Ursolic acid promotes the release of macrophage migration inhibitory factor via ERK2 activation in resting mouse macrophages.

abstract：:A method to evaluate interactions between biologically active agents is presented. Synergism, zero interaction, and antagonism were easily detected with the three-dimensional approach proposed herein. This method is compatible with a checkerboard design to diagnose the interaction between agents and obviate the need t...

journal_title：Biochemical pharmacology

authors： Martinez-Irujo JJ,Villahermosa ML,Alberdi E,Santiago E

更新日期：1996-03-08 00:00:00

abstract：:The chemotherapeutic drug cisplatin is an important treatment for many types of solid tumours, in particular non-small cell lung cancer (NSCLC). Platinum(IV) complexes offer several advantages to cisplatin due to their requirement for reduction to the active platinum(II) form to elicit cytotoxicity. This should minimi...

journal_title：Biochemical pharmacology

authors： Mellor HR,Snelling S,Hall MD,Modok S,Jaffar M,Hambley TW,Callaghan R

更新日期：2005-10-15 00:00:00

abstract：:1-(3'-Chlorophenyl)-3-[2-(3,3-dimethyl-1-azetidinyl)ethyl] imidazolidin-2-one, zetidoline, a new neuroleptic agent, when incubated with rat liver microsomes was rapidly metabolized to six free (mets B, D, I, L, M and N) and two conjugated metabolites (mets E and F). Sites of the metabolic attack (oxidation) were prima...

journal_title：Biochemical pharmacology

authors： Assandri A,Galliani G,Zerilli L,Tuan G,Tarzia G,Barone D

更新日期：1986-05-01 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：BACKGROUND:Flavonoids form a diverse class of naturally occurring polyphenols ascribed various biological activities, including inhibition of amyloid β (Aβ) fibrillisation and neurotoxicity of relevance to Alzheimer's disease. Cannabis contains a unique subset of prenylated flavonoids, the cannflavins. While selected c...

journal_title：Biochemical pharmacology

authors： Eggers C,Fujitani M,Kato R,Smid S

更新日期：2019-11-01 00:00:00

abstract：:Resveratrol, a natural phytoalexin that shows health-promoting benefits, is an inhibitor of store-operated calcium entry (SOCE). Knowledge of the molecular mechanism underlying this inhibition is required for the proper design of therapies that include resveratrol or related stilbenoids, but remains largely unknown. T...

journal_title：Biochemical pharmacology

authors： Casas-Rua V,Alvarez IS,Pozo-Guisado E,Martín-Romero FJ

更新日期：2013-12-01 00:00:00

abstract：:A newly synthesized compound, 2-[N-(2-aminoethyl)-N-(5-isoquinolinesulfonyl)]amino-N-(4-chlorocinnamyl )-N-methylbenzylamine (CKA-1306), was found to inhibit cyclic AMP-dependent protein kinase (PKA) and Ca2+/calmodulin-dependent protein kinase I (CaMK I) with IC50 values of 1.6+/-0.14 and 2.5+/-0.16 microM, respectiv...

journal_title：Biochemical pharmacology

authors： Sakaguchi H,Yokokura H,Terada O,Naito Y,Nimura Y,Hidaka H

更新日期：1998-08-01 00:00:00

abstract：:The (Na+ + K+)-ATPase is localized to the cerebral endothelium, i.e. the blood-brain barrier, and is important for the maintenance of the brain electrolyte environment. Data from the present study indicate that Pb2+ inhibits the binding of [3H]ouabain to the cerebral microvascular (Na+ + K+)-ATPase in a time- and dose...

journal_title：Biochemical pharmacology

authors： Caspers ML,Kwaiser TM,Grammas P

更新日期：1990-06-15 00:00:00

abstract：:Local anaesthetics and opioid drugs function synergistically to provide analgesia. In the present study, the nature of this synergy has been investigated using in vitro radioligand binding to determine whether the local anaesthetics bupivacaine and tetracaine modulate the binding of two kappa-opioid receptor ligands, ...

journal_title：Biochemical pharmacology

authors： Fraser GL,Fowler CJ

更新日期：1995-03-30 00:00:00

abstract：:The antitumor activity of 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) has been shown previously to be enhanced markedly by the co-administration of pyrimidine deoxyribonucleosides (Lin and Prusoff, Cancer Res 47: 394-397, 1987). In the present study, we examined the cellular mechanisms underlying the augmentation effe...

journal_title：Biochemical pharmacology

authors： Poo WJ,Guo X,Haslund B,Mozdziesz DE

更新日期：1997-03-07 00:00:00

abstract：:The effect of the calcium channel blocker verapamil (VRP) on the accumulation and retention of vincristine (VCR) has been examined in mice bearing xenografts of human rhabdomyosarcomas. The tumors were Rh18, moderately sensitive to VCR, and its subline, Rh18/VCR3, selected in vivo for primary resistance to VCR. Admini...

journal_title：Biochemical pharmacology

authors： Horton JK,Thimmaiah KN,Houghton JA,Horowitz ME,Houghton PJ

更新日期：1989-06-01 00:00:00

abstract：:Novel therapies for the treatment of solid tumors have generally failed to improve patient overall survival. These therapeutic approaches are typically focused on targeting signaling pathways implicated in cell growth and/or survival in order to shrink the malignant mass and achieve an objective clinical response; how...

journal_title：Biochemical pharmacology

authors： Winquist RJ,Boucher DM,Wood M,Furey BF

更新日期：2009-08-15 00:00:00

abstract：:The effects of beta 1- and beta 1 + beta 2-antagonists on the myocardial adaptation to exercise training were investigated in male Sprague-Dawley rats randomly divided into trained (treadmill, 1 hr/day, 5 days/week for 10 weeks at 27 m/min, 15% grade) without drug (TC), sedentary without drug (SC), trained treated wit...

journal_title：Biochemical pharmacology

authors： Ji LL,Stratman FW,Lardy HA

更新日期：1987-10-15 00:00:00

abstract：:Induction of cytosolic long-chain acyl-CoA hydrolases was investigated in rat liver after administration of various peroxisome proliferators and related compounds. Treatment of rats with di-(2-ethylhexyl)-phthalate, di-(2-ethylhexyl)-adipate or tiadenol induced hydrolases I and II, while acetylsalicylic acid induced o...

journal_title：Biochemical pharmacology

authors： Katoh H,Nakajima S,Kawashima Y,Kozuka H,Uchiyama M

更新日期：1984-04-01 00:00:00

abstract：:An imbalance of T helper cell type 1 (Th1) versus type 2 (Th2) polarization in favor of Th1 cell subsets appears to be a key pathogenic mechanism in chronic inflammatory bowel disease (IBD), in particular in Crohn's disease. The interferon gamma-inducing factor interleukin (IL)-18 acts in strong synergism with the Th1...

journal_title：Biochemical pharmacology

authors： Siegmund B

更新日期：2002-07-01 00:00:00

abstract：:Calcium signaling robustly inhibits AC6 activity in membrane preparations and in intact cells via capacitative calcium entry (CCE). However, the release of intracellular calcium has not been demonstrated to robustly alter AC6 signaling and activation of Galpha(q)-coupled receptors in tissues that express AC6 enhances ...

journal_title：Biochemical pharmacology

authors： Beazely MA,Watts VJ

更新日期：2005-07-01 00:00:00

abstract：:Sustained activation of AMP-activated protein kinase (AMPK) induces apoptosis in several cell types. In pancreatic beta cells this occurs under glucose limitation, or in the presence of the pharmacological AMPK activator 5-aminoimidazole-4-carboxamide-riboside (AICAR). It is unknown whether Akt activation can countera...

journal_title：Biochemical pharmacology

authors： Cai Y,Wang Q,Ling Z,Pipeleers D,McDermott P,Pende M,Heimberg H,Van de Casteele M

更新日期：2008-05-15 00:00:00

abstract：:Certain anticonvulsant drugs require N-acetylation as a major route of metabolic clearance. Single point mutations of the polymorphic N-acetyltransferase gene (pNAT) are the primary cause for impaired drug acetylation. Pharmacokinetic parameters are altered in slow acetylator phenotypes and this may compromise drug sa...

journal_title：Biochemical pharmacology

authors： Borlak JT,Harsany V,Schneble H,Haegele KD

更新日期：1994-11-01 00:00:00

abstract：:Cobalt is suspected to cause memory deficit in humans and was reported to induce neurotoxicity in animal models. We have studied the effects of cobalt in primary cultures of mouse astrocytes. CoCl(2) (0.2-0.8mM) caused dose-dependent ATP depletion, apoptosis (cell shrinkage, phosphatidylserine externalization and chro...

journal_title：Biochemical pharmacology

authors： Karovic O,Tonazzini I,Rebola N,Edström E,Lövdahl C,Fredholm BB,Daré E

更新日期：2007-03-01 00:00:00

abstract：:Human CYP2A6 is a cytochrome P450 (CYP) isoform responsible for the metabolism of nicotine, coumarin, tegafur, and valproic acid, and metabolic activation of nitrosamines. Genetic polymorphisms of the CYP2A6 gene are a major causal factor of the large interindividual differences in nicotine metabolism. In the present ...

journal_title：Biochemical pharmacology

authors： Fukami T,Nakajima M,Higashi E,Yamanaka H,McLeod HL,Yokoi T

更新日期：2005-09-01 00:00:00

abstract：:A series of trifluoromethanesulfonamides (TFMS) was synthesized and tested for uncoupling activity in rat liver mitochondria. With succinate as the mitochondrial substrate, and the respiratory control index (RCI) as an indicator of their uncoupling ability, we found that all of the TFMS tested were uncouplers of oxida...

journal_title：Biochemical pharmacology

authors： McCracken RO,Carr AW,Stillwell WH,Lipkowitz KB,Boisvenue R,O'Doherty GO,Wickiser DI

更新日期：1993-05-05 00:00:00

abstract：:Current evidence demonstrates that protein kinase C (PKC) belongs to a group of cell-signaling molecules that are sensitive targets for redox modifications and functional alterations that mediate oxidant-induced cellular responses. Our studies have demonstrated that diminished intracellular GSH was associated to inact...

journal_title：Biochemical pharmacology

authors： Domenicotti C,Marengo B,Nitti M,Verzola D,Garibotto G,Cottalasso D,Poli G,Melloni E,Pronzato MA,Marinari UM

更新日期：2003-10-15 00:00:00

abstract：:The glutathione-glutathione peroxidase system is an important defense against oxidative stress. The ability of this system to protect against iron-catalyzed microsomal production of hydroxyl radicals [oxidation of 4-methylmercapto-2-oxo-butyrate (KMBA)] and lipid peroxidation was evaluated. When rat liver cytosol was ...

journal_title：Biochemical pharmacology

authors： Beloqui O,Cederbaum AI

更新日期：1986-08-15 00:00:00

abstract：:Members of the homologous series of nine antitumour dimethanesulphonic acid esters, with the exception of ethylene dimethanesulphonate (EDMS), were found to cause DNA-DNA interstrand crosslinking in cells derived from the transplantable rodent Yoshida lymphosarcoma. The ability of the series to induce interstrand cros...

journal_title：Biochemical pharmacology

authors： Bedford P,Fox BW

更新日期：1983-08-01 00:00:00

abstract：:Uptake of two ellipticine derivatives, 2-N-methyl-ellipticinium (NME) and 2-N-methyl-9-hydroxy-ellipticinium, by sensitive and resistant Chinese hamster lung cells was studied. The results show that uptake and retention of these molecules by both types of cells were identical, thus indicating that the resistance to el...

journal_title：Biochemical pharmacology

authors： Charcosset JY,Salles B,Jacquemin-Sablon A

更新日期：1983-03-15 00:00:00

abstract：:The human ether-a-go-go-related gene (hERG) encodes the rapidly activating, delayed rectifier potassium channel (IKr) important for cardiac repolarization. Dysfunction of the hERG channel can cause Long QT Syndrome (LQTS). A wide variety of structurally diverse therapeutic compounds reduce the hERG current by acute di...

journal_title：Biochemical pharmacology

authors： Zhang Y,Dong Z,Jin L,Zhang K,Zhao X,Fu J,Gong Y,Sun M,Yang B,Li B

更新日期：2013-01-01 00:00:00

abstract：:Net cadmium uptake in the isolated perfused rat liver was half-maximal at 5 microM, and the maximal rate of uptake was 22 nmoles/min per gram liver wet weight. Uptake was augmented when a permeable thiol, dithioerythritol, was infused, whereas it was restricted when glutathione as a nonpermeable thiol or also when bov...

journal_title：Biochemical pharmacology

authors： Graf P,Sies H

更新日期：1984-02-15 00:00:00

abstract：:Elongator, a multi-subunit complex assembled by the IkappaB kinase-associated protein (IKAP)/hELP1 scaffold protein is involved in transcriptional elongation in the nucleus as well as in tRNA modifications in the cytoplasm. However, the biological processes regulated by Elongator in human cells only start to be elucid...

journal_title：Biochemical pharmacology

authors： Cornez I,Creppe C,Gillard M,Hennuy B,Chapelle JP,Dejardin E,Merville MP,Close P,Chariot A

更新日期：2008-06-01 00:00:00

abstract：:Pelargonidin is a natural red pigment found in fruits and vegetables, and has been reported to exhibit various effects potentially beneficial for human health. However, the possible preventive effects of pelargonidin toward atherosclerosis and mechanisms involved have not been investigated to date. Here, we compared t...

journal_title：Biochemical pharmacology

authors： Son JE,Jeong H,Kim H,Kim YA,Lee E,Lee HJ,Lee KW

更新日期：2014-05-15 00:00:00

abstract：:Human red blood cells and male Sprague-Dawley rats were treated in vitro and in vivo, respectively, with phenylhydrazine in order to determine whether the release of volatile hydrocarbons can serve as a suitable index for phenylhydrazine-induced red blood cell peroxidation. Lipid peroxidation following phenylhydrazine...

journal_title：Biochemical pharmacology

authors： Clemens MR,Remmer H,Waller HD

更新日期：1984-06-01 00:00:00