Attenuation of 6-hydroxydopamine (6-OHDA)-induced nuclear factor-kappaB (NF-kappaB) activation and cell death by tea extracts in neuronal cultures.

abstract：:Bupropion is a widely used antidepressant and smoking cessation aid and a strong inhibitor of CYP2D6 in vivo. Bupropion is administered as a racemic mixture of R- and S-bupropion and has stereoselective pharmacokinetics. Four primary metabolites of bupropion, threo- and erythro-hydrobupropion and R,R- and S,S-OH-bupro...

journal_title：Biochemical pharmacology

authors： Sager JE,Tripathy S,Price LS,Nath A,Chang J,Stephenson-Famy A,Isoherranen N

更新日期：2017-01-01 00:00:00

abstract：:Dinucleotides of adenosine and thymidine in the ApnT series (n = 3,4,5 and 6) and their corresponding phosphonate analogues, where a methylene group replaces the oxygen between the alpha and beta phosphorus atoms adjacent to thymidine, have been evaluated as inhibitors of human leukaemic thymidylate kinase (dTMP kinas...

journal_title：Biochemical pharmacology

authors： Orr RM,Davies LC,Stock JA,Taylor GA,Powles RL,Harrap KR

更新日期：1988-02-15 00:00:00

abstract：:The relationship between cytotoxicity and fluoropyrimidine effects on the production of mature cytoplasmic 28S and 18S ribosomal RNA was studied in S-180 cells for the fluoropyrimidines: 5-fluorouracil (FUra), 5-fluorouridine (FUrd), 5-fluorodeoxyuridine (FdUrd), and 5'-deoxy-5-fluorouridine (5'-dFUrd). After a 6-hr d...

journal_title：Biochemical pharmacology

authors： Takimoto CH,Tan YY,Cadman EC,Armstrong RD

更新日期：1987-10-01 00:00:00

abstract：:Certain anticonvulsant drugs require N-acetylation as a major route of metabolic clearance. Single point mutations of the polymorphic N-acetyltransferase gene (pNAT) are the primary cause for impaired drug acetylation. Pharmacokinetic parameters are altered in slow acetylator phenotypes and this may compromise drug sa...

journal_title：Biochemical pharmacology

authors： Borlak JT,Harsany V,Schneble H,Haegele KD

更新日期：1994-11-01 00:00:00

abstract：:A major problem in the treatment of cancer is cellular resistance to cytotoxic drugs. In tumor cells in vitro, the development of multidrug resistance is usually accompanied by increased expression of drug transporters, either P-glycoprotein (P-gp) or multidrug resistance-associated protein (MRP(1)). Both proteins bel...

journal_title：Biochemical pharmacology

authors： Marbeuf-Gueye C,Priebe W,Garnier-Suillerot A

更新日期：2000-11-15 00:00:00

abstract：:The p53 tumor suppressor protein provides a major anti-cancer defense mechanism, as underscored by the fact that the p53 gene is the most frequent target for genetic alterations in human cancer. Recent work has led to the realization that p53 lies at the hub of a very complex network of signaling pathways, which integ...

journal_title：Biochemical pharmacology

authors： Oren M,Damalas A,Gottlieb T,Michael D,Taplick J,Leal JF,Maya R,Moas M,Seger R,Taya Y,Ben-Ze'ev A

更新日期：2002-09-01 00:00:00

abstract：:AM404 is a synthetic TRPV1/CB(1) hybrid ligand with inhibitory activity on the anandamide transporter and is used for the pharmacological manipulation of the endocannabinoid system. It has been recently described that acetaminophen is metabolised in the brain to form the bioactive N-acylphenolamine AM404 and therefore...

journal_title：Biochemical pharmacology

authors： Caballero FJ,Navarrete CM,Hess S,Fiebich BL,Appendino G,Macho A,Muñoz E,Sancho R

更新日期：2007-04-01 00:00:00

abstract：:Fundamental progresses have been made in pain research with a comprehensive understanding of the neuronal pathways which convey painful sensations from the periphery and viscera to the central nervous system and of the descending modulating pathways. Nevertheless, many patients still suffer from various painful condit...

journal_title：Biochemical pharmacology

authors： Ceruti S

更新日期：2020-12-28 00:00:00

abstract：:The biological effects of 1-methyl-2-nitrosoimidazole (INO), the 2 electron reduction product of biologically active 1-methyl-2-nitroimidazole, were examined in HT-29 human colon cancer cells by clonogenic assay and glutathione (GSH) determination. INO was very toxic towards HT-29 cells and was equally toxic under aer...

journal_title：Biochemical pharmacology

authors： Mulcahy RT,Gipp JJ,Ublacker GA,Panicucci R,McClelland RA

更新日期：1989-05-15 00:00:00

abstract：:A serine peptidase (RLK1) was partially purified from rat liver homogenates. Its molecular weight was 80,000, and its optimum pH was 7.5. Bz-Tyr-O-Et was hydrolyzed by the enzyme, which was inhibited by Ip2PF, PMSF and by Tos-Phe-CH2Cl. The bonds cleaved by the enzyme were Phe5-Ser6 and Phe8-Arg9, when bradykinin was ...

journal_title：Biochemical pharmacology

authors： Da Graça M,Mazzacoratti N,Sampaio CA

更新日期：1982-03-01 00:00:00

abstract：:The effect of febrifugine, the main alkaloidal constituent of an antimalarial crude drug, Dichroa febrifuga Lour., on protective immunity in mice infected with erythrocytic stage Plasmodium berghei NK65 was investigated. Febrifugine was administered orally, at a dose of 1 mg/kg/day, to mice before and/or after they we...

journal_title：Biochemical pharmacology

authors： Murata K,Takano F,Fushiya S,Oshima Y

更新日期：1999-11-15 00:00:00

abstract：:The capabilities of 1alpha, 25-dihydroxyvitamin D3 (1,25(OH)2D3), and two novel vitamin D analogues, EB1089 and KH1060, to induce the differentiation of two established leukaemia cell lines, U937 and HL-60, were assessed alone or in combination with the retinoid compounds, 9-cis retinoic acid (9-cis RA) and all-trans ...

journal_title：Biochemical pharmacology

authors： James SY,Williams MA,Kelsey SM,Newland AC,Colston KW

更新日期：1997-09-01 00:00:00

abstract：:DT-diaphorase has been implicated in the activation and mechanism of cytotoxicity of the investigational indoloquinone anticancer drug EO9. Here, we have used a highly purified DT-diaphorase isolated from rat Walker tumour cells to provide unambiguous evidence for the ability of this enzyme to catalyze reduction of EO...

journal_title：Biochemical pharmacology

authors： Bailey SM,Lewis AD,Knox RJ,Patterson LH,Fisher GR,Workman P

更新日期：1998-09-01 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：:Carboxylesterases (CESs) play important roles in the metabolism of many ester-drugs. In the present study, we identified and characterized dexamethasone-induced methylprednisolone hemisuccinate (MPHS) hydrolase in rat liver microsomes. Intraperitoneal injection of dexamethasone resulted in a significant increase in th...

journal_title：Biochemical pharmacology

authors： Furihata T,Hosokawa M,Fujii A,Derbel M,Satoh T,Chiba K

更新日期：2005-04-15 00:00:00

abstract：:The transient receptor potential vanilloid-4 (TRPV4) belongs to a family of ion channels and can be activated by warm temperature, hypotonicity, cell swelling or lipid mediators of the arachidonic cascade. The metabolites or events responsible for TRPV4 activation are associated with inflammation, arguing in favor of ...

journal_title：Biochemical pharmacology

authors： Vergnolle N

更新日期：2014-05-15 00:00:00

abstract：:Extrahepatic cytochrome P450 enzymes (CYP450) are pivotal in the metabolism of endogenous substrates and xenobiotics. CYP2J2 is a major cardiac CYP450 and primarily metabolizes polyunsaturated fatty acids such as arachidonic acid to cardioactive epoxyeicosatrienoic acids. Due to its role in endobiotic metabolism, CYP2...

journal_title：Biochemical pharmacology

authors： Karkhanis A,Hong Y,Chan ECY

更新日期：2017-07-01 00:00:00

abstract：:We previously demonstrated that the widely used immunosuppressive drugs cyclosporin A (CsA) and tacrolimus (FK506), independent of immunophilin binding, can activate profibrogenic transforming growth factor β (TGFβ)/Smad signaling cascades in rat renal mesangial cells (MC). Here we report that both peptidyl-prolyl cis...

journal_title：Biochemical pharmacology

authors： Akool el-S,Gauer S,Osman B,Doller A,Schulz S,Geiger H,Pfeilschifter J,Eberhardt W

更新日期：2012-01-15 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：:We reported that differentiation-inducing factor-1 (DIF-1), synthesized by Dictyostelium discoideum, inhibited proliferation of various tumor cell lines in vitro by suppressing the Wnt/β-catenin signaling pathway. However, it remained unexplored whether DIF-1 also inhibits tumor growth in vivo. In the present study, t...

journal_title：Biochemical pharmacology

authors： Takahashi-Yanaga F,Yoshihara T,Jingushi K,Igawa K,Tomooka K,Watanabe Y,Morimoto S,Nakatsu Y,Tsuzuki T,Nakabeppu Y,Sasaguri T

更新日期：2014-06-01 00:00:00

abstract：:Vectorial secretion of cationic compounds across tubular epithelial cells is an important function of the kidney. This uni-directed transport is mediated by two cooperative functions, which are membrane potential-dependent organic cation transporters at the basolateral membranes and H+/organic cation antiporters at th...

journal_title：Biochemical pharmacology

authors： Terada T,Inui K

更新日期：2008-05-01 00:00:00

abstract：:Male weanling F-344 rats were maintained on selenium-supplemented or -deficient diets and were exposed to fresh cigarette smoke daily for 28 weeks. The deficient status of animals was demonstrated by a significant reduction in the pulmonary and hepatic glutathione peroxidase (GSH-Px) activity of rats on selenium-defic...

journal_title：Biochemical pharmacology

authors： Gairola CG,Tai HH

更新日期：1986-07-15 00:00:00

abstract：:Oxyntomodulin (Oxm) is a hormone which has been shown to exhibit a range of potentially beneficial actions for alleviation of obesity-diabetes. However, exploitation of Oxm-based therapies has been severely restricted due to degradation by the enzyme dipeptidylpeptidase-IV (DPP-IV). Thus, the aim of this study was to ...

journal_title：Biochemical pharmacology

authors： Kerr BD,Flatt PR,Gault VA

更新日期：2010-12-01 00:00:00

abstract：:The human platelet thromboxane A2/prostaglandin H2 receptor has been purified 6100-fold to apparent homogeneity by a three-step chromatographic procedure with an overall yield of 6%. A 6-fold purification of the receptor was first achieved by chromatography of 3-[(3-cholamidopropyl)dimethyl-ammonio]-1-propanesulfonate...

journal_title：Biochemical pharmacology

authors： Kim SO,Lim CT,Lam SC,Hall SE,Komiotis D,Venton DL,Le Breton GC

更新日期：1992-01-22 00:00:00

abstract：:A series of isoquinolines, N-methyl-1,2-dihydroisoquinolines, N-methyl-1,2,3,4-tetrahydroisoquinolines, 1,2,3,4-tetrahydroisoquinolines, and N-methylisoquinolinium ions were tested as inhibitors of monoamine oxidases A and B. All compounds were found to act as reversible and time-independent MAO inhibitors, often with...

journal_title：Biochemical pharmacology

authors： Thull U,Kneubühler S,Gaillard P,Carrupt PA,Testa B,Altomare C,Carotti A,Jenner P,McNaught KS

更新日期：1995-09-07 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：:Lactate, once considered a metabolic dead-end, has been recently proposed to support neuron bioenergetics. To better understand how lactate specifically influences cell energy metabolism, we studied the effects of lactate supplementation on SH-SY5Y human neuroblastoma cell bioenergetic fluxes. Lactate supplementation ...

journal_title：Biochemical pharmacology

authors： E L,Swerdlow RH

更新日期：2016-01-01 00:00:00

abstract：:Human leukemia K562 and HeLa cells were treated with daunomycin (DA) for 1-4 hr. With the indirect immunofluorescence technique, we observed that the nucleolar protein nucleophosmin/B23 (NPM) shifted its location from the nucleolus to the nucleoplasm (NPM-translocation). The degree of NPM-translocation was determined ...

journal_title：Biochemical pharmacology

authors： Chan PK,Chan FY

更新日期：1999-06-01 00:00:00

abstract：:SARM is the fifth and most conserved member of the Toll/Il-1 Receptor (TIR) adaptor family. However, unlike the other TIR adaptors, MyD88, Mal, TRIF and TRAM, SARM does not participate in transducing signals downstream of TLRs. By contrast SARM inhibits TLR signalling by interacting with the adaptors TRIF and MyD88. I...

journal_title：Biochemical pharmacology

authors： Carty M,Bowie AG

更新日期：2019-03-01 00:00:00

abstract：:The participation of mitochondria in the mechanism of tumor cell death induced by non-steroid anti-inflammatory drugs is uncertain. Here we show that ibuprofen induces death of Walker 256 tumor cells independently on mitochondrial depolarization as estimated by flow cytometry using DioC(6)(3). Oligomycin increased mit...

journal_title：Biochemical pharmacology

authors： Campos CB,Degasperi GR,Pacífico DS,Alberici LC,Carreira RS,Guimarães F,Castilho RF,Vercesi AE

更新日期：2004-12-01 00:00:00