Mechanism of the protective action of thiol compounds in ethanol-induced liver injury.

abstract：:20-Hydroxyvitamin D(3) (20(OH)D(3)), the major product of CYP11A1 action on vitamin D(3), is biologically active and is produced in vivo. As well as potentially having important physiological actions, it is of interest as a therapeutic agent due to its lack of calcemic activity. In the current study we have examined t...

journal_title：Biochemical pharmacology

authors： Tieu EW,Tang EK,Chen J,Li W,Nguyen MN,Janjetovic Z,Slominski A,Tuckey RC

更新日期：2012-12-15 00:00:00

abstract：:Endosulfan (E) is an organochloric insecticide, which is quickly metabolized and eliminated from the body system. Toxic effects of E and its metabolites have been reported. The influence of E and its metabolites, viz. endosulfan sulfate (ES), endosulfan diol (ED) and endosulfan lactone (EL), has been examined on rat l...

journal_title：Biochemical pharmacology

authors： Dubey RK,Beg MU,Singh J

更新日期：1984-11-01 00:00:00

abstract：:U73122 ((1-[6-(( 17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)exyl]-1H-p yrrole-2,5-dione)) is generally used as a selective inhibitor of phospholipase C (PLC) and the related rise in cytosolic Ca2+. Recently, by using hepatocytes, it was suggested that its action sites are different for PLC activation and increa...

journal_title：Biochemical pharmacology

authors： Pulcinelli FM,Gresele P,Bonuglia M,Gazzaniga PP

更新日期：1998-12-01 00:00:00

abstract：:Nitric oxide sensitive guanylyl cyclase (NOsGC) is a heterodimeric enzyme consisting of an α and a β subunit. Two heterodimeric enzymes are known to be important for NO-signalling in humans: α(1)/β(1) and α(2)/β(1). No difference had so far been detected with respect to their pharmacological properties, but as we show...

journal_title：Biochemical pharmacology

authors： Haase N,Haase T,Kraehling JR,Behrends S

更新日期：2010-12-01 00:00:00

abstract：:Carvedilol, a non-selective beta-adrenoreceptor blocker, has been shown to possess a high degree of cardioprotection in experimental models of myocardial damage. Reactive oxygen species have been proposed to be implicated in such situations, and antioxidants have been demonstrated to provide partial protection to the ...

journal_title：Biochemical pharmacology

authors： Santos DJ,Moreno AJ

更新日期：2001-01-15 00:00:00

abstract：:Exposure of lung tissue to Co(II) ions both in vivo and in vitro results in toxicity, a relatively early event of which is the oxidation of cellular glutathione. In this study we have attempted to delineate the relationship between this oxidation of glutathione and the subsequent development of cellular dysfunction. S...

journal_title：Biochemical pharmacology

authors： Lewis CP,Demedts M,Nemery B

更新日期：1992-02-04 00:00:00

abstract：:The aim of this work is the in vitro and ex vivo assessment of the leishmanicidal activity of camptothecin and three analogues used in cancer therapy: topotecan (Hycantim®), gimatecan (ST1481) and the pro-drug irinotecan (Camptosar®) as well as its active metabolite SN-38 against Leishmania infantum. The activity of c...

journal_title：Biochemical pharmacology

authors： Prada CF,Alvarez-Velilla R,Balaña-Fouce R,Prieto C,Calvo-Álvarez E,Escudero-Martínez JM,Requena JM,Ordóñez C,Desideri A,Pérez-Pertejo Y,Reguera RM

更新日期：2013-05-15 00:00:00

abstract：:5-Hydroxytryptamine (serotonin, 5-HT) stimulates basal adenylyl cyclase activity in membranes from guinea pig or rat hippocampi, but 5-HT inhibits forskolin-stimulated adenylyl cyclase activity in these same membranes. The opposing effects of 5-HT on adenylyl cyclase activity indicate that distinct 5-HT receptors, pos...

journal_title：Biochemical pharmacology

authors： De Vivo M,Maayani S

更新日期：1990-10-01 00:00:00

abstract：:The interaction of the anti-tumor anthraquinones, ametantrone and mitoxantrone, with rat hepatic microsomes has been studied with a fluorescence technique using 7,12-dimethylbenzanthracene as a new fluorescent probe. The two drugs were able to quench the intrinsic fluorescence of microsomal suspension. Mitoxantrone wa...

journal_title：Biochemical pharmacology

authors： al-Gailany KA,Alwan AH

更新日期：1988-10-15 00:00:00

abstract：:The mammalian thioredoxin reductase (TrxR) isoenzymes, TrxR1 in cytosol or nucleus, TrxR2 in mitochondria, and TrxR3 in testis, are essential seleno-flavoenzymes with a conserved penultimate selenocysteine (Sec) residue at the C-terminus, and have attracted increasing interests as potential targets for development of ...

journal_title：Biochemical pharmacology

authors： Zhang J,Li Y,Duan D,Yao J,Gao K,Fang J

更新日期：2016-02-15 00:00:00

abstract：:The partition coefficients (Kp) of three prototype Ca2+ antagonists, nitrendipine, (-)-desmethoxyverapamil and flunarizine were determined in native synaptic plasma membranes (SPM) isolated from sheep brain cortex and in liposomes prepared with the total lipids extracted from the membranes. We found that at 25 degrees...

journal_title：Biochemical pharmacology

authors： Carvalho CM,Oliveira CR,Lima MP,Leysen JE,Carvalho AP

更新日期：1989-07-01 00:00:00

abstract：:Paraquat and the structurally similar polyamines, such as putrescine and spermidine, are accumulated actively and selectively by the alveolar type II cells via the polyamine uptake system. We report the uptake kinetics of paraquat and putrescine and their mutual inhibition in freshly isolated rat type II cell suspensi...

journal_title：Biochemical pharmacology

authors： Chen N,Bowles MR,Pond SM

更新日期：1992-09-25 00:00:00

abstract：:The binding of indapamide to isolated serum proteins and erythrocytes was studied in order to understand its blood distribution. In serum, indapamide was mainly bound to alpha 1-acid glycoprotein with a high affinity (K = 73.4/mM), and to albumin and lipoproteins. Indapamide was bound to erythrocytes via a saturable p...

journal_title：Biochemical pharmacology

authors： Urien S,Riant P,Renouard A,Coulomb B,Rocher I,Tillement JP

更新日期：1988-08-01 00:00:00

abstract：:Class B peptide hormone GPCRs are targets for the treatment of major chronic disease. Peptide ligands of these receptors display biased agonism and this may provide future therapeutic advantage. Recent active structures of the calcitonin (CT) and glucagon-like peptide-1 (GLP-1) receptors reveal distinct engagement of ...

journal_title：Biochemical pharmacology

authors： Dal Maso E,Zhu Y,Pham V,Reynolds CA,Deganutti G,Hick CA,Yang D,Christopoulos A,Hay DL,Wang MW,Sexton PM,Furness SGB,Wootten D

更新日期：2018-04-01 00:00:00

abstract：:In congenital jaundice, which is due to defects of bilirubin gluruconidation, bilirubin is degraded by an alternative pathway into unidentified products. Previously, it was shown that plasma bilirubin levels can be decreased in rats with this defect by inducers of CYP1A enzymes. Here, liver microsomes from rats or mic...

journal_title：Biochemical pharmacology

authors： Zaccaro C,Sweitzer S,Pipino S,Gorman N,Sinclair PR,Sinclair JF,Nebert DW,De Matteis F

更新日期：2001-04-01 00:00:00

abstract：:The population growth rate of HeLa cells treated with 60 microM 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB) in reinforced Eagle's minimum essential medium was directly related to the concentration of fetal bovine serum in the range from 5 to 30%. Control cells proliferated at a maximal rate (doubling time: ...

journal_title：Biochemical pharmacology

authors： Tamm I

更新日期：1984-02-15 00:00:00

abstract：:Growing evidence suggests that hepatic-insulin resistance is sufficient to promote progression to cardiovascular disease. We have shown previously that liver-specific protein-tyrosine-phosphatase 1B (PTP1B) deficiency improves hepatic-insulin sensitivity and whole-body glucose homeostasis. The aim of this study was to...

journal_title：Biochemical pharmacology

authors： Agouni A,Tual-Chalot S,Chalopin M,Duluc L,Mody N,Martinez MC,Andriantsitohaina R,Delibegović M

更新日期：2014-12-15 00:00:00

abstract：:The cytotoxicity anti-tumour intercalating agents such as the anthraquinone mitoxantrone is thought to relate to DNA binding and the trapping of DNA topoisomerase II complexes on cellular DNA. We have studied the uptake, nuclear location, DNA binding mode and DNA damaging capacity of mitoxantrone in a small cell lung ...

journal_title：Biochemical pharmacology

authors： Smith PJ,Morgan SA,Fox ME,Watson JV

更新日期：1990-11-01 00:00:00

abstract：:Cytarabine (ara-C), a major antileukemic agent, is phosphorylated in the cell to cytarabine triphosphate (ara-CTP), which is then partly incorporated into DNA. The drug incorporation into DNA poisons the extending primer against further incorporation of deoxyribonucleotides including dCTP, ultimately inhibiting DNA sy...

journal_title：Biochemical pharmacology

authors： Yamauchi T,Ueda T

更新日期：2005-06-15 00:00:00

abstract：:The role of the intracellular messengers inositol 1,4,5-triphosphate (IP3) and protein kinase C (PKC) in the thrombin (3 U/mL)-induced contraction of endothelium-denuded porcine pulmonary arteries was investigated. Thrombin induced a sustained contractile response with an initial transient increase in IP3 to about 160...

journal_title：Biochemical pharmacology

authors： Bretschneider E,Paintz M,Glusa E

更新日期：1995-01-06 00:00:00

abstract：:Clinical use of fibrate hypolipidaemic agents has been associated with an increased incidence of hepatobiliary dysfunction including increased bile lithogenicity, gallstone formation, and cholestasis. The hepatic transport of bile acids plays an important role in bile formation and flow, and interference with the hepa...

journal_title：Biochemical pharmacology

authors： Sabordo L,Sallustio BC

更新日期：1997-07-01 00:00:00

abstract：:Although the induction of cytochromes P450 3A (CYP3A) is relatively well characterized in liver, its inducibility in an easily available tissue such as the peripheral leukocytes is not known. The purpose of this study was, therefore, to determine if CYP3A is inducible in vivo in peripheral leukocytes. Microsomes from ...

journal_title：Biochemical pharmacology

authors： Mahnke A,Roos PH,Hanstein WG,Chabot GG

更新日期：1996-06-14 00:00:00

abstract：:Desipramine (DMI) is an important antidepressant drug and a lysosomotropic substance. In cultured fibroblasts it interferes with lysosomal functions, e.g. phospholipid degradation. Chronic exposure of cells with DMI induces storage of phospholipids. Subcellular fractionations of cultured human fibroblasts that had bee...

journal_title：Biochemical pharmacology

authors： Stoffel P,Burkart T,Honegger UE,Wiesmann UN

更新日期：1987-03-01 00:00:00

abstract：:Two novel halogenated pyrrolopyrimidine analogues of adenosine, isolated from marine sources, have been examined for pharmacological and biochemical activities. 4-Amino-5-bromo-pyrrolo[2,3-d]pyrimidine, from a sponge of the genus Echinodictyum, had bronchodilator activity at least as potent as theophylline but with a ...

journal_title：Biochemical pharmacology

authors： Davies LP,Jamieson DD,Baird-Lambert JA,Kazlauskas R

更新日期：1984-02-01 00:00:00

abstract：:Uteroglobin, a steroid-dependent secretory protein first discovered in the rabbit uterus during early pregnancy, is a potent phospholipase A2 inhibitor. We found that uteroglobin also inhibited human and rabbit phagocyte chemotaxis in response to formyl peptide attractants in a dose-dependent manner. Half-maximal inhi...

journal_title：Biochemical pharmacology

authors： Vasanthakumar G,Manjunath R,Mukherjee AB,Warabi H,Schiffmann E

更新日期：1988-02-01 00:00:00

abstract：:Ethyl 2[5(4-chlorophenyl)pentyl]oxirane-2-carboxylate (POCA) is strongly hypoglycaemic in fasted normal and diabetic rats [H. P. O. Wolf, K. Eistetter and G. Ludwig, Diabetologia 22, 456 (1982)]. POCA was fed for 12 weeks to rats on a standard low-fat (3%) diet at levels of 0.05% and 0.2% to give daily intakes of abou...

journal_title：Biochemical pharmacology

authors： Koundakjian PP,Turnbull DM,Bone AJ,Rogers MP,Younan SI,Sherratt HS

更新日期：1984-02-01 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：:Tumor cells are more sensitive to methionine restriction than normal tissues, a phenomenon known as methionine auxotrophy. Previous studies showed that 5-fluorouracil and methionine restriction act synergistically against a variety of tumors. The purpose of the current studies was to determine the molecular mechanism(...

journal_title：Biochemical pharmacology

authors： Lu S,Chen GL,Ren C,Kwabi-Addo B,Epner DE

更新日期：2003-09-01 00:00:00

abstract：:Cancer develops through a series of genetic changes leading to malignant transformation. Numerous gene and pathways involved in stages of progression to frank malignancy have been elucidated. These genetic changes result in aberrations in fundamental cellular processes controlling proliferation, apoptosis, differentia...

journal_title：Biochemical pharmacology

authors： Pinkas J,Teicher BA

更新日期：2006-08-28 00:00:00

abstract：:The metabolism of tienilic acid, a drug containing a thiophene ring, was reinvestigated in man, rat and dog. The major urinary metabolite in man and rat was isolated and completely characterized by comparison with a synthetic compound. This metabolite derives from the hydroxylation of the thiophene ring of tienilic ac...

journal_title：Biochemical pharmacology

authors： Mansuy D,Dansette PM,Foures C,Jaouen M,Moinet G,Bayer N

更新日期：1984-05-01 00:00:00