Effects of benfluron and its two metabolites on respiratory processes in P388 murine leukemia and Ehrlich ascites cells.

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 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：:Herbal antidiabetic preparations are often used as an add-on therapy in diabetes and such herbal preparations often contains quercetin that can inhibit cytochrome P450 (CYP) 3A4. This enzyme is responsible for metabolizing pioglitazone, a commonly used antidiabetic agent. Hence, it was speculated that quercetin may in...

journal_title：Biochemical pharmacology

authors： Umathe SN,Dixit PV,Kumar V,Bansod KU,Wanjari MM

更新日期：2008-04-15 00:00:00

abstract：:Intracellular cyclic AMP accumulation following exposure to dopamine (DA) agonists and and antagonists was measured in striatal slices from rats with a unilateral 6-hydroxydopamine (6-OHDA) lesion of the nigrostriatal pathway and which showed contralateral circling to apomorphine. Both DA (10-320 microM) and the D-1 a...

journal_title：Biochemical pharmacology

authors： Thomas KL,Rose S,Jenner P,Marsden CD

更新日期：1992-07-07 00:00:00

abstract：:Pyridine N-oxide derivatives represent a new class of anti-HIV compounds for which some members exclusively inhibit HIV-1 RT, whereas other members act, additionally or alternatively, at a post-integrational event in the replicative cycle of HIV. A prototype pyridine N-oxide derivative, JPL-32, inhibited tumor necrosi...

journal_title：Biochemical pharmacology

authors： Stevens M,Pannecouque C,De Clercq E,Balzarini J

更新日期：2006-04-14 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 human α7 neuronal nicotinic acetylcholine receptor gene (CHRNA7) is a candidate gene for schizophrenia and an important drug target for cognitive deficits in the disorder. Activation of the α7*nAChR, results in opening of the channel and entry of mono- and divalent cations, including Ca(2+), that presynaptically p...

journal_title：Biochemical pharmacology

authors： Araud T,Graw S,Berger R,Lee M,Neveu E,Bertrand D,Leonard S

更新日期：2011-10-15 00:00:00

abstract：:We compared the anti-proliferative properties of 4-benzylphenoxy-N ethyl morpholine (morpho-BPE) and trifluopromazine (TFP) on both the human breast cancer cell lines, MCF7, and its tamoxifen-resistant variant RTx6. We found that the calmodulin antagonist trifluopromazine (TFP) which bound ABS weakly, inhibited MCF7 c...

journal_title：Biochemical pharmacology

authors： Poirot M,Garnier M,Bayard F,Riviere I,Traore M,Wilson M,Fargin A,Faye JC

更新日期：1990-08-01 00:00:00

abstract：:Studies have been carried out to analyze the phosphoprotein composition of plasma membranes from Chinese hamster lung cells resistant to the action of adriamycin. Gel electrophoretic analysis of [32Pi]-labeled proteins revealed that plasma membranes from resistant cells contain a phosphoprotein of 180,000 molecular we...

journal_title：Biochemical pharmacology

authors： Garman D,Albers L,Center MS

更新日期：1983-12-01 00:00:00

abstract：:Diethyl esters of the glutathione S-conjugate S-p-bromobenzylglutathione, an inhibitor of glyoxalase I, and S-p-nitrobenzoxycarbonylglutathione, an inhibitor of glyoxalase II, induced growth arrest and toxicity in human leukaemia 60 cells in culture. The median growth inhibitory concentration IC50 values were 8.3 micr...

journal_title：Biochemical pharmacology

authors： Lo TW,Thornalley PJ

更新日期：1992-12-15 00:00:00

abstract：:Dolastatin 15, a seven-subunit depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent dolastatin 10, a five-subunit peptide obtained from the same organism. We have compared dolastatin 15 with dolastatin 10 for its effects on cells grown in culture ...

journal_title：Biochemical pharmacology

authors： Bai R,Friedman SJ,Pettit GR,Hamel E

更新日期：1992-06-23 00:00:00

abstract：:Glutathione (GSH) contributes to the detoxification of anticancer drugs through the operation of specific glutathione S-transferases (GST) and innate, or acquired, overexpression of this enzyme family has been frequently observed in tumor cell lines. In the GMA32 line of Chinese hamster fibroblasts, we showed that GSH...

journal_title：Biochemical pharmacology

authors： Lunel-Orsini C,Buttin G,De Saint Vincent BR

更新日期：1995-01-31 00:00:00

abstract：:Only very low levels of peroxidase activity were detected in castrated male hamster kidneys [1.0 +/- 0.8(S.E.) units/g protein], and chronic estrogen administration, either diethylstilbestrol (DES) or 17 beta-estradiol, for 1-5 months did not result in any appreciable increase in this activity. In contrast, hamster li...

journal_title：Biochemical pharmacology

authors： Klicka JK,Li SA,Li JJ

更新日期：1983-02-01 00:00:00

abstract：:Vascular disrupting agents show selective effects on tumor established vasculature, and achieve encouraging results in both pre-clinical and clinical experiments. In the present study, we investigated the effects of a new CA4 derivative MDS-11 and its prodrug MDS-11P on vascular disrupting activity in vitro and in viv...

journal_title：Biochemical pharmacology

authors： Deng ZT,Feng T,Wang P,Qi X,Chen XH,Li YX,Song CL,Geng MY,Li J

更新日期：2011-12-15 00:00:00

abstract：:The mitomycin C (MC) analog BMS-181174 (previously designated as BMY25067) has been shown to be active against a variety of solid tumors in mice. The activity of this compound against tumor cell lines resistant to MC and the different toxicity profiles of BMS-181174 and MC suggested that there may be significant diffe...

journal_title：Biochemical pharmacology

authors： Rockwell S,Kemple B,Kelley M

更新日期：1995-10-12 00:00:00

abstract：:Lesions to DNA trigger the DNA-damage response (DDR), a complex, multi-branched cell-intrinsic process targeted to DNA repair, or elimination of the damaged cells by apoptosis. DDR aims at reducing permanence of mutated cells, decreasing the risk of tumor development: the more stringent the response, the lower the lik...

journal_title：Biochemical pharmacology

authors： Caputo F,Vegliante R,Ghibelli L

更新日期：2012-11-15 00:00:00

abstract：OBJECTIVE:The evolution of the "cholinergic anti-inflammatory pathway" and the fact that the α 7 subunit of the nicotinic acetylcholine receptor (α7nAChR) is present in the spleen, joint and on the surface of lymphocytes, opened up the prospective in this study of targeting the α7nAChR by the anticholinesterase and cho...

journal_title：Biochemical pharmacology

authors： Gowayed MA,Rothe K,Rossol M,Attia AS,Wagner U,Baerwald C,El-Abhar HS,Refaat R

更新日期：2019-12-01 00:00:00

abstract：:We investigated whether morphine and its pro-drug codeine are substrates of the highly genetically polymorphic organic cation transporter OCT1 and whether OCT1 polymorphisms may affect morphine and codeine pharmacokinetics in humans. Morphine showed low transporter-independent membrane permeability (0.5 × 10⁻⁶ cm/s). ...

journal_title：Biochemical pharmacology

authors： Tzvetkov MV,dos Santos Pereira JN,Meineke I,Saadatmand AR,Stingl JC,Brockmöller J

更新日期：2013-09-01 00:00:00

abstract：:Cyclic AMP (cAMP) and cyclic GMP (cGMP) are two second messengers that have been proposed to act as a dualistic system in biological regulation. To determine if cGMP plays a role in the mediation of circadian rhythmicity of the adenylate cyclase (AC)-cAMP-phosphodiesterase (PDE) system in the achlorophyllous ZC mutant...

journal_title：Biochemical pharmacology

authors： Tong J,Edmunds LN Jr

更新日期：1993-05-25 00:00:00

abstract：:What does it mean to be a mentor in science? Definitions of mentorship are freely spouted in publications and include concepts such as academic support, professional development, role modeling, interaction, impartment of knowledge, evaluation of work, demonstration of methodology, etc. Perhaps most of us would agree w...

journal_title：Biochemical pharmacology

authors： Smith SL

更新日期：2015-11-15 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：:Treatment of immature 21-day-old female Sprague-Dawley rats with 17 beta-estradiol (E2) (0.5 microgram/rat) caused a significant increase in uterine wet weight, DNA synthesis, progesterone receptor (PR) binding, and peroxidase activity. At doses as high as 40 mg/rat, the bioflavonoid naringenin did not cause a signifi...

journal_title：Biochemical pharmacology

authors： Ruh MF,Zacharewski T,Connor K,Howell J,Chen I,Safe S

更新日期：1995-10-26 00:00:00

abstract：:Multidrug resistance (MDR) is a phenomenon where cancer cells become simultaneously resistant to anticancer drugs with different structures and mechanisms of action. MDR has been shown to be associated with overexpression of ATP-binding cassette (ABC) transporters. Here, we report that telatinib, a small molecule tyro...

journal_title：Biochemical pharmacology

authors： Sodani K,Patel A,Anreddy N,Singh S,Yang DH,Kathawala RJ,Kumar P,Talele TT,Chen ZS

更新日期：2014-05-01 00:00:00

abstract：:Epothilones constitute a novel class of antitubulin agents that are active in patients who relapse after treatment with other chemotherapeutics. This study investigated the molecular mechanisms leading to the onset of epothilone-B (patupilone) resistance in ovarian cancer. Results demonstrated that the Gli family of t...

journal_title：Biochemical pharmacology

authors： Mozzetti S,Martinelli E,Raspaglio G,Prislei S,De Donato M,Filippetti F,Shahabi S,Scambia G,Ferlini C

更新日期：2012-12-01 00:00:00

abstract：:Liver mitochondrial low-Km aldehyde dehydrogenase (ALDH2, EC 1.2.1.3), the isoform responsible for the conversion of acetaldehyde to acetate, is inhibited by the sulfoxide bioactivation products of Et2NC(O)SMe (from the alcohol aversion drug disulfiram), Pr2NC(O)SEt (the herbicide S-ethyl N,N-dipropylthiocarbamate), a...

journal_title：Biochemical pharmacology

authors： Staub RE,Quistad GB,Casida JE

更新日期：1999-11-01 00:00:00

abstract：:Four pseudo-symmetrical tamoxifen derivatives, RID-B (13), RID-C (14), RID-D (15), and bis(dimethylaminophenetole) (16), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of these pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 13 ...

journal_title：Biochemical pharmacology

authors： Shiina I,Sano Y,Nakata K,Kikuchi T,Sasaki A,Ikekita M,Nagahara Y,Hasome Y,Yamori T,Yamazaki K

更新日期：2008-03-01 00:00:00

abstract：:When rat peritoneal leucocytes were incubated with carbon tetrachloride, a PLA2 was activated, eicosanoids were generated and lysosomal and cytoplasmic enzymes were released. The predominant eicosanoid generated was TXB2 with lesser amounts of PGE2, 6-keto PGF1 alpha and LTB4. Preincubation of the cells with two struc...

journal_title：Biochemical pharmacology

authors： Lynch TJ,Blackwell GJ,Moncada S

更新日期：1985-05-01 00:00:00

abstract：:Milacemide (CP 1552 S, 2-n-pentylaminoacetamide), a drug with anti-epileptic potency, increases the gamma-aminobutyric acid (GABA) content specifically in the substantia nigra of rat brain. The effect is dose-related from 25 to 100 mg/kg p.o. The time course shows that at 100 mg/kg p.o. after 2, 3 and 4 hr the substan...

journal_title：Biochemical pharmacology

authors： de Varebeke PJ,Niebes P,Pauwels G,Roba J,Korf J

更新日期：1983-09-15 00:00:00

abstract：:5-Fluorouracil (FUra) has been administered to mice bearing xenografts of human colon adenocarcinomas. In two tumor lines, HxGC3 and HxVRC5, intrinsically resistant to FUra, 2'-deoxyuridylate (dUMP) accumulated 13.4- and 23.9-fold above basal levels. In HxELC2 xenografts, which demonstrated some sensitivity to FUra, t...

journal_title：Biochemical pharmacology

authors： Houghton JA,Weiss KD,Williams LG,Torrance PM,Houghton PJ

更新日期：1986-04-15 00:00:00

abstract：:Phomopsins comprise a family of peptide mycotoxins containing a 13-membered ring formed by an ether bridge, produced by the fungus Phomopsis leptostromiformis, the causal agent in lupin poisoning (lupinosis). The biochemical actions of two naturally occurring phomopsins, phomopsin A and B, and the chemical derivatives...

journal_title：Biochemical pharmacology

authors： Lacey E,Edgar JA,Culvenor CC

更新日期：1987-07-01 00:00:00