Search results for "polycyclic compounds"
showing 10 items of 373 documents
Permissive and suppressive effects of dexamethasone on enzyme induction in hepatocyte co-cultures.
2002
1. Steroids are known to act as permissive factors in hepatocytes. This study shows that dexamethasone (DEX) is a permissive factor for induction of CYP2B1/2, CYP3A1, CYP2A1 and probably also CYP2C11 in cultures with primary rat hepatocytes. 2. The induction factor of phenobarbital (PB)-induced formation of 16beta-hydroxytestosterone (OHT), a testosterone biotransformation product predominantly formed by CYP2B1, is increased 18-fold by the addition of 32 nM DEX to the culture medium. Interestingly, higher concentrations of DEX up to 1000 nM led to a concentration-dependent maximally 5-fold decrease (p = 0.002) of phenobarbital-induced 16beta-OHT formation compared with the effect observed w…
Stacking as a key property for creating nanoparticles with tunable shape: The case of squalenoyl-doxorubicin
2019
The development of elongated nanoparticles for drug delivery is of growing interest in recent years, due to longer blood circulation and improved efficacy compared to spherical counterparts. Squalenoyl-doxorubicin (SQ-Dox) conjugate was previously shown to form elongated nanoparticles with improved therapeutic efficacy and decreased toxicity compared to free doxorubicin. By using experimental and computational techniques, we demonstrate here that the specific physical properties of SQ-Dox, which include stacking and electrostatic interactions of doxorubicin as well as hydrophobic interactions of squalene, are involved in the formation of nanoassemblies with diverse elongated structures. We …
Chlorine as a Discriminant Element to Establish the Provenance of Central Mediterranean Obsidians
2020
Abstract Chlorine is a minor element present in obsidians in quantities greater than in average igneous rocks. The chlorine concentration in obsidians is generally low, of the order of tenths of wt %, but it exhibits an appreciable differentiation among geological sources. Despite these characteristics, chlorine has rarely been taken into consideration as a possible indicator of obsidian provenance and it does not appear in the chemical analytical tables accompanying the geochemical characterisation of obsidian samples. In this work, after an overview of chlorine geochemistry and cycle, we present thirty-one new electron microprobe (EPMA) analyses, including Cl, of geologic obsidians sample…
Toxic cyanobacterial blooms in reservoirs under a semiarid Mediterranean climate: the magnification of a problem
2007
Sicilian reservoirs constitute the most important water resources available on the island. During summer 2001, the intense water utilization of Lake Arancio reservoir reduced the water level significantly. This coincided with the formation of intense blooms formed by the microcystin-producing cyanobacterium Microcystis aeruginosa. During summer 2003, Lake Arancio was continuously filled and the vertical stratification of the water column was maintained, resulting in 5-6 fold lower cell numbers of Microcystis aeruginosa. For both years a significant linear relationship between microcystin net production and Microcysytis cell division was observed, implying that Microcystis cell numbers can b…
Facile formation of a meso–meso linked porphyrin dimer catalyzed by a manganese(iv)–oxo porphyrin
2011
A manganese(IV)-oxo porphyrin catalyzes C-C bond formation between zinc porphyrins at the meso-position with a two-electron oxidant to afford the meso-meso linked porphyrin dimer efficiently. The meso-meso linked dimer is formed via formation of the porphyrin radical cation, and the rate-determining step in the catalytic cycle is the formation of a manganese(IV)-oxo porphyrin with a two-electron oxidant.
In vitro fungicidal activities of echinocandins against Candida metapsilosis, C. orthopsilosis, and C. parapsilosis evaluated by time-kill studies.
2010
ABSTRACT Anidulafungin, micafungin, and caspofungin in vitro activities against Candida metapsilosis , C. orthopsilosis , and C. parapsilosis were evaluated by MICs and time-kill methods. All echinocandins showed lower MICs (mean MICs, 0.05 to 0.71 mg/liter) and the highest killing rates (−0.06 to −0.05 CFU/ml/h) for C. metapsilosis and C. orthopsilosis rather than for C. parapsilosis (mean MICs, 0.59 to 1.68 mg/liter). Micafungin and anidulafungin killing rates were greater than those determined for caspofungin. None of the echinocandins had fungicidal activity against C. parapsilosis .
Characterization of Acinetobacter baumannii from intensive care units and home care patients in Palermo, Italy.
2011
AbstractIn this study 45 isolates of Acinetobacter baumannii identified from patients in intensive care units of three different hospitals and from pressure ulcers in home care patients in Palermo, Italy, during a 3-month period in 2010, were characterized. All isolates were resistant to at least three classes of antibiotics, but susceptible to colistin and tygecycline. Forty isolates were non-susceptible to carbapenems. Eighteen and two isolates, respectively, carried the blaOXA-23-like and the blaOXA-58-like genes. One strain carried the VIM-4 gene. Six major rep-PCR subtype clusters were defined, including isolates from different hospitals or home care patients. The sequence type/pulsed …
Outbreak of infection with Klebsiella pneumoniae sequence type 258 producing Klebsiella pneumoniae Carbapenemase 3 in an intensive care unit in Italy
2010
Gram-negative pathogens producing carbapenemases represent an alarming clinical threat with serious effects on patient outcomes ([3][1], [7][2]). In 2001, Yigit et al. ([11][3]) reported a novel β-lactamase termed “ K lebsiella pneumoniae carbapenemase” (KPC-1) in North Carolina. KPC-producing
New β-Lactam-β-Lactamase Inhibitor Combinations.
2020
The limited armamentarium against drug-resistant Gram-negative bacilli has led to the development of several novel β-lactam-β-lactamase inhibitor combinations (BLBLIs). In this review, we summarize their spectrum of in vitro activities, mechanisms of resistance, and pharmacokinetic-pharmacodynamic (PK-PD) characteristics. A summary of available clinical data is provided per drug. Four approved BLBLIs are discussed in detail. All are options for treating multidrug-resistant (MDR) Enterobacterales and Pseudomonas aeruginosa Ceftazidime-avibactam is a potential drug for treating Enterobacterales producing extended-spectrum β-lactamase (ESBL), Klebsiella pneumoniae carbapenemase (KPC), AmpC, an…
In vitro activity of linezolid, clarithromycin and moxifloxacin against clinical isolates of Mycobacterium kansasii
2005
To compare the activity of linezolid with a range of drugs used in the treatment of Mycobacterium kansasii infections.The percentages of resistant isolates against isoniazid, rifampicin and ethambutol were 2.9%, 1.9% and 2.9%, respectively. All isolates were susceptible to clarithromycin and moxifloxacin both with MIC(90) values of 0.125 mg/L. Linezolid was active against all isolates with MIC(50) and MIC(90) values of 0.5 and 1 mg/L, respectively, both below the susceptibility breakpoint established for mycobacteria.Linezolid, clarithromycin or moxifloxacin, could be used as alternative drugs for treatment of infections due to rifampicin-resistant isolates as well as short-course or interm…