• To compare the abilities of chicoric acid and its metabolites in scavenging free radicals and their effects on the viability of 3T3-L1 preadipocytes, an in vitro study of the metabolism of chicoric acid in rat liver microsomes was performed using liquid tandem mass spectrometry (HPLC-MS/MS). The results indicated that caffeic acid and caftaric acid were the hepatic phase I metabolites of chicoric acid. (rsc.org)
  • Triazolam biotransformation by human liver microsomes in vitro: effects of metabolic inhibitors and clinical confirmation of a predicted interaction with ketoconazole. (aspetjournals.org)
  • 1. The inhibitory effects of cimetidine, nizatidine and omeprazole on the metabolic activity of CYP2C9, 2C19, 2D6 and 3A were investigated in human liver microsomes. (nih.gov)
  • In-vitro metabolic inhibition studies using rat and human liver microsomes and intestinal absorption studies of riluzole in a rat everted gut-sac model were conducted to elucidate the mechanism of interaction. (researchgate.net)
  • Polyclonal antibodies were raised to CYP2C9 purified from human liver, and were then back-adsorbed against recombinant CYP2C19 coupled to a solid-phase support. (aspetjournals.org)
  • Catabolism of 3'-azido-3'-deoxythymidine in hepatocytes and liver microsomes, with evidence of formation of 3'-amino-3'-deoxythymidine, a highly toxic catabolite for human bone marrow cells. (aspetjournals.org)
  • Because the liver is probably the major site of AZT catabolism, the metabolism and transmembrane distribution of AZT were evaluated in freshly isolated rat hepatocytes, a model for the study at the cellular level of biosynthetic, catabolic, and transport phenomena in the liver. (aspetjournals.org)
  • Biotransformation of the triazolobenzodiazepine alprazolam (ALP) was studied in vitro using hepatic microsomal preparations from human, monkey, mouse, and rat liver tissue. (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)
  • This study provides the first detailed catabolic profile of AZT at the hepatic site and emphasizes the critical role that the liver plays in drug clearance. (aspetjournals.org)
  • Biochem Pharmacol 37: 665-671, 1988 and 37: 2839-2845, 1988), these data indicate that the model glucuronidated substrates paracetamol, morphine and 4-methyllumbelliferone may be used to differentiate at least four human liver UDPGT isozyme activities. (edu.au)
  • IC 50 values for Sacchrosome inhibition by known CYP inhibitors are similar to those published using human-liver-microsomes (HLMs). (oreilly.com)
  • In the present study we further examined the roles of several human P450 enzymes, as well as P450 2D6, in the hydroxylation of (+/-)-bufuralol, using liver microsomes from several human samples and human P450 enzymes expressed in human lymphoblastoid cell lines or Escherichia coli. (unboundmedicine.com)
  • Quinidine and anti-rat P450 2D1 antibody almost completely inhibited bufuralol 1'-hydroxylation in human sample HL-18 at a substrate concentration of 0.4 mM, whereas these effects were not so drastic when liver microsomes from human sample HL-67 were used. (unboundmedicine.com)
  • Monospecific anti-CYP2C9 was also found to inhibit rates of tolbutamide hydroxylation by 93 ± 4 and 78 ± 6% in CYP2C19-deficient and CYP2C19-containing human liver microsomes, respectively. (aspetjournals.org)
  • 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)
  • While the human liver microsomal system demonstrated rapid clearance by CYP enzymes, the hepatocyte incubations showed much slower clearance, possibly providing some insight into the long duration of carfentanils effects. (diva-portal.org)
  • Myricetin inhibited the liver metabolizing enzymes CYP3A4 and CYP2C9 [ 12 ]. (hindawi.com)
  • Human CYP450 enzymes, naturally bound to livers' endoplasmic reticular (ER) membranes, are used for drug-metabolism studies and commercially produced from genetically engineered insect/bacterial cells. (oreilly.com)
  • 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)
  • Activity assays were conducted using recombinant enzymes as well as human liver and intestinal microsomes. (helsinki.fi)
  • Many tests of liver biochemistry measure liver enzymes that are released into the bloodstream (eg, release of aminotransferases from injured liver cells or of alkaline phosphatase due to cholestasis) or assess liver function by evaluating hepatobiliary excretion (eg, bilirubin). (msdmanuals.com)
  • Further studies of the induction of the liver microsomal drug-hydroxylating enzyme system by pretreatment of rats with various drugs are presented. (rupress.org)
  • Relevant of mutagenicity and clastogenici- angiosarcomas of the liver, which carcinogens discussed in this chap- ty, including the induction of sister are rare tumours, were identified in ter do not include pharmaceutical chromatid exchange (SCE), chro- humans, rats, and mice exposed to drugs classified in Group 1, which mosomal aberrations (CA), and mi- vinyl chloride. (who.int)
  • or each of these agents, carcinogenicity in rats and/or mice, els, differences in exposure con- there was sufficient evidence of car- for example for the liver (aflatoxins, ditions between studies in animals cinogenicity from studies in rats and/ trichloroethylene [TCE], and vinyl and in humans, or limitations in Part 1 · Chapter 1. (who.int)
  • NADPH- and GSH-supplemented human liver microsomal incubations of flutamide gave rise to a novel GSH conjugate where GSH moiety was conjugated to the flutamide molecule via the amide nitrogen, resulting in a sulfenamide. (unboundmedicine.com)
  • The transformation of phenelzine by rat liver microsomes yields 2-phenylacetaldehyde, 2-phenylethanol and ethyl-benzene. (usp.br)
  • In human liver microsomes, ratios of 4-OH-ALP/alpha-OH-ALP reaction velocities calculated at clinically relevant plasma concentrations of ALP ranged from 7 to 17, qualitatively consistent with, but numerically larger than, the ratio of the plasma levels of the two metabolites during clinical use of ALP in humans. (nih.gov)
  • Biotransformation of the triazolobenzodiazepine triazolam to its hydroxylated metabolites, alpha-hydroxy (OH)- and 4-OH-triazolam, was studied in vitro using microsomal preparations of human liver. (aspetjournals.org)
  • Besides, the fragmentation behaviors of aristolochic acid Ⅰ, aristolochic acid Ⅱ and their metabolites in rat liver microsomes S9 fractions were characterized and summarized. (edu.hk)
  • Dive into the research topics of 'Research of aristolochic acid I, aristolochic Acid II and their metabolites in rat liver microsomes using HPLC-MS/MS'. Together they form a unique fingerprint. (edu.hk)
  • Since human liver microsomes formed BCP-NG, we investigated the metabolites of BCP excreted in the urine of a patient after oral administration of BCP (600 mg). (scirp.org)
  • An in vitro-in vivo scaling model, using these plasma ketoconazole concentrations together with liver partition ratios and the in vitro Ki values, predicted a decrement of triazolam clearance due to ketoconazole coadministration that was consistent with the 88% decrement in clearance actually observed in vivo. (aspetjournals.org)
  • We conducted in vitro Phase I oxidation and Phase II glucuronidation assays on OJT007 using rat liver microsomes. (houstonmethodist.org)
  • In vitro and clinical studies were conducted on human liver microsomes and healthy human subjects, respectively. (hindawi.com)
  • In in vitro studies, microsomes were incubated with NADPH in presence and absence of different concentrations of seeds extract. (hindawi.com)
  • The human liver microsomes were employed for in vitro investigation, while in vivo study was conducted on healthy human subjects. (hindawi.com)
  • Interestingly, the same adduct was formed when flutamide was incubated with human liver microsomes in the presence of GSSG and NADPH. (unboundmedicine.com)
  • Studies using rat and human liver microsomes demonstrated that the rate of formation of AMT and GAMT increased in the presence of NADPH, suggesting the involvement of a NADPH-dependent enzyme system. (aspetjournals.org)
  • mice developed severe liver toxicity, which probably tio is less than 1, while in mouse liver the ratio is about contributed to the cause of death. (cdc.gov)
  • Indirect Immunofluorescence method Biochip Titerplane Technique * Rat kidney and liver sections treated with patient's serum followed by polyvalent conjugate immunofluorescence staining. (apollohospitals.com)
  • Liver tissue, kidney tissue, blood and lung lavage fluid were collected and analyzed. (cdc.gov)
  • Electron spin resonance results showed an increase in hydroxyl radical formation in liver and kidney tissue from Cr, day 1, as well as Cd & Ni on days 3 and 7, at the highest exposure levels. (cdc.gov)
  • 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)
  • Although expression of CYP2C19 in human liver is less than that of CYP2C9, it may play an important role in tolbutamide disposition in subjects expressing either high levels of CYP2C19 or a catalytically deficient CYP2C9 enzyme. (aspetjournals.org)
  • The main clinical features are liver insufficiency and abnormalities of the heart and nervous system. (medscape.com)
  • See also American College of Gastroenterology [ACG] Clinical Guideline: Evaluation of Abnormal Liver Chemistries and the European Association for Study of Liver-Asociación Latinoamericana para el Estudio del Hígado Clinical Practice Guidelines . (msdmanuals.com)
  • Echinococcosis [10] [11] of the liver, lung, and peritoneum (caused by the larval form of the dog tapeworm , or of the alveoli (caused by E. multilocularis ) when surgical excision is not possible. (wikipedia.org)
  • Liver tissue showed an increase in oxidative damage, through lipid peroxidation and hydrogen peroxide production, in all metal exposures with Cr being the most dramatic and Ni showing damage at days 3 and 7. (cdc.gov)
  • GSD type Ia demonstrates deficient G6Pase activity in the fresh and frozen liver tissue. (medscape.com)
  • Liver inflammation has been reported and those with prior liver problems are at greater risk. (wikipedia.org)
  • Serology Acute viral hepatitis is diffuse liver inflammation caused by specific hepatotropic viruses that have diverse modes of transmission and epidemiologies. (msdmanuals.com)
  • A systematic approach including laboratory tests, imaging studies, and liver biopsy should be used. (msdmanuals.com)
  • As a result, BCP-NG formation (pmol equivalents/min/mg protein) was observed with microsomes expressing hUGT1A1 (142), 1A3 (196), 1A4 (8), 1A7 (8), 1A8 (66), 1A9 (38), 1A10 (9), 2B4 (7) and 2B7 (16). (scirp.org)
  • The most useful laboratory tests to screen for liver disorders are serum aminotransferases (the most commonly used liver tests), bilirubin, and alkaline phosphatase. (msdmanuals.com)
  • Identifying the etiology of abnormal liver tests requires a combination of history and laboratory testing. (msdmanuals.com)
  • Other etiologies of liver disease are diagnoses of exclusion and are made through characteristic pattern in laboratory results, together with patient history and exclusion of other causes. (msdmanuals.com)
  • A specific high performance liquid Chromatographie assay has been developed for the measurement of paracetamol glucuronide formation by the microsomal fraction of human liver. (edu.au)
  • Urinary copper excretion Wilson disease results in accumulation of copper in the liver and other organs. (msdmanuals.com)
  • The results indicated that the production of aristololactams is the main cause of the toxicity of aristolochic acid Ⅰ and aristolochic acid Ⅱ in the metabolism of rat liver microsome S9. (edu.hk)