Changes in the biliary excretion of organic anions following exhaustive exercise in rats.

Abstract:

:The effect of exhaustive exercise on the hepatobiliary transport of organic anions was investigated in rats. Animals were run on a rodent treadmill at 24 m/min up a 12% grade (152 +/- 15 min). Exercise resulted in significant hypoglycaemia (-46%) and increased plasma levels of lactate (+12%), together with a marked reduction of glycogen concentration in the liver (-72%). When bromosulphthalein was administered i.v., its maximal biliary excretion (Tm) was significantly reduced (-30%), and plasma and liver concentrations of the dye were increased (+31% and +56%, respectively). The decrease corresponded both to the excretion of the conjugated and unconjugated dye (-30% and -33%, respectively). Cytosolic glutathione S-transferase activity in the liver was not affected by exercise, but there was a significant reduction in the hepatic concentration of glutathione (-50%). The Tm of dibromosulphthalein was also significantly reduced (-36%) and its plasma and liver concentrations increased (+67% and +33%, respectively) in exercised rats. The results suggest that, in addition to the direct effect of liver glutathione depletion, other factors must be involved in the impairment of the biliary excretion of organic anions caused by exercise.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Villa JG,Collado PS,Almar MM,Gonzalez J

doi

10.1016/0006-2952(90)90094-2

subject

Has Abstract

pub_date

1990-12-01 00:00:00

pages

2519-24

issue

11

eissn

0006-2952

issn

1873-2968

pii

0006-2952(90)90094-2

journal_volume

40

pub_type

杂志文章
  • Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor.

    abstract::Inflammation-induced microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal enzyme that synthesizes prostaglandin E(2) (PGE(2)) downstream of cyclooxygenase-2 (COX-2). The efficacy of nonsteroidal anti-inflammatory drugs and COX-2 inhibitors in the treatment of the signs and symptoms of osteoarthritis, rheuma...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.01.003

    authors: Mbalaviele G,Pauley AM,Shaffer AF,Zweifel BS,Mathialagan S,Mnich SJ,Nemirovskiy OV,Carter J,Gierse JK,Wang JL,Vazquez ML,Moore WM,Masferrer JL

    更新日期:2010-05-15 00:00:00

  • Altered gene expression in human leukemia K562 cells selected for resistance to etoposide.

    abstract::Sublines of K562 human leukemia cells were selected for resistance (30- to 80-fold) to etoposide by continuous exposure to 0.5 microM VP-16. Two etoposide-resistant cell lines, K/VP.5 and K/VP.5-1, showed a 5-fold reduction in levels of topoisomerase II alpha protein compared with K562 cells. Northern analysis indicat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90643-b

    authors: Ritke MK,Yalowich JC

    更新日期:1993-12-03 00:00:00

  • Quilamine HQ1-44, an iron chelator vectorized toward tumor cells by the polyamine transport system, inhibits HCT116 tumor growth without adverse effect.

    abstract::Tumor cell growth requires large iron quantities and the deprivation of this metal induced by synthetic metal chelators is therefore an attractive method for limiting the cancer cell proliferation. The antiproliferative effect of the Quilamine HQ1-44, a new iron chelator vectorized toward tumor cells by a polyamine ch...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2015.06.001

    authors: Renaud S,Corcé V,Cannie I,Ropert M,Lepage S,Loréal O,Deniaud D,Gaboriau F

    更新日期:2015-08-01 00:00:00

  • Involvement of inositol 1,4,5-triphosphate and protein kinase C in thrombin-induced contraction of porcine pulmonary artery.

    abstract::The role of the intracellular messengers inositol 1,4,5-triphosphate (IP3) and protein kinase C (PKC) in the thrombin (3 U/mL)-induced contraction of endothelium-denuded porcine pulmonary arteries was investigated. Thrombin induced a sustained contractile response with an initial transient increase in IP3 to about 160...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)00404-a

    authors: Bretschneider E,Paintz M,Glusa E

    更新日期:1995-01-06 00:00:00

  • JNK-AKT-NF-κB controls P-glycoprotein expression to attenuate the cytotoxicity of deoxynivalenol in mammalian cells.

    abstract::P-glycoprotein (P-gp) plays critical roles in mediating the cytotoxicity of many drugs that are P-gp substrates. Previously, we reported that P-glycoprotein (P-gp) is the foremost efflux transporter of deoxynivalenol (DON), which is one of the most abundant mycotoxins. However, whether DON changes the expression of P-...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2018.08.020

    authors: Li X,Mu P,Qiao H,Wen J,Deng Y

    更新日期:2018-10-01 00:00:00

  • Effect of chronic phenobarbital treatment on folates and one-carbon enzymes in the rat.

    abstract::Chronic oral phenobarbital treatment (50 mg/kg every 12 hr for 8 weeks), which was nontoxic and continuously protective against seizures in rats, significantly decreased folate concentration in liver (29%) but not in brain or plasma. The apparent activity of 5,10-methylenetetrahydrofolate reductase (MTR) in liver decr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(84)90120-5

    authors: Carl GF,Smith DB

    更新日期:1984-11-01 00:00:00

  • Phospholipase A2 activity in carrageenin-induced inflammatory tissue of rats.

    abstract::Phospholipase A2 activity was detected in 7-day-old carrageenin-induced inflammatory tissue of rats using a synthetic substrate. 1-acyl-2-[3H]arachidonyl-phosphatidylcholine. The inflammatory tissue was homogenized in saline containing 1 M KCl, and the 105,000 g supernatant fraction was placed on a Sephadex G-100 colu...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90275-1

    authors: Ohuchi K,Watanabe M,Numajiri N,Tsurufuji S

    更新日期:1982-09-15 00:00:00

  • Bioavailability of phylloquinone and menaquinones after oral and colorectal administration in vitamin K-deficient rats.

    abstract::Rats were made vitamin K-deficient by feeding them a diet devoid of vitamin K and by rigorously preventing coprophagy. After one week, circulating prothrombin concentrations were between 5 and 10% of initial values, and various amounts of phylloquinone, menaquinone-4, and menaquinone-9 were given in a single dose eith...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(95)00202-b

    authors: Groenen-van Dooren MM,Ronden JE,Soute BA,Vermeer C

    更新日期:1995-09-07 00:00:00

  • A study of the expression of the xenobiotic-metabolising cytochrome P450 proteins and of testosterone metabolism in bovine liver.

    abstract::The expression of xenobiotic-metabolising cytochrome P450 proteins in the liver of cattle was determined using substrate probes and immunologically by Western blot analysis. Compared to the rat, cattle displayed much higher coumarin 7-hydroxylase (CYP2A) and ethoxyresorufin O-deethylase (CYP1) activity but, in contras...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(01)00710-9

    authors: Sivapathasundaram S,Magnisali P,Coldham NG,Howells LC,Sauer MJ,Ioannides C

    更新日期:2001-09-01 00:00:00

  • Control of [3H]ouabain binding to cerebromicrovascular (Na+ + K+)-ATPase by metal ions and proteins.

    abstract::The (Na+ + K+)-ATPase is localized to the cerebral endothelium, i.e. the blood-brain barrier, and is important for the maintenance of the brain electrolyte environment. Data from the present study indicate that Pb2+ inhibits the binding of [3H]ouabain to the cerebral microvascular (Na+ + K+)-ATPase in a time- and dose...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(90)90606-l

    authors: Caspers ML,Kwaiser TM,Grammas P

    更新日期:1990-06-15 00:00:00

  • Characterization of the purine-reactive site of the rat testis cytosolic adenylate cyclase.

    abstract::Naturally soluble rat germ cell adenylate cyclase was inhibited by adenosine and the adenosine analogs, 9-beta-D-arabinofuranosyl adenine (AFA) and 2',5'-dideoxyadenosine (DDA), all of which inhibited hormone-sensitive adenylate cyclases at the "P" site. The IC50 values for adenosine and DDA were approximately 0.1 and...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(87)90487-4

    authors: Onoda JM,Braun T,Wrenn SM Jr

    更新日期:1987-06-15 00:00:00

  • Resveratrol, a dietary polyphenolic phytoalexin, is a functional scavenger of peroxynitrite.

    abstract::Oxidant damage from reactive oxygen species (ROS) and reactive nitrogen species (RNS) is a major contributor to the cellular damage seen in numerous types of renal injury. Resveratrol (trans-3,4',5-trihydroxystilbene) is a phytoalexin found naturally in many common food sources. The anti-oxidant properties of resverat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.06.027

    authors: Holthoff JH,Woodling KA,Doerge DR,Burns ST,Hinson JA,Mayeux PR

    更新日期:2010-10-15 00:00:00

  • Isothiocyanates as novel cytotoxic and cytostatic agents: molecular pathway on human transformed and non-transformed cells.

    abstract::Cancer chemoprevention is a new approach in the management of cancer. Traditional cytotoxic chemotherapeutic approaches cannot cure most advanced solid malignancies. Chemoprevention can be defined as the use of non-cytotoxic drugs and natural agents to block the progression to invasive cancer. Recently, isothiocyanate...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2004.03.044

    authors: Fimognari C,Nüsse M,Berti F,Iori R,Cantelli-Forti G,Hrelia P

    更新日期:2004-09-15 00:00:00

  • Inhibition of phosphate transport in rat heart mitochondria by 3'-azido-3'-deoxythymidine due to stimulation of superoxide anion mitochondrial production.

    abstract::In order to gain some insight into the mechanism by which 3'-azido-3'-deoxythymidine (AZT) damages mitochondria, we investigated whether externally added AZT can stimulate reactive oxygen species (ROS) production by rat heart mitochondria (RHM). An increase in superoxide anion ((O(2)(.-)) production was measured in RH...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(02)01065-1

    authors: Valenti D,Atlante A,Barile M,Passarella S

    更新日期:2002-07-15 00:00:00

  • Cerebral and extracerebral cholesterol metabolism and CSF markers of Alzheimer's disease.

    abstract::The disturbances of the cholesterol synthesis and metabolism described in Alzheimer's disease (AD) may be both a consequence of the neurodegenerative process and a contributor to the pathogenesis. These putative relationships and their underlying mechanisms are not well understood. The aim of this study was to evaluat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2012.12.007

    authors: Popp J,Meichsner S,Kölsch H,Lewczuk P,Maier W,Kornhuber J,Jessen F,Lütjohann D

    更新日期:2013-07-01 00:00:00

  • Changes in methionine metabolism induced by D-galactosamine in isolated rat hepatocytes.

    abstract::We studied several steps of methionine metabolism in isolated rat hepatocytes both with and without the presence of a hepatotoxic agent (D-galactosamine). By use of selective labelling either on methyl or on carboxyl groups, we showed that intracellular methionine is used preferentially for the methylation of phosphol...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(86)90699-4

    authors: Ozturk M,Lemonnier F,Cresteil D,Lemonnier A

    更新日期:1986-12-01 00:00:00

  • Role of AKT1 in 17beta-estradiol- and insulin-like growth factor I (IGF-I)-dependent proliferation and prevention of apoptosis in MCF-7 breast carcinoma cells.

    abstract::AKT1 (c-AKT, PKBalpha) is the cellular homolog of the protein-serine/threonine kinase oncogene, v-akt. AKT1 is activated through the insulin and platelet-derived growth factor signaling pathways in transfected fibroblasts, but little is known about the regulation of endogenous AKT1 in tumor cells. AKT1 levels were hig...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(99)00125-2

    authors: Ahmad S,Singh N,Glazer RI

    更新日期:1999-08-01 00:00:00

  • TGF-beta in cancer and as a therapeutic target.

    abstract::Cancer develops through a series of genetic changes leading to malignant transformation. Numerous gene and pathways involved in stages of progression to frank malignancy have been elucidated. These genetic changes result in aberrations in fundamental cellular processes controlling proliferation, apoptosis, differentia...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2006.03.004

    authors: Pinkas J,Teicher BA

    更新日期:2006-08-28 00:00:00

  • Comparisons of ESR and HPLC methods for the detection of OH. radicals in ischemic/reperfused hearts. A relationship between the genesis of free radicals and reperfusion arrhythmias.

    abstract::In this study we compared two methods, electron spin resonance (ESR) spectroscopy and high performance liquid chromatography (HPLC), which are currently used to detect directly hydroxyl radical (OH.) formation in the ischemic and reperfused heart. Isolated buffer-perfused rat hearts were subjected to 30 min of normoth...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90182-v

    authors: Tosaki A,Bagchi D,Pali T,Cordis GA,Das DK

    更新日期:1993-02-24 00:00:00

  • A sensitive new method for clinically monitoring cytarabine concentrations at the DNA level in leukemic cells.

    abstract::Cytarabine (ara-C), a major antileukemic agent, is phosphorylated in the cell to cytarabine triphosphate (ara-CTP), which is then partly incorporated into DNA. The drug incorporation into DNA poisons the extending primer against further incorporation of deoxyribonucleotides including dCTP, ultimately inhibiting DNA sy...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2005.03.013

    authors: Yamauchi T,Ueda T

    更新日期:2005-06-15 00:00:00

  • The acetaminophen-derived bioactive N-acylphenolamine AM404 inhibits NFAT by targeting nuclear regulatory events.

    abstract::AM404 is a synthetic TRPV1/CB(1) hybrid ligand with inhibitory activity on the anandamide transporter and is used for the pharmacological manipulation of the endocannabinoid system. It has been recently described that acetaminophen is metabolised in the brain to form the bioactive N-acylphenolamine AM404 and therefore...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2006.12.001

    authors: Caballero FJ,Navarrete CM,Hess S,Fiebich BL,Appendino G,Macho A,Muñoz E,Sancho R

    更新日期:2007-04-01 00:00:00

  • Effects of chain length and sulphur position of thia fatty acids on their incorporation into phospholipids in 7800 C1 hepatoma cells and isolated rat hepatocytes, and their effects on fatty acid composition of phospholipids.

    abstract::Incorporation of thia fatty acids and their effects on the fatty acid composition in phospholipids has been investigated in 7800 C1 hepatoma cells and cultured hepatocytes. 3-Thia fatty acids of chain lengths from dodecyl-to hexadecyl-thioacetic acid were incorporated into phospholipids during a 3-day incubation. Long...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(95)02182-5

    authors: Wu P,Grav HJ,Horn R,Bremer J

    更新日期:1996-03-22 00:00:00

  • Evaluation of in vitro PXR-based assays and in silico modeling approaches for understanding the binding of a structurally diverse set of drugs to PXR.

    abstract::The pregnane X-receptor (PXR) is a promiscuous nuclear receptor primarily responsible for the induction of genes from the cytochrome P450 3A family. In this study, we used a previously described PXR/SRC tethered protein to establish two in vitro assays for identifying PXR ligands: automated ligand identification syste...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.12.003

    authors: Xiao L,Nickbarg E,Wang W,Thomas A,Ziebell M,Prosise WW,Lesburg CA,Taremi SS,Gerlach VL,Le HV,Cheng KC

    更新日期:2011-03-01 00:00:00

  • Inhibition of calmodulin-activated cyclic nucleotide phosphodiesterase: multiple binding-sites for tricyclic drugs on calmodulin.

    abstract::A cyclic nucleotide phosphodiesterase from guinea-pig heart is activated by calmodulin in the presence of calcium ions. Activation was measured over a range of calmodulin concentrations, and is antagonised by several tricyclic psychotropic drugs including trifluoperazine, imipramine, chlorpromazine and amitriptyline. ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90192-7

    authors: Reynolds CH,Claxton PT

    更新日期:1982-02-01 00:00:00

  • Cigarette smoke-induced alterations in the release of arachidonate metabolites by pulmonary alveolar macrophage from selenium-fed and selenium-deficient rats.

    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

    pub_type: 杂志文章

    doi:10.1016/0006-2952(86)90471-5

    authors: Gairola CG,Tai HH

    更新日期:1986-07-15 00:00:00

  • Interleukin-1beta converting enzyme (caspase-1) in intestinal inflammation.

    abstract::An imbalance of T helper cell type 1 (Th1) versus type 2 (Th2) polarization in favor of Th1 cell subsets appears to be a key pathogenic mechanism in chronic inflammatory bowel disease (IBD), in particular in Crohn's disease. The interferon gamma-inducing factor interleukin (IL)-18 acts in strong synergism with the Th1...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0006-2952(02)01064-x

    authors: Siegmund B

    更新日期:2002-07-01 00:00:00

  • Inhibition by lipoxygenase products of TXA2-like responses of platelets and vascular smooth muscle. 14-Hydroxy from 22:6n-3 is more potent than 12-HETE.

    abstract::Lipoxygenase products, which are formed in great amounts in platelets during their activation, have been prepared from arachidonic acid (20:4n-6), the main polyunsaturated fatty acid (PUFA) esterified in platelet phospholipids, and from two major PUFAs of fish fat, eicosapentaenoic (20:5n-3) and docosahexaenoic (22:6n...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(88)90782-4

    authors: Croset M,Sala A,Folco G,Lagarde M

    更新日期:1988-04-01 00:00:00

  • Parkin is transcriptionally regulated by the aryl hydrocarbon receptor: Impact on α-synuclein protein levels.

    abstract::Parkin (PRKN) is a ubiquitin E3 ligase that catalyzes the ubiquitination of several proteins. Mutations in the human Parkin gene, PRKN, leads to degeneration of dopaminergic (DA) neurons, resulting in autosomal recessive early-onset parkinsonism and the loss of PRKN function is linked to sporadic Parkinson's disease (...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2019.08.002

    authors: González-Barbosa E,García-Aguilar R,Vega L,Cabañas-Cortés MA,Gonzalez FJ,Segovia J,Morales-Lázaro SL,Cisneros B,Elizondo G

    更新日期:2019-10-01 00:00:00

  • Indirect evidence for the metabolic dehalogenation of tetrafluorodiethylstilbestrol by rat and hamster liver and kidney microsomes. Species- and organ-dependent differences.

    abstract::In order to assess the significance of the catechol pathway for the carcinogenic activity of diethylstilbestrol (DES), the stability of 3',5',3",5"-tetrafluoro-DES (TF-DES) against metabolic catechol formation was examined in vitro. A radioenzymatic assay was used for determining the estrogen hydroxylase activity of l...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(86)90582-4

    authors: Hey MM,Haaf H,McLachlan JA,Metzler M

    更新日期:1986-07-01 00:00:00

  • Effect of okadaic acid on immunologic and non-immunologic histamine release in rat mast cells.

    abstract::We have studied the effect of the protein phosphatase (PP) inhibitor, okadaic acid (OKA) on histamine release elicited by immunologic and non-immunologic stimuli in peritoneal and pleural rat mast cells. When cells were stimulated with antigen (egg albumin), OKA strongly inhibited histamine release. This finding sugge...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90194-5

    authors: Estévez MD,Vieytes MR,Louzao MC,Botana LM

    更新日期:1994-02-09 00:00:00