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Biomedical subjects

P Franke

Publications and source records attributed to P Franke.

At least 109 records · Page 6Linked to original sources
PubMed1989

[Biotransformation of pyridazines. 1. Pyridazine and 3-methylpyridazine].

Pyridazin (1) and 3-methylpyridazine (6) undergo oxidative biotransformation in an unexpected high degree. Beside the unchanged compounds, after administration of 1 two isomeric monohydroxylated products (2, 3), 4,5-dihydrodihydroxypyridazine (4) and 4,5-dihydroxypyridazine (5) and after administration of 6 one ringhydroxylated 6-derivative (7), 3-hydroxymethylpyridazine (8), one ringhydroxylated 3-hydroxymethylpyridazine derivative (9) and 4,5-dihydroxy-3-methylpyridazine (10) were suggested as urinary metabolites in rats. 2 and 7 are the main metabolites of 1 and 6, respectively.

Animals↗
PubMed1989

[Clemastine metabolites in the feces and urine of the rat].

After oral application of clemastine [(1), (+)-2-(2-[1-(4-chlorophenyl)-1-phenylethoxy]-ethyl)-1-methylpyrrol idine- hydrogenfumarate], to rats (200 mg/kg) 18 phase I- and II-metabolites have been detected and isolated from urine and faeces. They are products of fission of the ether bond, of aromatic and aliphatic oxidation, respectively, of alcoholic dehydration, decarboxylation, N-oxidation, O-methylation and conjugation as phase II steps. Phenolic compounds represent-in contrast to some other diphenylmethane derivatives, especially basic benzilates (propiverine, denaverine)-the main metabolic products formed by dihydrodiol mechanism or direct oxigenation. The structure of metabolites were elucidated by MS.

Animals↗
PubMed1989

[Biotransformation of 5-phenyl-1,3,4-benzotriazepines].

After administration of three 2-aminosubstituted 5-phenyl-1,3,4-benzotriazepines with hypoglycemic effects to rats 10 metabolites were isolated from urine and feces besides traces of the unchanged drugs. N-Dealkylation, aromatic hydroxylation, N-acetylation and ring contraction by hydrolytic processes beginning in the stomach occurred. The main excretion route is with the feces.

Animals↗
PubMed1989

[Immunosuppressive and virostatic actions of sterones from Petunia hybrida Vilm].

10 Ergostan-3-on derivatives presumably in the majority ergosta-1,4-dien-3-on derivatives could be isolated from Petunia hybrida VILM. Two were identified as the known compounds petuniasterone A and petuniasterone-C-22-O-acetate. The structures of two other compounds named petuniasterone-D-diacetate and 30-hydroxypetuniasterone A could be elucidated. The molecular formulas of the remaining substances were ascertained by mass spectroscopy. The petuniasterones inhibited the proliferation of stimulated human lymphocytes in non-cytotoxic concentrations, possessing therefore possibly immunosuppressive effects. Extracts of the plant and fractions containing a synergistically effective blue fluorescing substance retarded the multiplication speed of influenza viruses; pure petuniasterones were ineffectiv under our conditions in this regard.

Antiviral Agents↗
PubMed1988

Interactions between bladder tumor cells as tumor spheroids from the cell line J82 and human endothelial cells in vitro.

Multicellular tumor spheroids (MCTS) are a reliable model of nonvascularized tumor cell aggregates showing a well defined three-dimensional growth pattern and are comparable with small metastatic cancer cell complexes in blood circulation. In the present study we have established a co-culture system of multicellular bladder tumor spheroids with human endothelial cells on extracellular matrix (ECM) in order to investigate morphological and proliferative changes of endothelial and tumor cells within a defined time of cell-cell interaction. The MCTS--endothelial cell--extracellular matrix complex was observed within coculture periods from 1/2 to seven days. Morphological changes (light microscopy, scanning and electron microscopy) indicated that MCTS are not influenced by cocultured endothelial cells. The tumor cells invaded into the ECM after degradation of endothelial cells in the center of the contact zone. Endothelial cells, however, showed degenerative changes as well as a complex reaction in their proliferation activities. We could recognize an initial increase of proliferation of endothelial cells next to the MCTS. Later on, endothelial cells next to invading tumor cells showed changes in morphological polarity. The model system used has the advantage of using human tumor tissue. It distinguishes between basic cellular mechanisms like adherence, migration, DNA synthesis and proliferation in the study of the contact of tumor cells and vascular endothelial cells as an important event in hematogenous tumor spread.

Cell Communication↗
PubMed1988

[Triperiden (Norakin): biotransformation in vivo and in vitro].

After oral application of triperiden (1; Norakin) to male Wistar rats besides the unchanged isomers of 1 (1a and 1b, respectively [3]) six hydroxy metabolites and an artifact were isolated from urine and also identified in faeces. All metabolites are hydroxy derivatives of the piperidine and the tricyclic moieties of the molecule 1a. No hydroxylation of the phenyl ring was observed. 10-20% of the metabolites were sulfate and/or glucuronide conjugates. Main metabolites were 2 and 3 (greater than 50% of the total excretion products). About 70% of 1a, 1b and metabolites were excreted with the urine. The in vivo metabolites also could be identified in the 9000 g supernatant of rat and human liver homogenates.

Animals↗
PubMed1988

[Biotransformation of denaverin (Spasmalgan) in the rat].

After oral application of denaverine hydrochloride to rats (200-250 mg/kg) 12 metabolites have been detectecd in urine. Besides the unchanged drug, 8 metabolites were identified by MS as 2,2-diphenyl-(2-dimethylaminoethyl) acetate (3), diphenylacetic (5) and benzilic acid (6); methyl-and ethyl [2-(2-ethylbutoxy)-2,2-diphenyl]acetate (7, 11), methylbenzilate (10), N-demethyl-1 (12) and 3,3-diphenyl-morpholin-2-one (13). 6 and the metabonate 13 represent the main metabolic products. Compounds 7 and 11 indicate the metabolic pathway about an alkoxybenzilic acid (4). Phenols resp. conjugates were not detected.

Analgesics↗
PubMed1988

[The stability of bromhexine and the structure of its degradation products].

Refluxed acid or neutral aqueous solutions of Bromhexine (1) show four degradation products. 1 is decomposed at room temperature (20 degrees C; 1 year) less than 1%. Degradation products of crystalline 1 are not detectable in the temperature-moisture-test. Under normal storage conditions a 5-year stability for aqueous solutions and a more than 10-year stability for crystalline 1 are estimated. Very small amounts of three degradation products were isolated by TLC. According to MS-, UV- and IR-analysis their structures are 3-cyclohexyl-6,8-dibromo-chinazoline-4-one (2a), 3-cyclohexyl-6,8-dibromo-chinazoline (2b) and 3-amino-4,6-dibromo-benzaldehyde (3). The structure of N-Methylcyclohexylamine is supposed for a further product. Ms fragmentation and degradation mechanisms are discussed.

Bromhexine↗
PubMed1988

[The biotransformation of propiverin hydrochloride (Mictonorm)].

Propiverine hydrochloride [1; hydrochloride of O-n-Propyl-(N-methylpiperidinyl-4)-benzilate; Mictonorm] is metabolized after p.o. application of 25 mg/kg on rats almost completely. Besides of small amounts of unchanged 1 in urine were detected the phase-I metabolites N-methylpiperidinyl(4)-benzilate (2), 2,2-diphenyl-5-methyl-1, 4-dioxan-3-on (3), N-oxide of 2 (4), benzilic acid (5) and O-n-propylbenzilic acid (6) using ms, dc and hplc comparison of the isolated compounds with authentic samples. The structure of further metabolites, i.e. monohydroxy-benzophenone (7), acetoxy-1-derivatives (8) and ethylbenzilate (9) were elucidated by high resolution MS.

Animals↗
PubMed1987

[Nosocomial infection].

Sepsis is a systemic disease caused by pathogenic microorganisms and their toxic products in blood. Very often it is not possible to identify the pathogenic organisms before therapeutic treatment. Thus, diagnosis has to be made based on the patients' disposition as well as clinical symptoms. In septic patients clear alterations of plasma protein fractions are found. Depending on the clinical degree of severity, the low molecular proteins, detectable by column chromatography in plasma fraction III, are considerably increased. Population of implanted synthetic materials (such as catheters and cardiac valves) with facultative pathogenic microorganisms that may persist under antibiotic influence due to extracellular polymeric substances, is also of great importance. Therapy with antibiotic combinations is the most important therapeutic principle for sepsis and can be intensified by simultaneous administration of immunoglobulins.

Anti-Bacterial Agents↗
PubMed1986

[AIDS in a woman having had sexual relations with a patient with hemophilia A. Characteristic findings in DNA image cytometry].

A 37-year-old female patient reported marked weight loss, prolonged alopecia, recurrent infections and watery diarrhoea. Examination revealed Salmonella infection, candidiasis and immunological signs of previous toxoplasmosis. Between 1978 and 1981, the patient had had close sexual relations to a patient with haemophilia A. Due to this fact, AIDS was suspected. Serological tests for HIV were not available at the time. The findings in DNA image cytometry (nuclear DNA inclusion bodies, polyploid lymphocyte nuclei and binuclear lymphocytes) suggested a viral infection of the lymphoid cells. Electron microscopy revealed in hepatocytes and cerebral cells intranuclear inclusion bodies whose size and contents were not compatible with an infection caused by cytomegalovirus, herpes virus or Epstein-Barr virus. In autopsy, infections of various organ systems such as pneumonia, tracheobronchitis, urocystitis, pyelonephritis, Candida oesophagitis and enteritis were found.

Acquired Immunodeficiency Syndrome↗
PubMed1986

CCA paper: a new two-dimensional cyanuric chloride-activated matrix for universal application in molecular biology.

A novel two-dimensional cyanuric chloride-activated (CCA) paper has been developed. It is composed of a cellulosic base, covalently bound cyanuric chloride, and microprecipitated complex cyanuric chloride-sodium chloride crystals on its surface. CCA paper covalently binds nucleic acids and proteins. Its binding capacity for nucleic acids is about 400 micrograms/cm2. Sealed into nitrogen-filled bags and stored at -20 degrees C, it retains its binding activity for at least a year and is always ready for use. CCA paper has been successfully used for capillary and electroblotting of DNA, RNA, and proteins (Southern, Northern, and Western blotting) as well as for dot tests. Furthermore, it was applied to colony and plaque hybridization. A unique property of it is that it permits the staining of proteins after blotting and subsequent performance of radioimmunological detection of specific protein components. This has proven advantageous in two-dimensional Western blotting experiments. Of further importance is its ability to bind DNA fragments from one up to several hundred bp from polyacrylamide sequencing gels.

Animals↗