A5049261961- Pain Mechanisms and Treatments
- Cancer Treatment and Pharmacology
- Enzyme function and inhibition
- Pharmacological Receptor Mechanisms and Effects
- Cholinesterase and Neurodegenerative Diseases
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis and Catalytic Reactions
- Neuroscience and Neuropharmacology Research
- Adenosine and Purinergic Signaling
- Phenothiazines and Benzothiazines Synthesis and Activities
- Neuropeptides and Animal Physiology
- Nicotinic Acetylcholine Receptors Study
- Pharmacological Effects of Natural Compounds
- Receptor Mechanisms and Signaling
- Cannabis and Cannabinoid Research
- Inflammatory mediators and NSAID effects
- Gastrointestinal motility and disorders
- Eicosanoids and Hypertension Pharmacology
- Plant-based Medicinal Research
- Genomics, phytochemicals, and oxidative stress
- Ion channel regulation and function
- Synthesis and Biological Evaluation
- Biochemical Acid Research Studies
- Sulfur Compounds in Biology
University of Florence
2016-2025
Institute of Pharmacology
2023
University of Turin
2022
Pharmaceutical Biotechnology (Czechia)
2022
University of Milan
2022
Florence (Netherlands)
2020
SDN Istituto di Ricerca Diagnostica e Nucleare
2020
University of Florida
2018
Memorial Sloan Kettering Cancer Center
2015
Istituto di Farmacologia Traslazionale
2013
The gut-brain axis and the intestinal microbiota are emerging as key players in health disease. Shifts composition affect a variety of systems; however, evidence their direct impact on cognitive functions is still lacking. We tested whether faecal transplant (FMT) from aged donor mice into young adult recipients altered hippocampus, an area central nervous system (CNS) known to be affected by ageing process related functions.Young were transplanted with either or age-matched mice. Following...
Magnetic nanoparticles, MNPs, mineralized within a human ferritin protein cage, HFt, can represent an appealing platform to realize smart therapeutic agents for cancer treatment by drug delivery and magnetic fluid hyperthermia, MFH. However, the constraint imposed inner diameter of shell (ca. 8 nm) prevents its use as heat mediator in MFH when MNPs comprise pure iron oxide. In this contribution, we demonstrate how limitation be overcome through controlled doping core with small amount...
Significance This study addresses the need to phase out opioids as major analgesic drugs for moderate severe chronic pain. We establish that a highly selective and potent inhibitor of α9α10 nicotinic acetylcholine receptor (nAChR) subtype prevents expression chemotherapy-induced neuropathic Thus, antagonists nAChR are potential leads nonopioid drug development. The effects inhibitors receptor, together with genetic studies, suggest key role in an intercellular signaling network can be...
Neuropathic syndromes which are evoked by lesions to the peripheral or central nervous system extremely difficult treat, and available drugs rarely joint an antihyperalgesic with a neurorestorative effect. N-Palmitoylethanolamine (PEA) exerts antinociceptive effects in several animal models inhibits inflammation rodents. Aimed evaluate antineuropathic properties of PEA, damage sciatic nerve was induced mice chronic constriction injury (CCI) subcutaneous daily treatment 30 mg kg(-1) PEA...
We report the synthesis of a series hybrid compounds incorporating 6- and 7-substituted coumarins (carbonic anhydrase, CA inhibitors) derivatized with clinically used NSAIDs (indomethacin, sulindac, ketoprofen, ibuprofen, diclofenac, ketorolac, etc., cyclooxygenase as agents for management rheumatoid arthritis (RA). Most were effective in inhibiting RA overexpressed hCA IX XII, KI values low nanomolar-subnanomolar ranges. The antihyperalgesic activity such was assessed by means paw-pressure...
The hydrochlorothiazide (HCT) low solubility and permeability give rise to limited variable bioavailability; its stability makes it difficult develop stable aqueous liquid formulations; dose the achievement of a homogeneous drug distribution very difficult. Thus, aim this study was investigate effectiveness strategy based on development nanostructured lipid carriers (NLC) as an innovative oral pediatric formulation HCT with improved therapeutic efficacy. performance various synthetic natural...
Neuropathic pain affects millions of people worldwide, causing substantial disability and greatly impairing quality life. Commonly used analgesics or antihyperalgesic compounds are generally characterized by limited therapeutic outcomes. Thus, there is a compelling need for novel strategies able to prevent nervous tissue alterations responsible chronic pain. The α9α10 nicotinic acetylcholine receptor antagonist α-conotoxin RgIA (RgIA), peptide isolated from the venom carnivorous cone snail,...
6-Substituted sulfocoumarins bearing the carboxamido, trimethylammonium as well cyano and methoxy moieties with interesting inhibitory activity/selectivity against tumor associated carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA IX XII are reported. Moieties leading to best inhibition were tert-butylcarboxamido, phenylcarboxamido, 4-pyridylcarboxamido, KI values of 2.1–8.1 nM. No off-target II I was observed. A number these compounds evaluated HT-29 colon cancer cell lines ex vivo....
Ischemia of brain areas is a global health problem, causing death or long-term disability. Current pharmacological options have limited impact on ischemic damages. Recently, relationship between hypoxia and carbonic anhydrase (CA) over-expression has been highlighted suggesting CA inhibition as possible target. This study aimed to evaluate the profile sulfonamide coumarin inhibitors in rats underwent permanent middle cerebral artery occlusion (pMCAO). The neurological score pMCAO was...
Cadmium (Cd) is a highly toxic environmental pollutant released from the smelting and refining of metals cigarette smoking. Oral exposure to cadmium may result in adverse effects on number tissues, including central nervous system (CNS). In fact, its toxicity has been related neurological disorders, as well neurodegenerative diseases such Alzheimer's Parkinson's diseases. Under normal conditions, Cd barely reaches brain adults because presence blood-brain barrier (BBB); however, it...
Sirtuin 1 (SIRT1) enzyme plays a pivotal role in the regulation of many physiological functions. In particular, it is implicated ageing-related diseases, such as cardiac hypertrophy, myocardial infarct, and endothelial dysfunction; moreover, its expression decreases with age. Therefore, an effective strategy to extend lifespan improve cardiovascular function enhancement expression/activity SIRT1 exogenous agents. The Citrus flavonoid naringenin (NAR) presents structural similarity natural...
The A3 adenosine receptor (A3AR) has emerged as a therapeutic target with A3AR agonists to tackle the global challenge of neuropathic pain, and investigation into its mode action is essential for ongoing clinical development. Immune cell A3ARs, their activation during pathology, modulate cytokine release. Thus, use immune cells cellular substrate pharmacological enticing, but unknown. present study discovered that Rag-KO mice lacking T B cells, compared WT mice, are insensitive...
Target organ toxicity is often a reason for attritions in nonclinical and clinical drug development. Leveraging emerging safety biomarkers studies provides an opportunity to monitor such toxicities early efficiently, potentially translating trials. As part of the European Union's Innovative Medicines Initiative (IMI), two projects have focused on evaluating nervous system (NS) toxicity: Translational Safety Biomarker Pipeline (TransBioLine) Neurotoxicity De-Risking Preclinical Drug Discovery...
Neurotoxicity is a main side effect of the anticancer drug oxaliplatin. The development neuropathic syndrome impairs quality life and potentially results in chemotherapy dose reductions and/or early discontinuation. In complex pattern molecular morphological alterations induced by oxaliplatin nervous system, an important activation glia has been preclinically evidenced. N-Palmitoylethanolamine (PEA) modulates glial cells exerts antinociceptive effects several animal models. order to improve...