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Engineering blood: synthetic substitutes from fluorinated compounds.

Concerns about blood safety and the logistical problems associated with conventional transfusion have fuelled the search for effective alternatives (so-called blood substitutes). Such materials include hemoglobin derivatives and those based on synthetic, highly fluorinated, inert organic compounds called perfluorochemicals (PFCs). PFCs dissolve large volumes of oxygen and other gases, are unreactive in the body, and are excreted primarily as a vapor by exhalation. Liquid PFCs are immiscible with blood and other body fluids, but can be injected safely into the bloodstream as submicron emulsions. Emulsified PFCs have been evaluated in clinical trials as temporary, intravascular tissue-oxygenating fluids. One such emulsion, a commercial perflubron-based, phospholipid-stabilized formulation, is in advanced clinical trials as an alternative to transfusing donated (allogeneic) blood during surgery. Basic and clinical studies have shown that this emulsion can adequately maintain tissue oxygenation during acute blood loss with no abnormal hemodynamic changes. The use of PFC emulsions as an efficacious, short-term transfusion alternative underpins the longer term objective of producing a totally synthetic, bioengineered blood substitute.

Animals↗

Applications of fluorinated compounds as phases and additives in chromatography and their uses in pharmaceutical analysis.

A review is presented of the use of fluorinated phases and fluorine-containing surfactants in chromatography. Additionally, new information is provided on the application of two nonionic perfluorosurfactants as reversed-phase mobile phase additives to enhance chromatographic performance of aromatic amines and some amines of pharmaceutical significance.

Chromatography↗

Gel-derived materials of a CaO-P(2)O(5)-SiO(2) system modified by boron, sodium, magnesium, aluminum, and fluorine compounds.

Bioactive glass-ceramic materials of the CaO-P(2)O(5)-SiO(2) system modified by adding boron, magnesium, sodium, fluorine, and aluminum were obtained using the sol-gel method. Gel-derived materials were produced in the pellet form obtained by compression of powders as well as in coatings on glass slides. The materials obtained were examined in vitro with regard to the ability of calcium phosphate layer to form on the material surface as the result of contact with simulated body fluid (SBF). SBF pH changes and calcium solubility in this solution were determined and scanning electron microscopy, energy-dispersive X-ray analysis, and infrared spectroscopy studies were conducted before and after contact of the materials with SBF. The gels modified by aluminum were amorphous, whereas the sodium and fluorine additives promoted the bulk crystallization of gel-derived materials. The ability of calcium phosphates to crystallize on the surface of gel-derived materials depended only slightly on the types of additives applied, and the character of this dependence was different from that observed in melted glasses. Moreover, to estimate the biocompatibility of gel-derived coatings, we examined the proliferation, collagen synthesis, adhesion, and morphology of fibroblasts (NRK cells) cultured in the presence of gel-derived materials. The results of these experiments showed that none of the tested materials significantly reduced any cell function.

Animals↗

1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1H-pyrrol-1-yl)-quinoline-3-carb oxylic acid, a new fluorinated compounds of oxacin family with high broad-spectrum antibacterial activities.

The synthesis of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1H-pyrrol-1-yl)quinoline-3-carboxy lic acid, a new fluorinated high broad-spectrum antibacterial agent related to nalidixic acid is described. The title compound has been prepared by the reaction of 4-fluoro-3-(1H-pyrrol-1-yl)aniline with diethyl ethoxymethylenemalonate, cyclization of the malonate obtained to the quinolinecarboxylate ester, ethylation of the ester, followed by hydrolysis with aqueous sodium hydroxide. The new derivative proved very active against both gram-positive and gram-negative bacteria. Its activities in comparison with those of nalidixic acid, pipemidic acid, piromidic acid and enoxacin were found to be greatly superior with regard to the unfluorinated compounds and somewhat superior also to enoxacin. The known 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(pyrrolidin-1-yl)quinoline-3- carboxylic acid, here prepared by catalytic hydrogenation of the pyrrole moiety of the title compound, has been found to be less active as an antibacterial agent.

Anti-Bacterial Agents↗