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E Boldrini

Publications and source records attributed to E Boldrini.

29 records · Page 2Linked to original sources

Benzisothiazole-1,1-dioxide alkanoic acid derivatives as inhibitors of rat lens aldose reductase.

Derivatives of 4-substituted 1,2-benzisothiazole-1,1-dioxide alkanoic acids were prepared and their in vitro aldose reductase inhibitory activity was tested in rat lens enzyme. The acetic derivatives 10, 12, and 16a-d proved to be much more potent inhibitors than the propionic derivatives 11, 13, and 17a-d. The presence of an acyl moiety on the amino group in position 4 of the acetic derivatives 16a-d led to a significant increase in activity with respect to the parent compound 14. One of the most active compounds in vitro, 10, was also evaluated in vivo as an inhibitor of glutathione lens depletion in galactosemic rats, but it did not show any activity in maintaining the rat lens glutathione level, probably due to problems of ocular bioavailability or metabolism.

Aldehyde Reductase↗

[Blood doping].

Explore the source record for details and available documents.

Doping in Sports↗

In vitro activity of metronidazole alone and in combination with clotrimazole against clinical isolates of Trichomonas vaginalis.

Trichomonas vaginalis vaginitis is generally treated with oral metronidazole. Widespread use of this drug has led, however, to selection of resistant strains. Topical therapy seems appropriate whenever systemic high dosage schedule cannot be adopted in order to overcome resistance. This study was designed to assess the activity of metronidazole alone and in combination with clotrimazole, an imidazole derivative for topical use, against T. vaginalis. Tests were performed employing the antitrichomonas activity of a fixed ratio of metronidazole with clotrimazole (5:1) which has been recently suggested for topical therapy and the checkerboard technique. All tests were carried out under aerobic conditions to maximize T. vaginalis resistance traits. Minimum inhibitory concentrations (MICs) of metronidazole for the 12 strains studied were in the range reported in the literature (0.5-32 micrograms/ml). The interaction of metronidazole with clotrimazole as assessed by the checkerboard technique gave an indifferent outcome with all the strains assayed (FIC = 1-2). The fixed concentration of drugs, however, produced synergism (FIC = 0.5) in 5 of 12 isolates. Spontaneous resistant strains were not selected from T. vaginalis exposed to sub-lethal levels of the drugs or by culturing a large inoculum in the presence of 1, 2, 4 and 8 times the MICs of metronidazole alone or in combination with clotrimazole. These results confirm and extend previous reports highlighting the good in vitro efficacy of the association of metronidazole plus clotrimazole against T. vaginalis.

Animals↗

[Spontaneous bacterial peritonitis in liver cirrhosis. What tests to perform on the ascitic fluid?].

Spontaneous bacterial perionitis (SBP) is a relatively frequent complication of liver cirrhosis and is associated with a high mortality if not early recognized and immediately treated. The text-books of Medicine available in Italy suggest the use of traditional laboratory tests (gravity, total protein concentration, Rivalta's test) to whom add white blood cell count for the assessment of the nature transudative (not infected) or exudative (infected) of ascitic fluid; nevertheless, in every day clinical practice, the association between total protein concentration and type of ascitic fluid may be misleading with respect to the diagnosis of SPB. The aim of this retrospective study, undertaken on 86 patients with liver cirrhosis consecutively admitted and separated in two groups, one without and the other with PSB (white blood cell count > 500/mm3), was to identify criteria for diagnosis of PSB. The traditional laboratory tests were significantly different in the two groups but Rivalta's test. Yet, none of them showed a diagnostic measurement sufficient for the use in the diagnosis of PSB (positive predittive value: gravity 41%, Rivalta's test 36%, total protein concentration 40%). The results of this work show the traditional laboratory tests unable to define the nature of the ascitic fluid. For the diagnosis of PSB the only reliable parameter is the white blood cell count.

Aged↗

Acid derivatives of benzisothiazole-1,1-dioxide as inhibitors of rat lens aldose reductase.

A number of 6-substituted 1, 2-benzisothiazole-1, 1-dioxide alkanoic acids were synthesized and evaluated for crude rat lens aldose reductase inhibitory activity. The inhibitory potency of the acetic (6a, 10a), propionic (6b, 10b, 11b), and isopropionic (6c, 10c, 11c) derivatives was very similar and generally lower than that of the reference compound, Sorbinil. The presence of an acyl moiety on the amino group in position 6, as in the acetic and propionic derivatives 14a-f and 15a, b, respectively, resulted in a significant increase in activity. A good potency was shown by compounds 14g and 15g, in which a second carboxylic function is present on the 6-acylamino group. Also the open products 16, which contain the phenylsulfonyl fragment found in several known inhibitors of aldose reductase, were obtained and tested in the rat lens assay.

Aldehyde Reductase↗

Effects of radiographic contrast media on the serum complement system.

The authors explored the activation of the complement system produced by a nonionic organic iodine compound, namely iopamidol, which is proposed as a contrast medium for radiographic examination by intravenous and intra-arterial injection. The study was conducted in vitro versus established ionic contrasts (diatrizoate, iothalamate, acetrizoate) and a nonionic compound (metrizamide). The adopted experimental model was the immunohemolytic detector system, in which the immune complex consisted of goat erythrocytes sensitized with the corresponding antibody (hemolysin), and complement (C') was supplied by guinea pig serum. All the products caused complement activation. The results show that nonionic contrast media produce less activation of the complement system than the traditional ionic contrast. Thus the use of nonionic contrast for radiological procedures necessitating the introduction of contrast material into the blood compartment would imply a reduced risk of anaphylactoid reactions.

Animals↗

Competitive action of contrast media on the uric acid-albumin binding.

We investigated the competitive effect of iodinated contrast media on the binding of uric acid to albumin. This was an in vitro study utilizing the technique of equilibrium dialysis, with bovine serum albumin (BSA) as the protein substrate. It was demonstrated that some compounds, used for radiological visualization of the biliary passages, compete with uric acid for albumin binding. The meaning and clinical repercussions of this finding are discussed.

Animals↗

Simultaneous assay of bromosulfophthalein and phenolsulfonphthalein in the blood as a test of hepatic and renal functional capacity.

A spectrophotometric procedure for the assay of bromosulfophthalein and phenolsulfonphthalein in the plasma of various animal species and the half-life of the two dyes in plasma representing respectively the rate of liver depuration and that of kidney depuration are described. The method is easy to execute and lends itself particularly well for the simultaneous assessment of hepatic and renal function in the same animal.

Animals↗

Effect of xyloglucan (tamarind seed polysaccharide) on conjunctival cell adhesion to laminin and on corneal epithelium wound healing.

PURPOSE: To explore the role of a natural polysaccharide extracted from tamarind seed (xyloglucan, or tamarind seed polysaccharide, TSP) on the integrin-substrate recognition system and on repair of corneal wounds. METHODS: a) Cultured human conjunctival cells were labeled by addition of a tritiated amino acid mixture. Their adhesion to laminin-coated culture wells in the absence or presence of TSP was checked by radioactivity count. b) The corneal epithelium of albino rabbits was damaged by applying a paper disc soaked with n-heptanol. The eyes were then treated with TSP, with a hyaluronate reference formulation and with normal saline solution (controls). The diameter of corneal wounds was measured daily, after fluorescein staining. RESULTS: Compared to hyaluronate, TSP slightly but significantly increased the wound healing rate. TSP 1.0% exerted a positive influence on cell adhesion to laminin, up to a certain laminin concentration. CONCLUSIONS: The ability of the polysaccharide to promote corneal wound healing might depend on its influence on the integrin recognition system.

Animals↗

A difficult early diagnosis of pancreatic body neoplasia.

The Authors report the case of a 60-year-old man, V.A., a smoker with type II diabetes and cholelithiasis. One month after the onset of symptoms in March 1995, his clinical picture led us to suspect a pancreatic adenocarcinoma. Only 110 days after the initial discovery of a high CA 19-9, following the failure of numerous techniques and the solution of various problems of differential diagnosis, the first unclear X-ray image of a suspected pancreatic neoplasia was obtained. A new computed tomography scan and a further increase in CA 19-9 later confirmed the diagnosis. Duodenopancreatectomy with splenectomy for adenocarcinoma was performed. The thread connecting 150 days of clinical history is CA 19-9, which acted as an ideal marker. It enabled a clinical "rarity" (pancreatic neoplasia in its initial stages) to be diagnosed and it increased as the neoplasia developed. After surgical removal of the tumor, the marker is now returning to normal levels and will be used to monitor the post-operative phase, when any increase in level could mean a recrudescence of the disease.

Adenocarcinoma↗