A5076233600- Receptor Mechanisms and Signaling
- Heme Oxygenase-1 and Carbon Monoxide
- Synthesis and Biological Evaluation
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and biological activity
- Synthesis and Reactions of Organic Compounds
- Eicosanoids and Hypertension Pharmacology
- Synthesis of heterocyclic compounds
- Phenothiazines and Benzothiazines Synthesis and Activities
- Nitric Oxide and Endothelin Effects
- Hemoglobin structure and function
- Synthesis and Characterization of Heterocyclic Compounds
- Cannabis and Cannabinoid Research
- Neuropeptides and Animal Physiology
- Quinazolinone synthesis and applications
- Fluorine in Organic Chemistry
- Neuroscience and Neuropharmacology Research
- Research on Leishmaniasis Studies
- Electron Spin Resonance Studies
- Synthesis and Reactivity of Heterocycles
- Pharmacological Effects and Assays
- Viral Infections and Vectors
- Neurotransmitter Receptor Influence on Behavior
- Cyclopropane Reaction Mechanisms
- Synthesis and Catalytic Reactions
University of Catania
2014-2023
Istituto Zooprofilattico Sperimentale della Lombardia e dell'Emilia Romagna "Bruno Ubertini"
2021-2023
Istituto di Farmacologia Traslazionale
2014
Vrije Universiteit Amsterdam
2009
Polish Academy of Sciences
2008
University of Siena
2003-2005
Mario Negri Institute for Pharmacological Research
2005
Smith-Kettlewell Eye Research Institute
2004
University of Milano-Bicocca
2001
University of Cambridge
2001
The term ferroptosis refers to a peculiar type of programmed cell death (PCD) mainly characterized by extensive iron-dependent lipid peroxidation. Recently, has been suggested as potential new strategy for the treatment several cancers, including breast cancer (BC). In particular, among BC subtypes, triple negative (TNBC) is considered most aggressive, and conventional drugs fail provide long-term efficacy. this context, our study's purpose was investigate mechanism in lines reveal...
Oxygen quenching of the luminescence mononuclear and dinuclear Ir(III) cyclometalated complexes immobilized in pPEGMA matrixes has been studied. Linear Stern−Volmer plots, even when experiments at different emission wavelengths have performed, were evidenced. Despite lifetimes chromophores absence quencher, similar slopes calculated. This behavior was tentatively interpreted by taking into account size charge chromophores. Increased sizes lower charges seem to enhance sensitivity systems....
A series of new compounds containing a benzimidazole, benzothiazole, or benzoxazole nucleus linked to an arylpiperazine by different thioalkyl chains was prepared. They were tested in radioligand binding experiments evaluate their affinity for 5-HT1A and 5-HT2A serotonergic, α1 adrenergic, D1, D2 dopaminergic receptors. Many showed interesting profile; particular, 36 displayed very high receptor selectivity over all the other investigated Selected compounds, evaluated functional assays,...
In this paper, the design, synthesis, and molecular modeling of a new azole-based HO-1 inhibitors was reported, using compound 1 as lead compound, in which an imidazole moiety is linked to hydrophobic group by means ethanolic spacer. The tested compounds showed good inhibitor activity possessed IC50 values micromolar range. These results were obtained targeting western region. Molecular studies confirmed consolidated binding mode nitrogen imidazolyl coordinated heme ferrous iron, meanwhile...
Serotonin 5-HT7 receptor (5-HT7R) has been the subject of intense research efforts because its presence in brain areas such as hippocampus, hypothalamus, and cortex. Preclinical data link 5-HT7R to a variety central nervous system processes including regulation circadian rhythms, mood, cognition, pain processing, mechanisms addiction. blockade antidepressant effects may ameliorate cognitive deficits associated with schizophrenia. recently shown modulate neuronal morphology, excitability,...
Background:Heme Oxygenase-1 (HO-1) is a metabolic enzyme strongly involved in processes including cytoprotection, modulation of inflammatory response, anti-oxidative functions, regulation cellular proliferation, angiogenesis, cardiovascular homeostasis, and immuno-modulation. HO-1 induction and/or activation able to counterbalance, at least part, oxidative stress inflammation. For this reason, can be regarded as an attractive target ameliorate different stress-related pathologies. Caffeic...
Lipid-based nanocarriers (LNs) have made it possible to prolong corneal residence time and improve the ocular bioavailability of ophthalmic drugs. In order investigate how LNs interact with mucosa reach posterior eye segment, we formulated lipid that were designed bear a traceable fluorescent probe in present work. The chosen was obtained by conjugation reaction between fluoresceinamine solid excipient stearic acid, forming chemically synthesized adduct (ODAF, N-(3′,6′-dihydroxy-3-oxospiro...
Heme oxygenase-1 (HO-1) promotes heme catabolism exercising cytoprotective roles in normal and cancer cells. Herein, we report the design, synthesis, molecular modeling, biological evaluation of novel HO-1 inhibitors. Specifically, an amide linker central spacer imidazole were fixed, hydrophobic moiety required by pharmacophore was largely modified. In many tumors, overexpression correlates with poor prognosis chemoresistance, suggesting inhibition as a possible antitumor strategy....
Eggplant fruit is a very rich source of polyphenol compounds endowed with antioxidant properties. The aim this study was to extract polyphenols from eggplant entire fruit, pulp, or skin, both fresh and dry, compare results between conventional extraction microwave-assisted (MAE). effects time exposure (15, 30, 60, 90 min) solvent (water 100% ethanol/water 50%) were also evaluated. highest amount found in the obtained dry peeled skin treated 50% aqueous ethanol, irradiated microwave;...
Abstract Due to increasing interest in the field of heme oxygenases (HOs), we built a ligand database called HemeOxDB that includes entire set known HO‐1 and HO‐2 inhibitors, resulting more than 400 compounds. The is available online at http://www.researchdsf.unict.it/hemeoxdb/ , having robust search engine allows end users build complex queries, sort tabulated results, generate color‐coded two‐ three‐dimensional graphs. This will grow be tool for design potent selective or inhibitors. We...
The data have been obtained from the Heme Oxygenase Database (HemeOxDB) and refined according to 2D-QSAR requirements. These provide information about a set of more than 380 Oxygenase-1 (HO-1) inhibitors. development model has undertaken with use CORAL software using SMILES, molecular graphs hybrid descriptors (SMILES graph together). regressions for HO-1 half maximal inhibitory concentration (IC50) expressed as pIC50 (pIC50=−LogIC50) are here included. was also employed predict pIC50values...
Abstract A 3D quantitative structure–activity relationship (3D‐QSAR) model for predicting the activity of heme oxygenase 1 (HO‐1) inhibitors was constructed with aim providing a useful tool identification, design, and optimization novel HO‐1 inhibitors. The built using set 222 recovered from Heme Oxygenase Database (HemeOxDB) developed software Forge. present showed high statistical quality, as confirmed by its robust predictive potential satisfactory descriptive capability. drawn‐up map...