepared. A modificati...
Article
The interest in DNA based nanostructures arises from their potential applications in diagnostics and drug delivery and in the development of new hybrid and conducting materials. Guanine-rich oligonucleotides can multimerize forming long and stable supramolecular structures, known as G-wires, based on the G-quadruplex (G4) motif. Herein, we report a...
Article
Full-text available
Herein, we reported on the synthesis of a novel Pt(II) neutral complex having as ligand the nucleoside tubercidin, a potent anti-tumor agent extracted from the bacterium Streptomyces Tubercidicus. In detail, the chelation of the metal by a diamine linker installed at C6 purine position of tubercidin assured the introduction of a cisplatin-like unit...
Article
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Marine sponges, a well-documented prolific source of natural products, harbor highly diverse microbial communities. Their extracts were previously shown to contain quorum sensing (QS) signal molecules of the N-acyl homoserine lactone (AHL) type, known to orchestrate bacterial gene regulation. Some bacteria and eukaryotic organisms are known to prod...
Poster
Chitosan (CS) is a cationic linear polysaccharide consisting of D-glucosamine linked with N-acetyl Dglucosamine residues by β-1-4-linkages. It can be obtained by the deacetylation of chitin, a polymer found in the exoskeleton of crustaceans and insects. Due to its biodegradability, biocompatibility, non-toxicity, and low immunogenicity, chitosan is...
Article
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Mature microRNAs are short non-coding RNA sequences which upon incorporation into the RISC ribonucleoprotein complex, play a crucial role in regulation of gene expression. However, miRNAs can exist within the cell also as free molecules fulfilling their biological activity. Therefore, it is emerging that in addition to sequence even the structure a...
Article
Full-text available
ε-poly-l-Lysine (ε-PLL) peptide is a product of the marine bacterium Bacillus subtilis with antibacterial and anticancer activity largely used worldwide as a food preservative. ε-PLL and its synthetic analogue α,ε-poly-l-lysine (α,ε-PLL) are also employed in the biomedical field as enhancers of anticancer drugs and for drug and gene delivery applic...
Preprint
Full-text available
Marine sponges, a well documented prolific source of natural products, harbors numerous microbial communities believed to possess N-acyl homoserine lactones (AHLs) mediated Quorum sensing (QS) as one of the mechanisms of interaction. Bacteria and eukaryotic organisms are known to produce molecules that can interfere with QS signaling, thus affectin...
Article
Full-text available
Herein, we report on the synthesis of a small set of linear precursors of an inosine analogue of cyclic ADP-ribose (cADPR), a second messenger involved in Ca2+ mobilization from ryanodine receptor stores firstly isolated from sea urchin eggs extracts. The synthesized compounds were obtained starting from inosine and are characterized by an N1-alkyl...
Article
Full-text available
Aptamers are artificial nucleic acid ligands identified and obtained from combinatorial libraries of synthetic nucleic acids through the in vitro process SELEX (systematic evolution of ligands by exponential enrichment). Aptamers are able to bind an ample range of non-nucleic acid targets with great specificity and affinity. Devices based on aptame...
Article
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G-quadruplexes (G4s) are unusual secondary structures of DNA occurring in guanosine-rich oligodeoxynucleotide (ODN) strands that are extensively studied for their relevance to the biological processes in which they are involved. In this study, we report the synthesis of a new kind of G4-forming molecule named double-ended-linker ODN (DEL-ODN), in w...
Article
The B-cell lymphoma 2 (Bcl-2) gene encodes for an antiapoptotic protein associated with the onset of many human tumors. Several oligonucleotides (ONs) and ON analogues are under study as potential tools to counteract the Bcl-2 expression. Among these are Peptide Nucleic Acids (PNAs). The absence of charges on PNA backbones allows the formation of P...
Article
Full-text available
The development of new strategies for enhancing drug delivery to the brain represents a major challenge in treating cerebral diseases. In this paper, we report on the synthesis and structural characterization of a biocompatible nanoparticle (NP) made up of poly(lactic-co-glycolic acid) (PLGA)-polyethylene glycol (PEG) co-polymer (namely PELGA) func...
Article
Full-text available
Herein, we reported on the synthesis of cpIPP, which is a new structurally-reduced analogue of cyclic ADP-ribose (cADPR), a potent Ca2+-releasing secondary messenger that was firstly isolated from sea urchin eggs extracts. To obtain cpIPP the "northern" ribose of cADPR was replaced by a pentyl chain and the pyrophosphate moiety by a phophono-phosph...
Article
By combining the ability of short G-rich oligodeoxynucleotides (ODNs) containing the sequence 5'CGGA3' to form higher-order G-quadruplex (G4) complexes with the tetra-end-linked (TEL) concept to produce aptamers targeting the HIV envelope glycoprotein 120 (gp120), three new TEL-ODNs (1–3) having the sequence 5'CGGAGG3' were synthesized with the aim...
Article
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This article describes the synthesis of Thy-(Phe-Phe) and Thy-(Tyr-Tyr), two thymine-bearing dipeptides based on L-phenylalanine and L-tyrosine, the circular dichroism (CD), UV and dynamic light scattering (DLS) characterization of their self-assemblies, and a CD study of their interaction with nucleic acids (using homoadenine DNA and RNA) and seru...
Article
Herein, we report on the synthesis and the evaluation of preliminary antitumor properties of a small collection of platinum(II) complexes in which a cisplatin-like unit is tethered to 7-deazaadenosine through linear alkyl chains (from 1 to 6 carbon atoms) installed at the C6 purine position. The complexation is performed by exploiting the reactivit...
Article
Full-text available
Cystic Fibrosis (CF) is one of the most common life shortening conditions in Caucasians. CF is caused by mutations in the CF Transmembrane Conductance Regulator (CFTR) gene which result in reduced or altered CFTR functionality. Several microRNAs (miRNAs) downregulate the expression of CFTR, thus causing or exacerbating the symptoms of CF. In this c...
Article
Full-text available
Obtaining DNA nanostructures with potential applications in drug discovery, diagnostics, and electronics in a simple and affordable way represents one of the hottest topics in nanotechnological and medical sciences. Herein, we report a novel strategy to obtain structurally homogeneous DNA G-wire nanostructures of known length, starting from the sho...
Article
The interaction of the porphyrin derivative H2TCPPSpm4, having spermine pendants in the four meso positions, with the G-quadruplex (GQ) structure formed by the DNA aptamer TGGGAG has been investigated by means of UV, electronic circular dichroism and PAGE studies. The results here reported demonstrate that porphyrin derivative is capable of stabili...
Article
Full-text available
A thorough investigation of the minor oxidation products of two penta-tetrahydrofuran compounds with pyridinium chlorochromate has been carried out. Isolation of ring-B oxygenated spiroketal and degradation products, including polycyclic mono- and bis-lactone compounds, supports the previously postulated involvement of cyclic enolether intermediate...
Article
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The title compound, C 12 H 20 N 4 O 5 , crystallizes in the monoclinic space group P 2 1 , with four crystallographically independent molecules in the asymmetric unit. The four molecules have a very similar conformation that is basically determined by the formation of two intramolecular hydrogen bonds between the amino NH 2 donors and the carbonyl...
Article
Background: G-quadruplex DNA is involved in many physiological and pathological processes. Both clinical and experimental studies on DNA G-quadruplexes are slowed down by their enzymatic instability. In this frame, more stable chemically modified analogs are needed. Methods: The bis-end-linked-(gggt)2 PNA molecule (BEL-PNA) was synthesized using...
Article
Human α-thrombin (TB) is a serine protease with a crucial role in coagulation and hemostasis. The monitoring of TB level in blood serum could be of great importance in order to prevent serious damages to human health. In this work, an aptasensor is realized by in situ synthesis of a 17-mer Thrombin Binding Aptamer analogue (TBATT) on silanized macr...
Article
By using a new rapid screening platform set on molecular docking simulations and fluorescence quenching techniques, three new anti-HIV aptamers targeting the viral surface glycoprotein 120 (gp120) were selected, synthesized and assayed. The use of the short synthetic fluorescent peptide V35-Fluo mimicking the V3 loop of gp120, as the molecular targ...
Article
Full-text available
Efficient biorecognition of thrombin (TB), a serine protease with crucial role in physiological and pathological blood coagulation, is a hot topic in medical diagnostics. In this work, we investigate the ability of synthetic thrombin aptamer (TBA), immobilized on a gold substrate, to bind thrombin by two different label-free techniques: the quartz...
Article
Full-text available
Cyclic N (1)-pentylinosine monophosphate (cpIMP), a novel simplified inosine derivative of cyclic ADP-ribose (cADPR) in which the N (1)-pentyl chain and the monophosphate group replace the northern ribose and the pyrophosphate moieties, respectively, was synthesized. The role played by the position of the phosphate group in the key cyclization step...