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Biomedical subjects

A Fini

Publications and source records attributed to A Fini.

At least 37 records · Page 2Linked to original sources
PubMed1998

Study of the antioxidant effect of several selenium and sulphur compounds.

Four selenium derivatives (sodium selenate, sodium selenite, selenourea and selenomethionine) and the sulphur analogues (sodium sulfate, sodium sulfite, thiourea and methionine), together with urea, were examined by means of polarography to study their reactivity towards superoxide ion O2. In order that experimental results could be applied to physiological conditions and to control the electroreduction of oxygen, most reactions were carried out in model systems (in the presence and in the absence of triphenyl phosphine oxide and at increasing pH) which are briefly described and discussed. Sodium sulfite and thiourea react with molecular oxygen; selenourea originates an anodic wave, although under other pH conditions. Other compounds (selenate, selenite, seleno-methionine and methionine) display an interesting antioxidant capacity because they catalyse the disproportion of the superoxide ion, as documented by the increase in the limiting current. Methionine appears to be particularly efficient in this respect, since it retains its catalytic ability in a poorly protic environment. Experimental results support the view that exogenous compounds, administered for particular purposes, can display unanticipated, and sometimes positive, side effects.

Antioxidants↗
PubMed1998

[Prevalence of goiter and urine iodine in a school population in an area of the Bolognese Apennines].

We evaluated goiter prevalence and urinary iodine excretion (UIE) in schoolchildren living in three villages of the Appennines in the Bologna district-Castel d'Aiano (CA), Gaggio Montano (GM) and Pietracolora (PC). 175 age-matched schoolchildren living in the urban area of Bologna were considered as control group. In the control area the presence of goiter was documented in 11 out of 175 subjects (6.3%). In the mountain area the presence of goiter was documented in 42 out of 233 subjects (18%) (p < 0.0001 vs control area). In the urban control area the UIE was 159 micrograms/l (median; range 19-298). In the mountain area the UIE was 119 micrograms/l (median; range 10-286) (p < 0.001 vs control area). We observed the highest prevalence of goiter and UIE levels < 100 micrograms/l only in the village of PC, which is still characterized by geographical isolation and rural economy.

Biomarkers↗
PubMed1998

Myocardial perfusion, glucose utilization and oxidative metabolism in a patient with left bundle branch block, prior myocardial infarction and diabetes.

A diabetic patient affected by insulin-dependent diabetes, significant stenosis of left anterior descending (LAD) coronary, thrombolyzed myocardial infarction and complete left bundle branch block (LBBB) was examined by PET. Myocardial perfusion, glucose utilization and oxidative metabolism were evaluated by 13N-ammonia, 18F-fluorodeoxyglucose (FDG) and 11C-acetate, respectively. Despite severe damage in 18F-FDG uptake in the septum, with a septum-to-lateral ratio (S/L R) equal to 0.38, the oxidative metabolism in this area, evaluated quantitatively by dynamic acquisition, was relatively preserved (S/L R = 0.82), with a distribution similar to perfusion (S/L R = 0.87). These data reveal selective damage in glucose utilization in the septum in LBBB, unrelated to perfusion reduction and with preserved oxidative metabolism. Moreover, our experience could suggest an overestimation of the necrotic area by 18F-FDG in LBBB patients.

Acetic Acid↗
PubMed1997

Interaction of iron(II) with bile salts.

Iron(II) ions react with small aggregates of cholate, glycocholate, chenodeoxycholate, and deoxycholate to form soluble and colloidal compounds. Taurocholate under conditions used does not react with the Fe2+ ion. Small aggregates of dihydroxy bile salts (predominating in the premicellar region, at concentrations of the bile salt above 1 mmol dm-3) have a larger affinity for Fe2+ compared to those formed from cholate anions. In their interactions with small aggregates of cholate anions, the Fe2+ ion shows an affinity comparable to that of Cu2+ and Cd2+ and somewhat larger than that of Zn2+. Small aggregates of cholate show a higher ability to mask Fe2+ than those of taurocholate and glycocholate. Interaction of glycocholic acid anions with Fe2+ ions is sufficient to prevent iron(II) precipitation.

Anions↗
PubMed1997

Fractal analysis of beta-cyclodextrin-indomethacin particles compacted by ultrasound.

An association between indomethacin and beta-cyclodextrin (beta-CD) was obtained by compacting a 1:2 molar physical mixture by ultrasound. The product prepared by this technique was compared with the initial physical mixture and with materials having the same composition but prepared by a simple compaction and kneading process. The samples examined by scanning electron microscopy revealed morphological differences related to the methods of preparation. In particular the material obtained by ultrasound had a smooth surface and on milling produced particles of uniform size; moreover EDAX analysis (energy dispersion analysis by X-rays) also revealed a homogeneous distribution of the two components in each particle examined. Surface fractal dimension of the surface of these particles is very low, suggesting the presence of a regular and smooth surface whereas the sample obtained by kneading had a higher value. The reactive dimension related to dissolution was much higher than the corresponding surface dimension in all cases and had comparable values for all samples regardless of the techniques used. This behavior was attributed to the hydrophilicity of beta-CD, which levels the differences during dissolution and which could be originated by surface imperfections. Experimental results suggested that the material obtained by ultrasound had a dissolution rate comparable to that measured with the kneaded material. The use of ultrasound, however, can both reduce the production time and improve the homogeneity of the association between indomethacin and beta-CD.

Cyclodextrins↗
PubMed1996

Interaction between trace elements: selenium and cadmium ions.

The interaction between several inorganic and organic selenium-containing compounds (selenite, selenate, selenourea and selenomethionine) and Cd2+ ions was studied by polarography. The changes in polarographic currents and half-wave potentials of the metal ions as a function of the Se-derivative concentration were followed. Experimental results suggest a different behaviour depending on the oxidation state of selenium. Any interaction between selenate and Cd2+ ions can be excluded. In the case of selenite, the presence of complexes in the solution was demonstrated. The shift in the Cd2+ reduction half-wave potential when a relatively high concentration of selenourea is present indicates formation of complexes, while the decrease in limiting current reflects the limited solubility of the complex itself. Results concerning selenomethionine suggest a very weak interaction with Cd2+ ions. These preliminary results are discussed in comparison with previous findings in cellular systems and may prove helpful in understanding cadmium ion toxicity and the in vivo altered distribution of various metal ions following the administration of selenium compounds.

Cadmium↗
PubMed1996

Fractal analysis of sodium cholate particles.

A fractal analysis was carried out on the powder particles of two samples of sodium cholate. A commercial sample had very irregular particles agglomerated, and accordingly the fractal dimension of the surface was 2.98, suggesting a noteworthy roughness of the particle surface; scanning electron microscopy showed that this was due to irregularities caused by a disordered agglomeration of very small particles, resulting in larger particles showing polygonal and smooth but limited facets. A second sample was obtained by recrystallization from ethanol of the commercial sodium cholate and contained large and regular particles, with very smooth surfaces. The fractal dimension therefore was accordingly low. Despite these differences, the two samples had similar, high reactive dimension values to dissolution (2.96 and 2.76, respectively), suggesting that the surfactant behavior of sodium cholate is an important parameter in driving the dissolution of the solid particles and leveling the surface defects.

Cholic Acid↗
PubMed1995

Interaction between Cu2+ ions and cholic acid derivatives followed by polarography.

Interaction of bile salts with Cu2+ ions in unbuffered systems containing 0.15 M NaNO3 was followed by measuring polarographic limiting currents and half-wave potentials. Whereas taurocholate forms neither soluble complexes nor compounds of limited solubility, cholate, glycocholate, and dehydrocholate from both soluble complexes and slightly soluble salts of copper(II) with small aggregates of bile salts. The stability of soluble complexes is comparable for cholates, dehydrocholates, acetates, and acetylglycinates, but smaller for glycocholates. The solubility of the copper(II) salts with small aggregates decreases in the sequence: glycocholate > cholate >> dehydrocholate. It is proposed that these salts are formed by interaction of a copper(II) ion with two carboxylic groups located on the small aggregate in a sufficiently small distance. In the presence of excess cholate the precipitated copper(II) salts are dissolved. It is assumed that at high bile salt concentrations, where precipitates are not observed, larger aggregates are formed that have free carboxylate groups, which increase their solubility in aqueous solutions. For glycocholate, within the accessible concentration range and within the time-frame used (24 h for the establishment of the equilibrium), the formation of such larger aggregates was not observed, even when its "cmc" is comparable with that of cholate. The absence of formation of larger aggregates for dehydrocholate parallels its tendency not to form "micelles".

Carboxylic Acids↗
PubMed1995

Experimental evaluation of a model for predicting micellar composition and concentration of monomeric species in bile salt binary mixtures.

The critical micellar concentration (cmc) values of some mixed systems containing two bile salts were determined by a maximum pressure bubble method and compared with those derived from a theoretical model developed for nonionic surfactants to assess the applicability of this model to such systems. Some assumptions on which the presumed validity of this model was based are discussed. The following binary mixtures were investigated: sodium chenodeoxycholate with cholate, ursocholate and ursodeoxycholate, either unconjugated or conjugated with taurine and glycine at different mole fractions (0, 0.25, 0.5, 0.75, 1) in 0.15 M NaCl. For these mixtures, experimentally determined data were in good agreement with values predicted by the theoretical model: both the cmc and the surface tension at this concentration of the mixtures were intermediate between those of the two pure bile salts; also, as the total bile salt concentration increased, the mixed micelles became enriched with the bile salt having the highest cmc, whereas the total monomer activity, determined by a potentiometric method employing a bile salt-selective electrode, increased only slightly. To test this model in an in vitro system, surface tension was also measured in ox bile samples that were enriched by 50% with sodium ursodeoxycholate, chenodeoxycholate, or their taurine amidates. The cmc and the surface tension at this concentration of the artificial bile increased when enriched with a bile salt with a cmc higher than that of endogenous salts (e.g. ursodeoxycholate versus taurocholate), whereas the reverse occurred for mixtures enriched with a bile salt with a lower cmc, such as chenodeoxycholate.(ABSTRACT TRUNCATED AT 250 WORDS)

Bile Acids and Salts↗
PubMed1993

Cancer in a young population in a dioxin-contaminated area.

An industrial accident in Seveso, Italy, in 1976, caused contamination of the residential community with 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). We investigated cancer occurrence in the first post-accident decade (1977-1986) among nearly 20,000 subjects aged 0-19 years. People who left the area were actively followed with a 99% follow-up rate. For reported cancer cases confirmation was obtained through consultation with original medical records. Two ovarian cancers were observed versus none expected. A suggestive increase was seen for Hodgkin's lymphoma (relative risk [RR] = 2.0; 95% confidence interval [CI] = 0.5-7.6). Myeloid leukaemia showed a clear, but not statistically significant increase (RR = 2.7; 95% CI = 0.7-11.4). The most prominent result concerned thyroid cancer, not just for the magnitude of the increase (two cases, RR = 4.6; 95% CI = 0.6-32.7), but also for its consistency with experimental findings and previous observations in humans. Any conclusive interpretation would be premature because of the short time since initial exposure, ecological definition of exposure status, and limited number of events.

Adolescent↗
PubMed1993

Diclofenac/N-(2-hydroxyethyl)pyrrolidine: a new salt for an old drug.

Twenty-four diclofenac salts were prepared using inorganic and organic, linear and cyclic, hydrophilic and hydrophobic bases and their behaviour in polar and poorly polar solvents was examined. Most salts were found more soluble in 1-octanol than in water, suggesting a fair hydrophobicity of these compounds and their existence as ion pairs in non-polar solvents. The salt diclofenac/N-(2-hydroxyethyl)pyrrolidine (DHEP) is the most soluble of this group in 1-octanol (8.39% w/w) and in water (1.89% w/w), where it displays a surfactant behaviour above 1.44% w/w, which can be considered as a critical micellar concentration. It was possible to study the surface activity of diclofenac only using DHEP, since all other salts of this group are not soluble enough to overcome the critical concentration. The mild detergent properties of DHEP were confirmed by the solubilization of lecithin and the formation of mixed micelles with bile salts: these properties appear very interesting in developing new pharmaceutical forms containing DHEP, as a chemical form for the delivery of the active principle diclofenac.

Diclofenac↗
PubMed1992

Effect of basic cholane derivatives on intestinal cholic acid metabolism: in vitro and in vivo activity.

A representative series of hydroxy-5 beta-cholanyl-24-amines were tested both in vitro and in vivo with respect to their activity against the intestinal bacteria responsible for bile acid metabolism. For the in vitro studies, radiolabeled [14C]cholic acid was incubated with human stools both in aerobic and anaerobic conditions in the presence of the title compounds at a dose of 10 micrograms/mL, and the biotransformation of cholic acid into radiolabeled deoxycholic acid and other metabolites was followed by TLC-radiochromatography. Of the compounds studied, 3 alpha, 12 alpha-dihydroxy-5 beta-cholan-24-N-methylamine showed the highest activity. This compound was used for the in vivo studies and was shown to inhibit the formation of endogenous secondary bile acids when chronically administered to rats at a dose of 60 micrograms/day for 15 days. The treated rats showed an increased ratio of taurocholic acid (primary bile acid) to taurodeoxycholic acid (secondary bile acid) in bile, a fact further suggesting a potent antibacterial activity of the compound toward bacteria responsible for bile acid metabolism.

Aerobiosis↗
PubMed1992

Basic cholane derivatives. XI: Comparison between acid and basic derivatives.

A series of hydroxycholan-24-amines was synthesized; the carboxyl group of starting unconjugated bile acids was transformed into a basic moiety [-NH2, -NHCH3, -N(CH3)2, or -NHCH2C6H5] at C-24. Solubilities, acidities, partition coefficients, and critical micellar concentrations were measured and compared with those of the corresponding bile acids. Because the steroid nucleus in the amines is the same as that in the bile acids, most of the physical-chemical properties of the two compound classes were similar. The amines were more soluble than the corresponding acids; solubilities depended mainly on the number of steroid hydroxyls and, to a lesser extent, on the side chain. Amines are strong bases in water, whereas unconjugated bile acids can be classified as weak acids. N-Benzylamino derivatives have higher log P (P is partition coefficient) values, as a consequence of the bulky hydrophobic substituent; the log P values were almost the same for the amines and the bile acids and depended on the steroid hydroxyls. Amines can self-aggregate at an acidic pH and form cationic micelles; the critical micellar concentrations of amines were of the same order of magnitude as those of bile acids. The introduction of a basic function in the side chain of the cholane moiety increased the antimicrobial activity toward most gram-positive strains.

Bile Acids and Salts↗
PubMed1992

Chemical properties of bile acids. V. Interaction with concentrated sulfuric acid.

The reaction between concentrated sulfuric acid and steroid hydroxy compounds, previously studied for a series of sterols, was used to develop an analytical method for bile acids. The reaction generates species absorbing in the wavelength ranges 300-320 and 370-390 nm, corresponding to isomeric allylic and dienylic carbocations. Eleven bile acids were examined and influence of time, temperature and sulfuric acid concentration on the chromogenic reaction was studied. The linear dependence of absorbance on concentration of individual bile acids demonstrates that the method can be used to measure spectrophotometrically micromolar concentrations of bile acids.

Adsorption↗
PubMed1991

Release of ketoprofen from dermal bases in presence of cyclodextrins: effect of the affinity constant determined in semisolid vehicles.

We describe a method to determine the affinity constant values between Ketoprofen and beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin in semisolid vehicles. The method is based on the diffusion of the drug, released from semisolid vehicles, through a lipidic non porous membrane. The affinity constants of Ketoprofen towards cyclodextrins as determined in semisolid media better represent the release of the drug from dermal bases than the corresponding values in aqueous systems.

Chemical Phenomena↗
PubMed1991

Antimicrobial activity of basic cholane derivatives. X. Synthesis of 3 alpha- and 3 beta-amino-5 beta-cholan-24-oic acids.

A simple and convenient route to 3 alpha- and 3 beta-amino-5 beta-cholan-24-oic acids was developed via Leuckart-Wallach amination reduction and subsequent acid hydrolysis. Two epimeric formylamino derivatives were produced (alpha and beta), approximately in a 1:1 ratio, as determined by 13C nuclear magnetic resonance spectroscopy. The two isomers were separated by making use of their different solubilities in ethyl ether. The absolute configuration of the two amino acids was assigned by comparison with authentic reference samples.

Lithocholic Acid↗
PubMed1991

Chemical properties-dissolution relationship. IV. Behaviour in solution of the diclofenac/N-(2-hydroxyethyl) pyrrolidine salt (DHEP).

The behaviour in solution of the salt formed between diclofenac and N-(2-hydroxyethyl) pyrrolidine (DHEP) was examined. This salt is more soluble and dissolves more rapidly than sodium diclofenac and tends to give rise to supersaturated solutions, that only slowly evolve to equilibrium. Above 35 mM of DHEP, the solutions show unexpected solubilization ability towards sparingly soluble materials. The faster plasma level found, when DHEP is administered per os, can be associated to this weak detergency. These properties make DHEP a suitable pharmaceutical form to prepare extemporary solutions for short term analgesic therapy.

Diclofenac↗