当前位置： SCI文献检索 > BIOCHEMICAL PHARMACOLOGY期刊下所有文献 > Low-affinity uptake of the fluorescent organic cation 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (4-Di-1-ASP) in BeWo cells.

Low-affinity uptake of the fluorescent organic cation 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (4-Di-1-ASP) in BeWo cells.

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 published substrate for OCT1 and OCT2, the fluorescent compound 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (4-Di-1-ASP) was chosen as a candidate for studying placental OCT function in BeWo cells. The expression of OCT1 and OCT2 was also investigated in BeWo cells, an established human choriocarcinoma trophoblastic cell line frequently used as an in vitro model of the rate-limiting barrier for maternal-fetal exchange of drugs and nutrients within the placenta. 4-Di-1-ASP was taken up into BeWo cells by a low-affinity, carrier-mediated process exhibiting a Km of 580+/-110 microM and Vmax of 97+/-9 nmol/mg protein/30 min, and asymmetric transport was observed, with greater permeability in the apical to basolateral (maternal-to-fetal) direction. However, RT-PCR revealed no expression of OCT1 or OCT2 in either BeWo cells or primary cultured human cytotrophoblast cells, and OCT substrates such as TEA and choline did not inhibit the uptake of 4-Di-1-ASP. Although the uptake of this fluorescent compound in BeWo cells is not mediated by an OCT, the colocalization experiments with fluorescence microscopy and inhibition studies confirmed significant mitochondrial uptake of 4-Di-1-ASP. Transport of 4-Di-1-ASP into the nuclear region of BeWo cells was also observed, which is likely mediated by a nucleoside transporter.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Rytting E,Bryan J,Southard M,Audus KL

doi

10.1016/j.bcp.2006.11.020

subject

Has Abstract

pub_date

2007-03-15 00:00:00

pages

891-900

issue

6

eissn

0006-2952

issn

1873-2968

pii

S0006-2952(06)00783-0

journal_volume

73

pub_type

杂志文章

相关文献

BIOCHEMICAL PHARMACOLOGY文献大全
  • Binding of [3H]quinuclidinyl benzilate to intestinal mucus. An artifact in identification of epithelial cell muscarinic receptors.

    abstract：:The widely used muscarinic receptor ligand [3H]quinuclidinyl benzilate ([3H]QNB) was found to bind in a site-specific but artifactual manner to rat intestinal mucus, obscuring specific binding to muscarinic receptors on intestinal epithelial cells. Atropine inhibited [3H]QNB binding to mucus with an apparent IC50 of 2...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90153-8

    authors： Rimele TJ,Gaginella TS

    更新日期：1982-02-15 00:00:00

  • Thiourea toxicity in mouse C3H/10T1/2 cells expressing human flavin-dependent monooxygenase 3.

    abstract：:Human flavin-dependent monooxygenase (FMO) isoforms 1 and 3 were expressed by retroviral gene transfer in mouse C3H/10T1/2 cells. FMO function was determined by the sulfoxidation of p-tolylmethylsulfide (TMS). Enzyme activity ranged from 4 to 30 nmol p-tolylmethylsulfoxide (TMSO)/30 min/mg cell protein for FMO 3 clone...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(02)00978-4

    authors： Smith PB,Crespi C

    更新日期：2002-06-01 00:00:00

  • Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an "infinite dilution" procedure.

    abstract：:The effects of two competitive antagonists and two allosteric ligands on the rate of dissociation of [3H]N-methylscopolamine ([3H]NMS) were studied at atrial muscarinic acetylcholine M2 receptors by the technique of "infinite dilution." The dissociation rate for [3H]NMS, initiated by diluting the incubation mixture in...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(96)00814-3

    authors： Christopoulos A,Lanzafame A,Ziegler A,Mitchelson F

    更新日期：1997-03-21 00:00:00

  • PI3K/AKT/mTOR signaling as a molecular target in head and neck cancer.

    abstract：:The aim of this review is to summarize current available information about the role of PI3K/AKT/mTOR signaling in head and neck cancer as a potential target for new therapy options. 90% of all head and neck cancers are squamous cell carcinomas (HNSCC). The most common genetic alteration is inactivation of p16 gene whi...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2019.113729

    authors： Marquard FE,Jücker M

    更新日期：2020-02-01 00:00:00

  • 86Rb+ efflux mediated by alpha4beta2*-nicotinic acetylcholine receptors with high and low-sensitivity to stimulation by acetylcholine display similar agonist-induced desensitization.

    abstract：:The nicotinic acetylcholine receptors (nAChR) assembled from alpha4 and beta2 subunits are the most densely expressed subtype in the brain. Concentration-effect curves for agonist activation of alpha4beta2*-nAChR are biphasic. This biphasic agonist sensitivity is ascribed to differences in subunit stoichiometry. The s...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2010.06.040

    authors： Marks MJ,Meinerz NM,Brown RW,Collins AC

    更新日期：2010-10-15 00:00:00

  • Phenylhydrazine-induced lipid peroxidation of red blood cells in vitro and in vivo: monitoring by the production of volatile hydrocarbons.

    abstract：:Human red blood cells and male Sprague-Dawley rats were treated in vitro and in vivo, respectively, with phenylhydrazine in order to determine whether the release of volatile hydrocarbons can serve as a suitable index for phenylhydrazine-induced red blood cell peroxidation. Lipid peroxidation following phenylhydrazine...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(84)90338-1

    authors： Clemens MR,Remmer H,Waller HD

    更新日期：1984-06-01 00:00:00

  • Molecular and functional characterization of flavin-containing monooxygenases in cynomolgus macaque.

    abstract：:Flavin-containing monooxygenases (FMOs), drug-metabolizing enzymes essential for the metabolism of endogenous biochemicals and foreign compounds, have been characterized in human (including FMO1-5 and FMO6P), but remain to be investigated in cynomolgus macaque. In this study, cDNAs of cynomolgus FMO1-5 and FMO6 were i...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2013.04.012

    authors： Uno Y,Shimizu M,Yamazaki H

    更新日期：2013-06-15 00:00:00

  • Ebselen-binding equilibria between plasma and target proteins.

    abstract：:The antiinflammatory drug ebselen (2-phenyl-1,2-benzisoselenazo-3(2H)-one) is known to bind covalently to thiols to form seleno disulfides that, directly or indirectly, are responsible for its pharmacological effects. Due to its reactive thiol group and high plasma concentration, albumin is a preferred target of ebsel...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(96)00109-8

    authors： Ullrich V,Weber P,Meisch F,von Appen F

    更新日期：1996-07-12 00:00:00

  • Non-immunological toxicological mechanisms of metamizole-associated neutropenia in HL60 cells.

    abstract：:Metamizole is an analgesic and antipyretic, but can cause neutropenia and agranulocytosis. We investigated the toxicity of the metabolites N-methyl-4-aminoantipyrine (MAA), 4-aminoantipyrine (AA), N-formyl-4-aminoantipyrine (FAA) and N-acetyl-4-aminoantipyrine (AAA) on neutrophil granulocytes and on HL60 cells (granul...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2019.01.011

    authors： Rudin D,Lanzilotto A,Bachmann F,Housecroft CE,Constable EC,Drewe J,Haschke M,Krähenbühl S

    更新日期：2019-05-01 00:00:00

  • Involvement of ROS in chlorogenic acid-induced apoptosis of Bcr-Abl+ CML cells.

    abstract：:Chlorogenic acid (Chl) has been reported to possess a wide range of biological and pharmacological properties including induction of apoptosis of Bcr-Abl(+) chronic myeloid leukemia (CML) cell lines and clinical leukemia samples via inhibition of Bcr-Abl phosphorylation. Here we studied the mechanisms of action of Chl...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2010.08.013

    authors： Rakshit S,Mandal L,Pal BC,Bagchi J,Biswas N,Chaudhuri J,Chowdhury AA,Manna A,Chaudhuri U,Konar A,Mukherjee T,Jaisankar P,Bandyopadhyay S

    更新日期：2010-12-01 00:00:00

  • Expression of drug resistance-associated mdr-1, GST pi, and topoisomerase II genes during cell cycle traverse.

    abstract：:The expression of drug resistance-associated mdr-1, GST pi, and topoisomerase II genes was analyzed in cell cycle phase enriched populations of doxorubicin-resistant murine leukemic P388/R-84 cells. Flow cytometric analysis of bromodeoxyuridine (BrdU) incorporation and staining with anti-BrdU antibodies was used to co...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(94)00443-p

    authors： Ramachandran C,Mead D,Wellham LL,Sauerteig A,Krishan A

    更新日期：1995-02-14 00:00:00

  • Discovery of substituted sulfonamides and thiazolidin-4-one derivatives as agonists of human constitutive androstane receptor.

    abstract：:The constitutive androstane receptor (CAR; NR1I3) is a nuclear receptor responsible for the recognition of potentially toxic endo- and exogenous compounds whose elimination from the body is accelerated by the CAR-mediated inducible expression of metabolizing enzymes and transporters. Despite the importance of CAR, few...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2008.08.014

    authors： Küblbeck J,Jyrkkärinne J,Poso A,Turpeinen M,Sippl W,Honkakoski P,Windshügel B

    更新日期：2008-11-15 00:00:00

  • Characterization of the benzene monooxygenase system in rabbit bone marrow.

    abstract：:The microsomal fraction of bone marrow contains cytochrome P-450 (39 +/- 11 pmoles/mg microsomal protein) and monooxygenase activity could be demonstrated by the O-dealkylation of 7-ethoxycoumarin (114 +/- 65 pmoles/(min X mg microsomal protein] and the hydroxylation of benzene to phenol (51 +/- 8.6 pmol/45 min X mg m...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(84)90143-6

    authors： Gollmer L,Graf H,Ullrich V

    更新日期：1984-11-15 00:00:00

  • Pharmacodynamic and pharmacokinetic analysis of apoE4 [L261A, W264A, F265A, L268A, V269A], a recombinant apolipoprotein E variant with improved biological properties.

    abstract：:Physiological levels of wild-type (wt) apolipoprotein E (apoE) in plasma mediate the clearance of cholesterol-rich atherogenic lipoprotein remnants while higher than normal plasma apoE concentrations fail to do so and trigger hypertriglyceridemia. This property of wt apoE reduces significantly its therapeutic value as...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2012.09.006

    authors： Lampropoulou A,Zannis VI,Kypreos KE

    更新日期：2012-12-01 00:00:00

  • In vivo induction of cytochrome P450 CYP3A expression in rat leukocytes using various inducers.

    abstract：:Although the induction of cytochromes P450 3A (CYP3A) is relatively well characterized in liver, its inducibility in an easily available tissue such as the peripheral leukocytes is not known. The purpose of this study was, therefore, to determine if CYP3A is inducible in vivo in peripheral leukocytes. Microsomes from ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(96)00095-0

    authors： Mahnke A,Roos PH,Hanstein WG,Chabot GG

    更新日期：1996-06-14 00:00:00

  • Stereoselective sulfoxidation of sulindac sulfide by flavin-containing monooxygenases. Comparison of human liver and kidney microsomes and mammalian enzymes.

    abstract：:The stereoselective sulfoxidation of the pharmacologically active metabolite of sulindac, sulindac sulfide, was characterized in human liver, kidney, and cDNA-expressed enzymes. Kinetic parameter estimates (pH = 7.4) for sulindac sulfoxide formation in human liver microsomes (N = 4) for R- and S-sulindac sulfoxide wer...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(00)00301-4

    authors： Hamman MA,Haehner-Daniels BD,Wrighton SA,Rettie AE,Hall SD

    更新日期：2000-07-01 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

  • Effect of disodium cromoglycate and cyclic AMP-active drugs on cytotoxic histamine release from rat mast cells.

    abstract：:Disodium cromoglycate and compounds which elevated levels of cyclic AMP in the mast cell variously inhibited cytotoxic histamine release induced by the surface active agents melittin, Tween 20 and Triton X-100. These results are inconsistent with the postulated effects of the drugs on receptor mediated calcium channel...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90109-5

    authors： Pearce FL,Clements J

    更新日期：1982-07-01 00:00:00

  • Inhibitory effect of eugenol on non-enzymatic lipid peroxidation in rat liver mitochondria.

    abstract：:The anti-peroxidative activity of eugenol on Fe(2+)-ascorbate- and Fe(2+)-H2O2-induced lipid peroxidation was studied using rat liver mitochondria. Eugenol inhibited thiobarbituric acid reactive substance (TBARS) formation induced by both the systems in addition to oxygen uptake and mitochondrial swelling induced by F...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(92)90318-d

    authors： Nagababu E,Lakshmaiah N

    更新日期：1992-06-09 00:00:00

  • Depletion of cardiac norepinephrine in rats and mice by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP).

    abstract：:1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) is a commercially available chemical reagent. Although little has been known about its biological effects, recently MPTP has been reported to cause irreversible Parkinson's disease-like symptoms in humans and in monkeys. We describe here another pharmacologic effect ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(84)90593-8

    authors： Fuller RW,Hahn RA,Snoddy HD,Wikel JH

    更新日期：1984-10-01 00:00:00

  • 2-Bromoethylamine as a potent selective suicide inhibitor for semicarbazide-sensitive amine oxidase.

    abstract：:Semicarbazide-sensitive amine oxidase (SSAO) catalyzes the deamination of methylamine and aminoacetone to produce toxic aldehydes, i.e. formaldehyde and methylglyoxal, as well as hydrogen peroxide and ammonia. An increase of SSAO activity was detected by different laboratories in patients suffering from vascular disor...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(01)00524-x

    authors： Yu PH,Davis BA,Deng Y

    更新日期：2001-03-15 00:00:00

  • Transforming growth factor-beta3 protection of epithelial cells from cycle-selective chemotherapy in vitro.

    abstract：:The transforming growth factor-beta (TGF-beta) family of regulatory growth factors can reversibly arrest cell division in the G1 phase of the cell cycle. Previously, TGF-beta3 was shown to protect epithelial cells and hematopoietic cells from cytotoxic damage in vitro and in vivo, and to reduce the severity and durati...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(97)00094-4

    authors： McCormack ES,Borzillo GV,Ambrosino C,Mak G,Hamablet L,Qu GY,Haley JD

    更新日期：1997-04-25 00:00:00

  • Relative importance of maternal and embryonic microsomal epoxide hydrolase in 7,12-dimethylbenz[a]anthracene-induced developmental toxicity.

    abstract：:Microsomal epoxide hydrolase (mEH) catalyzes the hydrolysis of epoxide intermediates derived from drugs and environmental chemicals. The response of in vivo (embryo) and in vitro (embryo fibroblast) tests were analyzed using mEH-null and wild-type mice to determine the relative role of maternal and embryonic mEH in th...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(02)00847-x

    authors： Miyata M,Motoki K,Tamura E,Furukawa M,Gonzalez FJ,Yamazoe Y

    更新日期：2002-03-15 00:00:00

  • In vitro drug metabolism and pharmacokinetics of diazepam in cynomolgus monkey hepatocytes during culture for six days.

    abstract：:Diazepam (DZ), N-desmethyl diazepam (NOR) and temazepam (TEM) were used as substrates in drug metabolism studies to characterize the changes in cytochrome P-450 mono-oxygenase pathways in hepatocytes isolated from cynomolgus monkeys, during culture for 6 days. Hepatocytes were incubated with DZ (20 microM), NOR (6 mic...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(89)90547-9

    authors： Seddon T,Lockwood GF,Chenery RJ

    更新日期：1989-08-15 00:00:00

  • Effects of chronic low-level lead exposure on mRNA expression, ADP-ribosylation and photoaffinity labeling with [alpha-32P]guanine triphosphate-gamma-azidoanilide of GTP-binding proteins in neurons isolated from the brain of neonatal and adult rats.

    abstract：:The effects of chronic lead exposure on mRNA expression, ADP-ribosylation and photoaffinity labeling with [alpha-32P]guanine triphosphate-gamma-azidoanilide ([32P]GTP-A) of alpha i or alpha s subunit of G protein were investigated in neurons isolated from the brain of neonatal and adult rats exposed to lead acetate or...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(93)90255-u

    authors： Singh AK

    更新日期：1993-03-09 00:00:00

  • Current status of terpenoids as inflammasome inhibitors.

    abstract：:Increasing evidence supports NLRP3 inflammasome as a new target to control inflammation. Dysregulation of NLRP3 inflammasome has been reported to be involved in the pathogenesis of several human inflammatory diseases. However, no NLRP3 inflammasome inhibitors are available in clinic. Terpenoids are natural products wi...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2019.113739

    authors： Hortelano S,González-Cofrade L,Cuadrado I,de Las Heras B

    更新日期：2020-02-01 00:00:00

  • Prevention of insulin-dependent diabetes mellitus by 2'-deoxycoformycin in the BB Wistar rat.

    abstract：:The effect of the adenosine deaminase (ADA) inhibitor 2'-deoxycoformycin (dCF) on the development of insulin-dependent diabetes mellitus (IDDM) was assessed in the BB Wistar rat. Sixty-one male rats were treated from days 30 to 120 with 0, 0.5, 1.0 or 1.5 mg dCF/kg/week. The incidence of IDDM was 78% in the controls a...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(93)90672-j

    authors： Thliveris JA,Begleiter A,Kobrinsky NL,Verburg L,Dean HJ,Johnston JB

    更新日期：1993-09-14 00:00:00

  • Differential effects of phosphodiesterase inhibitors on accumulation of cyclic AMP in isolated ventricular cardiomyocytes.

    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

    pub_type： 杂志文章

    doi：10.1016/0006-2952(94)00476-3

    authors： Kelso EJ,McDermott BJ,Silke B

    更新日期：1995-02-14 00:00:00

  • Pharmacokinetics relevant to the anti-carcinogenic and anti-tumor activities of glucarate and the synergistic combination of glucarate:retinoid in the rat.

    abstract：:Alone and in synergistic combination with retinoids, dietary glucarate inhibits both the chemical induction and growth of rat mammary tumors. To investigate the pharmacokinetics of glucarate, [14C]glucarate was synthesized, converted to the calcium salt, and administered to rats bearing primary mammary tumors. When gi...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(94)90544-4

    authors： Webb TE,Pham-Nguyen MH,Darby M,Hamme AT 2nd

    更新日期：1994-04-29 00:00:00

  • Enhancement of vincristine- and adriamycin-induced cytotoxicity by verapamil in P388 leukemia and its sublines resistant to vincristine and adriamycin.

    abstract：:A calcium antagonist, verapamil, enhanced the cellular uptake and cytotoxicity of vincristine (VCR) in adriamycin-resistant P388 leukemia (P388/ADM) cells and also enhanced the cellular uptake and cytotoxicity of adriamycin (ADM) in vincristine-resistant P388 leukemia (P388/VCR) and P388/ADM cells. The enhancement of ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90097-1

    authors： Tsuruo T,Iida H,Yamashiro M,Tsukagoshi S,Sakurai Y

    更新日期：1982-10-01 00:00:00