Inhibition of proliferation of human leukaemia 60 cells by diethyl esters of glyoxalase inhibitors in vitro.

abstract：:The multidrug resistance (MDR) phenotype is the major cause of failure of cancer chemotherapy. This phenotype is mainly due to the overexpression of the human MDR1 (hMDR1) gene. Several studies have shown that transcriptional regulation of this gene is unexpectedly complex and is far from being completely understood. ...

journal_title：Biochemical pharmacology

authors： Labialle S,Gayet L,Marthinet E,Rigal D,Baggetto LG

更新日期：2002-09-01 00:00:00

abstract：:The diterpenes andrographolide (I), andrographiside (II) and neoandrographolide (III) isolated from Andrographis paniculata were investigated for their protective effects on hepatotoxicity induced in mice by carbon tetrachloride or tert-butylhydroperoxide (tBHP) intoxication. Pretreatment of mice with the diterpenes (...

journal_title：Biochemical pharmacology

authors： Kapil A,Koul IB,Banerjee SK,Gupta BD

更新日期：1993-07-06 00:00:00

abstract：:trans-Resveratrol is a dietary polyphenolic compound present in grapes, which has been shown to exhibit strong anti-inflammatory, antioxidant, and chemopreventive activities. In this study we have compared the in vitro and in vivo effects of resveratrol on the development of various cell-mediated immune responses, inc...

journal_title：Biochemical pharmacology

authors： Gao X,Deeb D,Media J,Divine G,Jiang H,Chapman RA,Gautam SC

更新日期：2003-12-15 00:00:00

abstract：:We tested the influence of IFNgamma on proteasome activity in parental Hep G2 cells that do not metabolize ethanol, as well as in recombinant Hep G2-derived cells that express either or both alcohol dehydrogenase (ADH) and cytochrome P4502E1 (CYP2E1). IFNgamma treatment increased proteasome activity in VL-17A (ADH(+),...

journal_title：Biochemical pharmacology

authors： Osna NA,Clemens DL,Donohue TM Jr

更新日期：2003-09-01 00:00:00

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

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

更新日期：2008-12-01 00:00:00

abstract：:The ability of the fetus to detoxify transplacental drugs and chemicals can be a critical determinant of teratogenesis and developmental toxicity. Developmentally regulated expression of alpha class glutathione S-transferases (GSTs) is of particular interest, since these isozymes have high activity toward peroxidative...

journal_title：Biochemical pharmacology

authors： Gallagher EP,Gardner JL

更新日期：2002-06-01 00:00:00

abstract：:The beta 2-adrenoceptor agonist, clenbuterol (initially 5 mg/kg), was found to significantly reduce plasma tyrosine and raise brain tryptophan levels (P less than 0.01). By comparison, decreases in plasma tryptophan and increases in brain tyrosine were small and often nonsignificant. Amino acid levels measured in diff...

journal_title：Biochemical pharmacology

authors： Edwards DJ,Sorisio DA,Knopf S

更新日期：1989-09-15 00:00:00

abstract：:In order to study the metabolism of benzo[a]pyrene (BP), it must be dissolved in an organic solvent vehicle for delivery to the tissue. We studied the effects of five organic solvent vehicles, i.e. dimethyl sulfoxide (DMSO), acetone, methanol, ethanol, and ethyl acetate, on benzo[a]pyrene hydroxylase activity and the ...

journal_title：Biochemical pharmacology

authors： Kontir DM,Glance CA,Colby HD,Miles PR

更新日期：1986-08-01 00:00:00

abstract：:8-Chloro-cAMP and 8-chloro-adenosine (8-Cl-Ado) are known to inhibit proliferation of cancer cells by converting 8-Cl-Ado into an ATP analog, 8-chloro-ATP (8-Cl-ATP). Because type II topoisomerases (Topo II) are ATP-dependent, we infer that 8-Cl-Ado exposure might interfere with Topo II activities and DNA metabolism i...

journal_title：Biochemical pharmacology

authors： Yang SY,Jia XZ,Feng LY,Li SY,An GS,Ni JH,Jia HT

更新日期：2009-02-01 00:00:00

abstract：:Several aspects of the effects of zinc on the metabolism of glutathione were examined in the Chinese hamster cell (line CHO) and in three derived sublines which differ in their resistance to the thiol reactive heavy metal cadmium. In the parental CHO cell, which does not induce the synthesis of metallothionein in resp...

journal_title：Biochemical pharmacology

authors： Seagrave J,Tobey RA,Hildebrand CE

更新日期：1983-10-15 00:00:00

abstract：:The metabolism of 2-acetylaminofluorene (AAF) to its six oxidative metabolites has been used to investigate the effect of dexamethasone on cytochrome P-450 activity in cultured rat hepatocytes. In control hepatocytes the metabolism of AAF to its 1-, 5-, 7-, 9- and N-hydroxylated metabolites rapidly declined in culture...

journal_title：Biochemical pharmacology

authors： McManus ME,Edwards AM,Stupans I,Burgess W,Lucas C,Birkett DJ

更新日期：1987-01-15 00:00:00

abstract：:The abilities of liver cytosol fractions from the suncus and Sprague-Dawley (SD) rats to N-acetylate aniline, p-aminobenzoic acid, p-aminosalicylic acid and 2-aminofluorene (AF) were compared. The cytosol from rats N-acetylated these substrates at efficient rates, whereas the cytosol from the suncus did not N-acetylat...

journal_title：Biochemical pharmacology

authors： Nakura H,Itoh S,Kusano H,Ishizone H,Deguchi T,Kamataki T

更新日期：1995-10-12 00:00:00

abstract：:A set of sulfamides designed, synthesized and evaluated against maximal electroshock seizure (MES) and pentilenetetrazol (PTZ) tests with promising results, were tested for their affinity for the benzodiazepine binding site of the GABA(A) receptor. The most active compounds, N,N'-dicyclohexylsulfamide (7) and N,N'-dip...

journal_title：Biochemical pharmacology

authors： Wasowski C,Gavernet L,Barrios IA,Villalba ML,Pastore V,Samaja G,Enrique A,Bruno-Blanch LE,Marder M

更新日期：2012-01-15 00:00:00

abstract：:The effect of dichlorvos (200 mg/kg body weight) with or without nimodipine (6 mg/kg body weight/day for 3 days, starting 1 day prior to the administration of dichlorvos) on calcium homeostasis was studied in the rat brain. The delayed neurotoxic potential of dichlorvos was assessed in terms of neuropathy target ester...

journal_title：Biochemical pharmacology

authors： Choudhary S,Gill KD

更新日期：2001-11-01 00:00:00

abstract：:Reoxygenation of hypoxic (120 min at 37 degrees) rabbit kidney cortical slices in vitro resulted in a rapid increase in lipid peroxidation and phosphatidylinositol hydrolysis. No changes in phosphatidylinositol breakdown occurred during hypoxia or upon reoxygenation in the absence of calcium. Incubation of renal slice...

journal_title：Biochemical pharmacology

authors： Cotterill LA,Gower JD,Clark PK,Fuller BJ,Thorniley MS,Goddard JG,Green CJ

更新日期：1993-05-25 00:00:00

abstract：:The present investigation addressed the role of verapamil for oral pharmacokinetics of morphine-6-beta-glucuronide (M6G). Male Sprague-Dawley rats received 62.5 mg kg(-1) M6G-dihydrate orally w/wo pre-treatment with 70 mg kg(-1) verapamil. Intravenous M6G (3.9 mg kg(-1) ) and oral morphine (52.7 mg kg(-1) morphine-hyd...

journal_title：Biochemical pharmacology

authors： Lötsch J,Sperker B,Kroemer HK,Geisslinger G

更新日期：2002-04-15 00:00:00

abstract：:Inflammatory events are tightly associated with the death caused by Herpes simplex virus 1 (HSV-1) infection of the brain. Heat shock protein 90 (Hsp90) is a molecular chaperone that is stimulated in response to many stressful conditions (e.g., inflammation and hypoxia) and Hsp90 inhibitors are suggested to be potent ...

journal_title：Biochemical pharmacology

authors： Li F,Song X,Su G,Wang Y,Wang Z,Qing S,Jia J,Wang Y,Huang L,Zheng K,Wang Y

更新日期：2019-08-01 00:00:00

abstract：:Polychlorinated biphenyls (PCBs) induce drug metabolism that may lead to the bioactivation of PCBs themselves or alternatively may lead to oxidative events within the cell. The goal of the present study was to determine the influence of congeneric PCBs, selected as substrates for or inducers of drug metabolism, upon h...

journal_title：Biochemical pharmacology

authors： Twaroski TP,O'Brien ML,Robertson LW

更新日期：2001-08-01 00:00:00

abstract：:HOE 731, a substituted thienoimidazole derivative, was studied on [14C] aminopyrine uptake and oxygen consumption in isolated rabbit gastric glands. HOE 731 caused a concentration-dependent inhibition of [14C]aminopyrine uptake during histamine and dbcAMP stimulation. The inhibition during dbcAMP stimulation was in ac...

journal_title：Biochemical pharmacology

authors： Herling AW,Becht M,Lang HJ,Scheunemann KH,Weidmann K,Scholl T,Rippel R

更新日期：1990-10-15 00:00:00

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

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

更新日期：1996-07-12 00:00:00

abstract：:Diabetic retinopathy (DR) is a secondary complication of diabetes. DR can cause irreversible blindness, and its pathogenesis is considered multifactorial. DR can progress from non-proliferative DR to proliferative DR, characterized by retinal neovascularization. The main cause of vision loss in diabetic patients is di...

journal_title：Biochemical pharmacology

authors： Lazzara F,Fidilio A,Platania CBM,Giurdanella G,Salomone S,Leggio GM,Tarallo V,Cicatiello V,De Falco S,Eandi CM,Drago F,Bucolo C

更新日期：2019-10-01 00:00:00

abstract：:9-(2-Phosphonylmethoxyethyl)-N6-cyclopropyl-2,6-diaminopurine (cpr-PMEDAP) is an acyclic nucleotide analog of the [9-(2-phosphonylmethoxyethyl)-] (PME) series containing a cyclopropyl substituent on the N6 position of the 2,6-diaminopurine (DAP) base. Growth inhibition assays in a broad range of tumor cell lines demon...

journal_title：Biochemical pharmacology

authors： Compton ML,Toole JJ,Paborsky LR

更新日期：1999-08-15 00:00:00

abstract：:The Transforming Growth Factor-β (TGF-β) signaling pathway plays a versatile role in diverse physiological and disease conditions. Outcomes of TGF-β signaling are divergent, sometimes even opposite, on cellular functions and disease progression through context-dependent transcriptional programs. For example, TGF-β sig...

journal_title：Biochemical pharmacology

authors： Li X,Feng XH

更新日期：2020-10-01 00:00:00

abstract：:Rat hepatic microsomes catalyzed the formation of two distinct glutathione conjugates of bilirubin dimethylester (DMB). The two conjugates were identical to those isolated from the bile of Gunn rats infused with DMB. The microsomal reaction was dependent on NADPH, oxygen and glutathione and was inhibited by nitrogen a...

journal_title：Biochemical pharmacology

authors： Shore LJ,Mogilevsky WS,Smith PB,Fenselau C,Odell GB

更新日期：1991-10-24 00:00:00

abstract：:The effect of histamine on the release of endogenous noradrenaline and 5-hydroxytryptamine (5-HT) has been examined in slices of rat cerebral cortex. Histamine was found to produce a marked release of both amines from rat cerebral cortex at concentrations between 0.1 and 1 mM. This response to histamine was relatively...

journal_title：Biochemical pharmacology

authors： Young CS,Mason R,Hill SJ

更新日期：1988-07-15 00:00:00

abstract：:Hyperactivated macrophages play a key role in the initiation and perpetuation of mucosal inflammation in Crohn's disease (CD). Increasing evidence suggests that the basic helix-loop-helix (bHLH) repressor Twist1 can suppress activation of nuclear factor-κB (NF-κB) and the subsequent production of TNF-α, which are both...

journal_title：Biochemical pharmacology

authors： Tu T,Yu M,Zhang Y,Shi X,Xu J,Hu J,Gan J,He W,Dong L,Han J,Huang Z,Pan Y,Zhang J

更新日期：2018-09-01 00:00:00

abstract：:The mechanisms by which amiloride and 4,4'-diisothiocyano-2,2'-disulfonic stilbene (DIDS) inhibit hepatic uptake of cholate and taurocholate (TC) were investigated in isolated rat hepatocytes. Amiloride inhibited Na(+)-dependent uptake of cholate and TC only when hepatocytes were preincubated with amiloride, indicatin...

journal_title：Biochemical pharmacology

authors： Anwer MS,Branson AU,Atkinson JM

更新日期：1991-12-11 00:00:00

abstract：:3'-Phosphoadenosine 5'-phosphosulfate (PAPS) is the high-energy "sulfate donor" for reactions catalyzed by sulfotransferase (SULT) enzymes. The strict requirement of SULTs for PAPS suggests that PAPS synthesis might influence the rate of sulfate conjugation. In humans, PAPS is synthesized from ATP and SO(4)(2-) by two...

journal_title：Biochemical pharmacology

authors： Xu ZH,Thomae BA,Eckloff BW,Wieben ED,Weinshilboum RM

更新日期：2003-06-01 00:00:00

abstract：:Retinoic acid (RA) induces HL-60 and THP-1 leukemic cell lines to differentiate into granulocyte-like and monocyte-like cells. Limited data are available concerning the effects of RA on components of the cyclic AMP pathway in human myeloid leukemic cells. We showed previously a decrease in adenylate cyclase activity i...

journal_title：Biochemical pharmacology

authors： de Cremoux P,Zimber A,Calvo F,Lanotte M,Mercken L,Abita JP

更新日期：1991-11-06 00:00:00

abstract：:A new triazinoaminopiperidine derivative, Servier 9788 (S9788), was investigated for its ability to increase Adriamycin (ADR) accumulation and retention in two rodent (P388/ADR and DC-3F/AD) and three human (KB-A1, K562/R and COLO 320DM) cell lines displaying the P-glycoprotein (P-gp)-mediated multidrug resistance (MD...

journal_title：Biochemical pharmacology

authors： Léonce S,Pierré A,Anstett M,Pérez V,Genton A,Bizzari JP,Atassi G

更新日期：1992-11-03 00:00:00