Oxidative activation of 2-aminofluorene by human red blood cell cytosol.

abstract：:Leukemia cells aberrantly overexpress senescence-suppression telomerase reverse transcriptase (TERT) and down-regulate key senescence-promoting genes to escape complete senescence, resulting in immortalization and malignant progression. Accordingly, induction of complete senescence is a sensible strategy for anti-leuk...

journal_title：Biochemical pharmacology

authors： Pan Y,Meng M,Zheng N,Cao Z,Yang P,Xi X,Zhou Q

更新日期：2017-02-15 00:00:00

abstract：:Incubation of human carcinoma cells with mitoxantrone resulted in an intracellular distribution of the drug into cytoplasmic, nuclear and cytoskeletal compartments occurring within 1 min of drug treatment. Incubation of the cells in drug-free medium resulted in an efflux of the drug such that 80% of the intracellular ...

journal_title：Biochemical pharmacology

authors： Roberts RA,Cress AE,Dalton WS

更新日期：1989-12-01 00:00:00

abstract：:Rats were killed after 6 weeks of continuous ingestion of the pneumotoxic alkaloid monocrotaline (2.2 mg/kg/day), the neutrophil elastase inhibitor SC39026 (60 mg/kg/day), or both. Pulmonary reactions were evaluated by light and electron microscopy. Lung endothelial function was monitored by angiotensin converting enz...

journal_title：Biochemical pharmacology

authors： Molteni A,Ward WF,Ts'ao CH,Hinz JM

更新日期：1989-08-01 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：:The present study describes the isolation of the first neurotoxin (acantoxin IVa) from Acanthophis sp. Seram death adder venom and an examination of its activity at nicotinic acetylcholine receptor (nAChR) subtypes. Acantoxin IVa (MW 6815; 0.1-1.0 microM) caused concentration-dependent inhibition of indirect twitches ...

journal_title：Biochemical pharmacology

authors： Wickramaratna JC,Fry BG,Loiacono RE,Aguilar MI,Alewood PF,Hodgson WC

更新日期：2004-07-15 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：:We studied the effect of DW2282-,[(S)-(+)-4-phenyl-1-[N-(4-aminobenzoyl)-indoline-5-sulfonyl-4,5-dihydro-2-imidazolone].hydrochloride], a newly developed anti-cancer agent, on cell proliferation, cell cycle progression, and induction of apoptosis in human promyelocytic leukemia (HL-60) cells. DW2282, a diarylsulfonylu...

journal_title：Biochemical pharmacology

authors： Piao W,Yoo J,Lee DK,Hwang HJ,Kim JH

更新日期：2001-12-01 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：:5-Phenylthioacyclouridine (PTAU or 1-[(2-hydroxyethoxy)methyl]-5-phenylthiouracil) was synthesized as a highly specific and potent inhibitor of uridine phosphorylase (UrdPase, EC 2.4.2.3). PTAU has inhibition constant (K(is)) values of 248 and 353 nM towards UrdPase from mouse and human livers, respectively. PTAU was ...

journal_title：Biochemical pharmacology

authors： el Kouni MH,Goudgaon NM,Rafeeq M,Al Safarjalani ON,Schinazi RF,Naguib FN

更新日期：2000-09-15 00:00:00

abstract：:Auranofin (AF) is a newly introduced oral gold compound having antirheumatic properties, and its efficacy in the treatment of bronchial asthma is now under investigation. In this study, we examined the effects of AF on leukotriene (LT) formation by human polymorphonuclear leukocytes (PMNs) stimulated with the calcium ...

journal_title：Biochemical pharmacology

authors： Honda Z,Iizasa T,Morita Y,Matsuta K,Nishida Y,Miyamoto T

更新日期：1987-05-01 00:00:00

abstract：:Dichlorodi[U-14C]phenyltrichloroethane ( [14C]DDT), incubated with rat hepatic microsomes and NADPH, produced reactive intermediates which covalently bound to microsomal protein and lipids. In atmospheric oxygen, DDT bound to microsomal protein; however, binding was increased up to approximately 70% by oxygen depletio...

journal_title：Biochemical pharmacology

authors： Baker MT,Van Dyke RA

更新日期：1984-01-15 00:00:00

abstract：:The inhibition of thymidylate synthase (TS) by 5-fluorouracil (5-FU) was known to increase the incorporation of radiolabelled iododeoxyuridine (IdUrd) into DNA. The relatively non-toxic compounds such as thiol-containing antioxidant pyrrolidinodithiocarbamte (PDTC) or aromatic fatty acid phenylbutyrate (PB) had been r...

journal_title：Biochemical pharmacology

authors： Wang HE,Wu HC,Kao SJ,Tseng FW,Wang YS,Yu HM,Chou SL,Yen SH,Chi KH

更新日期：2005-02-15 00:00:00

abstract：:The inhibition of rat liver monoamine oxidase by a number of N-propargyl and alpha-methyl amine derivatives has been examined. The results indicate that alpha-methyl-substituted primary and secondary amine derivatives tend to show selectivity as reversible inhibitors towards the A-form of the enzyme. The structural fe...

journal_title：Biochemical pharmacology

authors： Tipton KF,McCrodden JM,Kalir AS,Youdim MB

更新日期：1982-04-01 00:00:00

abstract：:The C-18 hydroxy fatty acids ricinelaidic acid and ricinoleic acid diminish the oleic acid-stimulated agonist benzodiazepine binding in the rat brain in vitro. The oleic acid-induced enhancement of [3H]diazepam binding was completely abolished in membranes from the cerebellum, but only partially decreased in membranes...

journal_title：Biochemical pharmacology

authors： Witt MR,Nielsen M

更新日期：1994-02-11 00:00:00

abstract：:The O2 dependence of the metabolism of benzylamine to benzaldehyde, benzoate and hippurate was studied in isolated rat hepatocytes. The initial oxidation to benzaldehyde, catalyzed by monoamine oxidase, had an apparent Kmo2 value of 34 microM in cells and 40 microM in isolated rat liver mitochondria. The conversion of...

journal_title：Biochemical pharmacology

authors： Jones DP

更新日期：1984-02-01 00:00:00

abstract：:A number of synthetic manganese complexes exhibit both in vitro and in vivo catalytic antioxidant activities. This study reports that the antioxidant potencies of a new series of meso-N,N'-dialkyl-imidazolium substituted manganese(III) porphyrins are dependent, in part, on their ability to redox cycle with endogenous ...

journal_title：Biochemical pharmacology

authors： Kachadourian R,Johnson CA,Min E,Spasojevic I,Day BJ

更新日期：2004-01-01 00:00:00

abstract：:We studied several steps of methionine metabolism in isolated rat hepatocytes both with and without the presence of a hepatotoxic agent (D-galactosamine). By use of selective labelling either on methyl or on carboxyl groups, we showed that intracellular methionine is used preferentially for the methylation of phosphol...

journal_title：Biochemical pharmacology

authors： Ozturk M,Lemonnier F,Cresteil D,Lemonnier A

更新日期：1986-12-01 00:00:00

abstract：:Vanadate (VO3-) was found to activate adenylyl cyclase (AC) in ocular ciliary process membrane. This response was additive to that of isoproterenol (ISO) and vasoactive intestinal peptide (VIP), but it was potentiative with forskolin (FSK) and also with Ca2+/calmodulin activation of AC activity. The potentiated respon...

journal_title：Biochemical pharmacology

authors： Mittag TW,Guo WB,Taniguchi T

更新日期：1993-03-24 00:00:00

abstract：:Chronic ethanol (EtOH) use during pregnancy can be associated with fetal injury including the fetal alcohol syndrome (FAS). A contributing factor in this fetal injury may be the effect of EtOH on the placenta. In this study, we have examined the effect of in vitro EtOH treatment on adenosine 3':5'-cyclic monophosphate...

journal_title：Biochemical pharmacology

authors： Karl PI,Divald A,Fisher SE

更新日期：1994-10-07 00:00:00

abstract：:The well-known analgesic and antipyretic drug N-acetyl-p-aminophenol (acetaminophen; APAP) has been previously reported to affect MDR1 expression in rat liver. In this study, we have investigated the effect of subtoxic doses of APAP on MDR1 expression and activity in rat intestine and human intestinal cells. Administr...

journal_title：Biochemical pharmacology

authors： Ghanem CI,Arias A,Novak A,Carpini GD,Villanueva S,Blazquez AG,Marin JJ,Mottino AD,Rubio MC

更新日期：2011-01-15 00:00:00

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

authors： Lyles GA,Callingham BA

更新日期：1982-04-01 00:00:00

abstract：:The first-generation histamine H1-receptor antagonists, chlorpheniramine (CPHE) and diphenhydramine (DPH), may activate histamine release from basophils and mast cells. Because CPHE and DPH are cationic-amphiphilic and because several substances with such physicochemical properties activate heterotrimeric regulatory g...

journal_title：Biochemical pharmacology

authors： Burde R,Dippel E,Seifert R

更新日期：1996-01-26 00:00:00

abstract：:Diethyldithiocarbamate-methyl ester (DDTC-Me), a metabolite of disulfiram, has been shown recently to produce a disulfiram-ethanol reaction (DER). Studies were carried out to compare the ethanol-sensitizing properties of DDTC-Me with those of disulfiram and diethyldithiocarbamate (DDTC) in the rat. All three drugs inh...

journal_title：Biochemical pharmacology

authors： Yourick JJ,Faiman MD

更新日期：1989-02-01 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

abstract：:Interleukin (IL)-22 plays protective roles in infections and in inflammatory diseases that have been linked to its meditation of innate immunity via multiple mechanisms. IL-22 binds specifically to its heterodimeric receptor, which is expressed on a variety of epithelial tissues. UTTR1147A is a recombinant fusion prot...

journal_title：Biochemical pharmacology

authors： Stefanich EG,Rae J,Sukumaran S,Lutman J,Lekkerkerker A,Ouyang W,Wang X,Lee D,Danilenko DM,Diehl L,Loyet KM,Herman A

更新日期：2018-06-01 00:00:00

abstract：:The aim of this study was to test if human platelet leukotriene C4-synthase (LTC4-S) is pharmacologically different from cloned and expressed LTC4-S and, in light of the significant homologies between 5-lipoxygenase activating protein (FLAP) and LTC4-S, if different potencies of leukotriene synthesis inhibitors acting...

journal_title：Biochemical pharmacology

authors： Sala A,Folco G,Henson PM,Murphy RC

更新日期：1997-03-21 00:00:00

abstract：:A number of tumour cells, including Ehrlich ascites tumour cells (EATC), possess a polyamine uptake system which selectively accumulates endogenous polyamines and structurally related compounds by an active energy dependent system(s). We suggest that it may be possible to utilize this uptake system to target certain c...

journal_title：Biochemical pharmacology

authors： Holley J,Mather A,Cullis P,Symons MR,Wardman P,Watt RA,Cohen GM

更新日期：1992-02-18 00:00:00

abstract：:The enzyme steroid 5 alpha-reductase (EC 1.3.99.5) catalyzes the NADPH-dependent reduction of the double bond of a variety of 3-oxo-Delta(4) steroids including the conversion of testosterone to 5 alpha-dihydrotestosterone. In humans, 5 alpha-reductase activity is critical for certain aspects of male sexual differentia...

journal_title：Biochemical pharmacology

authors： Hiipakka RA,Zhang HZ,Dai W,Dai Q,Liao S

更新日期：2002-03-15 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：:Three grams of nafazatrom (Bay g 6575), given orally to healthy male volunteers in a single dose, significantly reduce the formation of leukotriene B4 in polymorphonuclear leukocytes. LTB4 synthesis fell from 57.1 +/- 17.0 ng/10(7) PMNL, mean +/- S.D., in control to 34.3 +/- 14.4 ng/10(7) PMNL 3 hr after nafazatrom (2...

journal_title：Biochemical pharmacology

authors： Strasser T,Fischer S,Weber PC

更新日期：1985-06-01 00:00:00