• AZT) has been studied in human renal, gut and hepatic microsomes. (nih.gov)
  • Western blotting revealed that the absorbed anti-human CYP2C9 preparation reacted with only recombinant CYP2C9 and the corresponding native protein in hepatic microsomes, and no longer recognized CYP2C19 and CYP2C8. (aspetjournals.org)
  • 15%) inhibitory effect on S -mephenytoin 4′-hydroxylation by purified CYP2C19 or hepatic microsomes containing CYP2C19. (aspetjournals.org)
  • The KM was 2.10 +/- 0.44 mM and the Vmax was 0.252 +/- 0.0312 nmol/min/mg protein in untreated microsomes. (aspetjournals.org)
  • Diclofenac 4'-hydroxylation displayed single enzyme Michaelis-Menten kinetics and was similar in microsomes from one poor and five extensive metabolizers of debrisoquin (CYP2D6), with a Km of 5.6 +/- 1.5 microM (mean +/- sd) and a Vmax of 60.6 +/- 23.5 nmol/mgP/h. (nih.gov)
  • Taken together, our results indicate that both CYP2C9 and CYP2C19 are involved in tolbutamide hydroxylation by human liver microsomes, and that CYP2C19 underlies at least 14 to 22% of tolbutamide metabolism. (aspetjournals.org)
  • Fipronil was incubated with human liver microsomes (HLM) and several recombinant cytochrome P450 (CYP) isoforms obtained from BD Biosciences. (cdc.gov)
  • Cytochrome P-450 (P-450) 2A6 was purified by chromatography of human liver microsomes. (aspetjournals.org)
  • The glucuronide was also formed in Triton-X-100-activated liver microsomes and isolated guinea pig hepatocytes. (aspetjournals.org)
  • Here we show that six major human liver CYP enzymes (1A2/2C9/2C19/2D6/2E1/3A4), isolated from baker's yeast as ER-bound microsomes (Sacchrosomes™) in yields of 120-325 nmol/L, are 0.5-25 fold more active than commercial enzymes. (oreilly.com)
  • IC 50 values for Sacchrosome inhibition by known CYP inhibitors are similar to those published using human-liver-microsomes (HLMs). (oreilly.com)
  • We investigated the metabolism of 1,8-cineole by liver microsomes of rats and humans and by recombinant cytochrome P450 (P450 or CYP) enzymes in insect cells in which human P450 and NADPH-P450 reductase cDNAs had been introduced. (unboundmedicine.com)
  • In rats, pregenolone-16alpha-carbonitrile (PCN) and phenobarbital induced the 1,8-cineole 2-hydroxylation activities by liver microsomes. (unboundmedicine.com)
  • The rates observed using human liver microsomes and recombinant CYP3A4 were very high among other CYP3A4 substrates reported so far. (unboundmedicine.com)
  • These results suggest that 1,8-cineole, a monoterpenoid present in nature, is one of the effective substrates for CYP3A enzymes in rat and human liver microsomes. (unboundmedicine.com)
  • Incubation of MDA with human liver microsomes demonstrated that production of both glutathione adducts are related to cytochrome P450 2D6 isoform activity. (mdma.net)
  • These results indicate that MDA can be converted into two glutathione regioisomers by human liver microsomes, but only the 5-(glutathion-S-yl)-alpha-MeDA adduct is behaviourally active in the rat. (mdma.net)
  • The nature of the enzyme(s) catalyzing the major metabolic pathway of diclofenac, 4'-hydroxylation, was investigated in human liver microsomes. (nih.gov)
  • The procedure has been used to characterize paracetamol glucuronidation kinetics in human liver microsomes and to assess the substrate specificity of the paracetamol UDP-glucuronosyltransferase (UDPGT) activity. (edu.au)
  • This contrasts to the approximately three-fold activation of 4-methylumbelliferone, morphine and 4-nitrophenol glucuronidation observed following Brij 58 treatment of human liver microsomes. (edu.au)
  • The optical purities of monool and diol metabolites formed were found to be dependent on the nature of cytochrome P-450 isozymes present in liver microsomes. (archive.org)
  • Metabolites formed by liver microsomes from untreated, phenobarbital-treated, 3-methylcholanthrene-treated, and polychlorinated biphenyls (Aroclor 1254)-treated male Sprague-Dawley rats were quantified by using specifically tritium-labeled [10-3H]-7,8-H2BaP and liquid scintillation counting of fractions collected from reversed-phase HPLC. (archive.org)
  • The final preparation was electrophoretically homogeneous and contained 16 nmol of P-450/mg of protein. (aspetjournals.org)
  • The rates of oxidation of racemic 2-butanol, (+)-2-butanol, and (-)-2-butanol were the same for (a) model -OH-generating systems, (b) microsomes from chow-fed rats, and (c) microsomes from phenobarbital-treated rats. (mssm.edu)
  • Microsomes have the potential to oxidize alcohols by two pathways, one dependent on hydroxyl radicals (·OH) and the other dependent on cytochrome P-450 in which ·OH does not seem to be involved. (mssm.edu)
  • These results suggest that the ·OH-dependent and the cytochrome P-450 dependent pathways of alcohol oxidation by these microsomes do not display stereospecificity. (mssm.edu)
  • Thus, the stereochemical preference displayed by microsomes from chronic alcohol fed rats may be due to the induction of a particular cytochrome P-450. (mssm.edu)
  • A portion (2-7% depending on the type of microsomes used) of the BaP found was formed nonenzymatically in microsomal metabolism of 7,8-H2BaP. (archive.org)
  • By contrast, microsomes from the chronic ethanol-fed rats catalyzed the oxidation of the (+) enantiomer at rates twice that of the (-) enantiomer of 2-butanol. (mssm.edu)
  • This enzymatic 25-hydroxylase reaction is mostly due to the actions of CYP2R1, present in microsomes, although other enzymes such as mitochondrial CYP27A1 can contribute. (wikipedia.org)
  • Following intracerebroventricular administration (180 nmol) of either GSH adduct into Dark Agouti or Sprague-Dawley rats only 5-(glutathion-S-yl)-alpha-MeDA produced behavioural effects characterised by hyperactivity, teeth chattering, tremor/trembling, head weaving, splayed posture, clonus and wet dog shakes. (mdma.net)
  • A type 2 binding spectrum was observed for the interaction of 2-butanol with microsomes from ethanol-fed rats, but not with controls. (mssm.edu)
  • Soluble extracts of chicken peripheral nerve contain detectable amounts of phenyl valerate esterase (PVase) activity (about 2000 nmol/min per g of fresh tissue). (inrae.fr)
  • The reversal of the antisecretory activity of the inhibitors in dogs is suggested to be due to the action of endogenous extracellular GSH, in addition to de novo synthesis of the proton pump, because bullfrog gastric mucosae were found in the present study to secrete GSH into the mucosal solution at the rate of about 0.25 nmol/min/g tissue. (shengsci.com)
  • A broad reference range of 20 to 150 nmol/L (8-60 ng/mL) has also been suggested, while other studies have defined levels below 80 nmol/L (32 ng/mL) as indicative of vitamin D deficiency. (wikipedia.org)
  • Other countries use nmol/L. Multiply ng/mL by 2.5 to convert to nmol/L. This test can be used to diagnose vitamin D deficiency, and is performed in people with high risk for vitamin D deficiency, when the results of the test can be used to support beginning replacement therapy with vitamin D supplements. (wikipedia.org)
  • The current study quantifies the contribution of cytochromes P450 (P450s), including CYP3A4 and CYP3A5, to vincristine metabolism with a bank of human liver microsomes (HLMs). (aspetjournals.org)
  • Fipronil was incubated with human liver microsomes (HLM) and several recombinant cytochrome P450 (CYP) isoforms obtained from BD Biosciences. (cdc.gov)
  • for rat liver microsomes (RLM) the Km and Vmax are 19.9 microM and 0.39 nmol/mg protein min, respectively. (cdc.gov)
  • Glucuronidation using human liver microsomes has traditionally involved disruption of the membrane barrier, usually by detergent treatment, to attain maximal enzyme activity. (aspetjournals.org)
  • Because hepatic cytochromes P450 (CYPs) 2 are responsible for a large percentage of the metabolism of drugs in vivo, human liver microsomes appear to be the in vitro drug metabolism screening system of choice ( Rodrigues, 1994 ). (aspetjournals.org)
  • Comparative metabolism of chloroacetamide herbicides and selected metabolites in human and rat liver microsomes. (nih.gov)
  • The current study extends our earlier studies with alachlor and demonstrates that rat liver microsomes metabolize acetochlor and metolachlor to CMEPA (0.065 nmol/min/mg and 0.0133 nmol/min/mg, respectively), whereas human liver microsomes can metabolize only acetochlor to CMEPA (0.023 nmol/min/mg). (nih.gov)
  • Midazolam (MDZ) is metabolized in human liver microsomes by the cytochrome P450 (CYP) 3A subfamily to 1'-hydroxy (1'-OH) and 4-hydroxy (4-OH) metabolites. (aspetjournals.org)
  • Naringenin, a flavonoid present in grapefruit juice, also inhibited MDZ metabolism in human liver microsomes. (aspetjournals.org)
  • Liver microsomes were prepared from male Wistar and Gunn rats as well as guinea pigs. (europa.eu)
  • UDPGT specific activity for linalool in liver microsomes from Wistar rats induced by either phenobarbital or 3 -methylcholanthrene, and in livermicrosomes from guinea pigs induced by phenobarbital are summarized in the table below. (europa.eu)
  • Liver microsomes were prepared from male Wistar and Gunn rats as well as guinea pigs, and induced with phenobarbital, 3-methylcholanthrene or with vehicle only (controls). (europa.eu)
  • In vitro experiments in human liver microsomes demonstrate that budesonide is rapidly and extensively biotransformed, mainly by CYP3A4, to its 2 major metabolites, 6β-hydroxy budesonide and 16α-hydroxy prednisolone. (nih.gov)
  • Several cytochrome P-450 isozymes were thus purified from the liver microsomes of mammals and their role in oxygenation of amphetamines and cannabinoids were elucidated. (go.jp)
  • Human liver microsomes were from the pool of 50 individuals of mixed gender, race (Caucasian, African, and Hispanic) and age (6 to 78 years old with most of them between 30 and 50 years), 31 of them died from cerebrovascular stroke, 11 from head trauma, 4 from anoxia, 2 from cardiac arrest, and 2 from aortic aneurysm. (europa.eu)
  • In parallel studies using cDNA-expressed human CYP3A4 microsomes, the KM for 1'-OH formation was 1.56 microM, and the corresponding Vmax was 0.16 nmol/mg/min. (aspetjournals.org)
  • alpha-Naphthoflavone stimulated 1'-OH metabolite formation in human and cDNA-expressed human CYP3A4 microsomes at low concentration (10 microM). (aspetjournals.org)
  • Conditions: Substrate concentrations: 0.25mM NADPH, 0.1nmol FPP in a volume of 200µL. (guidetopharmacology.org)
  • The buffer containing NADPH and liver or lung microsomes were placed in vials and sealed with open-hole screwcaps fitted with Teflon®/silicone septa. (europa.eu)
  • The goals of the current work were to develop a universal method to glucuronidate xenobiotic substrates using microsomes, and to apply this method to sequential oxidation-glucuronidation reactions. (aspetjournals.org)
  • Finally, alamethicin treatment of microsomes was found to be effective in facilitating the sequential oxidation-glucuronidation of 7-ethoxycoumarin. (aspetjournals.org)
  • During times 0 to 3, 5?nmol/L rapamycin treatment improved the total cellular number of EBs weighed against the DMSO\treated group. (mdm-inhibitors.com)
  • But 20?nmol/L rapamycin treatment inhibited the growth of EBs. (mdm-inhibitors.com)
  • A broad reference range of 20 to 150 nmol/L (8-60 ng/mL) has also been suggested, while other studies have defined levels below 80 nmol/L (32 ng/mL) as indicative of vitamin D deficiency. (wikipedia.org)
  • Formation of estradiol-3-glucuronide displayed atypical kinetics, and data best fit the Hill equation, yielding apparent kinetic parameters of K m app = 0.017 mM, V max app = 0.4 nmol/mg/min, and n = 1.8. (aspetjournals.org)
  • Formation of acetaminophen- O -glucuronide also best fit the Hill equation, with K m app = 4 mM, V max app = 1.5 nmol/mg/min, and n = 1.4. (aspetjournals.org)
  • Alternatively, morphine-3-glucuronide formation displayed Michaelis-Menten kinetics, with K m app = 2 mM and V max app = 2.5 nmol/mg/min. (aspetjournals.org)
  • Earlier, we have already shown that rutin inhibited lipid peroxidation of lecithin liposomes, bovine heart microsomes,I and rat brain homogenates.2 It was proposed that the inhibitory effects of rutin are explained by both the reaction with superoxide ion and other free radicals (the antioxidant effect) and the formation of an inactive iron-rutin complex (the chelating effect). (osri.asia)
  • revealed the current presence of at least two primary GSTs (27.8- and 25.6-kDa subunits) in the cytosol of EH5, whereas the main 27.8-kDa subunit was the just GST in microsomes. (igesip.org)