A5059309705- Sulfur Compounds in Biology
- Synthesis and Biological Evaluation
- Synthesis and biological activity
- Malaria Research and Control
- Phenothiazines and Benzothiazines Synthesis and Activities
- Inflammatory mediators and NSAID effects
- Synthesis and Characterization of Heterocyclic Compounds
- Botanical Research and Chemistry
- Pharmacological Receptor Mechanisms and Effects
- Research on Leishmaniasis Studies
- HIV/AIDS drug development and treatment
- Synthesis and Reactivity of Heterocycles
- Mast cells and histamine
- Synthesis and Reactions of Organic Compounds
- Synthesis of heterocyclic compounds
- Eicosanoids and Hypertension Pharmacology
- Computational Drug Discovery Methods
- Trypanosoma species research and implications
- Nitric Oxide and Endothelin Effects
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Chemical synthesis and alkaloids
- Cancer therapeutics and mechanisms
- Organic Chemistry Cycloaddition Reactions
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Folate and B Vitamins Research
University of Milan
2014-2024
National Cancer Institute
2012
United States Army Medical Research Institute of Infectious Diseases
2012
LMU Klinikum
2012
Ludwig-Maximilians-Universität München
2012
Starnberg Hospital
2012
John Radcliffe Hospital
2010
University of Oxford
2010
University of British Columbia
2010
Istituto di Farmacologia Traslazionale
1991-2008
The main lesion in Parkinson disease (PD) is loss of substantia nigra dopaminergic neurons. Levodopa (l-DOPA) the most widely used therapy, but it does not arrest progression. Some possible contributing factors to continuing neuronal are oxidative stress, including oxidation l-DOPA, and neurotoxins generated by locally activated microglia astrocytes. A method reducing these produce l-DOPA hybrid compounds that have antioxidant antiinflammatory properties. Here we demonstrate properties four...
Superoxide (O(2)(*-)), derived from nicotinamide adenine dinucleotide phosphate (NADPH) oxidase, is associated with acute respiratory distress syndrome (ARDS). NADPH oxidase activity and expression are blocked by nitric oxide (NO) sildenafil. As another gas, hydrogen sulphide (H(2)S) formed blood vessels, the effect of sodium hydrosulphide (NaHS) H(2)S-donating derivative sildenafil, ACS6, on O(2)(*-) formation gp91(phox) (a catalytic subunit oxidase) in porcine pulmonary arterial...
The activity of NADPH oxidase (NOX) is blocked by nitric oxide (NO). Hydrogen sulfide (H(2)S) also produced blood vessels. It reasonable to suggest that H(2)S may have similar actions NO on NOX. In order test this hypothesis, the effect sodium hydrosulfide (NaHS) O(2)(-) formation, expression NOX-1 (a catalytic subunit NOX) and Rac(1) (essential for full NOX activity) in isolated vascular smooth muscle cells (hVSMCs) was investigated. hVSMCs were incubated with thromboxane A(2) analogue...
Abstract Endogenously generated hydrogen sulfide (H 2 S) may have multiple functions in brain. It has been shown that H S attenuates the expression of pro‐inflammatory cytokines by lipopolysaccharide (LPS)‐activated microglia. Here we demonstrate a neuroprotective effect NaSH and three S‐releasing compounds, ADT‐OH, S‐diclofenac, S‐aspirin. When activated LPS γ‐interferon, human microglia THP‐1 cells release materials are toxic to neuroblastoma SH‐SY5Y cells. These phenomena also occur with...
OBJECTIVE To study the effect of H(2)S-donating derivative sildenafil (ACS6) compared to citrate and sodium hydrosulphide (NaHS) on relaxation, superoxide formation NADPH oxidase type 5 phosphodiesterase (PDE5) expression in isolated rabbit cavernosal tissue smooth muscle cells (CSMCs), vivo indices oxidative stress induced with buthionine sulphoximine (BSO). MATERIALS AND METHODS Relaxation was studied an organ bath response carbachol after incubation interleukin-1beta for 12 h. CSMCs were...
Angiogenesis involves multiple signaling pathways that must be considered when developing agents to modulate pathological angiogenesis. Because both cyclooxygenase inhibitors and dithioles have demonstrated anti-angiogenic properties, we investigated the activities of a new class anti-inflammatory drugs containing dithiolethione moieties (S-NSAIDs) S-valproate.
Hydrogen sulphide (H(2)S) is an endogenous gaseous mediator active in the multilevel regulation of pathophysiological functions mammalian cardiovascular tissues.This study investigated pharmacological activity a new H(2)S-releasing derivative diclofenac, S-diclofenac (2-[(2,6-dichlorophenyl)amino]benzeneacetic acid 4-(3H-1,2-dithiole-3-thione-5-yl)-phenyl ester) isolated rabbit heart submitted to low-flow ischaemia-reperfusion damage.S-diclofenac (3, 10 and 30 microM), despite inhibiting...
Parkinson's disease (PD), characterized by loss of dopaminergic neurons in the substantia nigra, is a neurodegenerative disorder central nervous system. The present study was designed to investigate therapeutic effect ACS84, hydrogen sulfide-releasing-L-Dopa derivative compound, 6-hydroxydopamine (6-OHDA)-induced PD model. ACS84 protected SH-SY5Y cells against 6-OHDA-induced cell injury and oxidative stress. protective resulted from stimulation Nrf-2 nuclear translocation promotion...
Purpose. To determine the neuroprotective properties of a latanoprost acid derivative (ACS67) that donates gas hydrogen sulfide (H(2)S). Methods. Ischemia to rat retina was induced by elevation intraocular pressure. Electroretinograms (ERGs) were recorded and retinas analyzed 2 days later immunohistochemistry, Western blot analysis, RT-PCR. Hydrogen peroxide (H(2)O(2)) used impose an insult on RGC-5 cells in culture. The nature cultures quantified resazurin-reduction assay procedure,...
Hydrogen sulfide (H(2)S)-releasing NSAIDs exert potent anti-inflammatory effects beyond classical cyclooxygenase inhibition. Here, we compared the platelet inhibitory of H(2)S-releasing aspirin derivative ACS14 with its mother compound to analyze additional on platelets.In platelets mice fed for 6 days (50 mg/kg per day), not only arachidonic acid-induced aggregation but also ADP-dependent was decreased, an effect that observed equimolar dose (23 day). led a significantly longer arterial...
Multitarget therapeutic leads for Alzheimer's disease were designed on the models of compounds capable maintaining or restoring cell protein homeostasis and inhibiting β-amyloid (Aβ) oligomerization. Thirty-seven thioxanthen-9-one, xanthen-9-one, naphto- anthraquinone derivatives tested direct inhibition Aβ(1-40) aggregation electric eel acetylcholinesterase (eeAChE) horse serum butyrylcholinesterase (hsBChE). These are characterized by basic side chains, mainly quinolizidinylalkyl moieties,...
Two sets of benzimidazole derivatives were synthesised and tested in vitro for activity against promastigotes Leishmania tropica L. infantum. Most the compounds resulted active both species, with IC50 values low micromolar/sub-micromolar range. Among set 2-(long chain)alkyl benzimidazoles, whose heterocyclic head was quaternised, compound 8 about 100-/200-fold more potent than miltefosine, even if selectivity index (SI) versus HMEC-1 cells only moderately improved. In 2-benzyl 2-phenyl...
Impaired lung function in severe acute pancreatitis is the primary cause of morbidity and mortality this condition. Hydrogen sulfide (H(2)S) a naturally occurring gas that has been shown to be potent vasodilator. Diclofenac nonsteroidal anti-inflammatory drug have anti-inflammatory, analgesic, antipyretic activity. ACS15 an H(2)S-releasing derivative diclofenac. Little known about its effectiveness as drug. In report, we describe effect diclofenac on associated injury mouse. Acute was...
The aim of this study was to examine the effect ACS14, a hydrogen sulfide (H(2)S)-releasing derivative aspirin (Asp), on Asp-induced gastric injury. Gastric hemorrhagic lesions were induced by intragastric administration Asp (200 mg/kg, suspended in 0.5% carboxymethyl cellulose solutions) volume 1 ml/100 g body weight. ACS14 (1, 5 or 10 mg/kg) given 30 min before administration. total area erosions, H(2)S concentration and oxidative stress tissues measured three hours after Asp. Treatment...
Hydrogen sulphide (H(2)S) and prostaglandins are both involved in inflammation, cancer bone turnover, non-steroidal anti-inflammatory drugs (NSAIDs) H(2)S donors exhibit anti-tumour properties. H(2)S-releasing diclofenac (S-DCF) derivatives a novel class of NSAIDs combining the properties donor with those conventional NSAID.We studied effects S-DCF ACS15 ACS32 on osteoclast osteoblast differentiation activity vitro, human mouse breast cells support for formation signalling osteolysis ex...