DNA-DNA interstrand crosslinking by dimethyanesulphonic acid esters. Correlation with cytotoxicity and antitumour activity in the Yoshida lymphosarcoma model and relationship to chain length.

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

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

更新日期：2004-09-15 00:00:00

abstract：:We have previously found that repeated exposure to heroin reduces liver synthesis of morphine-3-glucuronide (M3G) and increases the production of morphine-6-glucuronide (M6G), which normally is not formed in the rat. By contrast repeated exposure to naltrexone does not activate M6G synthesis but increases the V(max) o...

journal_title：Biochemical pharmacology

authors： Antonilli L,Brusadin V,Milella MS,Sobrero F,Badiani A,Nencini P

更新日期：2008-09-01 00:00:00

abstract：:Dimebolin (Dimebon), is a non-selective antihistamine approved in Russia for the treatment of allergy. Recently, this drug has been shown to be neuroprotective in cellular models of Alzheimer's disease and Huntington's disease, and to preserve cognitive function when chronically administered to AF64A lesioned rats. In...

journal_title：Biochemical pharmacology

authors： Schaffhauser H,Mathiasen JR,Dicamillo A,Huffman MJ,Lu LD,McKenna BA,Qian J,Marino MJ

更新日期：2009-10-15 00:00:00

abstract：:A 4',5'-unsaturated 5'-fluoroadenosine inhibitor of S-adenosyl-L-homocysteine hydrolase (SAH hydrolase; EC 3.3.1.1), MDL 28842, was found to inhibit markedly the growth of Plasmodium falciparum in vitro and Plasmodium berghei in mice. Inhibition of P. berghei growth was associated with a large increase in the concentr...

journal_title：Biochemical pharmacology

authors： Bitonti AJ,Baumann RJ,Jarvi ET,McCarthy JR,McCann PP

更新日期：1990-08-01 00:00:00

abstract：:The protein tyrosine kinase (PTK) inhibitor genistein has been demonstrated to inhibit platelet-activating factor-stimulated prostaglandin E2 (PGE2) production in lipopolysaccharide (LPS)-primed P388D1 macrophage-like cells (Glaser et al., J Biol Chem 265: 8658-8664, 1990). Therefore, the role of PTK in eicosanoid bio...

journal_title：Biochemical pharmacology

authors： Glaser KB,Sung A,Bauer J,Weichman BM

更新日期：1993-02-09 00:00:00

abstract：:In this study, using a combination of immunological and enzymatic characterizations, we compared the forms of cytochrome P-450 induced by ethanol and glutethimide in primary cultures of chicken embryo hepatocytes. Recently we purified a cytochrome P-450 of 50K molecular weight from chicken embryo liver using glutethim...

journal_title：Biochemical pharmacology

authors： Sinclair JF,Wood SG,Smith EL,Sinclair PR,Koop DR

更新日期：1989-02-15 00:00:00

abstract：:Agents that inhibit hepatic cholesterol biosynthesis reduce circulating cholesterol levels in experimental animals and humans, and may be of pharmacological importance in the prevention of atherosclerosis. Azalanstat (RS-21607), a synthetic imidazole, has been shown to inhibit cholesterol synthesis in HepG2 cells, hum...

journal_title：Biochemical pharmacology

authors： Burton PM,Swinney DC,Heller R,Dunlap B,Chiou M,Malonzo E,Haller J,Walker KA,Salari A,Murakami S

更新日期：1995-08-08 00:00:00

abstract：:Aminoglycoside antibiotics induce a lysosomal phospholipidosis in kidney proximal tubules after conventional therapy in animals and man. We have previously demonstrated that these drugs bind to negatively charged phospholipid bilayers at acid pH and inhibit the activity of lysosomal acid phospholipases in vitro and in...

journal_title：Biochemical pharmacology

authors： Brasseur R,Carlier MB,Laurent G,Claes PJ,Vanderhaeghe HJ,Tulkens PM,Ruysschaert JM

更新日期：1985-04-01 00:00:00

abstract：:We employed both [5-3H] ara-C and ([2-14C] ara-C labeled L1210 DNA for analysis following exposure to alkali under various conditions. The results demonstrated that the tritium label on C5 of ara-C molecules incorporated in DNA was exchanged with water under alkaline conditions and, therefore, radioactivity was subseq...

journal_title：Biochemical pharmacology

authors： Major PP,Egan EM,Herrick D,Kufe DW

更新日期：1982-03-01 00:00:00

abstract：:Superoxide radicals have been implicated in the pathogenesis of aging, cataract, ischemia-reperfusion, cancer and inflammatory diseases. In the present work, we found that deferiprone (L1), an iron-chelating drug, and dietary dihydroxycinnamic acids (catechols) were much more effective at protecting isolated rat hepat...

journal_title：Biochemical pharmacology

authors： Moridani MY,O'Brien PJ

更新日期：2001-12-15 00:00:00

abstract：:Human CYP2E1 is one of the pharmacologically and toxicologically important cytochrome P450 isoforms. Earlier studies have reported that the CYP2E1 expression is extensively regulated by post-transcriptional and post-translational mechanisms, but the molecular basis remains unclear. In the present study, we examined th...

journal_title：Biochemical pharmacology

authors： Mohri T,Nakajima M,Fukami T,Takamiya M,Aoki Y,Yokoi T

更新日期：2010-04-01 00:00:00

abstract：:The deamination of 5-hydroxytryptamine, tryptamine and benzylamine by porcine dental pulp membrane preparations is brought about not only by monoamine oxidase, but also by a clorgyline (and deprenyl) resistant), semicarbazide sensitive enzyme. The semicarbazide sensitive enzyme was also inhibited by aminoguanidine, hy...

journal_title：Biochemical pharmacology

authors： Norqvist A,Oreland L,Fowler CJ

更新日期：1982-09-01 00:00:00

abstract：:Two resistant K562 sublines have been developed by treatment with AZQ (2,5-bis(carboethoxyamino)-3,6-diaziridinyl-1,4-benzoquinone) and BZQ (2,5-bis(2-hydroxyethylamino)-3,6-diaziridinyl-1,4-benzoquinone). The ID50 values of for AZQ on K562, the AZQ-resistant sublines (AZQR) and the BZQ-resistant sublines (BZQR) were ...

journal_title：Biochemical pharmacology

authors： Ward TH,Haran MS,Whittaker D,Watson AJ,Howard TD,Butler J

更新日期：1995-08-08 00:00:00

abstract：:This study was designed to investigate the effects of rhein, the active metabolite of diacerhein, on the metabolic functions of human chondrocytes cultured in alginate beads. Enzymatically isolated osteoarthritic (OA) chondrocytes were cultured in alginate beads in a well-defined culture medium for 12 days. Rhein was ...

journal_title：Biochemical pharmacology

authors： Sanchez C,Mathy-Hartert M,Deberg MA,Ficheux H,Reginster JY,Henrotin YE

更新日期：2003-02-01 00:00:00

abstract：:Endothelins exert their physiological effects through interaction with cell surface receptors that are members of the G-protein-coupled receptor family. The endothelin receptor subtype B (ET(B) receptor) is abundantly expressed in rat cerebellum. Since agonist binding to G-protein-coupled receptors may be modulated by...

journal_title：Biochemical pharmacology

authors： Ceccarelli F,Giusti L,Bigini G,Costa B,Grillotti D,Fiumalbi E,Lucacchini A,Mazzoni MR

更新日期：2001-09-01 00:00:00

abstract：:N-[5-[N-(3,4-Dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N- methylamino]-2-thenoyl]-L-glutamic acid (ZD1694) is a folate-based thymidylate synthase (TS; EC 2.1.1.45) inhibitor. Metabolism to higher chain length polyglutamates is essential for its optimal cytotoxic effect. A ZD1694-resistant (300-fold) human ileocecal...

journal_title：Biochemical pharmacology

authors： Lu K,Yin MB,McGuire JJ,Bonmassar E,Rustum YM

更新日期：1995-07-31 00:00:00

abstract：:The phenolic glucoside gastrodin, a main constituent of a Chinese traditional herbal medicine, has been known to display several biological and pharmacological properties. However, the role and precise molecular mechanisms explaining how gastrodin suppresses the inflammatory response in septic cardiac dysfunction are ...

journal_title：Biochemical pharmacology

authors： Yang P,Han Y,Gui L,Sun J,Chen YL,Song R,Guo JZ,Xie YN,Lu D,Sun L

更新日期：2013-04-15 00:00:00

abstract：:Cisplatin is a potent chemotherapeutic drug widely used for the treatment of human cancer. However, its efficacy against hepatocellular carcinoma (HCC) is poor for reasons that remain unclear. We show here that prothymosin-alpha (PTMA) is overexpressed in HCC cell lines. Silencing PTMA using short-hairpin RNA sensitiz...

journal_title：Biochemical pharmacology

authors： Lin YT,Liu YC,Chao CC

更新日期：2016-12-15 00:00:00

abstract：:Oridonin is a diterpene compound that regulates the activity of PPAR-γ (peroxisome proliferator-activated receptor gamma) transcription factor. Cumulative evidence indicates that AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid)-type glutamate receptors (AMPARs) play an important role in the treatment of de...

journal_title：Biochemical pharmacology

authors： Liu P,Du J

更新日期：2020-10-01 00:00:00

abstract：:Astroglia provide essential metabolic and neurotropic support to cells within the CNS and participate in the cellular immune response with microglia/macrophages following activation by the pro-inflammatory cytokine IFN-gamma. Activation of glial cells results in local oxidative stress and induction of a number of prot...

journal_title：Biochemical pharmacology

authors： Grant R,Kapoor V

更新日期：2003-09-15 00:00:00

abstract：:Adult hepatocytes from rat and man were maintained for 2 weeks between two gel layers in a sandwich configuration to study the influence of this culture technique on the preservation of basal activities of xenobiotic-metabolizing phase I and phase II enzymes. The response of these enzyme activities to an enzyme induce...

journal_title：Biochemical pharmacology

authors： Kern A,Bader A,Pichlmayr R,Sewing KF

更新日期：1997-10-01 00:00:00

abstract：:The concentrations of dopamine (DA), m-tyramine (mTA), p-tyramine (pTA) and serotonin (5-HT) in the striata of rats 18 hr after the administration of three different doses (5, 50, or 100 mg/kg) of beta-phenylethylhydrazine (phenelzine, PEH) were measured. These concentrations were compared to those following the admin...

journal_title：Biochemical pharmacology

authors： Dyck LE,Durden DA,Yu PH,Davis BA,Boulton AA

更新日期：1983-05-01 00:00:00

abstract：:Arylamine N-acetyltransferase 1 (NAT1) conjugates several aromatic amines and their N-hydroxylated metabolites by N- or O-acetylation. NAT1 genotype and phenotype is known to be variable in human populations. In this study, we set out to measure the functional relevance of the frequent NAT1 gene variants for the activ...

journal_title：Biochemical pharmacology

authors： Bruhn C,Brockmöller J,Cascorbi I,Roots I,Borchert HH

更新日期：1999-12-01 00:00:00

abstract：:Dopamine can exist in both charged and uncharged forms at physiological pH. At present it is unclear which of these forms is responsible for dopaminergic agonist activity. The purpose of this study was to determine whether permanently charged structural analogs of dopamine containing either a nitrogen, sulfur, or sele...

journal_title：Biochemical pharmacology

authors： Wallace RA,Farooqui T,Wallace L,Ares J,Chang YA,Miller D,Uretsky N

更新日期：1987-11-15 00:00:00

abstract：:With the increased availability of human liver tissue, recombinant (cDNA-expressed) cytochrome P450 proteins (rCYPs), and knowledge of the human CYP pool (e.g. immunoquantitated levels of each CYP form in native liver microsomes), it is now possible to carry out in vitro "CYP reaction phenotyping" in an integrated man...

journal_title：Biochemical pharmacology

authors： Rodrigues AD

更新日期：1999-03-01 00:00:00

abstract：:Cytogenetic lesions often alter kinase signaling in acute myeloid leukemia (AML) and the addition of kinase inhibitors to the treatment arsenal is of interest. We have screened a kinase inhibitor library and performed combination testing to find promising drug-combinations for synergistic killing of AML cells. Cytotox...

journal_title：Biochemical pharmacology

authors： Österroos A,Kashif M,Haglund C,Blom K,Höglund M,Andersson C,Gustafsson MG,Eriksson A,Larsson R

更新日期：2016-10-15 00:00:00

abstract：:CCl4 induced cellular injury and its modification by prostacyclin (PGI2) was studied in cultured rat hepatocytes. Biosynthesis of both intracellular and serum proteins and that of phospholipids decreased upon CCl4 treatments (IC50 7.0, 2.5 and 3.2 mM, respectively). After 1 hr exposure of the cells to CCl4, the reduct...

journal_title：Biochemical pharmacology

authors： Divald A,Jeney A,Nagy JO,Timár F,Lapis K

更新日期：1990-10-01 00:00:00

abstract：:Rat aortic smooth muscle cells in culture (A-10; ATCC CRL 1476) exhibited low levels of beta-adrenergic receptors as determined by specific binding of [125I]cyanopindolol ([125I]CYP) and marginal stimulation of adenylate cyclase in plasma membranes by (-)isoproterenol. When these cells were exposed to 5 mM sodium buty...

journal_title：Biochemical pharmacology

authors： Nambi P,Whitman MH,Schmidt DB,Heckman GD,Stassen FL,Crooke ST

更新日期：1986-11-01 00:00:00

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

authors： Miura T,Muraoka S,Fujimoto Y

更新日期：2000-07-01 00:00:00

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

authors： Sakowicz M,Szutowicz A,Pawelczyk T

更新日期：2004-10-01 00:00:00