Medicinal and Pharmaceutical Chemistry; Organic Synthesis; Drug Discovery; Heterocyclic Chemistry; Cell Biology; Pharmacology ; Mass Spectrometry ; High-Performance Liquid Chromatography ;Photocatalysis ; Photochemistry
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Scopus Publications
Scopus Publications
Nanoparticle based siRNA therapeutics for ovarian cancer overcoming drug resistance and future directions Roberta Di Fonte, Isabella Bolognino, Federica Sommonte, Simona Serratì, Rossella Fasano, Ilaria Arduino, Rosa Maria Iacobazzi, Nunzio Denora, Paola Perego, Giacomina Rossi, Diego Tosi, Letizia Porcelli, Amalia Azzariti Discover Nano, 2026 Recently, nanomedicine has made significant advancements, opening exciting new possibilities for treating a wide range of diseases. In this field, novel drug delivery systems (DDSs) are among the most noteworthy developments. The primary objective of DDSs is to ensure that treatments reach the intended targets while minimising adverse effects. In this context, nanoparticle (NP)-based DDSs have shown remarkable potential in oncology, particularly for ovarian cancer (OC), the deadliest type of gynecological cancer due to its mortality rate and the occurrence of treatment resistance. In this review, we provide a comprehensive description of the different types of NPs being explored for OC treatment, with a special emphasis on their involvement in delivering small interfering RNA (siRNA) treatments. We review various NP platforms shedding light on how they enhance drug stability, enable controlled release, and reduce toxicity. We also explore the techniques used to synthesise these NPs, emphasizing how modifying their physical and chemical properties can improve their ability to target cancer cells effectively. We also discuss the importance of 3D-tumor models, which more accurately replicate the complexity of real tumors. This enables us to examine the ability of NPs to penetrate tumors and consequently therapies are delivered in a setting that really resembles real-life situations. Recent advances in RNA-based therapeutics through DDS offer a highly targeted approach to shutting down oncogenes and drug resistance mechanisms, making them a powerful strategy to complement conventional treatments. The analysis of clinical trials results indicate a requirement for further studies in order to refine the clinical applications of drugs based on siRNAs. Despite the ongoing challenges, NP-based DDSs are paving the way for more precise and personalized OC treatments.
Comparison of Ten Metal-Doped LaFeO3 Samples on Photocatalytic Degradation of Antibiotics in Water under Visible Light: Role of Surface Area and Aqueous Phosphate Ions Isabella Bolognino, Renato Pelosato, Giuseppe Marcì, Isabella Natali Sora Molecules, 2023 Doping semiconducting oxides, such as LaFeO3 (LF), with metallic elements is a good strategy to improve the performance of photocatalysts. In this study, LF and ten different nanopowders metal-doped at the La or Fe site of LaFeO3 were evaluated in the photocatalytic degradation of ciprofloxacin (CP) and oxytetracycline (OTC). The following metals were used in the doping (mol%) process of LF: Pd 3% and 5%; Cu 10%; Mg 5%, 10%, and 20%; Ga 10%; Y 10% and 20%; and Sr 20%. The doped samples were synthetized using a citrate auto-combustion technique. From the X-ray diffraction (XRD) data, only a single crystalline phase, namely an orthorhombic perovskite structure, was observed except for trace amounts of PdO in the sample with Pd 5%. The specific surface area (SSA) ranged from 9 m2 g−1 (Ga 10%) to 20 m2 g−1 (Mg 20%). SEM images show that all samples were constituted from agglomerates of particles whose sizes ranged from ca. 20 nm (Mg 20%) to ca. 100 nm (Pd 5%). Dilute aqueous solutions (5 × 10−6 M) prepared for both CP and OTC were irradiated for 240 min under visible-light and in the presence of H2O2 (10−2 M). The results indicate a 78% removal of OTC with Cu 10% doped LF in a phosphate buffer (pH = 5.0). The degradation of CP is affected by pH and phosphate ions, with 78% (in unbuffered solution) and 54% (in phosphate buffer, pH = 5.0) removal achieved with Mg 10% doped LF. The reactions follow a pseudo-first order kinetic. Overall, this study is expected to deepen the assessment of photocatalytic activity by using substrates with different absorption capacities on photocatalysts.
Applications of Heterogeneous Photocatalysis to the Degradation of Oxytetracycline in Water: A Review Renato Pelosato, Isabella Bolognino, Francesca Fontana, Isabella Natali Sora Molecules, 2022 Photocatalytic processes are being studied extensively as potential advanced wastewater treatments for the removal of pharmaceuticals, pesticides and other recalcitrant micropollutants from the effluents of conventional wastewater treatment plants (WWTPs). Oxytetracycline (OTC) is a widespread antibiotic which is frequently detected in surface water bodies as a recalcitrant and persistent micropollutant. This review provides an update on advances in heterogeneous photocatalysis for the degradation of OTC in water under UV light, sunlight and visible-light irradiation. Photocatalysts based on pure semiconducting oxides are rarely used, due to the problem of rapid recombination of electron–hole pairs. To overcome this issue, a good strategy could be the coupling of two different semiconducting compounds with different conduction and valence bands. Several methods are described to enhance the performances of catalysts, such as doping of the oxide with metal and/or non-metal elements, surface functionalization, composites and nano-heterojunction. Furthermore, a discussion on non-oxidic photocatalysts is briefly provided, focusing on the application of graphene-based nanocomposites for the effective treatment of OTC.
Enantiomeric Separation and Molecular Modelling of Bioactive 4-Aryl-3,4-dihydropyrimidin-2(1H)-one Ester Derivatives on Teicoplanin-Based Chiral Stationary Phase Isabella Bolognino, Antonio Carrieri, Rosa Purgatorio, Marco Catto, Rocco Caliandro, Benedetta Carrozzini, Benny Danilo Belviso, Maria Majellaro, Eddy Sotelo, Saverio Cellamare, Cosimo Damiano Altomare Separations, 2022 The enantiomeric separation of 15 racemic 4-aryl-3,4-dihydropyrimidin-2(1H)-one (DHP) alkoxycarbonyl esters, some of which proved to be highly active as A2B adenosine receptor antagonists, was carried out by HPLC on ChirobioticTM TAG, a chiral stationary phase (CSP) bearing teicoplanin aglycone (TAG) as the chiral selector. The racemic compounds were separated under polar organic (PO) conditions. Preliminarily, the same selectands were investigated on three different Pirkle-type CSPs in normal-phase (NP) conditions. A baseline separation was successfully obtained on TAG-based CSPs for the majority of compounds, some of which achieved high enantioselectivity ratios (α > 2) in contrast with the smaller α values (1–1.5) and the lack of baseline resolution observed with the Pirkle-type CSPs. In particular, the racemic tetrazole-fused DHP ester derivatives, namely compounds 8 and 9, were separated on TAG-based HPLC columns with noteworthy α values (8.8 and 6.0, respectively), demonstrating the potential of the method for preparative purposes. A competition experiment, carried out with a racemic analyte (6) by adding N-acetyl-d-alanine (NADA) to the mobile phase, suggested that H-bonding interactions involved in the recognition of the natural dipeptide ligand d-Ala-d-Ala into the TAG cleft should be critical for enantioselective recognition of 4-aryl DHPs by TAG. The X-ray crystal structure of TAG was elucidated at a 0.77 Å resolution, whereas the calculation of molecular descriptors of size, polar, and H-bond interactions, were complemented with molecular docking and molecular dynamics calculations, shedding light on repulsive (steric effects) and attractive (H-bond—polar and apolar) interactions between 4-aryl DHP selectands and TAG chiral selectors.
Synthesis and Biological Evaluation of Dantrolene-Like Hydrazide and Hydrazone Analogues as Multitarget Agents for Neurodegenerative Diseases Isabella Bolognino, Nicola Giangregorio, Annamaria Tonazzi, Antón L. Martínez, Cosimo D. Altomare, María I. Loza, Sara Sablone, Saverio Cellamare, Marco Catto Chemmedchem, 2021 Dantrolene, a drug used for the management of malignant hyperthermia, had been recently evaluated for prospective repurposing as multitarget agent for neurodegenerative syndromes, including Alzheimer's disease (AD). Herein, twenty‐one dantrolene‐like hydrazide and hydrazone analogues were synthesized with the aim of exploring structure‐activity relationships (SARs) for the inhibition of human monoamine oxidases (MAOs) and acetylcholinesterase (AChE), two well‐established target enzymes for anti‐AD drugs. With few exceptions, the newly synthesized compounds exhibited selectivity toward MAO B over either MAO A or AChE, with the secondary aldimine 9 and phenylhydrazone 20 attaining IC50 values of 0.68 and 0.81 μM, respectively. While no general SAR trend was observed with lipophilicity descriptors, a molecular simplification strategy allowed the main pharmacophore features to be identified, which are responsible for the inhibitory activity toward MAO B. Finally, further in vitro investigations revealed cell protection from oxidative insult and activation of carnitine/acylcarnitine carrier as concomitant biological activities responsible for neuroprotection by hits 9 and 20 and other promising compounds in the examined series.
A prospective repurposing of dantrolene as a multitarget agent for alzheimer's disease Bolognino, Giangregorio, Pisani, de Candia, Purgatorio, Tonazzi, Altomare, Cellamare, Catto Molecules, 2019 The orphan drug dantrolene (DAN) is the only therapeutic treatment for malignant hyperthermia (MH), a pharmacogenetic pathology affecting 0.2 over 10,000 people in the EU. It acts by inhibiting ryanodine receptors, which are responsible for calcium recruitment in striatal muscles and brain. Because of its involvement in calcium homeostasis, DAN has been successfully investigated for its potential as neuroprotecting small molecule in several animal models of Alzheimer’s disease (AD). Nevertheless, its effects at a molecular level, namely on putative targets involved in neurodegeneration, are still scarcely known. Herein, we present a prospective study on repurposing of DAN involving, besides the well-known calcium antagonism, inhibition of monoamine oxidase B and acetylcholinesterase, cytoprotection from oxidative insult, and activation of carnitine/acylcarnitine carrier, as concurring biological activities responsible for neuroprotection.
