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Gotowe bibliografie tematyczne / Human liver microsomes / Artykuły w czasopismach

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Artykuły w czasopismach na temat „Human liver microsomes”

Autor: Grafiati

Data publikacji: 4 czerwca 2021

Data aktualizacji: 25 stycznia 2023

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1

Minoda, Yuko, and Evan D. Kharasch. "Halothane-dependent Lipid Peroxidation in Human Liver Microsomes Is Catalyzed by Cytochrome P4502A6 (CYP2A6)." Anesthesiology 95, no. 2 (August 1, 2001): 509–14. http://dx.doi.org/10.1097/00000542-200108000-00037.

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Background Halothane is extensively (approximately 50%) metabolized in humans and undergoes both oxidative and reductive cytochrome P450-catalyzed hepatic biotransformation. Halothane is reduced under low oxygen tensions by CYP2A6 and CYP3A4 in human liver microsome to an unstable free radical, and then to the volatile metabolites chlorodifluoroethene (CDE) and chlorotrifluoroethane (CTE). The free radical is also thought to initiate lipid peroxidation. Halothane-dependent lipid peroxidation has been shown in animals in vitro and in vivo but has not been evaluated in humans. This investigation

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2

Myllynen, P., P. Pienimäki, H. Raunio, and K. Vähäkangas. "Microsomal metabolism of carbamazepine and oxcarbazepine in liver and placenta." Human & Experimental Toxicology 17, no. 12 (December 1998): 668–76. http://dx.doi.org/10.1177/096032719801701204.

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Metabolism of both carbamazepine (CBZ) and oxcarbaze-pine (OCBZ) were catalyzed by human liver microsomes and microsomes from livers of CBZ-induced or non-induced C57BL/6 mice. Human placental microsomes metabolized only OCBZ. Mouse liver microsomes metabolized CBZ to carbamazepine-10,11-epoxide (CBZ-E), 10- hydroxy-10,11-dihydro-carbamazepine (10-OH-CBZ), 3- hydroxy-carbamazepine (3-OH-CBZ), 10,11-trans-dihydroxy-10,11-dihydro-carbamazepine (10,11-D) and to an unidentified metabolite. CBZ-pretreatment of mice increased both ethoxyresorufin O-deethylase activity in the liver and the amount of

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3

Barnes, T. S., M. D. Burke, and W. T. Melvin. "Differences in adult and foetal human cytochrome P-450 forms recognized by monoclonal antibodies with specificity for the P450III family." Biochemical Journal 260, no. 3 (June 15, 1989): 635–40. http://dx.doi.org/10.1042/bj2600635.

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Six murine monoclonal antibodies raised against a major human adult liver cytochrome P-450 (P-450) of the PCN family (P450III) detected a protein in human foetal liver microsomes (microsomal fractions) which had an approx. 1 kDa higher molecular mass on SDS/polyacrylamide-gel electrophoresis than the protein recognized in human adult liver microsomes. Although each of the antibodies recognized both the adult and the foetal forms, antibody HL4 showed higher affinity for the foetal form. Recognition by the monoclonal antibodies of peptides generated by proteolytic cleavage of microsomal proteins

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4

George, R., P. J. Davis, L. Luong, and M. J. Poznansky. "Cholesterol-mediated regulation of HMG-CoA reductase in microsomes from human skin fibroblasts and rat liver." Biochemistry and Cell Biology 68, no. 3 (March 1, 1990): 674–79. http://dx.doi.org/10.1139/o90-097.

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3-Hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase activity was determined in microsomes from human skin fibroblasts and rat liver that had been variously manipulated in vivo or in tissue culture to up- and down-regulate the enzyme. The cholesterol content of these microsomal preparations was then altered by depletion to or enrichment from either cholesterol-free or cholesterol-rich lipid vesicles. Microsomes from human skin fibroblasts responded to cholesterol depletion by increasing HMG-CoA reductase activity and by decreasing it in response to cholesterol enrichment. This was independent of

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5

Nguyen, Ngoc, Ngoc Cao, Thi Nguyen, Thien-Kim Le, Gun Cha, Soo-Keun Choi, Jae-Gu Pan, Soo-Jin Yeom, Hyung-Sik Kang, and Chul-Ho Yun. "Regioselective Hydroxylation of Phloretin, a Bioactive Compound from Apples, by Human Cytochrome P450 Enzymes." Pharmaceuticals 13, no. 11 (October 22, 2020): 330. http://dx.doi.org/10.3390/ph13110330.

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Phloretin, the major polyphenol compound in apples and apple products, is interesting because it shows beneficial effects on human health. It is mainly found as a form of glucoside, phlorizin. However, the metabolic pathway of phloretin in humans has not been reported. Therefore, identifying phloretin metabolites made in human liver microsomes and the human cytochrome P450 (P450) enzymes to make them is interesting. In this study, the roles of human liver P450s for phloretin oxidation were examined using human liver microsomes and recombinant human liver P450s. One major metabolite of phloreti

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6

Court, Michael H., Su X. Duan, Leah M. Hesse, Karthik Venkatakrishnan, and David J. Greenblatt. "Cytochrome P-450 2B6 Is Responsible for Interindividual Variability of Propofol Hydroxylation by Human Liver Microsomes." Anesthesiology 94, no. 1 (January 1, 2001): 110–19. http://dx.doi.org/10.1097/00000542-200101000-00021.

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Background Oxidation of propofol to 4-hydroxypropofol represents a significant pathway in the metabolism of this anesthetic agent in humans. The aim of this study was to identify the principal cytochrome P-450 (CYP) isoforms mediating this biotransformation. Methods Propofol hydroxylation activities and enzyme kinetics were determined using human liver microsomes and cDNA-expressed CYPs. CYP-specific marker activities and CYP2B6 protein content were also quantified in hepatic microsomes for correlational analyses. Finally, inhibitory antibodies were used to ascertain the relative contribution

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7

Milewich, L., P. C. MacDonald та B. R. Carr. "Activity of 17β-hydroxysteroid oxidoreductase in tissues of the human fetus". Journal of Endocrinology 123, № 3 (грудень 1989): 509–18. http://dx.doi.org/10.1677/joe.0.1230509.

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ABSTRACT The interconversion of oestrone and oestradiol, androstenedione and testosterone, and dehydroepi-androsterone and 5-androstene-3β,17β-diol in mammalian tissues is catalysed by 17β-hydroxysteroid oxidoreductase (17β-HSOR). To identify tissue sites of 17β-HSOR activity in the human fetus, microsomal fractions from 15 different fetal tissues obtained from first and second trimester pregnancies were used for evaluation of enzymatic activity by use of [17α-3H] oestradiol as the substrate and NADP+ as the co-factor. With these reagents, the enzyme-catalysed reaction led to the production of

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8

Wang, Li, Zhe Wang, Meng-ming Xia, Ying-ying Wang, Hai-yun Wang, and Guo-xin Hu. "Inhibitory effect of silybin on pharmacokinetics of imatinib in vivo and in vitro." Canadian Journal of Physiology and Pharmacology 92, no. 11 (November 2014): 961–64. http://dx.doi.org/10.1139/cjpp-2014-0260.

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The objective of this work was to investigate the effect of orally administered silybin on the pharmacokinetics of imatinib in rats and the metabolism of imatinib in human liver microsome and rat liver microsomes. Eighteen healthy male SD rats were randomly divided into 3 groups: group A (control group), group B (received multiple doses of 50 mg·kg−1 silybin for 15 consecutive days), and group C (received a single dose of 50 mg·kg−1 silybin). A single dose of imatinib was administered orally 30 min after administration of silybin (50 mg·kg−1). Imatinib plasma levels were measured by UPLC-MS/MS

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9

Senler, T. I., W. L. Dean, L. F. Murray, and J. L. Wittliff. "Quantification of cytochrome P-450-dependent cyclohexane hydroxylase activity in normal and neoplastic reproductive tissues." Biochemical Journal 227, no. 2 (April 15, 1985): 379–87. http://dx.doi.org/10.1042/bj2270379.

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It is well established that liver microsomal cytochrome P-450 participates in steroid metabolism and probably also in the metabolism of anti-oestrogens such as tamoxifen (Nolvadex). Thus it is possible that variations in cytochrome P-450 levels may influence the responsiveness of human breast and endometrial carcinomas to endocrine therapy. Therefore a simple sensitive spectrophotometric assay for determining levels of cytochrome P-450-dependent cyclohexane hydroxylation activity in breast and uterine microsomes (microsomal fractions) has been developed. Cyclohexane was chosen as a substrate b

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10

Svobodová, Martina, Markéta Martínková, Eva Frei, and Marie Stiborová. "Identification of human enzymes oxidizing a human metabolite of carcinogenic 2-nitroanisole, 2-nitrophenol. Evidence for its oxidative detoxification by human cytochromes P450." Collection of Czechoslovak Chemical Communications 75, no. 6 (2010): 703–19. http://dx.doi.org/10.1135/cccc2010023.

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2-Nitrophenol (2-NP) is the major detoxification metabolite of an important industrial pollutant and a potent carcinogen, 2-nitroanisole (2-NA). Here, we characterized the product of 2-NP metabolism catalyzed by human, rat, rabbit and mouse hepatic microsomes containing cytochromes P450 (CYPs) and identified the major human CYP enzymes participating in this process. The 2-NP metabolite was characterized by mass spectrometry and co-chromatography on HPLC with a synthetic standard, 2,5-dihydroxynitrobenzene (2,5-DNB) to be 2,5-DNB. No nitroreductive metabolism leading to the formation of N-(2-hy

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11

Wallin, R., S. D. Patrick, and L. F. Martin. "Vitamin K1 reduction in human liver. Location of the coumarin-drug-insensitive enzyme." Biochemical Journal 260, no. 3 (June 15, 1989): 879–84. http://dx.doi.org/10.1042/bj2600879.

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The antidotal effect of vitamin K in overcoming poisoning by coumarin anticoagulant drugs is mediated by a vitamin K-reducing enzyme of the endoplasmic reticulum [Wallin & Martin (1987) Biochem. J. 241, 389-396]. With microsomes obtained from human liver biopsies, we have investigated the localization and the transverse orientation of this enzyme in the endoplasmic reticulum and compared its orientation to that of the other enzymes of the vitamin K-dependent carboxylation system. All enzymes were protected by the microsomal membrane and thus appear to have a luminal orientation in the endo

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12

Möllenberg, Alexander, and Gerhard Spiteller. "Transformations of 12,13-Epoxy-ll-hydroxy-9-octadecenoic Acid and 4,5-Epoxy-N-acetylsphingosine by Incubation with Liver Homogenate and Liver Microsomes." Zeitschrift für Naturforschung C 55, no. 11-12 (December 1, 2000): 981–86. http://dx.doi.org/10.1515/znc-2000-11-1222.

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Transformation of 12,13-epoxy-11-hydroxy-9-octadecenoic acid and 4,5-epoxy-N-acetylsphingosine by addition of porcine liver homogenate and human liver microsomes, respectively was investigated. Both epoxides were converted to corresponding dioles by porcine liver homogenate, but not by human liver microsomes, suggesting location of the hydrolyzing enzymes not in the microsomes, but within the cell wall.

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13

Crosbie, Sarah J., PG Blain, and Faith M. Williams. "Metabolism of n-hexane by rat liver and extrahepatic tissues and the effect of cytochrome P-450 inducers." Human & Experimental Toxicology 16, no. 3 (March 1997): 131–37. http://dx.doi.org/10.1177/096032719701600301.

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1 The in vitro metabolism ofn-hexane was studied in rat liver, lung, brain and skeletal muscle microsomes and in microsomes prepared from cell lines expressing human cytochrome P-450 2E1 or 2B6. The hydro xylated metabolites ofn-hexane were quantified by gas chromatography-mass spectometry. 2 Rat liver and extensor digitorum longus (EDL, fast- twitch skeletal muscle) microsomes and the CYP 2B6 microsomes produced the pre-neurotoxic metabolite of n-hexane, 2-hexanol as a major metabolite in contrast to the other rat tissues examined. 3 Inhibition of 2- and 3-hexanol production from n- hexane by

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14

Tateishi, Tomonori, Pavel Soucek, Yoseph Caraco, F. Peter Guengerich, and Alastair J. J. Wood. "Colchicine biotransformation by human liver microsomes." Biochemical Pharmacology 53, no. 1 (January 1997): 111–16. http://dx.doi.org/10.1016/s0006-2952(96)00693-4.

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Miners, John O., Kerry J. Smith, Richard A. Robson, Michael E. McManus, Maurice E. Veronese, and Donald J. Birkett. "Tolbutamide hydroxylation by human liver microsomes." Biochemical Pharmacology 37, no. 6 (March 1988): 1137–44. http://dx.doi.org/10.1016/0006-2952(88)90522-9.

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Bangchang, Kesara Na, Juntra Karbwang, and David J. Back. "Mefloquine metabolism by human liver microsomes." Biochemical Pharmacology 43, no. 9 (May 1992): 1957–61. http://dx.doi.org/10.1016/0006-2952(92)90638-y.

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Li, Yan, Yanyan Zhou, Nan Si, Lingyu Han, Wei Ren, Shaokun Xin, Hongjie Wang, et al. "Comparative Metabolism Study of Five Protoberberine Alkaloids in Liver Microsomes from Rat, Rhesus Monkey, and Human." Planta Medica 83, no. 16 (April 11, 2017): 1281–88. http://dx.doi.org/10.1055/s-0043-108249.

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AbstractProtoberberine alkaloids including berberine, palmatine, jatrorrhizine, coptisine, and epiberberine are major components in many medicinal plants. They have been widely used for the treatment of cancer, inflammation, diabetes, depression, hypertension, and various infectious areas. However, the metabolism of five protoberberine alkaloids among different species has not been clarified previously. In order to elaborate on the in vitro metabolism of them, a comparative analysis of their metabolic profile in rat, rhesus monkey, and human liver microsomes was carried out using ultrahigh-per

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Barnes, T. S., P. M. Shaw, M. D. Burke та W. T. Melvin. "Monoclonal antibodies against human cytochrome P-450 recognizing different pregnenolone 16α-carbonitrile-inducible rat cytochromes P-450". Biochemical Journal 248, № 1 (15 листопада 1987): 301–4. http://dx.doi.org/10.1042/bj2480301.

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Six murine monoclonal antibodies against human hepatic cytochrome P-450 have been raised, using human liver microsomes (microsomal fractions) or semi-purified human cytochrome P-450 as immunogen. All six antibodies recognized the same highly purified of human liver cytochrome P-450 of molecular mass 53 kDa and gave rise to a single band at 53 kDa on immunoblots of human liver microsomes from 11 individuals. The antibodies also recognized proteins at 52 kDa and 54 kDa on immunoblots of control and induced male-rat liver microsomes, showing four different banding patterns. Antibodies HL4 and HP1

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19

Miles, J. S., A. W. McLaren, L. M. Forrester, M. J. Glancey, M. A. Lang, and C. R. Wolf. "Identification of the human liver cytochrome P-450 responsible for coumarin 7-hydroxylase activity." Biochemical Journal 267, no. 2 (April 15, 1990): 365–71. http://dx.doi.org/10.1042/bj2670365.

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1. We have constructed a full-length human liver cytochrome P450IIA cDNA from a partial-length clone by oligonucleotide-directed mutagenesis, and subcloned it into the monkey kidney (COS-7) cell expression vector, pSVL. 2. The cDNA encodes a 49 kDa protein with coumarin 7-hydroxylase (COH) activity which cross-reacts with antisera to the mouse cytochrome P-450 isoenzyme responsible for COH activity and comigrates with a human liver microsomal protein. 3. Western blot analysis of a panel of human livers indicates that the level of the 49 kDa protein, detected using antisera to either the mouse

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Williams, FM, E. Mutch, KW Woodhouse, D. Lambert, and MD Rawlins. "Ethoxyresorufin O-deethylation by human liver microsomes." British Journal of Clinical Pharmacology 22, no. 3 (September 1986): 263–68. http://dx.doi.org/10.1111/j.1365-2125.1986.tb02885.x.

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McManus, M. E., D. S. Davies, A. R. Boobis, P. H. Grantham, and P. J. Wirth. "Guanethidine N-oxidation in human liver microsomes." Journal of Pharmacy and Pharmacology 39, no. 12 (December 1987): 1052–55. http://dx.doi.org/10.1111/j.2042-7158.1987.tb03163.x.

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MIYAZAWA, Mitsuo, Atsushi SUGIE, and Masaki SHINDO. "Biotransformation of (−)-Verbenone by Human Liver Microsomes." Bioscience, Biotechnology, and Biochemistry 66, no. 11 (January 2002): 2458–60. http://dx.doi.org/10.1271/bbb.66.2458.

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MIYAZAWA, Mitsuo, and Kyousuke NAKANISHI. "Biotransformation of (−)-Menthone by Human Liver Microsomes." Bioscience, Biotechnology, and Biochemistry 70, no. 5 (May 23, 2006): 1259–61. http://dx.doi.org/10.1271/bbb.70.1259.

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Wandel, C., R. Bocker, A. Browne, H. Bohrer, and E. Martin. "METABOLISM OF DIAZEPAM IN HUMAN LIVER MICROSOMES." Anesthesiology 81, SUPPLEMENT (September 1994): A395. http://dx.doi.org/10.1097/00000542-199409001-00394.

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Paibir, Sheela G., William H. Soine, Diana F. Thomas, and Robert A. Fisher. "Phenobarbital N-glucosylation by human liver microsomes." European Journal of Drug Metabolism and Pharmacokinetics 29, no. 1 (March 2004): 51–59. http://dx.doi.org/10.1007/bf03190574.

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Kobayashi, Tsutomu, Judith E. Sleeman, Michael W. H. Coughtrie, and Brian Burchell. "Molecular and functional characterization of microsomal UDP-glucuronic acid uptake by members of the nucleotide sugar transporter (NST) family." Biochemical Journal 400, no. 2 (November 14, 2006): 281–89. http://dx.doi.org/10.1042/bj20060429.

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Transport of the co-substrate UDPGA (UDP-glucuronic acid) into the lumen of the endoplasmic reticulum is an essential step in glucuronidation reactions due to the intraluminal location of the catalytic site of the enzyme UGT (UDP-glucuronosyltransferase). In the present study, we have characterized the function of several NSTs (nucleotide sugar transporters) and UGTs as potential carriers of UDPGA for glucuronidation reactions. UDPGlcNAc (UDP-N-acetylglucosamine)-dependent UDPGA uptake was found both in rat liver microsomes and in microsomes prepared from the rat hepatoma cell line H4IIE. The

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Benga, Gheorghe, and William Ferdinand. "Amino acid composition of rat and human liver microsomes in normal and pathological conditions." Bioscience Reports 15, no. 2 (April 1, 1995): 111–16. http://dx.doi.org/10.1007/bf01200145.

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The amino acid composition of proteins from liver microsomes has been studied in rats and in human subjects with normal liver, with obstructive jaundice or liver cirrhosis. The pattern of the amino acid composition of microsomes appeared to be species-specific. Phenylalanine, threonine, serine, proline, histidine and [aspartic acid plus asparagine] were increased, while alanine, tyrosine, glycine and arginine were decreased in the human compared to the rat microsomes. In patients with obstructive jaundice of short duration (less than two months) only a slight decrease in leucine and phenylalan

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Richard, Kerry, Robert Hume, Ellen Kaptein, Jo P. Sanders, Hans van Toor, Wouter W. de Herder, Jan C. den Hollander, Eric P. Krenning, and Theo J. Visser. "Ontogeny of Iodothyronine Deiodinases in Human Liver1." Journal of Clinical Endocrinology & Metabolism 83, no. 8 (August 1, 1998): 2868–74. http://dx.doi.org/10.1210/jcem.83.8.5032.

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abstract The role of the deiodinases D1, D2, and D3 in the tissue-specific and time-dependent regulation of thyroid hormone bioactivity during fetal development has been investigated in animals but little is known about the ontogeny of these enzymes in humans. We analyzed D1, D2, and D3 activities in liver microsomes from 10 fetuses of 15–20 weeks gestation and from 8 apparently healthy adult tissue transplant donors, and in liver homogenates from 2 fetuses (20 weeks gestation), 5 preterm infants (27–32 weeks gestation), and 13 term infants who survived up to 39 weeks postnatally. D1 activity

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Kim, Sin-Eun, Hyung-Ju Seo, Yeojin Jeong, Gyung-Min Lee, Seung-Bae Ji, So-Young Park, Zhexue Wu, Sangkyu Lee, Sunghwan Kim, and Kwang-Hyeon Liu. "In Vitro Metabolism of Donepezil in Liver Microsomes Using Non-Targeted Metabolomics." Pharmaceutics 13, no. 7 (June 23, 2021): 936. http://dx.doi.org/10.3390/pharmaceutics13070936.

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Donepezil is a reversible acetylcholinesterase inhibitor that is currently the most commonly prescribed drug for the treatment of Alzheimer’s disease. In general, donepezil is known as a safe and well-tolerated drug, and it was not associated with liver abnormalities in several clinical trials. However, rare cases of drug-related liver toxicity have been reported since it has become commercially available. Few studies have investigated the metabolic profile of donepezil, and the mechanism of liver damage caused by donepezil has not been elucidated. In this study, the in vitro metabolism of don

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KRAMER, Werner, Hans-Joerg BURGER, William J. ARION, Daniel CORSIERO, Frank GIRBIG, Claudia WEYLAND, Horst HEMMERLE, Stefan PETRY, Paul HABERMANN, and Andreas HERLING. "Identification of protein components of the microsomal glucose 6-phosphate transporter by photoaffinity labelling." Biochemical Journal 339, no. 3 (April 26, 1999): 629–38. http://dx.doi.org/10.1042/bj3390629.

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The glucose-6-phosphatase system catalyses the terminal step of hepatic glucose production from both gluconeogenesis and glycogenolysis and is thus a key regulatory factor of blood glucose homoeostasis. To identify the glucose 6-phosphate transporter T1, we have performed photoaffinity labelling of human and rat liver microsomes by using the specific photoreactive glucose-6-phosphate translocase inhibitors S 0957 and S 1743. Membrane proteins of molecular mass 70, 55, 33 and 31 kDa were labelled in human microsomes by [3H]S 0957, whereas in rat liver microsomes bands at 95, 70, 57, 54, 50, 41,

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Park, Ria, Eun Jeong Park, Yong-Yeon Cho, Joo Young Lee, Han Chang Kang, Im-Sook Song, and Hye Suk Lee. "Tetrahydrofurofuranoid Lignans, Eudesmin, Fargesin, Epimagnolin A, Magnolin, and Yangambin Inhibit UDP-Glucuronosyltransferase 1A1 and 1A3 Activities in Human Liver Microsomes." Pharmaceutics 13, no. 2 (February 1, 2021): 187. http://dx.doi.org/10.3390/pharmaceutics13020187.

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Eudesmin, fargesin, epimagnolin A, magnolin, and yangambin are tetrahydrofurofuranoid lignans with various pharmacological activities found in Magnoliae Flos. The inhibition potencies of eudesmin, fargesin, epimagnolin A, magnolin, and yangambin on six major human uridine 5′-diphospho-glucuronosyltransferase (UGT) activities in human liver microsomes were evaluated using liquid chromatography–tandem mass spectrometry and cocktail substrates. Eudesmin, fargesin, epimagnolin A, magnolin, and yangambin inhibited UGT1A1 and UGT1A3 activities, but showed negligible inhibition of UGT1A4, UGT16, UGT1

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Pennanen, S., A. Kojo, M. Pasanen, J. Liesivuori, RO Juvonen, and H. Komulainen. "CYP enzymes catalyze the formation of a terminal olefin from 2-ethylhexanoic acid in rat and human liver." Human & Experimental Toxicology 15, no. 5 (May 1996): 435–42. http://dx.doi.org/10.1177/096032719601500512.

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1 The metabolism of 2-ethylhexanoic acid (2-EHA) was studied in rat, mouse and human liver microsomes in vitro. The metabolites of 2-EHA were identified as methylated derivatives by gas chromatography-mass spectrometry. 2 2-Ethyl-1,6-hexanedioic acid was the main metabolite produced in rat, mouse and human liver microsomes. Unsaturated 2-ethyl-5-hexenoic acid, a terminal ole fin, was produced only in human liver microsomes and phenobarbital-induced rat liver microsomes. The cytochrome P450 (CYP) inhibitors metyrapone, SKF 525A, triacetyloleandomycin (TAO), quinidine and the cytochrome P450 red

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Venkataramanan, Raman, Shimin Zang, Timothy Gayowski, and Nina Singh. "Voriconazole Inhibition of the Metabolism of Tacrolimus in a Liver Transplant Recipient and in Human Liver Microsomes." Antimicrobial Agents and Chemotherapy 46, no. 9 (September 2002): 3091–93. http://dx.doi.org/10.1128/aac.46.9.3091-3093.2002.

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ABSTRACT The purpose of this study was to assess the effect of voriconazole on the blood tacrolimus concentration in a liver transplant recipient and to examine the interaction between voriconazole and tacrolimus by using human liver microsomes. Two subjects were enrolled in the clinical study: one received voriconazole, and the other received a placebo. Tacrolimus metabolism was evaluated in human liver microsomes at various concentrations in the absence and presence of various concentrations of voriconazole. Coadministration of voriconazole and tacrolimus resulted in elevated (nearly 10-fold

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Trapnell, C. B., C. Jamis-Dow, R. W. Klecker, and J. M. Collins. "Metabolism of rifabutin and its 25-desacetyl metabolite, LM565, by human liver microsomes and recombinant human cytochrome P-450 3A4: relevance to clinical interaction with fluconazole." Antimicrobial Agents and Chemotherapy 41, no. 5 (May 1997): 924–26. http://dx.doi.org/10.1128/aac.41.5.924.

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Rifabutin and fluconazole are often given concomitantly as therapy to prevent opportunistic infections in individuals infected with the human immunodeficiency virus. Recent reports have shown increased levels of rifabutin and its 25-desacetyl metabolite, LM565, in plasma when rifabutin is administered with fluconazole. Since fluconazole is known to inhibit microsomal enzymes, this study was undertaken to determine if this rifabutin-fluconazole interaction was due to an inhibition of human hepatic enzymes. The metabolism of both rifabutin and LM565 was evaluated in human liver microsomes and re

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Buchmueller, Julia, Florian Kaltner, Christoph Gottschalk, Maria Maares, Albert Braeuning, and Stefanie Hessel-Pras. "Structure-Dependent Toxicokinetics of Selected Pyrrolizidine Alkaloids In Vitro." International Journal of Molecular Sciences 23, no. 16 (August 16, 2022): 9214. http://dx.doi.org/10.3390/ijms23169214.

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Phytochemicals like pyrrolizidine alkaloids (PAs) can affect the health of humans and animals. PAs can occur for example in tea, honey or herbs. Some PAs are known to be cytotoxic, genotoxic, and carcinogenic. Upon intake of high amounts, hepatotoxic and pneumotoxic effects were observed in humans. This study aims to elucidate different toxicokinetic parameters like the uptake of PAs and their metabolism with in vitro models. We examined the transport rates of differently structured PAs (monoester, open-chained diester, cyclic diester) over a model of the intestinal barrier. After passing the

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Waddell, I. D., H. Scott, A. Grant, and A. Burchell. "Identification and characterization of a hepatic microsomal glucose transport protein. T3 of the glucose-6-phosphatase system?" Biochemical Journal 275, no. 2 (April 15, 1991): 363–67. http://dx.doi.org/10.1042/bj2750363.

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A 52 kDa polypeptide in rat liver microsomes was identified as a glucose-binding protein by its ability to weakly bind cytochalasin B and by its cross-reactivity to an antibody raised against the human erythrocyte glucose transport protein. The microsomal glucose binding polypeptide was purified by affinity chromatography and an antibody was raised against it. The inhibitory effect of this antibody on rat microsomal glucose-6-phosphatase activity and on glucose transport out of microsomal vesicles indicates that this protein is a microsomal glucose transport protein.

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He, Kan, Bing He, James E. Grace, Baomin Xin, Donglu Zhang, Donald J. Pinto, Joseph M. Luettgen, et al. "Preclinical Pharmacokinetic and Metabolism of Apixaban, a Potent and Selective Factor Xa Inhibitor." Blood 108, no. 11 (November 16, 2006): 910. http://dx.doi.org/10.1182/blood.v108.11.910.910.

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Abstract Apixaban is a potent, orally available, highly selective, and reversible factor Xa inhibitor, and currently under development for prevention and treatment of thrombosis. The preclinical pharmacokinetic and metabolism attributes of apixaban feature a small volume of distribution, a low systemic clearance, good oral bioavailability, multiple elimination pathways and minimal potential for drug-drug interactions. Apixaban is well absorbed in chimpanzees, dogs and rats with a mean oral bioavailability of 51, 88 and 34%, respectively. The mean volume of distribution of apixaban is 0.17, 0.2

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Moreira da Silva, Rodrigo, Cristiane de Gaitani, Lucas Marques, Karina Fraige Baraco, Alberto Cavalheiro, Luiz de Moraes, Norberto Lopes, and Anderson de Oliveira. "Characterization of Casearin X Metabolism by Rat and Human Liver Microsomes." Planta Medica 85, no. 04 (October 29, 2018): 282–91. http://dx.doi.org/10.1055/a-0765-9523.

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AbstractCasearin X (CAS X) is the major clerodane diterpene isolated from the leaves of Casearia sylvestris and has been extensively studied due to its powerful cytotoxic activity at low concentrations. Promising results for in vivo antitumor action have also been described when CAS X was administered intraperitoneally in mice. Conversely, loss of activity was observed when orally administered. Since the advancement of natural products as drug candidates requires satisfactory bioavailability for their pharmacological effect, this work aimed to characterize the CAS X metabolism by employing an

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Chen, Hui, Ya Zhang, Xiaoying Wu, Candong Li, and Huan Wang. "In Vitro Assessment of Cytochrome P450 2C19 Potential of Naoxintong." Evidence-Based Complementary and Alternative Medicine 2012 (2012): 1–6. http://dx.doi.org/10.1155/2012/430262.

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The effects of Buchang Naoxintong Capsules (BNCs) on S-mephenytoin 4′-hydroxylation activities in human liver microsomes in vitro were assessed. Human liver microsome was prepared by different ultracentrifugation. Human liver microsome incubation experiment was carried out to assay BNC on S-mephenytoin 4′-hydroxylation activities. The 4′-hydroxylation of S-mephenytoin, a representative substrate toward CYP2C19, was increased by phenytoin sodium (positive control). After the incubation, the metabolites of the substrates (4′-OH-mephenytoin) were determined by HPLC. Results showed that both pheny

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Dai, Ziru, Guibo Sun, Jiada Yang, Jie Hou, Ping Zhou, Weijie Xie, Guangbo Ge, Xiaobo Sun, and Ling Yang. "Interspecies Variation in NCMN-O-Demethylation in Liver Microsomes from Various Species." Molecules 24, no. 15 (July 30, 2019): 2765. http://dx.doi.org/10.3390/molecules24152765.

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NCMN (N-(3-carboxy propyl)-4-methoxy-1,8-naphthalimide), a newly developed ratiometric two-photon fluorescent probe for human Cytochrome P450 1A (CYP1A), shows the best combination of specificity and reactivity for real-time detection of the enzymatic activities of CYP1A in complex biological systems. This study aimed to investigate the interspecies variation in NCMN-O-demethylation in commercially available liver microsomes from human, mouse, rat, beagle dog, minipig and cynomolgus monkey. Metabolite profiling demonstrated that NCMN could be O-demethylated in liver microsomes from all species

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Skjelbo, E., and K. Brosen. "Inhibitors of imipramine metabolism by human liver microsomes." British Journal of Clinical Pharmacology 34, no. 3 (September 1992): 256–61. http://dx.doi.org/10.1111/j.1365-2125.1992.tb04133.x.

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Kang, Ping, Deepak Dalvie, Evan Smith, Sue Zhou, Alan Deese, and James A. Nieman. "Bioactivation of Flutamide Metabolites by Human Liver Microsomes." Drug Metabolism and Disposition 36, no. 7 (April 14, 2008): 1425–37. http://dx.doi.org/10.1124/dmd.108.020370.

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Zhang, Mei, J. Paul Fawcett, Julia M. Kennedy, and John P. Shaw. "Stereoselective glucuronidation of formoterol by human liver microsomes." British Journal of Clinical Pharmacology 49, no. 2 (February 2000): 152–57. http://dx.doi.org/10.1046/j.1365-2125.2000.00133.x.

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McLure, James A., John O. Miners, and Donald J. Birkett. "Nonspecific binding of drugs to human liver microsomes." British Journal of Clinical Pharmacology 49, no. 5 (May 2000): 453–61. http://dx.doi.org/10.1046/j.1365-2125.2000.00193.x.

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Kharasch, Evan D., and Rita Labroo. "Metabolism of Ketamine Stereoisomers by Human Liver Microsomes." Anesthesiology 77, no. 6 (December 1, 1992): 1201–7. http://dx.doi.org/10.1097/00000542-199212000-00022.

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García-Agúndez, Jose Augusto, Antonio Luengo, and Julio Benítez. "Aminopyrine N-demethylase activity in human liver microsomes." Clinical Pharmacology and Therapeutics 48, no. 5 (November 1990): 490–95. http://dx.doi.org/10.1038/clpt.1990.184.

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Miyazawa, Mitsuo, and Masaki Shindo. "Biotransformation of 1,8-Cineole by Human Liver Microsomes." Natural Product Letters 15, no. 1 (January 2001): 49–53. http://dx.doi.org/10.1080/10575630108041257.

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Hoskins, J., G. Shenfield, M. Murray, and A. Gross. "Characterization of moclobemideN-oxidation in human liver microsomes." Xenobiotica 31, no. 7 (January 2001): 387–97. http://dx.doi.org/10.1080/00498250110055488.

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Wynalda, M. A., K. M. Wynalda, B. M. Amore, P. E. Fagerness, and L. C. Wienkers. "Characterization of bropirimineO-glucuronidation in human liver microsomes." Xenobiotica 33, no. 10 (October 2003): 999–1011. http://dx.doi.org/10.1080/00498250310001602757.

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Mckillop, D., A. D. Mccormick, G. S. Miles, P. J. Phillips, K. J. Pickup, N. Bushby, and M. Hutchison. "In vitrometabolism of gefitinib in human liver microsomes." Xenobiotica 34, no. 11-12 (January 2004): 983–1000. http://dx.doi.org/10.1080/02772240400015222.

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