Electrochemistry of flavonoids. Relationships between redox potentials, inhibition of mitochondrial respiration, and production of oxygen radicals by flavonoids.

abstract：:The abilities of lipophilic cannabinoid drugs to regulate adenylate cyclase activity in neuroblastoma cell membranes were analyzed by thermodynamic studies. Arrhenius plots of hormone-stimulated adenylate cyclase activity exhibited a break point at 20 degrees. The break point was reduced to 14 degrees by benzyl alcoho...

journal_title：Biochemical pharmacology

authors： Howlett AC,Scott DK,Wilken GH

更新日期：1989-10-01 00:00:00

abstract：:The identification of proliferation/survival pathways constitutively activated by genetic alterations in multiple myeloma (MM), or sustained by the bone marrow (BM) microenvironment, provides novel opportunities for the development of targeted therapies. The deregulated function of protein tyrosine kinases plays a cri...

journal_title：Biochemical pharmacology

authors： Cassinelli G,Ronchetti D,Laccabue D,Mattioli M,Cuccuru G,Favini E,Nicolini V,Greco A,Neri A,Zunino F,Lanzi C

更新日期：2009-11-01 00:00:00

abstract：:We have investigated the antitumor and apoptotic effects of 1, 25-dihydroxyvitamin D(3) (VD(3)) in glioma cell lines and in primary cultures derived from surgical specimens from patients. Our results showed that certain glioma cells underwent apoptosis, whereas others were resistant. In an attempt to search for parame...

journal_title：Biochemical pharmacology

authors： Zou J,Landy H,Feun L,Xu R,Lampidis T,Wu CJ,Furst AJ,Savaraj N

更新日期：2000-11-01 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：:An enzyme (NADPH-dependent diaphorase) present in rat brain microsomes has been solubilised and shown to utilise both nitrobluetetrazolium and cytochrome c as electron acceptors, when reduced by NADPH. The kinetics of the enzyme have been determined using cytochrome c (Km = 1.3 microM), NADPH (Km = 1.4 microM) and the...

journal_title：Biochemical pharmacology

authors： Kemp MC,Kuonen DR,Sutton A,Roberts PJ

更新日期：1988-08-15 00:00:00

abstract：:gamma-Carbolines are tricyclic aromatic compounds which intercalate into DNA base pairs and exhibit significant cytotoxic and antitumor activities. These compounds which are structurally related to ellipticine by deletion of an aromatic ring, induce DNA breaks in cultured L1210 cells. Since the mechanism of cytotoxic ...

journal_title：Biochemical pharmacology

authors： Fossé P,René B,Saucier JM,Nguyen CH,Bisagni E,Paoletti C

更新日期：1990-02-15 00:00:00

abstract：:The stereoselective binding of carprofen enantiomers and carprofen glucuronide diastereomers to human serum albumin (HSA) was studied using an ultrafiltration method. Carprofen glucuronides exhibit a considerable and stereoselective affinity to HSA, although less than that seen for the parent enantiomers. The (S)-gluc...

journal_title：Biochemical pharmacology

authors： Iwakawa S,Spahn H,Benet LZ,Lin ET

更新日期：1990-03-01 00:00:00

abstract：:The metabolism of (1R)[1-3H]ethanol, [2-3H]lactate or [2-3H]xylitol was studied in hepatocytes from fed or T3-treated rats in the presence or absence of fructose or xylitol. The yields of tritium in ethanol, lactate, water, glycerol and glucose were determined. A simple model, describing the metabolic fate of tritium ...

journal_title：Biochemical pharmacology

authors： Vind C,Grunnet N

更新日期：1985-03-01 00:00:00

abstract：:The formation of triacylglycerols containing fenoprofen was studied in rat isolated adipocytes and hepatocytes incubated with [3H]glycerol and R or S fenoprofen. In both hepatocytes and adipocytes there was a high-affinity enzymatic process for the synthesis of triacylglycerol containing fenoprofen which was stereospe...

journal_title：Biochemical pharmacology

authors： Sallustio BC,Meffin PJ,Knights KM

更新日期：1988-05-15 00:00:00

abstract：:Interferon and interferon inducers are well known to depress the cytochrome P450-dependent hepatic mixed-function oxidase system and cause a decrease in the capacity of the liver to metabolize drugs and xenobiotics. In this study we have shown that the interferon-mediated changes in an induced form of hepatic cytochro...

journal_title：Biochemical pharmacology

authors： Knickle LC,Spencer DF,Renton KW

更新日期：1992-08-04 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：:Spider venoms are replete with peptidic ion channel modulators, often with novel subtype selectivity, making them a rich source of pharmacological tools and drug leads. In a search for subtype-selective blockers of voltage-gated calcium (CaV) channels, we isolated and characterized a novel 39-residue peptide, ω-TRTX-C...

journal_title：Biochemical pharmacology

authors： Klint JK,Berecki G,Durek T,Mobli M,Knapp O,King GF,Adams DJ,Alewood PF,Rash LD

更新日期：2014-05-15 00:00:00

abstract：:A series of fucoidan [sulfated poly(L-fucopyranose)] derivatives were prepared by chemical sulfation and desulfation, and they were tested for their abilities to stimulate tissue plasminogen activator (t-PA)-catalyzed plasminogen activation, clot lysis, and the inhibition of fibrin polymer formation. The magnitude of ...

journal_title：Biochemical pharmacology

authors： Soeda S,Sakaguchi S,Shimeno H,Nagamatsu A

更新日期：1992-04-15 00:00:00

abstract：:The regulation of tissue transglutaminase (TG2) activity by the GPCR family is poorly understood. In this study, we investigated the modulation of TG2 activity by the A1 adenosine receptor in cardiomyocyte-like H9c2 cells. H9c2 cells were lysed following stimulation with the A1 adenosine receptor agonist N(6)-cyclopen...

journal_title：Biochemical pharmacology

authors： Vyas FS,Hargreaves AJ,Bonner PL,Boocock DJ,Coveney C,Dickenson JM

更新日期：2016-05-01 00:00:00

abstract：:Cell based studies have suggested that the diabetes drug metformin may combine with the anaplastic lymphoma kinase receptor (ALK) inhibitor crizotinib to increase ALK positive lung cancer cell killing and overcome crizotinib resistance. We therefore tested metformin alone and in combination with crizotinib in vivo, by...

journal_title：Biochemical pharmacology

authors： Bland AR,Shrestha N,Bower RL,Rosengren RJ,Ashton JC

更新日期：2021-01-01 00:00:00

abstract：:We employed both [5-3H] ara-C and ([2-14C] ara-C labeled L1210 DNA for analysis following exposure to alkali under various conditions. The results demonstrated that the tritium label on C5 of ara-C molecules incorporated in DNA was exchanged with water under alkaline conditions and, therefore, radioactivity was subseq...

journal_title：Biochemical pharmacology

authors： Major PP,Egan EM,Herrick D,Kufe DW

更新日期：1982-03-01 00:00:00

abstract：:Chiral inversion at a sulphoxide position of flosequinan enantiomers [(+/-)-7-fluoro-1-methyl-3-methylsulphinyl-4-quinolone] occurred in conventional rats but not in either germ-free rats or rats treated with antibiotics after an oral administration of each enantiomer. Thus, it was postulated that the chiral inversion...

journal_title：Biochemical pharmacology

authors： Kashiyama E,Yokoi T,Todaka T,Odomi M,Kamataki T

更新日期：1994-07-19 00:00:00

abstract：:Acute respiratory distress syndrome threatens public health with high morbidity and mortality due to ineffective intervention whereby lipopolysaccharide (LPS) induced acute lung injury (ALI) in mice provides a research model. The seeds of Euphorbia lathyris L. have a long history of usage in Traditional Chinese Medici...

journal_title：Biochemical pharmacology

authors： Zhang Q,Zhu S,Cheng X,Lu C,Tao W,Zhang Y,William BC,Cao X,Yi S,Liu Y,Zhao Y,Luo Y

更新日期：2018-09-01 00:00:00

abstract：:The development of pharmacological and biological inhibitors of receptor tyrosine kinases (RTKs) has changed the treatment paradigm of several neoplastic diseases. However, the occurrence of intrinsic and acquired resistance represents a limit to the efficacy of these drugs even in RTK-addicted cancers. The identifica...

journal_title：Biochemical pharmacology

authors： Lanzi C,Cassinelli G

更新日期：2020-08-01 00:00:00

abstract：:The effects on metabolism of the fluorinated dicarboxylic acid, perfluorosuccinate, were examined in hepatocytes from fasted rats. Perfluorosuccinate (5 mM) inhibited gluconeogenesis from lactate by 80% and from pyruvate by 40%. Significant inhibition (up to 30%) occurred at a concentration of perfluorosuccinate of 50...

journal_title：Biochemical pharmacology

authors： Gregory RB,Berry MN

更新日期：1989-09-01 00:00:00

abstract：:The effect of ethanol abuse on the lipid ordering of the human erythrocyte membranes was studied by steady-state and time-resolved fluorescence anisotropy measurements of DPH and its polar analogue TMA-DPH, which probe different membrane regions. Steady-state anisotropy values with DPH as a probe were slightly but sig...

journal_title：Biochemical pharmacology

authors： Beaugé F,Gallay J,Stibler H,Borg S

更新日期：1988-10-15 00:00:00

abstract：:Radioligand binding techniques are commonly used in the characterization of beta-adrenergic receptors on human peripheral leukocytes. Accurate interpretation of receptor binding parameters necessitates appropriate radioligand selection. In addition, cell isolation techniques should have minimal effect on the binding p...

journal_title：Biochemical pharmacology

authors： Szefler SJ,Edwards CK 3rd,Haslett C,Zahniser NR,Miller JA,Henson PM

更新日期：1987-05-15 00:00:00

abstract：:Isothiazole dioxides have been shown to inhibit Trypanosoma brucei protein farnesyltransferase (PFTase) in isolated enzyme, but elicited only a minor effect on mammalian PFTase. In the present study we have evaluated the effect of 3-diethylamino-4-(4-methoxyphenyl)-isothiazole 1,1-dioxides with different substituents ...

journal_title：Biochemical pharmacology

authors： Ferri N,Clerici F,Yokoyama K,Pocar D,Corsini A

更新日期：2005-12-05 00:00:00

abstract：:Studies were performed to characterise the phospholipase A2 (PLA2) responsible for the greatly increased capacity to release arachidonic acid (AA) of dimethyl sulphoxide (DMSO) differentiated U937 monocytic cells compared to undifferentiated cells (18-fold increase in response to Ca2+ ionophore A23187). Cytosolic PLA2...

journal_title：Biochemical pharmacology

authors： Withnall MT,Pennington A,Wiseman D

更新日期：1995-11-27 00:00:00

abstract：:Activation of protein kinase C (PKC) has been suggested to play a role in bone resorption. However, phorbol esters, which activate PKC, have been reported to have both stimulatory and inhibitory effects on bone resorption. To study the role of PKC in bone resorption further, we have measured calcium release elicited b...

journal_title：Biochemical pharmacology

authors： Lee SK,Stern PH

更新日期：2000-10-01 00:00:00

abstract：:Incubation of adriamycin resistant Chinese hamster lung cells with the calmodulin inhibitor trifluoperazine (TFP) resulted in a significant increase in the cellular accumulation of drug. When resistant cells were prelabeled with 32Pi and then treated with TFP, a major increase also occurred in the phosphorylation of a...

journal_title：Biochemical pharmacology

authors： Center MS

更新日期：1985-05-01 00:00:00

abstract：:The effects of schisanhenol (Sal) on Adriamycin (ADM)-induced rat heart mitochondrial toxicity in vitro were investigated. Malondialdehyde formation, lysis, disintegration and membrane rigidification in mitochondria treated with ADM were reduced significantly by Sal. In the electron spin resonance studies, Sal did not...

journal_title：Biochemical pharmacology

authors： Lin TJ,Liu GT,Pan Y,Liu Y,Xu GZ

更新日期：1991-10-09 00:00:00

abstract：:The interrelated signaling via TGF-beta1 and reactive oxygen species has a profound impact on fibrogenesis and is therefore selected as target for antifibrotic therapies. This prompted us to investigate the influence of the antioxidant N-acetyl-L-cysteine on TGF-beta signaling in culture-activated hepatic stellate cel...

journal_title：Biochemical pharmacology

authors： Meurer SK,Lahme B,Tihaa L,Weiskirchen R,Gressner AM

更新日期：2005-10-01 00:00:00

abstract：:A nuclear envelope-associated epoxide hydrolase in mouse liver that hydrates trans-stilbene oxide has been identified and characterized. This epoxide hydrolase is distinct from the enzyme in nuclear envelopes that hydrates benzo[a]pyrene 4,5-oxide and other arene oxides. This distinction was demonstrated by the criter...

journal_title：Biochemical pharmacology

authors： Guenthner TM

更新日期：1986-10-01 00:00:00

abstract：:Milrinone [2-methyl-5-cyano-(3,4'-bipyridin)-6(1H)-one] is a positive cardiac inotropic agent recently shown to have thyromimetic activity in vitro in a rabbit myocardial membrane Ca2+-ATPase system [K. M. Mylotte et al., Proc. natn. Acad. Sci. U.S.A. 82, 7974 (1985)]. In the present studies, milrinone was examined fo...

journal_title：Biochemical pharmacology

authors： Davis PJ,Cody V,Davis FB,Warnick PR,Schoenl M,Edwards L

更新日期：1987-11-01 00:00:00