当前位置： SCI文献检索 > BIOCHEMICAL PHARMACOLOGY期刊下所有文献 > Enhancing effect of bromovinyldeoxyuridine on antitumor activity of 5-fluorouracil against adenocarcinoma 755 in mice. Increased therapeutic index and correlation with increased plasma 5-fluorouracil levels.

Enhancing effect of bromovinyldeoxyuridine on antitumor activity of 5-fluorouracil against adenocarcinoma 755 in mice. Increased therapeutic index and correlation with increased plasma 5-fluorouracil levels.

Abstract：

:A marked inhibition of the growth of solid tumor adenocarcinoma 755 was achieved by the combination of 5-fluorouracil (5-FU) with bromovinyldeoxyuridine (BVDU). The therapeutic index (LD50/ED50) for the combination of BVDU plus 5-FU was 8.1 and 3.9 upon intraperitoneal (i.p.) or oral (p.o.) administration, respectively. The therapeutic index of i.p. 5-FU given alone was 2.3, whereas for p.o. 5-FU given alone no therapeutic index could be established because of insufficient activity of the compound. Thus, the therapeutic index of 5-FU increased significantly when combined with BVDU. Pharmacokinetic studies revealed that upon i.p. or p.o. 5-FU administration plasma 5-FU levels rapidly declined, but that, in the combination with BVDU, the plasma clearance of 5-FU, especially following p.o. administration, was slowed down considerably. Antitumor activity of 5-FU correlated with AUC (area under the concentration x time curve), within the plasma 5-FU concentration range from 0.02 to 0.4 microgram/ml.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Iigo M,Araki E,Nakajima Y,Hoshi A,De Clercq E

doi

10.1016/0006-2952(88)90025-1

subject

Has Abstract

pub_date

1988-04-15 00:00:00

pages

1609-13

issue

8

eissn

0006-2952

issn

1873-2968

pii

0006-2952(88)90025-1

journal_volume

37

pub_type

杂志文章

相关文献

BIOCHEMICAL PHARMACOLOGY文献大全
  • On the binding of a 3-alpha-methylated digitoxigenin-glucoside to ouabain receptors in heart muscle homogenate.

    abstract：:3-alpha-Methyl substituted digitoxigenin-3-beta-glucoside (methyl-dtg-gluc) displays unusual features, e.g. a high dissociation rate constant from its binding site leading to rapid reversibility of the inotropic and toxic effects, and a flat dose-response curve attaining higher inotropic maxima thus indicating an incr...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90059-4

    authors： Lüllmann H,Mohr K

    更新日期：1982-08-01 00:00:00

  • Effect of chronic hypoxia on acetaminophen metabolism in the rat.

    abstract：:The effect of chronic hypoxia (10.5% O2 for 8-9 days) on acetaminophen metabolism was studied in vivo or in isolated cell or microsomal systems. Results from in vivo studies with oral administration of acetaminophen showed that in hypoxic rats, the plasma appearance of the drug was delayed and the plasma half-life was...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(91)90285-d

    authors： Aw TY,Shan XQ,Sillau AH,Jones DP

    更新日期：1991-08-08 00:00:00

  • Effect of staurosporine on transcription factor NF-kappaB in human keratinocytes.

    abstract：:Activation of the transcription factor NF-kappaB is known to be important in the regulated expression of a large number of pro-inflammatory genes including interleukin-8 (IL-8). Previously, we showed that the protein kinase inhibitor staurosporine potentiates IL-1-stimulated IL-8 production in human keratinocytes. Mor...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(98)00117-8

    authors： Chabot-Fletcher M,Breton JJ

    更新日期：1998-07-01 00:00:00

  • Gen-27, a newly synthesized flavonoid, inhibits glycolysis and induces cell apoptosis via suppression of hexokinase II in human breast cancer cells.

    abstract：:We have previously reported that Gen-27, a newly synthesized flavonoid, exhibits anticancer effects against human colorectal cancer cells. In this study, we investigated the anticancer effects in human breast cancer cell lines and its underlying mechanisms. We demonstrated that Gen-27 inhibited the growth and prolifer...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2016.11.001

    authors： Tao L,Wei L,Liu Y,Ding Y,Liu X,Zhang X,Wang X,Yao Y,Lu J,Wang Q,Hu R

    更新日期：2017-02-01 00:00:00

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

    abstract：:Hepatic expression of multiple cytochrome P450 genes is suppressed in the livers of rats undergoing an inflammatory response. Nitric oxide (NO) released during inflammation has been implicated in the decreased activities and expression of several cytochrome P450 isozymes. We examined the role of cytokine-mediated NO r...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(97)00226-8

    authors： Sewer MB,Morgan ET

    更新日期：1997-09-15 00:00:00

  • Effect of bepridil on the activity of cytochrome c oxidase in solution and in proteoliposomes.

    abstract：:The interaction between bepridil and mitochondrial cytochrome c oxidase has been studied using the purified enzyme either in aqueous suspensions in the presence of detergents, or embedded into phospholipid vesicles. The investigation, systematically extended to nonactin and valinomycin for comparison, showed that: (a)...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(84)90377-0

    authors： Antonini E,Brunori M,Colosimo A,Sarti P

    更新日期：1984-01-01 00:00:00

  • Anti-allodynic property of flavonoid myricitrin in models of persistent inflammatory and neuropathic pain in mice.

    abstract：:The aim of the present study was to investigate the effects of myricitrin, a flavonoid with anti-inflammatory and antinociceptive action, upon persistent neuropathic and inflammatory pain. The neuropathic pain was caused by a partial ligation (2/3) of the sciatic nerve and the inflammatory pain was induced by an intra...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2006.08.028

    authors： Meotti FC,Missau FC,Ferreira J,Pizzolatti MG,Mizuzaki C,Nogueira CW,Santos AR

    更新日期：2006-12-15 00:00:00

  • Growth state dependent increase of glutathione by homocysteine and other thiols, and homocysteine formation in glutathione depleted mouse cell lines.

    abstract：:Homocysteine has been shown to increase glutathione levels in C3H/10T1/2 Cl 8 cells. The present paper confirms that this increase was specific for non-dividing cells. Several other thiols and disulfides, including cysteamine, mercaptoethanol and dithioerythritol, also increased glutathione, but the specificity for qu...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(90)90046-n

    authors： Djurhuus R,Svardal AM,Ueland PM

    更新日期：1990-02-01 00:00:00

  • Intracellular coupling of prostaglandin inhibition of acid secretion in isolated rabbit gastric parietal cells.

    abstract：:Acid secretion from isolated rabbit gastric parietal cells can be stimulated by gastric secretagogues, histamine (cyclic-AMP pathway) and carbachol (inositol phosphate pathway). Prostaglandins (PG) from E series are potent inhibitors of acid secretion. The intracellular mechanism of this inhibition was examined by usi...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(90)90608-n

    authors： Choquet A,Leonard A,Magous R,Bali JP

    更新日期：1990-06-15 00:00:00

  • Insulin and glucose induced changes in expression level of nucleoside transporters and adenosine transport in rat T lymphocytes.

    abstract：:Adenosine is an endogenous agent exerting potent action on the immune system including regulation of lymphocyte functioning. Impaired T lymphocyte functioning is a common feature of diabetes. The aims of this study were to examine the effects of glucose and insulin on nucleoside transporters (NT) expression level and ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2004.06.020

    authors： Sakowicz M,Szutowicz A,Pawelczyk T

    更新日期：2004-10-01 00:00:00

  • On the G protein-coupling selectivity of the native A2B adenosine receptor.

    abstract：:A2B adenosine receptor (A2BAR) activation induces Gs-dependent cyclic AMP accumulation. However, A2BAR G protein-coupling to other signaling events, e.g. ERK1/2 and calcium, is not well documented. We explored Gi, Gq/11 and Gs coupling in 1321 N1 astrocytoma, HEK293, and T24 bladder cancer cells endogenously expressin...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2017.12.003

    authors： Gao ZG,Inoue A,Jacobson KA

    更新日期：2018-05-01 00:00:00

  • Structure-activity relationships of alkylamines that inhibit rat liver hydroxysteroid sulfotransferase activities in vitro.

    abstract：:Tetraalkylammonium salts having n-propyl to n-amyl side chains inhibited rat liver sulfotransferase (ST) activities toward dehydroepiandrosterone and cortisol, but not ST activity toward 2-naphthol, whereas trialkylamines having ethyl to n-amyl side chains inhibited ST activity toward dehydroepiandrosterone, but not S...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(94)00495-8

    authors： Matsui M,Takahashi M,Miwa Y,Motoyoshi Y,Homma H

    更新日期：1995-03-01 00:00:00

  • Effect of pentylenetetrazol on carbaryl-induced changes in striatal catecholamines.

    abstract：:Administration of pentylenetetrazol (PTZ) (60 mg/kg, s.c.) to normal or carbaryl (200 mg/kg, p.o.) treated adult male albino rats produced characteristic changes in the steady-state levels of striatal dopamine (DA), noradrenaline (NA) and homovanillic acid (HVA) at different time intervals (0.5, 1.0 and 2.0 hr). The e...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(85)90189-3

    authors： Ray SK,Poddar MK

    更新日期：1985-02-15 00:00:00

  • Binding of indapamide to serum proteins and erythrocytes.

    abstract：:The binding of indapamide to isolated serum proteins and erythrocytes was studied in order to understand its blood distribution. In serum, indapamide was mainly bound to alpha 1-acid glycoprotein with a high affinity (K = 73.4/mM), and to albumin and lipoproteins. Indapamide was bound to erythrocytes via a saturable p...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(88)90282-1

    authors： Urien S,Riant P,Renouard A,Coulomb B,Rocher I,Tillement JP

    更新日期：1988-08-01 00:00:00

  • Role of CYP2A5 and 2G1 in acetaminophen metabolism and toxicity in the olfactory mucosa of the Cyp1a2(-/-) mouse.

    abstract：:Acetaminophen (AP) is a widely-used analgesic agent that has been linked to human liver and kidney disease with prolonged or high-dose usage. In rodents, the target organs that are affected include liver, kidney, and the olfactory mucosa. AP toxicity requires cytochrome P450(CYP)-mediated metabolic activation, and the...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(98)00004-5

    authors： Genter MB,Liang HC,Gu J,Ding X,Negishi M,McKinnon RA,Nebert DW

    更新日期：1998-06-01 00:00:00

  • Ascorbic acid: an endogenous inhibitor of isolated Na+,K+-ATPase.

    abstract：:During attempts to isolate and identify an endogenous ligand for the glycoside binding sites on Na+,K+-ATPase, bovine adrenal glands were found to contain a potent inhibitor of isolated Na+,K+-ATPase. The inhibitory principle was extracted from adrenal cortex, following homogenization in NaHCO3 solution and separation...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(85)90537-4

    authors： Ng YC,Akera T,Han CS,Braselton WE,Kennedy RH,Temma K,Brody TM,Sato PH

    更新日期：1985-07-15 00:00:00

  • Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents.

    abstract：:Four pseudo-symmetrical tamoxifen derivatives, RID-B (13), RID-C (14), RID-D (15), and bis(dimethylaminophenetole) (16), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of these pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 13 ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2007.11.005

    authors： Shiina I,Sano Y,Nakata K,Kikuchi T,Sasaki A,Ikekita M,Nagahara Y,Hasome Y,Yamori T,Yamazaki K

    更新日期：2008-03-01 00:00:00

  • Endothelin receptors in adult human and swine isolated ventricular cardiomyocytes.

    abstract：:The present study aimed to investigate endothelin-1 (ET-1) receptors in human and swine cardiomyocytes with binding studies using ET(A) and ET(B) selective receptor antagonists (BMS-182874 and BQ-788, respectively). Cell distribution of mRNA expression for ET(A) and ET(B) subtypes was investigated by in situ hybridiza...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00081-7

    authors： Modesti PA,Vanni S,Paniccia R,Perna A,Maccherini M,Lisi G,Sani G,Neri Serneri GG

    更新日期：1999-07-15 00:00:00

  • Protective effect of interleukin-6 against the death of PC12 cells caused by serum deprivation or by the addition of a calcium ionophore.

    abstract：:Interleukin-6 (IL-6) is known to differentiate the rat pheochromocytoma cell line PC12 to neuron-like cells. We examined the effect of IL-6 on the death of PC12 cells. IL-6 significantly blocked the death of PC12 cells by serum deprivation. The protective effect of IL-6 was increased by preincubation of PC12 with IL-6...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(96)00422-4

    authors： Umegaki H,Yamada K,Naito M,Kameyama T,Iguchi A,Nabeshima T

    更新日期：1996-09-27 00:00:00

  • Src-family kinase inhibitors block early steps of caveolin-1-enhanced lung metastasis by melanoma cells.

    abstract：:In advanced stages of cancer disease, caveolin-1 (CAV1) expression increases and correlates with increased migratory and invasive capacity of the respective tumor cells. Previous findings from our laboratory revealed that specific ECM-integrin interactions and tyrosine-14 phosphorylation of CAV1 are required for CAV1-...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2020.113941

    authors： Ortiz R,Díaz J,Díaz-Valdivia N,Martínez S,Simón L,Contreras P,Lobos-González L,Guerrero S,Leyton L,Quest AFG

    更新日期：2020-07-01 00:00:00

  • Molecular mechanism of L-DNase II activation and function as a molecular switch in apoptosis.

    abstract：:The discovery of caspase activation counts as one of the most important finds in the biochemistry of apoptosis. However, targeted disruption of caspases does not impair every type of apoptosis. Other proteases can replace caspases and several so called "caspase independent" pathways are now described. Here we review o...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2008.07.039

    authors： Torriglia A,Leprêtre C,Padrón-Barthe L,Chahory S,Martin E

    更新日期：2008-12-01 00:00:00

  • Modification of the plasma clearance and liver uptake of steroid ester-conjugated oligodeoxynucleotides by association with (lactosylated) low-density lipoprotein.

    abstract：:Low-density lipoprotein (LDL) has been proposed as carrier for the selective delivery of anticancer drugs to tumor cells. We reported earlier the association of several lipidic steroid-conjugated anticancer oligodeoxynucleotides (ODNs) with LDL. In the present study, we determined the stability of these complexes. Whe...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(00)00243-4

    authors： Rump ET,de Vrueh RL,Manoharan M,Waarlo IH,van Veghel R,Biessen EA,van Berkel TJ,Bijsterbosch MK

    更新日期：2000-06-01 00:00:00

  • Metabolism of protocatechuic acid influences fatty acid oxidation in rat heart: new anti-angina mechanism implication.

    abstract：:Protocatechuic acid (PA), a structurally typical phenolic acid in danshen, shows anti-angina efficacy. But until now, besides scavenging of oxygen free radicals, the understanding of its anti-angina mechanism has been limited. In our study, based on a novel metabolic route of PA identified in rat heart and its influen...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2008.11.029

    authors： Cao YG,Zhang L,Ma C,Chang BB,Chen YC,Tang YQ,Liu XD,Liu XQ

    更新日期：2009-03-15 00:00:00

  • Eicosapentaenoic acid as a modulator of inflammation. Effect on prostaglandin and leukotriene synthesis.

    abstract：:Products derived from arachidonic acid (AA) via both the cyclo-oxygenase and lipoxygenase pathways play a role in inflammation: prostaglandins (PGs), particularly PGE2, contribute to the formation of oedema, erythema and hyperalgesia whereas leukotriene B4 (LTB4), a product of the 5' lipoxygenase, may modulate the rec...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(86)90246-7

    authors： Terano T,Salmon JA,Higgs GA,Moncada S

    更新日期：1986-03-01 00:00:00

  • In vivo and in vitro effects of cyclosporin A on glucose transport by soleus muscles of mice.

    abstract：:The effect of cyclosporin A (CyA) on 2-deoxyglucose (2DG) uptake by soleus muscles of ICR mice was studied in vivo and in vitro. The basal and insulin-stimulated uptakes of 2DG by the muscles as well as the plasma insulin level were significantly decreased by the in vivo treatment of mice with 20 mg/kg/day of CyA for ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(92)90202-t

    authors： Ikeuchi M,Kida K,Goto Y,Kaino Y,Matsuda H

    更新日期：1992-04-01 00:00:00

  • Inhibition of bacterial cell division protein FtsZ by cinnamaldehyde.

    abstract：:Cinnamaldehyde is a natural product from spices that inhibits cell separation in Bacillus cereus. Cell division is regulated by FtsZ, a prokaryotic homolog of tubulin. FtsZ assembles into the Z-ring at the site of cell division. Here, we report the effect of cinnamaldehyde on FtsZ and hence on the cell division appara...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2007.06.029

    authors： Domadia P,Swarup S,Bhunia A,Sivaraman J,Dasgupta D

    更新日期：2007-09-15 00:00:00

  • Zardaverine as a selective inhibitor of phosphodiesterase isozymes.

    abstract：:The pyridazinone derivative zardaverine has recently been introduced as a potent bronchodilator in vivo and in vitro. In addition, zardaverine exerts a positive inotropic action on heart muscle in vitro. The actions of zardaverine are thought to be mediated via inhibition of phosphodiesterase (PDE) activity. Recent da...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(91)90694-z

    authors： Schudt C,Winder S,Müller B,Ukena D

    更新日期：1991-06-21 00:00:00

  • Tumor acidity, ion trapping and chemotherapeutics. I. Acid pH affects the distribution of chemotherapeutic agents in vitro.

    abstract：:Resistance to anti-cancer chemotherapies often leads to regional failure, and can be caused by biochemical and/or physiological mechanisms. Biochemical mechanisms include the overexpression of resistance-conferring proteins. In contrast, physiological resistance involves the tumor microenvironment, and can be caused b...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(03)00467-2

    authors： Mahoney BP,Raghunand N,Baggett B,Gillies RJ

    更新日期：2003-10-01 00:00:00

  • 5-Substituted-2,2'-anhydrouridines, potent inhibitors of uridine phosphorylase.

    abstract：:5-Substituted-2,2'-anhydrouridines are a new class of competitive inhibitors of uridine phosphorylase. The most potent member of the series is 2,2'-anhydro-5-ethyluridine with an apparent Ki value of 25 nM. These compounds are selective inhibitors of uridine phosphorylase and have no effect on thymidine phosphorylase....

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(85)90643-4

    authors： Veres Z,Szabolcs A,Szinai I,Dénes G,Kajtár-Peredy M,Otvös L

    更新日期：1985-05-15 00:00:00

  • Characterization of beta 1- and beta 2-adrenoceptors in rat skeletal muscles.

    abstract：:Binding studies with (-)-[125I]cyanopindolol (ICYP) were conducted to characterize beta-adrenoceptors in plantaris and soleus muscles of rats (male, 250-300 g). The distribution of beta 1- and beta 2-adrenoceptors in different muscle fiber types, identified in serial sections by succinic dehydrogenase (SDH) staining, ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(91)90516-8

    authors： Kim YS,Sainz RD,Molenaar P,Summers RJ

    更新日期：1991-10-09 00:00:00