The influence of ebselen on the toxicity of cisplatin in LLC-PK1 cells.


:LLC-PK1 cells have been used as an in vitro model to study the nephrotoxicity of the antitumor drug cisplatin. A concentration-dependent cytotoxicity of cisplatin, measured as lactate dehydrogenase leakage and amount of protein remaining attached to the culture plate, was observed. At a cisplatin concentration of 0.4 mM cell viability was reduced to 21% after 72 hr. Ebselen, a seleno-organic compound capable of forming selenol intermediates through reaction with thiols, was found to protect LLC-PK1 cells against cisplatin-induced toxicity at low concentrations (5-15 microM). The ebselen-induced protection against cisplatin toxicity in this in vitro test system apparently correlates well with a similar protection previously observed in vivo in mice and rats.


Biochem Pharmacol


Biochemical pharmacology


Baldew GS,Boymans AP,Mol JG,Vermeulen NP




Has Abstract


1992-07-22 00:00:00














  • Redox modulation of the DNA damage response.

    abstract::Lesions to DNA trigger the DNA-damage response (DDR), a complex, multi-branched cell-intrinsic process targeted to DNA repair, or elimination of the damaged cells by apoptosis. DDR aims at reducing permanence of mutated cells, decreasing the risk of tumor development: the more stringent the response, the lower the lik...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Caputo F,Vegliante R,Ghibelli L

    更新日期:2012-11-15 00:00:00

  • L-carnitine effect on halothane-treated mitochondria.

    abstract::Addition of halothane to the incubation medium is shown to lower respiratory control and transmembrane potential and to increase ATPase activity in isolated rat liver mitochondria. Evidence is presented that L-carnitine is able to substantially decrease the negative effects of halothane on the energy-linked processes ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Toninello A,Branca D,Scutari G,Siliprandi N,Vincenti E,Giron G

    更新日期:1986-11-15 00:00:00

  • Measurement of affective state during chronic nicotine treatment and withdrawal by affective taste reactivity in mice: the role of endocannabinoids.

    abstract::Despite tobacco being highly addictive, it is unclear if nicotine has significant affective properties. To address this, we studied taste reactions to gustatory stimuli, palatable sucrose and unpalatable quinine, which are believed to reflect ongoing affective state. Taste reactivity was assessed during chronic nicoti...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wing VC,Cagniard B,Murphy NP,Shoaib M

    更新日期:2009-10-01 00:00:00

  • New molecular targets for the treatment of osteoarthritis.

    abstract::Osteoarthritis (OA) is a chronic degenerative joint disorder characterized by destruction of the articular cartilage, subchondral bone alterations and synovitis. Current treatments are focused on symptomatic relief but they lack efficacy to control the progression of this disease which is a leading cause of disability...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Alcaraz MJ,Megías J,García-Arnandis I,Clérigues V,Guillén MI

    更新日期:2010-07-01 00:00:00

  • The possible involvement of the phospholipid phase of membranes in mediating the effects of verapamil on Ca2+ transport.

    abstract::The effect of verapamil in a model system of A23187-induced Ca2+-uptake into liposomes was studied. This was done in order to separate the effects of verapamil on the lipid phase of membranes from its effects on membraneous proteins. In the absence of A23187, the liposomes exhibited a very low Ca2+ permeability, which...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Erdreich A,Rahamimoff H

    更新日期:1987-06-01 00:00:00

  • Intestinal absorption of S-nitrosothiols: Permeability and transport mechanisms.

    abstract::S-Nitrosothiols, a class of NO donors, demonstrate potential benefits for cardiovascular diseases. Drugs for such chronic diseases require long term administration preferentially through the oral route. However, the absorption of S-nitrosothiols by the intestine, which is the first limiting barrier for their vascular ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Bonetti J,Zhou Y,Parent M,Clarot I,Yu H,Fries-Raeth I,Leroy P,Lartaud I,Gaucher C

    更新日期:2018-09-01 00:00:00

  • Studies on the activation of rat liver microsomal glutathione transferase in isolated hepatocytes.

    abstract::The mechanism of activation of microsomal glutathione transferase in isolated liver cells by diisapropylidene acetone (phorone) was investigated. Phorone (1 mM) causes a time-dependent increase (up to 2.6-fold) in the glutathione transferase activity of microsomes isolated from treated hepatocytes. Since phorone react...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lundqvist G,Morgenstern R

    更新日期:1992-01-22 00:00:00

  • Involvement of the macrolide antibiotic inducible cytochrome P-450 LM3c in the metabolism of midazolam by microsomal fractions prepared from rabbit liver.

    abstract::This report characterizes the cytochrome P-450 isozyme involved in midazolam metabolism. This study was undertaken into liver microsomal fractions prepared from untreated rabbits or animals treated with drugs known to specifically induce various cytochrome P-450 isozymes such as form LM2 by phenobarbital, LM4 and LM6 ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Fabre G,Crevat-Pisano P,Dragna S,Covo J,Barra Y,Cano JP

    更新日期:1988-05-15 00:00:00

  • Human ATP-Binding Cassette transporters ABCB1 and ABCG2 confer resistance to CUDC-101, a multi-acting inhibitor of histone deacetylase, epidermal growth factor receptor and human epidermal growth factor receptor 2.

    abstract::CUDC-101 is the first small-molecule inhibitor designed to simultaneously inhibit epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2) and histone deacetylase (HDAC) in cancer cells. Recently, in its first in human phase I study, CUDC-101 showed promising single agent activity again...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wu CP,Hsiao SH,Su CY,Luo SY,Li YQ,Huang YH,Hsieh CH,Huang CW

    更新日期:2014-12-15 00:00:00

  • A novel steroidal inhibitor of estrogen-related receptor alpha (ERR alpha).

    abstract::The orphan nuclear receptor estrogen-related receptor alpha (ERRalpha) has been implicated in the development of various human malignancies, including breast, prostate, ovary, and colon cancer. ERRalpha, bound to a co-activator protein (e.g., peroxisome proliferator receptor gamma co-activator-1alpha, PGC-1alpha), reg...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Duellman SJ,Calaoagan JM,Sato BG,Fine R,Klebansky B,Chao WR,Hobbs P,Collins N,Sambucetti L,Laderoute KR

    更新日期:2010-09-15 00:00:00

  • The effect of thiopurine drugs on DNA methylation in relation to TPMT expression.

    abstract::The thiopurine drugs 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) are well-established agents for the treatment of leukaemia but their main modes of action are controversial. Thiopurine methyltransferase (TPMT) metabolises thiopurine drugs and influences their cytotoxic activity. TPMT, like DNA methyltransferases ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hogarth LA,Redfern CP,Teodoridis JM,Hall AG,Anderson H,Case MC,Coulthard SA

    更新日期:2008-10-15 00:00:00

  • EMMPRIN-mediated induction of uterine and vascular matrix metalloproteinases during pregnancy and in response to estrogen and progesterone.

    abstract::Pregnancy is associated with uteroplacental and vascular remodeling in order to adapt for the growing fetus and the hemodynamic changes in the maternal circulation. We have previously shown upregulation of uterine matrix metalloproteinases (MMPs) during pregnancy. Whether pregnancy-associated changes in MMPs are local...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Dang Y,Li W,Tran V,Khalil RA

    更新日期:2013-09-15 00:00:00

  • Conversion of N-hydroxyamphetamine to phenylacetone oxime by rat liver microsomes.

    abstract::These in vitro studies indicate that N-oxidation of N-hydroxyamphetamine (NOHA) by rat liver homogenates yields phenylacetone oxime (PAOx) as the major metabolite. This oxidation was NADPH and oxygen dependent but was not appreciably increased in microsomes from phenobarbital-pretreated animals. The addition to micros...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Matsumoto RM,Cho AK

    更新日期:1982-01-01 00:00:00

  • A1 adenosine receptor-induced phosphorylation and modulation of transglutaminase 2 activity in H9c2 cells: A role in cell survival.

    abstract::The regulation of tissue transglutaminase (TG2) activity by the GPCR family is poorly understood. In this study, we investigated the modulation of TG2 activity by the A1 adenosine receptor in cardiomyocyte-like H9c2 cells. H9c2 cells were lysed following stimulation with the A1 adenosine receptor agonist N(6)-cyclopen...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Vyas FS,Hargreaves AJ,Bonner PL,Boocock DJ,Coveney C,Dickenson JM

    更新日期:2016-05-01 00:00:00

  • Electrochemistry of flavonoids. Relationships between redox potentials, inhibition of mitochondrial respiration, and production of oxygen radicals by flavonoids.

    abstract::We have investigated the redox behavior of a series of structurally related flavonoids employing cyclic voltammetry under physiological conditions. The flavonoids that auto-oxidized and produced oxygen radicals had oxidation potentials (E 1/2) significantly lower [-30 to +60 mV vs (SCE)] than those that did not underg...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hodnick WF,Milosavljević EB,Nelson JH,Pardini RS

    更新日期:1988-07-01 00:00:00

  • Glipentide and glucose metabolism in isolated rat hepatocytes.

    abstract::Glipentide, a second generation sulfonylurea, raised the cellular concentration of fructose 2,6-bisphosphate in isolated rat hepatocytes. Parallel to accumulating this regulatory metabolite, glipentide inhibited basal gluconeogenesis and increased the rate of L-lactate production, as well as the metabolic flux through...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: López-Alarcón L,Berbil-Bautista PR,Guijarro C,Felíu JE

    更新日期:1988-08-15 00:00:00

  • Structural requirements of Dictyostelium differentiation-inducing factors for their stalk-cell-inducing activity in Dictyostelium cells and anti-proliferative activity in K562 human leukemic cells.

    abstract::The differentiation-inducing factor-1 (DIF-1) is a lipophilic signal molecule (chlorinated alkylphenone) that induces stalk-cell differentiation in the cellular slime mould Dictyostelium discoideum. It has also been shown that DIF-1 and its derivative (DIF-3) suppress cell growth in mammalian tumor cells. In the prese...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gokan N,Kikuchi H,Nakamura K,Oshima Y,Hosaka K,Kubohara Y

    更新日期:2005-09-01 00:00:00

  • Testing double mutants of the enzyme nitroreductase for enhanced cell sensitisation to prodrugs: effects of combining beneficial single mutations.

    abstract::Prodrug activation gene therapy for cancer involves expressing prodrug-activating enzymes in tumour cells, so they can be selectively killed by systemically administered prodrug. For example, Escherichia colinfsB nitroreductase (E.C., sensitises cells to the prodrug CB1954 (5-[aziridin-1-yl]-2,4-dinitro...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Jaberipour M,Vass SO,Guise CP,Grove JI,Knox RJ,Hu L,Hyde EI,Searle PF

    更新日期:2010-01-15 00:00:00

  • Comparison of the inducing effect of dehydroepiandrosterone on hepatic peroxisome proliferation-associated enzymes in several rodent species. A short-term administration study.

    abstract::The in-vivo effect of dehydroepiandrosterone (DHEA) on hepatic enzyme activities of rats, mice, hamsters and guinea pigs was investigated. After DHEA treatment (300 mg/kg body weight, per os, 14 days), the activities of peroxisomal beta-oxidation, catalase, carnitine acetyltransferase, carnitine palmitoyltransferase, ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sakuma M,Yamada J,Suga T

    更新日期:1992-03-17 00:00:00

  • Inactivation of creatine kinase by Adriamycin during interaction with horseradish peroxidase.

    abstract::Oxidative damage of creatine kinase (CK) induced by Adriamycin((R)) (ADM) with peroxidase was investigated using horseradish peroxidase (HRP). ADM oxidatively inactivated CK during its interaction with HRP in the presence of H(2)O(2) (HRP-H(2)O(2)). The red color of ADM was lost during oxidation by HRP-H(2)O(2). Addin...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Miura T,Muraoka S,Fujimoto Y

    更新日期:2000-07-01 00:00:00

  • Differential sensitivity of phosphoinositide and cyclic GMP responses to short-term regulation by a muscarinic agonist in mouse neuroblastoma cells. Correlation with down-regulation of cell surface receptors.

    abstract::Short-term agonist-induced loss of cell surface muscarinic receptors and desensitization of receptor-mediated cyclic GMP (cGMP) formation and phosphoinositide hydrolysis were examined in mouse neuroblastoma cells (clone N1E-115) in suspension. This treatment resulted in a time-dependent reduction of approximately 40% ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Cioffi CL,el-Fakahany EE

    更新日期:1989-06-01 00:00:00

  • In vitro and in vivo inhibition by benserazide of clorgyline-resistant amine oxidases in rat cardiovascular tissues.

    abstract::Bernserazide (D,L-serine 2-[2,3,4-trihydroxybenzyl]-hydrazide) as been shown to inhibit the clorgyline-resistant amine oxidase (CRAO) activities which metabolize benzylamine in homogenates of rat aorta, heart and brown adipose tissue. In vitro studies showed a concentration- and time-dependent inhibition of CRAO in he...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lyles GA,Callingham BA

    更新日期:1982-04-01 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


    authors: Yu PH,Davis BA,Deng Y

    更新日期:2001-03-15 00:00:00

  • Celecoxib transiently inhibits cellular protein synthesis.

    abstract::To uncover the full spectrum of its pharmacological activities, the selective COX-2 inhibitor celecoxib is routinely being used at concentrations of up to 100 microM in cell culture. At these elevated concentrations, several COX-2-independent effects were identified, although many details of these events have remained...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Pyrko P,Kardosh A,Schönthal AH

    更新日期:2008-01-15 00:00:00

  • Inorganic polyphosphate protects against lipopolysaccharide-induced lethality and tissue injury through regulation of macrophage recruitment.

    abstract::Sepsis is an etiologically complex and often fatal inflammatory process involving a multitude of cytokine signaling pathways. Tumor necrosis factor α (TNFα) acts as a central regulator of the acute-phase inflammatory response by recruiting immune cells, including circulating monocyte/macrophages, to sites of infection...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Terashima-Hasegawa M,Ashino T,Kawazoe Y,Shiba T,Manabe A,Numazawa S

    更新日期:2019-01-01 00:00:00

  • Antitumor 1-nitroacridine derivative C-1748, induces apoptosis, necrosis or senescence in human colon carcinoma HCT8 and HT29 cells.

    abstract::C-1748 is a DNA-binding agent with potent antitumor activity, especially towards prostate and colon carcinoma xenografts in mice. Here, we elucidated the nature of cellular response of human colon carcinoma HCT8 and HT29 cells to C-1748 treatment, at biologically relevant concentrations (EC(90) and their multiplicity)...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Augustin E,Moś-Rompa A,Nowak-Ziatyk D,Konopa J

    更新日期:2010-05-01 00:00:00

  • Prodrug research: futile or fertile?

    abstract::The objective of this Commentary is to help clarify and illustrate what prodrugs are, what they are not, which benefits they can offer, and what their limits are. To this end, a number of criteria of classification and evaluation are presented. This is followed by a discussion of the pharmaceutical, pharmacokinetic an...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Testa B

    更新日期:2004-12-01 00:00:00

  • Modulatory effect of 4 beta-phorbol 12-myristate 13-acetate (PMA) on carbachol-induced Ca2+ mobilization in rat parotid acinar cells.

    abstract::Treatment of rat parotid acinar cells with 4 beta-phorbol 12-myristate 13-acetate (PMA) significantly inhibited an increase in cytosolic free Ca2+ concentration ([Ca2+]i) induced by carbachol (CCh), a muscarinic agonist. The CCh-induced increase in [Ca2+]i was also inhibited by another active phorbol ester, 4 beta-pho...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Tojyo Y,Tanimura A,Matsumoto Y

    更新日期:1994-06-01 00:00:00

  • Molecular pharmacology of endothelin converting enzymes.

    abstract::A critical processing step in endothelin biosynthesis is the conversion of the intermediate "big endothelin" to its biologically active product catalysed by endothelin converting enzyme (ECE). In this commentary we discuss critically the cellular location, structure, and activity of the isoforms of ECE. The current ev...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Turner AJ,Murphy LJ

    更新日期:1996-01-26 00:00:00

  • Recovery after hypoglycemic brain injury. Action of some biological substances on the cerebral metabolism.

    abstract::In artificially ventilated beagle dogs a severe hypoglycemic condition was induced by insulin injection, while the posthypoglycemic recovery was induced by glucose treatment at the end of a 20-min period of spontaneous electroencephalographic silence. The motor area of the cerebral cortex was analyzed for glycolytic m...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Benzi G,Gorini A,Dossena M,Taglietti M,Fulle D,Pastoris O

    更新日期:1983-03-15 00:00:00