Search results for "Microsome"
showing 10 items of 262 documents
Zur Bildung hydroxylierter Zwischenprodukte bei der mikrosomalen Fremdstoffoxydation / On the Possible Formation of Hydroxylated Intermediates during…
1969
Die oxydative Abspaltung von O-Methylgruppen ist eine haufig anzutreffende Arzneimittelabbaureaktion. Als Beispiel fur diesen Reaktionstyp diente uns die Demethylierung von p-substituierten Anisolen. Als instabiles Zwischenprodukt dieser Reaktion wurde schon lange eine C6H5−O−CH2OH-Gruppierung angenommen und 1965 von Renson et al. [1] wahrscheinlich gemacht durch 018-Einbauversuche an p-Methoxyacetanilid. Wenn diese Vorstellung richtig ist, mus das Ausmas der Abspaltung der Hydroxymethylgruppe als Formaldehyd von den Elektronen-aufnehmenden oder -abgebenden Eigenschaften eventueller p-Substituenten des Benzolrings abhangen: p-Nitroanisol mus Formaldehyd verlieren, wahrend sich bei p-Methyla…
Stereoselective metabolism of dibenz(a,h)anthracene to trans-dihydrodiols and their activation to bacterial mutagens.
1990
Dibenz(a,h)anthracene (DBA), a carcinogenic, polycyclic aromatic hydrocarbon ubiquitous in the environment, is metabolized by the hepatic microsomal fraction of immature Sprague-Dawley rats pretreated with Aroclor 1254 to 27 ethyl acetate-extractable metabolites. More than half of these metabolites (51%) consisted of trans-1,2-; -3,4-; and -5,6-dihydrodiols including their identified secondary metabolites. The three trans-dihydrodiols (4.9, 15.8, and 0.6% of total metabolic conversion) were highly enriched in their R,R enantiomers (85, 71, and 98%) as determined by high performance liquid chromatography on suitable chiral stationary phases. This is explained on the basis of the stereoselect…
Triterpene saponins from Billia rosea.
2017
Five previously undescribed triterpene saponins, billiosides A-E, and a known analogue, were isolated from the seeds of Billia rosea (Planch. & Linden) C. Ulloa & P. Jorg. Their structures were elucidated on the basis of extensive 1D and 2D NMR experiments (1H, 13C, DEPT, COSY, TOCSY, NOESY, ROESY, HSQC, and HMBC) and mass spectrometry as (3β,21β,22α)-3-[(2-O-β-D-glucopyranosyl-O-[α-L-arabinopyranosyl-(1 → 4)]-β-D-glucopyranosyl)oxy]-21-[((2E,6S)-2,6-dimethyl-6-hydroxyocta-2,7-dienoyl)oxy]-22-(acetyloxy)-24-hydroxyolean-12-en-28-oic acid, (3β,21β,22α)-3-[(2-O-β-D-galactopyranosyl-β-D-glucopyranosyl)oxy]-21,22-dihydroxyolean-12-en-28-yl O-α-L-arabinopyranosyl-(1 → 4)-β-D-glucopyranoside, (3β…
Subcellular localization and characterization of nitric oxide synthase(s) in endothelial cells: physiological implications.
1994
Endothelial cells (EC) contain a constitutive Ca2+/calmodulin-dependent nitric oxide (NO) synthase (cNOS) which plays an important role in the local control of vascular tone. We compared the subcellular distribution of this enzyme in cultured and freshly isolated pig EC by determination of specific cNOS activity and immunoblot analysis. Similar studies were also performed with cultured and freshly isolated bovine and cultured human EC. Enzyme activity was predominantly (> 70%) associated with the particulate fraction of all EC types tested and was highest in freshly isolated porcine EC. Both specific cNOS activity and immunoreactivity were substantially higher (> 3-fold) in th…
Effect of polybrominated biphenyls on bromobenzene lethality in mice.
1977
Polybrominated biphenyls (PBBs) are inducers of hepatic microsomal cytochrome P450 and P1 450 in rats and mice. The purpose of this study was to determine, in mice, the effect of PBBs on the lethality of the hepatotoxin bromobenzene. Female NMRI mice were administered a single ip injection of 150 mg/kg PBBs and other mice received phenobarbital (PB), 100 mg/kg daily for 3 days, or 3‐methylcholanthrene (MC), 20 mg/kg daily for 3 days. At 24 hr after PB or MC and 24, 48, and 96 hr after PBBs animals received 3,150 mg/kg bromobenzene ip (LD85) and the time to death was recorded. Both PB and MC enhanced bromobenzene lethality and decreased the median time to death (LT50) from 23 hr in controls …
Peroxisome proliferators and peroxisome proliferator activated receptors (PPARs) as regulators of lipid metabolism.
1997
Peroxisome proliferation (PP) in mammalian cells, first described 30 years ago, represents a fascinating field of modern research. Major improvements made in its understanding were obtained through basic advances that have opened up new areas in cell biology, biochemistry and genetics. A decade after the first report on PP, a new metabolic pathway (peroxisomal beta-oxidation) and its inducibility by peroxisome proliferators were discovered. More recently, a new type of nuclear receptor, the peroxisome proliferator-activated receptor (PPAR), has been described. The first PPAR was discovered in 1990. Since then, many other PPARs have been characterized. This original class of nuclear receptor…
Heme oxygenase-1 induction modulates microsomal prostaglandin E synthase-1 expression and prostaglandin E2 production in osteoarthritic chondrocytes
2009
Pro-inflammatory cytokines such as interleukin-1beta (IL-1beta) may participate in the pathogenesis of cartilage damage in osteoarthritis (OA) through the production of catabolic enzymes and inflammatory mediators. Induction of heme oxygenase-1 (HO-1) has previously been shown to exert anti-inflammatory effects in different cell types. We have investigated whether HO-1 induction may modify chondrocyte viability and the production of relevant mediators such as oxidative stress and prostaglandin E(2) (PGE(2)) elicited by IL-1beta in OA chondrocytes. Chondrocytes were isolated from OA cartilage and used in primary culture. Cells were stimulated with IL-1beta in the absence or presence of the H…
Interaction of valproic acid and some analogues with microsomal epoxide hydrolase.
1992
Abstract Valproic acid (VPA) and its analogues valpromide (VPM), valproyl-Coenzyme A (VP-CoA) and valproyl-ethylester (VPE) were examined as potential inhibitors of microsomal epoxide hydrolase (mEHb) using styrene-7,8-oxide (STO) and benzo(a)pyrene-4,5-oxide (BPO) as enzyme substrates. The effect of each potential inhibitor was examined using mEHb from rat liver, human livers (from a child, woman and man) and from human placenta. Of the compounds tested, only VPM (2 mM) expressed significant inhibition of mEHb activity with a maximum inhibition of 49%, 48%, 35% and 33% for liver microsomes from the child, woman, man and rat, respectively, using STO (2 mM) as substrate. Human placenta mEHb …
New Lipid Modulating Drugs: The Role of Microsomal Transport Protein Inhibitors
2011
Microsomal triglyceride transfer protein (MTP) is involved in the synthesis of very low density lipoprotein in the liver. Its deficiency results in abetalipoproteinemia. MTP inhibitors target the assembly and secretion of apolipoprotein B-containing lipoproteins. These agents may potentially play a role, alone or in combination, in the treatment of hypercholesterolemia or hypertriglyceridemia. Clinical applications of MTP inhibitors initially focused primarily on high-dose monotherapy in order to produce substantial reductions in LDL-cholesterol levels but these proved to induce significant hepatic steatosis and transaminase elevations. However, likely orphan indications for MTP inhibitors,…
A time course investigation of vitamin A level and lipid composition of the liver endoplasmic reticulum in rats following treatment with congeneric p…
1990
Abstract The drug metabolizing enzyme activities, the vitamin A content and the fatty acid composition in the endoplasmic reticulum membrane were studied in rat liver after a single injection of the polychlorobiphenyls (PCBs) 3,3′,4,4′-tetrachlorobiphenyl [(3,4)2Cl] or 2,2′,4,4′,5,5′-hexachlorobiphenyl [(2,4,5)2Cl], 300 μ mol/kg each. The microsomal vitamin A level was markedly lowered 3 days after treatment with (3,4)2Cl, a coplanar type inducer of cytochrome P-450. A marked increase in microsomal AHH and UDPGT activities occurred within 3 days after injection of (3,4)2Cl whereas (2,4,5,)2Cl treatment enhanced APDM activity only. Arachidonic, stearic and linoleic acid microsomal contents w…