Ritonavir (RTV) was used as a boosting agent to increase the clinical exposure of 11-ethyl-5,11-dihydro-5-methyl-8-[2-[(1-oxido-4-quinolinyl)oxy]ethyl]-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-one (BILR 355), an inhibitor of the human immunodeficiency virus, by inhibiting the CYP3A-mediated metabolism of BILR 355. However, although the levels of BILR 355 increased upon concomitant administrati...

Cyclophosphamide is converted by enzymes of mouse liver into two metabolites. Production of the first (aldophosphamide), which is uncharged, requires TPNH, is inhibited by CO, and is accomplished predominantly by the microsomal fraction. With the microsomal enzyme, the Km for Cyclophosphamide is 0.5 mM; nicotine, atropine, ephedrine, apomorphine, and cocaine are potent inhibitors. Phénobarbita...

HEN extracts of wild-type Drosophila are electrophoresed on agar gels and the gels stained with a tetrazolium solution containing benzaldehyde, a formazan band is formed at a location not identical to the xanthine dehydrogenase (XDH) band ( COURTRIGHT 1966a). This was a surprising observation since benzaldehyde has been reported to serve as a substrate for XDH (GLASSMAN and MITCHELL 1959a). Sin...

Human aldehyde oxidase (AO) is a molybdoflavoenzyme that commonly oxidizes azaheterocycles in therapeutic drugs. Although high metabolic clearance by AO resulted in several drug failures, existing in vitro-in vivo correlations are often poor and the extrahepatic role of AO practically unknown. This study investigated enzymatic activity of AO in fresh human skin, the largest organ of the body, f...

Diamine oxidase (EC 1.4.3.6) activity, measured as delta 1-[14C]pyrroline formation from [14C]putrescine, was studied in homogenates of regenerating liver and of 4-dimethylaminoazobenzene-induced by Yoshida AH 130 hepatomas of rat. The addition in the incubation medium of acetaldehyde increased delta 1-pyrroline formation in normal and regenerating liver that contained aldehyde dehydrogenase bu...

Background Any factor like diabetes that changes the oxidant/antioxidant balance in favor of oxidants could possibly disrupt the physiologic function of ovaries. So, we have investigated the effect of vitamin E and Se supplements on antioxidant defense in ovaries of diabetic rats with focus on Xanthine dehydrogenase/oxidase (XDH/XO) and Aldehyde oxidase (AO) activities. MaterialsAndMethods This...

5-Hydroxyindoleacetic acid (5-HIAA) is a major metabolite of serotonin, generated via a two step process, involving monoamine oxidase A (MAO-A) and aldehyde dehydrogenase. Measurement of 5HIAA in combination with serotonin may offer insight into mechanisms underlying various clinical symptoms. The ratio of serotonin to 5-HIAA may be used to evaluate serotonin turnover and monoamine oxidase acti...

The bioavailability of aromatic azaheterocyclic drugs can be affected by the activity of aldehyde oxidase (AO). Susceptibility to AO metabolism is difficult to predict computationally and can be complicated in vivo by differences between species. Here we report the use of bis(((difluoromethyl)sulfinyl)oxy)zinc (DFMS) as a source of CF2H radical for a rapid and inexpensive chemical "litmus test"...

The aldehyde oxidase (Aldox) distribution pattern was determined for wing discs of partial hybrids between D. melanogaster and D. simulans. In these animals the regulation of Aldox activity is not uniform over the disc epithelium as both cis-dominant and trans -acting control were evident in different regions of the disc. The Aldox expression was shown to be regulated by loci on the X chromosom...