Search results for "CA [MG]"
showing 10 items of 2161 documents
Paracentrin 1, a synthetic antimicrobial peptide from the sea-urchin Paracentrotus lividus, interferes with staphylococcal and Pseudomonas aeruginosa…
2014
The rise of antibiotic-resistance as well as the reduction of investments by pharmaceutical companies in the development of new antibiotics have stimulated the investigation for alternative strategies to conventional antibiotics. Many antimicrobial peptides show a high specificity for prokaryotes and a low toxicity for eukaryotic cells and, due to their mode of action the development of resistance is considered unlikely. We recently characterized an antimicrobial peptide that was called Paracentrin 1 from the 5-kDa peptide fraction from the coelomocyte cytosol of the Paracentrotus lividus. In this study, the chemically synthesized Paracentrin 1, was tested for its antimicrobial and antibiof…
Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors
2020
[Image: see text] Breast cancer (BC) is the most diffused cancer type in women and the second leading cause of death among the female population. Effective strategies to fight estrogen responsive (ER+) BC, which represents 70% of all BC cases, rely on estrogen deprivation, via the inhibition of the aromatase enzyme, or the modulation of its cognate estrogen receptor. Current clinical therapies significantly increased patient survival time. Nevertheless, the onset of resistance in metastatic BC patients undergoing prolonged treatments is becoming a current clinical challenge, urgently demanding to devise innovative strategies. In this context, here we designed, synthesized, and performed in …
Mesoporous Silica-Based Materials with Bactericidal Properties
2019
[EN] Bacterial infections are the main cause of chronic infections and even mortality. In fact, due to extensive use of antibiotics and, then, emergence of antibiotic resistance, treatment of such infections by conventional antibiotics has become a major concern worldwide. One of the promising strategies to treat infection diseases is the use of nanomaterials. Among them, mesoporous silica materials (MSMs) have attracted burgeoning attention due to high surface area, tunable pore/particle size, and easy surface functionalization. This review discusses how one can exploit capacities of MSMs to design and fabricate multifunctional/controllable drug delivery systems (DDSs) to combat bacterial …
Targeting a Targeted Drug: An Approach Toward Hypoxia-Activatable Tyrosine Kinase Inhibitor Prodrugs
2016
Tyrosine kinase inhibitors (TKIs), which have revolutionized cancer therapy over the past 15 years, are limited in their clinical application due to serious side effects. Therefore, we converted two approved TKIs (sunitinib and erlotinib) into 2-nitroimidazole-based hypoxia-activatable prodrugs. Kinetics studies showed very different stabilities over 24 h; however, fast reductive activation via E. coli nitroreductase could be confirmed for both panels. The anticancer activity and signaling inhibition of the compounds against various human cancer cell lines were evaluated in cell culture. These data, together with molecular docking simulations, revealed distinct differences in the impact of …
Development and biological investigations of hypoxia-sensitive prodrugs of the tyrosine kinase inhibitor crizotinib
2019
Despite the huge success of tyrosine kinase inhibitors as anticancer agents, severe side effects are a major problem. In order to overcome this drawback, the first hypoxia-activatable 2-nitroimidazole-based prodrugs of the clinically approved ALK and c-MET inhibitor crizotinib were developed. The 2-aminopyridine functionality of crizotinib (essential for target kinase binding) was considered as ideal position for prodrug derivatization. Consequently, two different prodrugs were synthesized with the nitroimidazole unit attached to crizotinib either via carbamoylation (A) or alkylation (B) of the 2-aminopyridine moiety. The successful prodrug design could be proven by docking studies and a dr…
Possible reason for preferential damage to renal tubular epithelial cells evoked by amphotericin B
1996
An important determinant of nephrotoxicity, which is the major complication of long-term amphotericin B treatment, is dysfunction of distal tubular epithelial cells. The underlying cause for this rather selective damage to the cells is unknown. In the present investigation, it was shown that kidney epithelial cells were initially damaged by amphotericin B at concentrations of 2.5 to 10 micrograms/ml, as demonstrable by a dramatic drop in cellular K+ levels. Cells could recover from the initial toxic action of the polyene if they were kept in medium of neutral pH, and cellular K+ levels returned to normal after 6 h. However, the recovery mechanisms failed at lower pHs of 5.6 to 6.0. At low p…
Improving adherence in osteoporosis: a new management algorithm for the patient with osteoporosis
2011
Introduction: Bisphosphonates are the first-choice treatment for osteoporosis. They effectively increase bone mineral density, reduce markers of bone resorption, and lower the incidence of new fractures in patients with osteoporosis-related fracture. However, the efficacy observed in clinical trials may not be realized in a real-life setting, partly due to poor adherence to therapy, with a significant worsening of clinical outcomes. Several issues contribute to poor adherence to osteoporosis medication, including inconvenient dosing regimens and concerns about possible adverse events. Although strategies to improve adherence have been investigated, new approaches are required. Areas covered…
Coexpression of vasoactive intestinal peptide, calcitonin gene-related peptide and substance P immunoreactivity in parasympathetic neurons of the rhe…
1995
Abstract By the use of light microscopic immunohistochemistry, the present study investigates whether substance P (SP) and calcitonin generelated peptide (CGRP), which are well documented neurotransmitter candidates in primary sensory fibers, are also expressed in parasympathetic neurons of the rhesus monkey lung. A combination of double fluorescence immunohistochemistry and staining of adjacent sections revealed triple coexistence of SP, CGRP and the cholinergic co-transmitter vasoactive intestinal peptide (VIP) in a large number of neuronal cell bodies in intrinsic peribronchial ganglia. In addition, there was co-localization of SP and CGRP in choline acetyltransferase (ChAT)-positive neu…
Knowledge and attitudes towards smoking cessation counselling: an Italian cross-sectional survey on tertiary care nursing staff
2021
Background One of the most effective smoking cessation strategies involves care and advice from nurses due to their role in the front line of treatment. Lack of education on smoking cessation counselling may be detrimental, and adequate smoking cessation training during healthcare studies is needed. Objectives The study aimed to examine nurses’ attitudes, belief, and knowledge of smoking cessation counselling; knowledge of the health risks associated with smoking was also assessed. Design A cross-sectional survey on 77 nurses from the nursing staff of Cardiology, Cardiac Intensive Care and Surgical Oncology Units of two tertiary hospitals. Methods Cronbach’s alpha was calculated to assess …
The policy of public health genomics in Italy.
2013
Abstract Italy has a monitoring system for genetic testing, consisting in a periodic census of clinical and laboratory activities performed in the country. The experience is limited, however, concerning the translation of genomic testing for complex diseases into clinical practice. For the first time the Italian Ministry of Health has introduced a policy strategic plan on genomics and predictive medicine within the 2010–2012 National Prevention Plan. This achievement was supported by the Italian Network for Public Health Genomics (GENISAP) and will likely contribute to the integration of public health genomics into health care in the country. Our experience might be of interest not only in …