Nitric oxide-independent suppression of P450 2C11 expression by interleukin-1beta and endotoxin in primary rat hepatocytes.

abstract：:Salinomycin, a polyether antibiotic, acts as a highly selective potassium ionophore and has anticancer activity on various cancer cell lines. Cisplatin has been proved as chemotherapy drug for advanced human non-small cell lung cancer (NSCLC). Thymidylate synthase (TS) is a key enzyme in the pyrimidine salvage pathway...

journal_title：Biochemical pharmacology

authors： Ko JC,Zheng HY,Chen WC,Peng YS,Wu CH,Wei CL,Chen JC,Lin YW

更新日期：2016-12-15 00:00:00

abstract：:Understanding the mechanisms of transport processes in the placenta can improve the safety and efficacy of drug delivery during pregnancy. Functional studies of organic cation transporters (OCTs) are usually carried out using radioactivity, and a fluorescent marker would add flexibility to experimental methods. As a p...

journal_title：Biochemical pharmacology

authors： Rytting E,Bryan J,Southard M,Audus KL

更新日期：2007-03-15 00:00:00

abstract：:N-[5-[N-(3,4-Dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N- methylamino]-2-thenoyl]-L-glutamic acid (ZD1694) is a folate-based thymidylate synthase (TS; EC 2.1.1.45) inhibitor. Metabolism to higher chain length polyglutamates is essential for its optimal cytotoxic effect. A ZD1694-resistant (300-fold) human ileocecal...

journal_title：Biochemical pharmacology

authors： Lu K,Yin MB,McGuire JJ,Bonmassar E,Rustum YM

更新日期：1995-07-31 00:00:00

abstract：:The present study set out to investigate whether plasma phosphatidylcholine hydroperoxide (PCOOH) levels could accurately reflect lipid peroxidation linking to liver damage due to ischemia--reperfusion. PCOOH is a primary peroxidative product of phosphatidylcholine (PC), which is the most important functional lipid in...

journal_title：Biochemical pharmacology

authors： Takayama F,Egashira T,Kudo Y,Yamanaka Y

更新日期：1993-11-17 00:00:00

abstract：:Compounds of the mevalonate pathway containing a terminal di- or triphosphate (mev-PP or mev-PPP) were tested as substrates of several enzyme ligases (T4 RNA ligase, T4 DNA ligase, firefly luciferase and other ligases) for the synthesis of ATP derivatives of the mev-pppA or mev-ppppA type. T4 RNA ligase, in the presen...

journal_title：Biochemical pharmacology

authors： Sillero MA,de Diego A,Tavares JE,Silva JA,Pérez-Zúñiga FJ,Sillero A

更新日期：2009-08-15 00:00:00

abstract：:(1) As a first step in studying the kinetics of the lipolytic system of rat adipocytes, the day-to-day variation between dose-response curves has been analysed. (2) Methods are described for the evaluation of large quantities of data relating noradrenaline to lipolysis. (3) A 'clustering' technique is presented which ...

journal_title：Biochemical pharmacology

authors： Davies JI,Cooper DM,Everett D

更新日期：1982-03-01 00:00:00

abstract：:N417/AMSA cells, about 80-fold resistant to mAMSA [4'-(9-acridinylamino)-methanesulfon-m-anisidide], were obtained by serial passages of the parental human small cell lung carcinoma NCI-N417 (N417/p) in stepwise drug concentrations. The N417/AMSA cells were found to be 114-, 100-, and 9-fold cross-resistant to the top...

journal_title：Biochemical pharmacology

authors： Prost S,Riou G

更新日期：1994-08-30 00:00:00

abstract：:We have used 2-(beta-(3-125iodo-4-hydroxyphenyl)-ethylaminoethyl)-tetr alo ne ([125I]HEAT or BE2254), an alpha 1-selective antagonist, and [3H]yohimbine, an alpha 2-selective antagonist, to demonstrate and characterize binding sites in basolateral membranes from rat kidney cortex. Parathyroid hormone (PTH) stimulated ...

journal_title：Biochemical pharmacology

authors： Matsushima Y,Akabane S,Ito K

更新日期：1986-08-01 00:00:00

abstract：:Male weanling F-344 rats were maintained on selenium-supplemented or -deficient diets and were exposed to fresh cigarette smoke daily for 28 weeks. The deficient status of animals was demonstrated by a significant reduction in the pulmonary and hepatic glutathione peroxidase (GSH-Px) activity of rats on selenium-defic...

journal_title：Biochemical pharmacology

authors： Gairola CG,Tai HH

更新日期：1986-07-15 00:00:00

abstract：:The effects of streptozotocin (STZ)-induced diabetes on acetaminophen metabolism and hepatotoxicity in male Sprague-Dawley (SD) and Long Evans Hooded (LEH) rats were compared. In agreement with earlier studies, normal SD rats were more resistant to acetaminophen-induced hepatic necrosis than normal LEH rats. In contra...

journal_title：Biochemical pharmacology

authors： Price VF,Jollow DJ

更新日期：1986-02-15 00:00:00

abstract：:The addition of atrial natriuretic peptide (ANP) to isolated human adipocytes in primary culture from very obese individuals resulted in an inhibition of leptin release after a 24- or 48-hr incubation. There was also an inhibition of leptin release by isoproterenol (ISO) that was partially reversed by insulin, whereas...

journal_title：Biochemical pharmacology

authors： Fain JN,Kanu A,Bahouth SW,Cowan GS,Lloyd Hiler M

更新日期：2003-06-01 00:00:00

abstract：:Alpha 2 adrenoceptors of the human platelet and rat and rabbit renal cortex were compared in binding studies using the selective antagonist ligand [3H]rauwolscine. Significant differences in the pharmacological characteristics of the alpha 2 adrenoceptor were observed between the tissues with reference to both absolut...

journal_title：Biochemical pharmacology

authors： Cheung YD,Barnett DB,Nahorski SR

更新日期：1986-11-01 00:00:00

abstract：:Cytogenetic lesions often alter kinase signaling in acute myeloid leukemia (AML) and the addition of kinase inhibitors to the treatment arsenal is of interest. We have screened a kinase inhibitor library and performed combination testing to find promising drug-combinations for synergistic killing of AML cells. Cytotox...

journal_title：Biochemical pharmacology

authors： Österroos A,Kashif M,Haglund C,Blom K,Höglund M,Andersson C,Gustafsson MG,Eriksson A,Larsson R

更新日期：2016-10-15 00:00:00

abstract：:Thyroid hormones play a role in the regulation of glutathione S-transferase (GST) expression. Here, co-cultures of rat hepatocytes with bile duct epithelial cells have been used to study the direct effects of both triiodothyronine (T3) and thyroxine (T4) on GST activities and proteins. Because T3 and T4 are poorly wat...

journal_title：Biochemical pharmacology

authors： Vanhaecke T,Derde MP,Vercruysse A,Rogiers V

更新日期：2001-05-01 00:00:00

abstract：:The chiral inversion properties of 4-(4-methylphenyl)-2-methylthiomethyl-4-oxobutanoic acid (KE-748), an active metabolite of 2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (KE-298), were compared with those of ibuprofen in rats. After administration of R(-)-[2 alpha-2H]KE-748, S(+)-KE-748 was present in the...

journal_title：Biochemical pharmacology

authors： Yoshida H,Kohno Y,Endo H,Yamaguchi J,Fukushima K,Suwa T,Hayashi M

更新日期：1997-01-24 00:00:00

abstract：:Glycerol enhances pulmonary tumorigenesis in mice treated with 4-nitroquinoline 1-oxide (4NQO). The present study shows that active oxygen formation by glycerol may be responsible for this enhanced tumorigenesis. Male ddY mice were treated with 4NQO and given a 5% glycerol solution instead of drinking water for up to ...

journal_title：Biochemical pharmacology

authors： Yano T,Ichikawa T

更新日期：1992-06-23 00:00:00

abstract：:DUP 785 (NSC 368390; Brequinar sodium) is a new inhibitor of pyrimidine de novo biosynthesis with antitumor activity against several experimental tumors. DUP 785 inhibits the mitochondrial enzyme dihydroorotate dehydrogenase, blocking the conversion of dihydroorotate to orotate. We examined the influence of exposure t...

journal_title：Biochemical pharmacology

authors： Schwartsmann G,Peters GJ,Laurensse E,de Waal FC,Loonen AH,Leyva A,Pinedo HM

更新日期：1988-09-01 00:00:00

abstract：:Cholesterol 7 alpha-hydroxylase (CH-7 alpha) activity in HepG2 cells depleted of glutathione (GSH) was reduced significantly (P < 0.05) compared to that in untreated controls. Northern blot analysis of poly A+ mRNA isolated from GSH-depleted and control HepG2 cells showed that there was a reduction in mRNA for CH-7 al...

journal_title：Biochemical pharmacology

authors： Hassan AS,Bunick D,Lund LA,Bottje WG

更新日期：1992-10-06 00:00:00

abstract：:The intracellular actions of phosphodiesterase (PDE) inhibitors on the accumulation of cyclic nucleotides were studied in isolated ventricular cardiomyocytes from adult Sprague-Dawley rats. Elevated levels of cyclic AMP, due to the effects of selective PDE inhibitors, were detected only when the levels of cyclic nucle...

journal_title：Biochemical pharmacology

authors： Kelso EJ,McDermott BJ,Silke B

更新日期：1995-02-14 00:00:00

abstract：:The effect of glutathione depletion on cytotoxicity of the anthracycline daunorubicin, and of a copper:bis-thiosemicarbazone chelate, was examined in the P388 murine leukemia and its anthracycline-resistant subline, P388/ADR. Depletion of intracellular glutathione was accomplished through exposure to buthionine sulfox...

journal_title：Biochemical pharmacology

authors： Romine MT,Kessel D

更新日期：1986-10-01 00:00:00

abstract：:Antibody-directed enzyme prodrug therapy (ADEPT) aims at the specific activation of a prodrug by an enzyme-immunoconjugate localized in tumor tissue. The use of an enzyme of human origin is preferable in ADEPT because it might not be immunogenic when administered to patients. In the case of human beta-glucuronidase, p...

journal_title：Biochemical pharmacology

authors： Houba PH,Leenders RG,Boven E,Scheeren JW,Pinedo HM,Haisma HJ

更新日期：1996-08-09 00:00:00

abstract：:Pelargonidin is a natural red pigment found in fruits and vegetables, and has been reported to exhibit various effects potentially beneficial for human health. However, the possible preventive effects of pelargonidin toward atherosclerosis and mechanisms involved have not been investigated to date. Here, we compared t...

journal_title：Biochemical pharmacology

authors： Son JE,Jeong H,Kim H,Kim YA,Lee E,Lee HJ,Lee KW

更新日期：2014-05-15 00:00:00

abstract：:Enzymes of the UDP-glucuronosyltransferase (UGT) superfamily are responsible for the metabolism of many drugs, environmental chemicals and endogenous compounds. Identification of the UGT(s) involved in the metabolism of a given compound ('reaction phenotyping') currently relies on multiple confirmatory approaches, whi...

journal_title：Biochemical pharmacology

authors： Miners JO,Knights KM,Houston JB,Mackenzie PI

更新日期：2006-05-28 00:00:00

abstract：:The levels and subcellular distribution of enzymes involved in defenses against reactive oxygen superoxide dismutase (SOD; E.C.1.15.1.1), glutathione peroxidase (GPX; E.C.1.11.1.9), catalase (CAT; E.C.1.11.1.6), and DT-diaphorase (DT; E.C.1.6.99.2) and of the conjugating enzymes glutathione transferase (GST; E.C.2.5.1...

journal_title：Biochemical pharmacology

authors： Eliasson M,Boström M,DePierre JW

更新日期：1999-10-15 00:00:00

abstract：:We have previously shown [8] that rat liver adenosine kinase can produce [14C]AMP from [14C]adenosine (Ado) and unlabelled adenosine monophosphate (AMP), in the absence of ATP, by an exchange reaction. In this study, we investigated whether Ado or AMP could be replaced in this exchange reaction by other nucleosides or...

journal_title：Biochemical pharmacology

authors： Mimouni M,Bontemps F,Van den Berghe G

更新日期：1995-11-09 00:00:00

abstract：:Metyrapone (2-methyl-1,2-di-3-pyridyl-1-propanone, MTP) is used as an inhibitor of cytochrome P-450 enzymes, particularly those induced by phenobarbital (PB). We examined the effects of MTP on the microsomal dependent mutagenesis of a newly isolated promutagen, 3-(2-chloroethoxy)-1,2-dichloropropene (CP), three S-chlo...

journal_title：Biochemical pharmacology

authors： Distlerath LM,Loper JC,Tabor MW

更新日期：1983-12-15 00:00:00

abstract：:Within the tissue surrounding the necrotic lesion, following a cryogenic injury of the brain, there is a definite activation of phospholipase A2 (at 2 and 4 hr post lesion) that accounts, at least in part, for the phospholipid breakdown. There is also an activation of cholinephosphotransferase (at 2 hr post lesion) th...

journal_title：Biochemical pharmacology

authors： Arrigoni E,Averet N,Cohadon F

更新日期：1987-11-01 00:00:00

abstract：:Adenosine is an endogenous nucleoside that regulates many physiological processes through the activation of its four receptors: A(1), A(2A), A(2B) and A(3). Previous studies have identified the involvement of A(2) receptors in the inhibitory activity of adenosine analogues on tumor necrosis factor-alpha (TNF-alpha) pr...

journal_title：Biochemical pharmacology

authors： Zhang JG,Hepburn L,Cruz G,Borman RA,Clark KL

更新日期：2005-03-15 00:00:00

abstract：:Although clofibrate has been shown to inhibit platelet aggregation that is caused by thrombin, ADP and epinephrine, by blocking the release of arachidonic acid from platelet phospholipids [8], here we have demonstrated that clofibrate enhanced platelet aggregation by arachidonic acid and PLC and reversed the effects o...

journal_title：Biochemical pharmacology

authors： Huzoor-Akbar,Witiak DT,Newman HA,Fertel RH,Feller DR

更新日期：1982-06-01 00:00:00

abstract：:Purinergic stimulation of surfactant secretion via exocytosis of lamellar bodies is mediated by an elevation of the intracellular Ca2+ concentration ([Ca2+](i)). We tested the dihydropyridine (DHP) analogues isradipine (+/-enantiomers), nifedipine and Bay K 8644 (racemic forms) on ATP-induced surfactant secretion and ...

journal_title：Biochemical pharmacology

authors： Frick M,Siber G,Haller T,Mair N,Dietl P

更新日期：2001-05-01 00:00:00