105 research outputs found
Erythrodermic psoriasis treated with ustekinumab: An Italian multicenter retrospective analysis
Erythrodermic psoriasis (EP) is one of the most severe
cutaneous conditions which may lead to serious morbidity and
even mortality. This condition is often difficult to manage and, due
to its rarity (estimated prevalence 1–2.25% of psoriatic patients)
there is a lack of high-quality medical literature examining
treatment options [1]
Advanced Technologies for Oral Controlled Release: Cyclodextrins for oral controlled release
Cyclodextrins (CDs) are used in oral pharmaceutical formulations, by means of inclusion complexes formation, with the following advantages for the drugs: (1) solubility, dissolution rate, stability and bioavailability enhancement; (2) to modify the drug release site and/or time profile; and (3) to reduce or prevent gastrointestinal side effects and unpleasant smell or taste, to prevent drug-drug or drug-additive interactions, or even to convert oil and liquid drugs into microcrystalline or amorphous powders. A more recent trend focuses on the use of CDs as nanocarriers, a strategy that aims to design versatile delivery systems that can encapsulate drugs with better physicochemical properties for oral delivery. Thus, the aim of this work was to review the applications of the CDs and their hydrophilic derivatives on the solubility enhancement of poorly water soluble drugs in order to increase their dissolution rate and get immediate release, as well as their ability to control (to prolong or to delay) the release of drugs from solid dosage forms, either as complexes with the hydrophilic (e.g. as osmotic pumps) and/ or hydrophobic CDs. New controlled delivery systems based on nanotechonology carriers (nanoparticles and conjugates) have also been reviewed
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Effects of multiple low-head dams on fish, macroinvertebrates, habitat, and water quality in the Fox River, Illinois
We examined the effects of low-head dams on aquatic biota, habitat, and water qualityin a 171-km reach of a midwestern warmwater river that was fragmented by 15 dams into a seriesof free-flowing and impounded habitats. Dams impounded 55% of the river\u27s surface area withinthe study reach and influenced distributions of 30 species of fish by restricting upstreammovements. Values for the Illinois index of biotic integrity (IBI) were higher in free-flowing areas(mean IBI = 46 out of a possible 60 at below-dam and midsegment free-flowing locations) thanimpounded areas (mean IBI \u3c 31 for above-dam and midsegment impounded locations).Likewise, scores from a macroinvertebrate condition index (MCI) were higher at stations in freeflowingreaches (mean MCI \u3e 415 out of a possible 700) than in nearshore areas of impoundedreaches (mean MCI \u3c 210). Ponar dredge samples taken only from open-water impounded areasshowed an offshore invertebrate community that consisted almost entirely of tolerant oligochaetesand chironomid larvae. Qualitative habitat evaluation index (QHEI) scores indicated good-qualityhabitat in free-flowing areas (mean QHEI \u3e 70 out of a possible 100) and severely degradedhabitat at impounded sites (mean QHEI \u3c 45). In impounded reaches, dissolved oxygen and pHshowed wide daily fluctuations (2.5û18.0 mg/L and 7.0û9.4 units) and often failed to meet Illinoiswater quality standards. In free-flowing portions of river, fluctuations in these parameters wereless extreme and water quality standards typically were met. We found little evidence ofcumulative effects of dams; however, our data suggest that low-head dams adversely affectwarmwater stream fish and macroinvertebrate communities by degrading habitat and waterquality and fragmenting the river landscape. These results should aid river managers andstakeholders in determining appropriate restoration practices (i.e., dam removal versus fishpassage structures) for warmwater rivers and streams that contain low-head dams
Symmetry-Dependent Vibrational Circular Dichroism Enhancement in Co(II) Salicylaldiminato Complexes
Chiral coordination compounds of Co(II) and other open-shell metal complexes display enhanced vibrational circular dichroism (VCD) spectra associated with the existence of low-lying excited states (LLESs). In addition to the enhancement, a series of Co(II) salicylaldiminato complexes exhibits an almost monosignate pattern of VCD bands, a unique feature if compared with the usual alternation of positive and negative signals. Frequency and excited-state calculations reveal that VCD enhancement and sign reversal selectively affect the normal modes of B symmetry of the C 2 -symmetric pseudotetrahedral species thanks to their combination with one or more LLES having the same B symmetry. This proves the strict relation between VCD enhancement and monosignate appearance and demonstrates an unprecedented symmetry dependence of the two phenomena
Gigantelline, gigantellinine and gigancrinine, cherylline- and crinine-type alkaloids isolated from Crinum jagus with anti-acetylcholinesterase activity
Three undescribed Amarylidaceae alkaloids, named gigantelline, gigantellinine and gigancrinine, were isolated from Crinum jagus (syn. = Crinum giganteum) collected in Senegal, together with the already known sanguinine, cherylline, lycorine, crinine, flexinine and the isoquinolinone derivative hippadine. Gigantelline, gigantellinine and gigancrinine were characterized as 4-(6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydro-isoquinolin-4-yl)-phenol, its 7-O-demethyl-5.-hydroxy-4.-methoxy derivative and 5,6a,7,7a,8a,9-hexahydro-6,9a-ethano[1,3]dioxolo[4,5j]oxireno[2,3-b]phenanthridin-9-ol, respectively, by using spectroscopic (1D and 2D H-1 and C-13 NMR and HRESIMS) and chemical methods. Their relative configuration was assigned by NOESY NMR spectra and NMR calculations, while the absolute configuration was assigned using electronic circular dichroism (ECD) experiments and calculations. Sanguinine, cherylline, crinine, flexinine, and the isoquinolinone hippadine, were isolated for the first time from C. jagus. Cherylline, gigantellinine, crinine, flexinine and sanguinine inhibited the activity of AChE in a dose-dependent manner, and inhibition by sanguinine was remarkably effective (IC50 = 1.83 +/- 0.01 mu M). Cherylline and hippadine showed weak cytotoxicity at 100 mu M
Synthesis, resolution, and absolute configuration of two novel and selective cyclooxygenase-2 inhibitors based on the 1,5-diarylpyrrole structure
Three racemic esters based on the 1,5-diarylpyrrole structure, which proved to be highly selective COX-2 inhibitors endowed with an appreciable anti-inflammatory activity in some animal models, were subjected to chiral resolution. Their absolute configurations were assigned by comparison of the CD spectrum measured on-line with a HPLC–CD detector, with that calculated by means of a TDDFT method
Phytotoxic Metabolites from Three Neofusicoccum Species Causal Agents of Botryosphaeria Dieback in Australia, Luteopyroxin, Neoanthraquinone, and Luteoxepinone, a Disubstituted Furo-α-pyrone, a Hexasubstituted Anthraquinone, and a Trisubstituted Oxepi-2-one from Neofusicoccum luteum
Different phytotoxic metabolites were isolated from the organic extract of Neofusicoccum luteum, Neofusicoccum australe, and Neofusicoccum parvum, causal agents of Botryosphaeria dieback in Australia. N. luteum produced a new disubstituted furo-α-pyrone, a hexasubstituted anthraquinone, and a trisubstituted oxepi-2(7H)-one, luteopyroxin (4), neoanthraquinone (5), and luteoxepinone (7), respectively, together with the known (±)-nigrosporione (6), tyrosol (8), (R)-(-)-mellein (1), and (3R,4S)-(-)- and (3R,4R)-(-)-4-hydroxymellein (2 and 3). The three melleins and tyrosol were also produced by N. parvum, while N. australe produced (R)-(-)-mellein (1), neoanthraquinone (5), tyrosol (8), and p-cresol (9). Luteopryoxin (4), neoanthraquinone (5), and luteoxepinone (7) were characterized by analyses of physical data, essentially one- and two-dimensional nuclear magnetic resonance and high-resolution electrospray ionization mass spectrometry. The relative and absolute configurations of luteopyroxin (4) were determined by nuclear Overhauser effect spectroscopy and experimental and calculated electronic circular dichroism data. When assayed on grapevine leaves, neoanthraquinone (5) showed the highest toxic effect, causing severe shriveling and withering. Luteopyroxin (4), nigrosporione (6), and luteoxepinone (7) also showed different degrees of toxicity, while p-cresol (9) displayed low phytotoxicity
Chiral/ring closed vs. achiral/open chain triazine-based organogelators: induction and amplification of supramolecular chirality in organic gels
The purpose of this study is to compare the gelling behavior of two molecules: a chiral compound and its achiral counterpart. The chiral partner is characterized by a rigid, chiral pyrrolidine nucleus, while the achiral one contains a flexible diethanolamine moiety. The chiral compound is an already known good organogelator, but also the achiral compound shows remarkable gelling properties. Very interestingly, a small fraction of the chiral compound induces chirality and strong CD effects in its aggregates with the achiral one. The observed chirality amplification corresponds to a peculiar sergeant-and-soldier effect. Molecular modelling and CD calculations suggested a model for the supramolecular assembly of hetero-aggregates that fits the experimental data
Organocatalytic alkylation of carbohydrate-containing aldehydes with dihydroquinoline N,O-acetals: Absolute configuration of 1,2-dihydroquinolines
The direct catalytic α-amidoalkylation of dihydroquinolines with aldehydes bearing oxygen functionalities at different positions in a Mannich-type reaction has been studied. β-Alkoxy-aldehyde 1d gave high enantioselectivity, albeit with an inherently poor diastereoselectivity, while the use of α-alkoxy aldehydes 1c was detrimental also to enantioselectivity. Mannich-type reactions have been studied for the first time using new chiral carbohydrate-derived aldehydes 1a,b showing a reactivity markedly influenced by the presence of water. The chiral glycidic backbone showed a slight but significant influence on the overall stereochemical outcome only when present in α-position of the aldehyde. The absolute stereochemistry of the products was studied by electronic circular dichroism (ECD) spectra and compared with theoretical calculations. ECD analysis easily provides the absolute configuration of 1,2-dihydroquinoline derivatives such as quinoline-1(2H)-carboxylates
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