Suppressive effect of biscoclaurine alkaloids on agonist-induced activation of phospholipase A2 in rabbit platelets.


:The effect of biscoclaurine (bisbenzylisoquinoline) alkaloids on phospholipase A2 and C activation in signal transduction system of rabbit platelet was studied. Isotetrandrine, cepharanthine and berbamine inhibited the aggregation induced by collagen but not by other stimuli such as thrombin and arachidonic acid, while tetrandrine equally inhibited the aggregation by any of these agonists. All these four alkaloids suppressed arachidonic acid liberation in response to collagen or thrombin, but not diacylglycerol formation and increase in cytoplasmic Ca2+ concentration in response to thrombin or arachidonic acid. In saponin-permeabilized platelets, they also suppressed arachidonic acid liberation induced by an addition of both GTP gamma S and Ca2+, whereas the liberation induced by an addition of Ca2+ alone was not prevented by them. These data suggest that isotetrandrine, cepharanthine and berbamine have a rather specific potency to suppress the phospholipase A2 activation by a mechanism other than direct inhibition of the enzyme or interference with the ligand-receptor interaction. They seem, at least in part, to exert the effect on the GTP-binding protein-phospholipase A2 complex in the platelet signal transduction system. In contrast, tetrandrine appears to inhibit a step following an increase in cytosolic free Ca2+ concentration in the agonist-induced signal transduction system, in addition to suppressing the phospholipase A2 activation.


Biochem Pharmacol


Biochemical pharmacology


Hashizume T,Yamaguchi H,Sato T,Fujii T




Has Abstract


1991-02-01 00:00:00














  • Increased Na+/K(+)-pump activity and adenosine triphosphate utilization after compound 48/80-induced histamine secretion from rat mast cells.

    abstract::The Na+/K(+)-pump activity and the utilization of adenosine triphosphate (ATP) were studied in rat peritoneal mast cells after histamine secretion induced by compound 48/80. We measured the ouabain-sensitive K(+)-uptake by a radioactive technique (86Rb+). The ATP content and the glycolytic ATP-production were measured...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Johansen T,Praetorius H

    更新日期:1994-05-18 00:00:00

  • Mechanism for Helicobacter pylori stimulation of interleukin-8 production in a gastric epithelial cell line (MKN 28): roles of mitogen-activated protein kinase and interleukin-1beta.

    abstract::Although it is known that the pathogenic mechanism of Helicobacter pylori involves the stimulated production of interleukin-8 (IL-8) as an inflammatory mediator, the details of the pathway remain unclear. The role of mitogen-activated protein kinase (MAPK) in IL-8 production by H. pylori has been examined in an in vit...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yamada H,Aihara T,Okabe S

    更新日期:2001-06-15 00:00:00

  • Induction of human breast cancer cell apoptosis from G2/M preceded by stimulation into the cell cycle by Z-1,1-dichloro-2,3-diphenylcyclopropane.

    abstract::We have shown previously that Z-1,1-dichloro-2,3-diphenylcyclopropane (a.k.a. Analog II, A(II)) inhibits human breast cancer cell proliferation regardless of estrogen receptor status or estrogen sensitivity, and that its cellular targets include microtubules. In the present study, we investigated the apoptosis-inducin...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Balachandran R,ter Haar E,Yalowich JC,Welsh MJ,Grant SG,Day BW

    更新日期:1999-01-01 00:00:00

  • Decreased polyphenol transport across cultured intestinal cells by a salivary proline-rich protein.

    abstract::Tannins are polyphenols commonly found in plant-derived foods. When ingested they can have various harmful effects, but salivary proline-rich proteins (PRPs) may provide protection against dietary tannins. The aim of this study was to investigate whether basic PRPs, a major family of salivary proteins, can prevent int...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Cai K,Hagerman AE,Minto RE,Bennick A

    更新日期:2006-05-28 00:00:00

  • 5-Substituted-2,2'-anhydrouridines, potent inhibitors of uridine phosphorylase.

    abstract::5-Substituted-2,2'-anhydrouridines are a new class of competitive inhibitors of uridine phosphorylase. The most potent member of the series is 2,2'-anhydro-5-ethyluridine with an apparent Ki value of 25 nM. These compounds are selective inhibitors of uridine phosphorylase and have no effect on thymidine phosphorylase....

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Veres Z,Szabolcs A,Szinai I,Dénes G,Kajtár-Peredy M,Otvös L

    更新日期:1985-05-15 00:00:00

  • Thromboxane A2 synthase inhibition and thromboxane A2 receptor blockade by 2-[(4-cyanophenyl)amino]-3-chloro-1,4-naphthalenedione (NQ-Y15) in rat platelets.

    abstract::The effects of 2-[(4-acetylphenyl)amino]-3-chloro-1,4-naphthalenedione (NQ-Y15), a synthetic 1,4-naphthoquinone derivative, on platelet activity and its mechanism of action were investigated. NQ-Y15 caused a concentration-dependent inhibition of the aggregation induced by thrombin, collagen, arachidonic acid (AA), and...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Chang TS,Kim HM,Lee KS,Khil LY,Mar WC,Ryu CK,Moon CK

    更新日期:1997-07-15 00:00:00

  • Chiral inversion of drug: role of intestinal bacteria in the stereoselective sulphoxide reduction of flosequinan.

    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

    pub_type: 杂志文章


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

    更新日期:1994-07-19 00:00:00

  • Inhibition of glutathione peroxidase and glutathione transferase in mouse liver by misonidazole.

    abstract::The mechanisms of toxicity and sensitization by the radiosensitizer misonidazole [1-(2-nitro-1-imidazolyl)-3-methoxy-2-propanol] are not well understood. We report here on the inhibition of total glutathione peroxidase (GSHPx), selenium-dependent glutathione peroxidase (selenium-GSHPx) and glutathione transferase (GSH...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Kumar KS,Weiss JF

    更新日期:1986-09-15 00:00:00

  • Inhibition of calmodulin-activated cyclic nucleotide phosphodiesterase: multiple binding-sites for tricyclic drugs on calmodulin.

    abstract::A cyclic nucleotide phosphodiesterase from guinea-pig heart is activated by calmodulin in the presence of calcium ions. Activation was measured over a range of calmodulin concentrations, and is antagonised by several tricyclic psychotropic drugs including trifluoperazine, imipramine, chlorpromazine and amitriptyline. ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Reynolds CH,Claxton PT

    更新日期:1982-02-01 00:00:00

  • Irreversible inhibition of S-adenosylmethionine decarboxylase in Plasmodium falciparum-infected erythrocytes: growth inhibition in vitro.

    abstract::Blocking spermidine and spermine synthesis in Plasmodium falciparum-infected erythrocytes with irreversible inhibitors of S-adenosylmethionine decarboxylase (AdoMet DC; EC, prevented the growth of the parasite in vitro. The most potent of these compounds, MDL 73811, inhibited growth of chloroquine-sensitive ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wright PS,Byers TL,Cross-Doersen DE,McCann PP,Bitonti AJ

    更新日期:1991-06-01 00:00:00

  • Curcumin induces electrical activity in rat pancreatic beta-cells by activating the volume-regulated anion channel.

    abstract::Curcumin, the principal active component of turmeric, is reported to exert a number of therapeutic actions, including a hypoglycaemic/antidiabetic action. The underlying mechanisms to this action are essentially unknown. We have investigated the hypothesis that a direct stimulatory action on the pancreatic beta-cell c...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Best L,Elliott AC,Brown PD

    更新日期:2007-06-01 00:00:00

  • Activation of misonidazole by rat liver microsomes and purified NADPH-cytochrome c reductase.

    abstract::Rat liver microsomes and purified NADPH-cytochrome c reductase metabolized [14C]misonidazole anaerobically to a reactive intermediate that covalently binds to tissue macromolecules. Air strongly inhibited the binding whereas carbon monoxide had no effect, indicating that misonidazole is activated via reduction and not...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: McManus ME,Lang MA,Stuart K,Strong J

    更新日期:1982-02-15 00:00:00

  • Induction of cytochrome P-450 by alcohols and 4-substituted pyrazoles. Comparison of structure-activity relationships.

    abstract::A comparison was made between 4-substituted pyrazoles and short-chain alcohols as inducers of cytochrome P-450. A quantitative structure-activity analysis of the data led to the following equations: (I) Pyrazoles: Log 1/C = 0.85 (+/- 0.21) Log P + 1.93 (+/- 0.38), r = 0.970 (II) Alcohols: Log 1/C = 0.78 (+/- 0.14) Log...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sinclair J,Cornell NW,Zaitlin L,Hansch C

    更新日期:1986-02-15 00:00:00

  • Beta tubulin affects the aryl hydrocarbon receptor function via an Arnt-mediated mechanism.

    abstract::We have been studying the requirement for the aryl hydrocarbon receptor nuclear translocator (Arnt)-dependent DNA complex formation, which precedes the activation of gene transcription. Using DEAE chromatography, we have obtained a Sf9 insect fraction F5 that is highly enriched with beta-tubulin. F5 inhibits the forma...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Zhang T,Wang X,Shinn A,Jin J,Chan WK

    更新日期:2010-04-15 00:00:00

  • Enhanced DNA excision repair in CCRF-CEM cells resistant to 1,3-bis(2-chloroethyl)-1-nitrosourea, quantitated using the single cell gel electrophoresis (Comet) assay.

    abstract::Enhanced DNA repair activity is important for the development of cellular resistance to alkylating agents. Here, we quantitated the kinetics of DNA excision repairs initiated by 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) in human leukemia CCRF-CEM cells. CEM cells that had been established resistant to BCNU (CEM-R) w...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yamauchi T,Kawai Y,Ueda T

    更新日期:2003-09-15 00:00:00

  • Chloroacetaldehyde-induced hepatocyte cytotoxicity. Mechanisms for cytoprotection.

    abstract::2-Chloroacetaldehyde (CAA)-induced cytotoxicity in isolated hepatocytes was enhanced markedly if hepatocyte alcohol or aldehyde dehydrogenase was inhibited prior to CAA addition. Hepatocyte GSH depletion, ATP depletion and lipid peroxidation by CAA were also enhanced markedly. Furthermore, CAA was about 10- and 70-fol...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sood C,O'Brien PJ

    更新日期:1994-08-30 00:00:00

  • Induction of human neutrophil apoptosis by nitric oxide donors: evidence for a caspase-dependent, cyclic-GMP-independent, mechanism.

    abstract::This study investigated the regulatory effects of the major inflammatory mediator, nitric oxide (NO), on human neutrophil apoptosis in vitro. Co-culture of human neutrophils with the NO donors GEA 3162 (1,2,3,4-oxatriazolium,5-amino-3-(3,4-dichlorophenyl)-chloride) (10-100 microM) and 3-morpholino-sydnonimine (SIN-1) ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ward C,Wong TH,Murray J,Rahman I,Haslett C,Chilvers ER,Rossi AG

    更新日期:2000-02-01 00:00:00

  • Innovative treatment programs against cancer: II. Nuclear factor-kappaB (NF-kappaB) as a molecular target.

    abstract::Nuclear factor-kappaB (NF-kappaB) activity affects cell survival and determines the sensitivity of cancer cells to cytotoxic agents as well as to ionizing radiation. Preventing the protective function of NF-kappaB may result in chemo- and radio-sensitization of cancer cells. Therefore, NF-kappaB has emerged as one of ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Waddick KG,Uckun FM

    更新日期:1999-01-01 00:00:00

  • Allosteric effects of antagonists on signalling by the chemokine receptor CCR5.

    abstract::Antagonists of the chemokine receptor, CCR5, may provide important new drugs for the treatment of HIV-1. In this study we have examined the mechanism of action of two functional antagonists of the chemokine receptor CCR5 (UK-396,794, UK-438,235) in signalling and internalisation assays using CHO cells expressing CCR5....

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Haworth B,Lin H,Fidock M,Dorr P,Strange PG

    更新日期:2007-09-15 00:00:00

  • Prostaglandin synthetase catalyzed activation of paracetamol.

    abstract::Prostaglandin synthetase has the ability to catalyze the metabolism of paracetamol to a reactive metabolite, which binds to protein and reduced glutathione (GSH). This was demonstrated with microsomes isolated from both sheep seminal vesicles (SSV) and rabbit kidney medulla. The activation of paracetamol occurred thro...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Moldéus P,Andersson B,Rahimtula A,Berggren M

    更新日期:1982-04-01 00:00:00

  • Drug metabolism in cirrhosis. Selective changes in cytochrome P-450 isozymes in the choline-deficient rat model.

    abstract::The effect of a choline-deficient diet on microsomal cytochrome P-450 and mixed-function oxidase (MFO) activity was investigated in relation to the development of nutritional cirrhosis. In rats that received the choline-deficient diet for 28 weeks cirrhosis was evident macroscopically and histologically; control rats ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Murray M,Zaluzny L,Farrell GC

    更新日期:1986-06-01 00:00:00

  • Regulation of expression and function of m2 and m4 muscarinic receptors in cultured embryonic chick heart cells by transforming growth factor-beta 1.

    abstract::Incubation of cultured embryonic chicken heart cells with transforming growth factor beta 1 (TGF-beta 1) resulted in a concentration- and time-dependent decrease in the number of muscarinic acetylcholine receptors (mAChR), which reached a maximum by 24 hr. Twenty-four hours following TGF-beta 1 treatment, cm2 and cm4 ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Jackson DA,Nathanson NM

    更新日期:1997-08-15 00:00:00

  • Effect of okadaic acid on immunologic and non-immunologic histamine release in rat mast cells.

    abstract::We have studied the effect of the protein phosphatase (PP) inhibitor, okadaic acid (OKA) on histamine release elicited by immunologic and non-immunologic stimuli in peritoneal and pleural rat mast cells. When cells were stimulated with antigen (egg albumin), OKA strongly inhibited histamine release. This finding sugge...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Estévez MD,Vieytes MR,Louzao MC,Botana LM

    更新日期:1994-02-09 00:00:00

  • A novel form of cytochrome P-450 in beagle dogs. P-450-D3 is a low spin form of cytochrome P-450 but with catalytic and structural properties similar to P-450d.

    abstract::A form of cytochrome P-450, P-450-D3, cross reactive with antibodies to rat P-450d was purified from liver microsomes of polychlorinated biphenyl (PCB)-treated female Beagle dogs to an electrophoretic homogeneity. Judging from the result of sodium dodecylsulfate-polyacrylamide gel electrophoresis (SDS-PAGE), the molec...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ohta K,Motoya M,Komori M,Miura T,Kitada M,Kamataki T

    更新日期:1989-01-01 00:00:00

  • The hydroxylation, dechlorination, and glucuronidation of 4,4'-dichlorobiphenyl (4-DCB) by human hepatic microsomes.

    abstract::Since chlorine placement and the degree of chlorination of the biphenyl nucleus play an important role in the metabolism and ultimate elimination of polychlorinated biphenyls (PCBs), we have studied the metabolism of 4,4'-dichlorobiphenyl (4-DCB) by human hepatic microsomes. This low molecular weight PCB congener is s...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Schnellmann RG,Volp RF,Putnam CW,Sipes IG

    更新日期:1984-11-01 00:00:00

  • Therapeutic and preventive properties of quercetin in experimental arthritis correlate with decreased macrophage inflammatory mediators.

    abstract::Pentahydroxyflavone dihydrate, quercetin (QU) is one of common flavonols biosynthesized by plants and has been suggested to modulate inflammatory responses in various models. In the present study, we investigated in vivo effects of oral or intra-cutaneous QU in chronic rat adjuvant-induced arthritis (AA). Growth delay...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Mamani-Matsuda M,Kauss T,Al-Kharrat A,Rambert J,Fawaz F,Thiolat D,Moynet D,Coves S,Malvy D,Mossalayi MD

    更新日期:2006-11-15 00:00:00

  • Intestinal cell-specific vitamin D receptor (VDR)-mediated transcriptional regulation of CYP3A4 gene.

    abstract::CYP3A4 is the most important drug-metabolizing enzyme that is involved in biotransformation of more than 50% of drugs. Pregnane X receptor (PXR) dominantly controls CYP3A4 inducibility in the liver, whereas vitamin D receptor (VDR) transactivates CYP3A4 in the intestine by secondary bile acids. Four major functional P...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Pavek P,Pospechova K,Svecova L,Syrova Z,Stejskalova L,Blazkova J,Dvorak Z,Blahos J

    更新日期:2010-01-15 00:00:00

  • Activation of 6-aminochrysene to genotoxic products by different forms of rat liver cytochrome P450 in an O-acetyltransferase-overexpressing Salmonella typhimurium strain (NM2009).

    abstract::Metabolic activation of a potent mutagen, 6-aminochrysene, to genotoxic products in a newly developed tester strain, Salmonella typhimurium NM2009, was studied in a rat liver microsomal monooxygenase system containing cytochrome P450 (P450). Since the tester strain was constructed by introducing an O-acetyltransferase...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yamazaki H,Shimada T

    更新日期:1992-09-01 00:00:00

  • Changes in methionine metabolism induced by D-galactosamine in isolated rat hepatocytes.

    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

    pub_type: 杂志文章


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

    更新日期:1986-12-01 00:00:00

  • Targeting cancer stem cells for more effective therapies: Taking out cancer's locomotive engine.

    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

    pub_type: 杂志文章


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

    更新日期:2009-08-15 00:00:00