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Digitale Medien

CP-82,996, a novel diglycoside polyether antibiotic related to monensin and produced byActinomadura sp. (1990)

Dirlam, John P. ; Belton, Annette M. ; Bordner, Jon ; [weitere]

Springer

Journal of industrial microbiology and biotechnology 6 (1990), S. 135-142

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ISSN: 1476-5535

Schlagwort(e): Ionophore ; Actinomadura sp. (ATCC 53764) ; Anticoccidial agent

Quelle: Springer Online Journal Archives 1860-2000

Thema: Biologie , Werkstoffwissenschaften, Fertigungsverfahren, Fertigung

Notizen: Summary A new polyether antibiotic CP-82,996 (C50H86O16) was isolated by solvent extraction from the fermentation broth ofActinomadura sp. (ATCC 63764). Following purification by silica gel column chromatography and crystallization, the structure of CP-82,996 was determined by a single crystal X-ray analysis. The structure is closely related to monensin, but is unique in that it contains two sugar groups, whereas monensin has none. The1H and13C NMR chemical shifts and assignments for CP-82, 996 were elucidated, and they were compared with those determined previously for monensin. CP-82,996 is active against certain Gram-positive bacteria, and is a very potent anticoccidial agent. It effectively controlled chicken coccidiosis caused by severalEimeria species at 5–10 ppm in feed, and is 10–20 times more potent than monensin.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1007/BF01576433

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Digitale Medien

CP-60,993, a new dianemycin-like ionophore produced byStreptomyces hygroscopicus ATCC 39305: fermentation, isolation and characterization (1990)

Cullen, Walter P. ; Bordner, Jon ; Huang, Liang H. ; [weitere]

Springer

Journal of industrial microbiology and biotechnology 5 (1990), S. 365-374

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ISSN: 1476-5535

Schlagwort(e): CP-60,993 ; 19-Epi-dianemycin ; Polyether ionophore ; Anticoccidial agent

Quelle: Springer Online Journal Archives 1860-2000

Thema: Biologie , Werkstoffwissenschaften, Fertigungsverfahren, Fertigung

Notizen: Summary CP-60,993, 19-epi-dianemycin, is a novel polycyclic ether antibiotic produced byStreptomyces hygroscopicus ATCC 39305. Fermentation recovery, purification and crystallization were achieved using standard procedures. CP-60,993 was characterized as a monocarboxylic acid. Elemental analysis suggested a molecular formula of C47H78O14 for the free acid and C47H77O14 Na for the sodium salt. Crystalline form CP-60,993 sodium salt shows the following properties: m.p. 193∼205°C, E 1 cm 1% =157 at 232 nm, [α] D 25°C +11.0 (c 1, methanol). The structure, determined by MS, PMR and CMR, differs from dianemycin only in the stereochemistry at position 19. This was confirmed by X-ray crystallography carried out on the rubidium salt of CP-60,993. It exhibited activity in vitro against Gram-positive and anaerobic bacteria, efficacy againstEimeria coccidia in vivo in poultry, and stimulation in vitro of rumen propionic acid production.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1007/BF01578095

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Digitale Medien

Proton-Cotransport of Pravastatin Across Intestinal Brush-Border Membrane (1995)

Tamai, Ikumi ; Takanaga, Hitomi ; Maeda, Hiroshi ; [weitere]

Springer

Pharmaceutical research 12 (1995), S. 1727-1732

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ISSN: 1573-904X

Schlagwort(e): pravastatin ; intestinal absorption ; active transport ; pH-dependent transport ; HMG-CoA reductase inhibitor

Quelle: Springer Online Journal Archives 1860-2000

Thema: Chemie und Pharmazie

Notizen: Abstract Purpose. The purpose of the present study is to clarify the intestinal brush-border transport mechanism of a weak organic acid, pravastatin, an HMG-CoA reductase inhibitor. Methods. The transport of pravastatin was studied by using intestinal brush-border membrane vesicles prepared from rabbit jejunum, and uptake by the membrane vesicles was measured using rapid filtration technique. Results. The initial uptake of [14C]pravastatin was markedly increased with decreases in extravesicular pH and showed a clear overshoot phenomenon in the presence of a proton gradient (pHin/out = 7.5/5.5). A protonophore, carbonylcyanide p-trifluoromethoxyphenylhydrazone, significantly reduced the uptake of [14C]pravastatin. In addition, an ionophore for sodium, potassium and proton, nigericin, stimulated the uptake of [14C]pravastatin in the presence of a potassium gradient ([K + ]in/[K+ ]out = 0/145 mM). On the other hand, neither the imposition of an inwardly directed sodium gradient nor an outwardly directed bicarbonate gradient stimulated the uptake of [14C]pravastatin. In the presence of a proton gradient (pHin/out = 7.5/5.5), the initial uptake of pravastatin was saturable with the apparent Kt of 15.2 ± 3.2 mM and Jmax of 10.6 ± 1.21 nmol/mg protein/10 sec. The uptake of pravastatin was significantly inhibited by monocarboxylic acid compounds such as acetic acid and nicotinic acid in a competitive manner but not by di- or tri-carboxylic acids, or acidic amino acid. Conclusions. It was concluded that a pH-dependent transport of pravastatin across the brush-border membrane occurs by a proton-gradient dependent carrier-mediated mechanism rather than by simple diffusion of its unionized form.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1023/A:1016269806840

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