Inhibition of rat liver hydroxysteroid sulfotransferase activity by alkylamines.

abstract：:The influence of age on the mixed function oxidase system from a non-human primate was studied. Microsomes were isolated from the livers of female Macaca nemestrina ranging from 2 to 21 years of age. No significant age-related change was observed in either the cytochrome P-450 content or the NADPH cytochrome c reducta...

journal_title：Biochemical pharmacology

authors： Sutter MA,Wood WG,Williamson LS,Strong R,Pickham K,Richardson A

更新日期：1985-08-15 00:00:00

abstract：:The microsomal fraction of bone marrow contains cytochrome P-450 (39 +/- 11 pmoles/mg microsomal protein) and monooxygenase activity could be demonstrated by the O-dealkylation of 7-ethoxycoumarin (114 +/- 65 pmoles/(min X mg microsomal protein] and the hydroxylation of benzene to phenol (51 +/- 8.6 pmol/45 min X mg m...

journal_title：Biochemical pharmacology

authors： Gollmer L,Graf H,Ullrich V

更新日期：1984-11-15 00:00:00

abstract：:Rat liver microsomes and purified NADPH-cytochrome c reductase metabolized [14C]misonidazole anaerobically to a reactive intermediate that covalently binds to tissue macromolecules. Air strongly inhibited the binding whereas carbon monoxide had no effect, indicating that misonidazole is activated via reduction and not...

journal_title：Biochemical pharmacology

authors： McManus ME,Lang MA,Stuart K,Strong J

更新日期：1982-02-15 00:00:00

abstract：:The intracellular actions of phosphodiesterase (PDE) inhibitors on the accumulation of cyclic nucleotides were studied in isolated ventricular cardiomyocytes from adult Sprague-Dawley rats. Elevated levels of cyclic AMP, due to the effects of selective PDE inhibitors, were detected only when the levels of cyclic nucle...

journal_title：Biochemical pharmacology

authors： Kelso EJ,McDermott BJ,Silke B

更新日期：1995-02-14 00:00:00

abstract：:A series of cytotoxic propenal (3-oxoprop-1-enyl) derivatives of pyrimidine bases and deoxynucleosides was evaluated for their ability to block thymidylate synthesis in intact and permeabilized murine leukemia L1210 cells. Several were potent inhibitors of this process, likely contributing to their cytotoxicity. The I...

journal_title：Biochemical pharmacology

authors： Kalman TI,Marinelli ER,Xu B,Reddy AR,Johnson F,Grollman AP

更新日期：1991-07-05 00:00:00

abstract：:Inflammation, especially chronic inflammation, is directly involvement in the pathogenesis of many diseases including cancer. An effective approach for managing inflammation is to employ chemicals to block activation of nuclear factor-κB (NF-κB), a key regulator for inflammatory processes. Piperlongumine (piplartine, ...

journal_title：Biochemical pharmacology

authors： Sun LD,Wang F,Dai F,Wang YH,Lin D,Zhou B

更新日期：2015-06-01 00:00:00

abstract：:The flavone L86-8275 [(-)cis-5,7-dihydroxy-2-(2-chlorophenyl)-8-[4-(3-hydroxy-1-methyl)- piperidinyl]-4H-1-benzopyran-4-one] delayed the progression of aphidicolin-synchronized MDA-468 breast carcinoma cells through S phase and prevented progression through G2. L86-8275 prevented the G2-related increase in histone H1 ...

journal_title：Biochemical pharmacology

authors： Worland PJ,Kaur G,Stetler-Stevenson M,Sebers S,Sartor O,Sausville EA

更新日期：1993-11-17 00:00:00

abstract：:Sulfation of tyrosyl residue(s) has been found to be a post-translational modification that precedes the secretion of many biologically active proteins or peptides. In the present paper, we report on the characterization of human liver tyrosylprotein sulfotransferase (TPST), the enzyme responsible for sulfation of tyr...

journal_title：Biochemical pharmacology

authors： Lin WH,Roth JA

更新日期：1990-08-01 00:00:00

abstract：:The disposition and metabolic fate of benzylpenicillin conjugated to a protein, human serum albumin (HSA), were compared with those of free penicillin in the rat. The conjugate was prepared by in vitro incubation of [3H]-benzylpenicillin and HSA at pH 10.8 for 24 hr at 37 degrees, conditions which favour the formation...

journal_title：Biochemical pharmacology

authors： Christie G,Kitteringham NR,Park BK

更新日期：1987-10-15 00:00:00

abstract：:The nuclear retinoid X receptor-α (RXRα) plays critical roles in cell homeostasis and in many physiological processes mainly through its transcriptional function. However, an N-terminal truncated form of RXRα, tRXRα, was frequently described in various cancer cells and tumor tissues, thus representing a new promising ...

journal_title：Biochemical pharmacology

authors： Wang PY,Zeng WJ,Liu J,Wu YL,Ma Y,Zeng Z,Pang JY,Zhang XK,Yan X,Wong AST,Zeng JZ

更新日期：2017-01-15 00:00:00

abstract：:The anticancer drug cis-diamminedichloroplatinum(II) (cisplatin) has been shown previously to form adducts preferentially within internucleosomal or linker DNA rather than to DNA within the nucleosome. To determine whether other "open" regions of chromatin have an increased affinity for cisplatin, adduct formation wit...

journal_title：Biochemical pharmacology

authors： Bubley GJ,Xu J,Kupiec N,Sanders D,Foss F,O'Brien M,Emi Y,Teicher BA,Patierno SR

更新日期：1996-03-08 00:00:00

abstract：:The nonspecies specific immunosuppressive and anti-inflammatory properties of a major protein (SV-IV) secreted from the epithelium of rat seminal vesicles (SV) are described. To detect the immunosuppressive effect, peripheral blood lymphocytes (PBL) were pretreated for 2 hr at 37 degrees with SV-IV, and the protein wa...

journal_title：Biochemical pharmacology

authors： Metafora S,Peluso G,Persico P,Ravagnan G,Esposito C,Porta R

更新日期：1989-01-01 00:00:00

abstract：:Casein-elicited mouse peritoneal macrophages cultured in the presence of phorbol 12-myristate 13-acetate (PMA) express u-PA. Induction is maximal after 4 hr of stimulation and u-PA activity is mainly recovered with the membrane fraction of the cellular lysate. This enzymatic activity is inhibited by isopropylmethylpho...

journal_title：Biochemical pharmacology

authors： Dubois P,Lison D,Lauwerys R

更新日期：1988-06-01 00:00:00

abstract：:The peroxisome proliferator-activated receptors (PPARs) are ligand-dependent transcription factors involved in lipid metabolism and glucose utilization, in cell growth, differentiation and apoptosis, and in the regulation of pro-inflammatory genes expression such as cyclooxygenase-2 (COX-2). PPARγ is the main isoform ...

journal_title：Biochemical pharmacology

authors： Casali CI,Weber K,Faggionato D,Gómez EM,Tome MC

更新日期：2014-08-15 00:00:00

abstract：:The metabolism of toluene in human liver microsomes and by cDNA-expressed human cytochrome P450s (CYPs) was investigated. Toluene was metabolized mainly to benzyl alcohol and slightly to o- and p-cresol by human liver microsomes. Formation of o-cresol was elevated in microsomes from human livers derived from cigarette...

journal_title：Biochemical pharmacology

authors： Nakajima T,Wang RS,Elovaara E,Gonzalez FJ,Gelboin HV,Raunio H,Pelkonen O,Vainio H,Aoyama T

更新日期：1997-02-07 00:00:00

abstract：:There is increasing evidence that human arylamine N-acetyltransferase type 1 (NAT1, EC 2.3.1.5), although first identified as a homologue of a drug-metabolising enzyme, appears to be a marker in human oestrogen receptor positive breast cancer. Mouse Nat2 is the mouse equivalent of human NAT1. The development of mouse ...

journal_title：Biochemical pharmacology

authors： Kawamura A,Westwood I,Wakefield L,Long H,Zhang N,Walters K,Redfield C,Sim E

更新日期：2008-04-01 00:00:00

abstract：:(1) As a first step in studying the kinetics of the lipolytic system of rat adipocytes, the day-to-day variation between dose-response curves has been analysed. (2) Methods are described for the evaluation of large quantities of data relating noradrenaline to lipolysis. (3) A 'clustering' technique is presented which ...

journal_title：Biochemical pharmacology

authors： Davies JI,Cooper DM,Everett D

更新日期：1982-03-01 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：:Previous studies of platinum(II) compounds with bidentate leaving ligands have emphasized the contrast between the stability of the bidentate leaving ligand in vitro (T1/2 greater than 11 days in water) and the apparent reactivity of these bidentate platinum compounds in vivo. However, none of these studies actually m...

journal_title：Biochemical pharmacology

authors： Mauldin SK,Plescia M,Richard FA,Wyrick SD,Voyksner RD,Chaney SG

更新日期：1988-09-01 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

abstract：:The effect of biscoclaurine (bisbenzylisoquinoline) alkaloids on phospholipase A2 and C activation in signal transduction system of rabbit platelet was studied. Isotetrandrine, cepharanthine and berbamine inhibited the aggregation induced by collagen but not by other stimuli such as thrombin and arachidonic acid, whil...

journal_title：Biochemical pharmacology

authors： Hashizume T,Yamaguchi H,Sato T,Fujii T

更新日期：1991-02-01 00:00:00

abstract：:The role of specific cytochrome P450 (P450) isoforms in the formation of adducts of 7,12-dimethylbenz(a)anthracene metabolites and membrane proteins has been investigated in vitro with microsomal fractions prepared from rats pretreated with various isoenzyme selective inducers. The effects of isoenzyme selective inhib...

journal_title：Biochemical pharmacology

authors： Lambard SE,Burnett AK,Wolf CR,Craft JA

更新日期：1991-09-27 00:00:00

abstract：:The effect of the adenosine deaminase (ADA) inhibitor 2'-deoxycoformycin (dCF) on the development of insulin-dependent diabetes mellitus (IDDM) was assessed in the BB Wistar rat. Sixty-one male rats were treated from days 30 to 120 with 0, 0.5, 1.0 or 1.5 mg dCF/kg/week. The incidence of IDDM was 78% in the controls a...

journal_title：Biochemical pharmacology

authors： Thliveris JA,Begleiter A,Kobrinsky NL,Verburg L,Dean HJ,Johnston JB

更新日期：1993-09-14 00:00:00

abstract：:Continuous in vitro cultivation of human lymphoid H9 cells in the presence of 0.5microM arabinosyl-cytosine (araC) resulted in cell variant, H9-araC cells, that was >600-fold resistant to the drug and cross resistant to its analogs and other unrelated nucleosides, e.g. dideoxycytidine (5-fold), thiacytidine (2-fold), ...

journal_title：Biochemical pharmacology

authors： Sarkar M,Han T,Damaraju V,Carpenter P,Cass CE,Agarwal RP

更新日期：2005-08-01 00:00:00

abstract：:The turnover rate of vitamin E is slow in nerve tissue. Therefore, we have developed in vitro techniques to study the biochemical reactions of this nutrient in brain. Subcellular fractions were isolated from the cerebral hemispheres of 4-month-old, male, Fisher 344 rats. Aliquots of fractions (500 micrograms protein) ...

journal_title：Biochemical pharmacology

authors： Vatassery GT

更新日期：1993-06-09 00:00:00

abstract：:We investigated the mechanism of phorbol 12-myristate 13-acetate (PMA)-induced migration of glioblastoma cells focusing on the p38 mitogen-activated protein kinase (MAPK)/heat shock protein 27 (Hsp27) pathway. PMA-induced cell migration and activation of p38MAPK in A172 glioblastoma cells. PMA-induced formation of lam...

journal_title：Biochemical pharmacology

authors： Nomura N,Nomura M,Sugiyama K,Hamada J

更新日期：2007-09-01 00:00:00

abstract：:Ephedrine and its alkaloids are used for the treatment of asthma, nasal congestion, and obesity. Ephedrine, with two chiral centers, exists as four isomers that exhibit direct and indirect effects on both alpha- and beta-adrenergic receptors (AR). Our main goal was to study the direct effects of the ephedrine isomers ...

journal_title：Biochemical pharmacology

authors： Vansal SS,Feller DR

更新日期：1999-09-01 00:00:00

abstract：:Carbamazepine is an anticonvulsant which is associated with a significant incidence of hypersensitivity reactions including agranulocytosis. We have postulated that many drug hypersensitivity reactions, especially agranulocytosis and lupus, are due to reactive metabolites generated by the myeloperoxidase (MPO) (EC 1.1...

journal_title：Biochemical pharmacology

authors： Furst SM,Uetrecht JP

更新日期：1993-03-24 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：:Curcumin (diferuoylmethane), the yellow pigment in the rhizome of tumeric (Curcuma longa), an ingredient of curry spice, is known to exhibit a variety of pharmacological effects including antitumor, antiinflammatory, and antiinfectious activities. Although its precise mode of action remains elusive, curcumin has been ...

journal_title：Biochemical pharmacology

authors： Sikora E,Bielak-Zmijewska A,Piwocka K,Skierski J,Radziszewska E

更新日期：1997-10-15 00:00:00