The interaction of oral hypoglycaemic drugs with insulin on steroid metabolism in hepatocytes isolated from control and diabetic male rats.


:The effects of the oral hypoglycaemic drugs, phenformin and tolbutamide, and insulin, alone and in combination, on steroid metabolism in hepatocytes isolated from control and streptozotocin-diabetic male rats has been studied. Both phenformin and tolbutamide mimic the action of insulin in stimulating hepatic steroid metabolism in a dose-dependent manner in control cells. Unlike insulin, however, both drugs give a similar effect in cells derived from diabetic animals although to a lesser extent. Both drugs can partially restore the effect of insulin in cells derived from diabetic animals. Biguanides and sulphonylureas, therefore, have a direct effect on liver cells to mimic insulin action and can still have an effect under conditions where insulin is inactive. Both types of oral hypoglycaemics can also affect insulin-insensitive cells isolated from diabetic rat liver to restore to a certain extent their response to insulin.


Biochem Pharmacol


Biochemical pharmacology


Hussin AH,Skett P




Has Abstract


1990-11-15 00:00:00














  • Fibrinolytic and anticoagulant activities of highly sulfated fucoidan.

    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

    pub_type: 杂志文章


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

    更新日期:1992-04-15 00:00:00

  • Attenuation of 6-hydroxydopamine (6-OHDA)-induced nuclear factor-kappaB (NF-kappaB) activation and cell death by tea extracts in neuronal cultures.

    abstract::Antioxidant and anti-inflammatory therapy approaches have been in the focus of attention in the treatment of neurodegenerative Parkinson's and Alzheimer's diseases where oxidative stress has been implicated. Tea extracts have been previously reported to possess radical scavenger, iron chelating and anti-inflammatory p...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Levites Y,Youdim MB,Maor G,Mandel S

    更新日期:2002-01-01 00:00:00

  • Clotrimazole inhibits and modulates heterologous association of the key glycolytic enzyme 6-phosphofructo-1-kinase.

    abstract::Clotrimazole is an antifungal azole derivative recently recognized as a calmodulin antagonist with promising anticancer effects. This property has been correlated with the ability of the drug to decrease the viability of tumor cells by inhibiting their glycolytic flux and consequently decreasing the intracellular conc...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Zancan P,Rosas AO,Marcondes MC,Marinho-Carvalho MM,Sola-Penna M

    更新日期:2007-05-15 00:00:00

  • Differential patterns of inhibition of the sugar transporters GLUT2, GLUT5 and GLUT7 by flavonoids.

    abstract::Only limited data are available on the inhibition of the sugar transporter GLUT5 by flavonoids or other classes of bioactives. Intestinal GLUT7 is poorly characterised and no information exists concerning its inhibition. We aimed to study the expression of GLUT7 in Caco-2/TC7 intestinal cells, and evaluate inhibition ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gauer JS,Tumova S,Lippiat JD,Kerimi A,Williamson G

    更新日期:2018-06-01 00:00:00

  • Intestinal absorption of S-nitrosothiols: Permeability and transport mechanisms.

    abstract::S-Nitrosothiols, a class of NO donors, demonstrate potential benefits for cardiovascular diseases. Drugs for such chronic diseases require long term administration preferentially through the oral route. However, the absorption of S-nitrosothiols by the intestine, which is the first limiting barrier for their vascular ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Bonetti J,Zhou Y,Parent M,Clarot I,Yu H,Fries-Raeth I,Leroy P,Lartaud I,Gaucher C

    更新日期:2018-09-01 00:00:00

  • Allosteric approaches to the targeting of G-protein-coupled receptors for novel drug discovery: a critical assessment.

    abstract::In recent years, the concept of allosteric modulation of G-protein-coupled receptors (GPCRs) has matured and now represents an increasingly viable approach to drug discovery. This is evident in the fact that allosteric modulators have been reported for every class of GPCR, and several are currently in clinical trials ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Raddatz R,Schaffhauser H,Marino MJ

    更新日期:2007-08-01 00:00:00

  • The interactions of apamin and tetraethylammonium are differentially affected by single mutations in the pore mouth of small conductance calcium-activated potassium (SK) channels.

    abstract::Valine residues in the pore region of SK2 (V366) and SK3 (V520) were replaced by either an alanine or a phenylalanine to evaluate the impact on the interactions with the allosteric blocker apamin. Unlike TEA which showed high sensitivity to phenylalanine mutated channels, the binding affinity of apamin to the phenylal...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Dilly S,Philippart F,Lamy C,Poncin S,Snyders D,Seutin V,Liégeois JF

    更新日期:2013-02-15 00:00:00

  • Ultrastructural morphology and localisation of cisplatin-induced platinum-DNA adducts in a cisplatin-sensitive and -resistant human small cell lung cancer cell line using electron microscopy.

    abstract::Ultrastructural morphology (transmission electron microscopy) and localisation of cisplatin-induced platinum (Pt)-DNA adducts (immunoelectron microscopy) were analysed in the human small cell lung cancer cell line GLC(4) and its 40-fold in vitro acquired cisplatin-resistant subline GLC(4)-CDDP, which is characterised ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Meijera C,van Luyn MJ,Nienhuis EF,Blom N,Mulder NH,de Vries EG

    更新日期:2001-03-01 00:00:00

  • Metabolism and RNA incorporation of cyclopentenyl cytosine in human colorectal cancer cells.

    abstract::We studied the cytotoxicity and metabolism of the investigational cytidine analogue cyclopentenyl cytosine (CPE-C) in three human colorectal cancer cell lines: HCT 116, SNU-C4, and NCI-H630. CPE-C potently inhibited cell growth and decreased clonogenic capacity at concentrations achieved in murine and primate pharmaco...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yee LK,Allegra CJ,Trepel JB,Grem JL

    更新日期:1992-04-01 00:00:00

  • Calcium ionophoretic and apoptotic effects of ferutinin in the human Jurkat T-cell line.

    abstract::We have investigated the ionophoretic and apoptotic properties of the daucane sesquiterpene ferutinin and three related compounds, ferutidin, 2-alpha-hydroxyferutidin and teferin, all isolated from various species of plants from the genus Ferula. Ferutinin induced a biphasic elevation of intracellular Ca2+ in the leuk...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Macho A,Blanco-Molina M,Spagliardi P,Appendino G,Bremner P,Heinrich M,Fiebich BL,Muñoz E

    更新日期:2004-09-01 00:00:00

  • 2,5-Hexanedione modifies skeletal proteins of the red blood cells and increases the binding of hemoglobin to the membrane.

    abstract::The effects of 2,5-hexanedione (2,5 HD) on skeletal proteins of red blood cells (RBCs) were investigated both in vitro (human RBCs) and in vivo in male Sprague-Dawley rats which had been treated with the drug for several days. We found that 2,5 HD induced the following major changes in the electrophoretic pattern of t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Mallozzi C,Scorza G,Frontali N,Minetti M

    更新日期:1989-08-15 00:00:00

  • Elevated K-ras activity with cholestyramine and lovastatin, but not konjac mannan or niacin in lung--importance of mouse strain.

    abstract::Our previous work established that hypocholesterolemic agents altered K-ras intracellular localization in lung. Here, we examined K-ras activity to define further its potential importance in lung carcinogenesis. K-ras activity in lungs from male A/J, Swiss and C57BL/6 mice was examined. For 3 weeks, mice consumed eith...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Calvert RJ,Tepper S,Kammouni W,Anderson LM,Kritchevsky D

    更新日期:2006-12-15 00:00:00

  • Modulation of eosinophil migration from bone marrow to lungs of allergic rats by nitric oxide.

    abstract::Chronic blockade of nitric oxide (NO) synthesis attenuates the eosinophil infiltration into airways of allergic rats. This study was designed to investigate whether the inhibition of eosinophil influx to the lung of allergic rats reflects modifications in the pattern of cell mobilization from the bone marrow to periph...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ferreira HH,Costa RA,Jacheta JM,Martins AR,Medeiros MV,Macedo-Soares MF,De Luca IM,Antunes E,De Nucci G

    更新日期:2004-08-15 00:00:00

  • Potentiation by febrifugine of host defense in mice against Plasmodium berghei NK65.

    abstract::The effect of febrifugine, the main alkaloidal constituent of an antimalarial crude drug, Dichroa febrifuga Lour., on protective immunity in mice infected with erythrocytic stage Plasmodium berghei NK65 was investigated. Febrifugine was administered orally, at a dose of 1 mg/kg/day, to mice before and/or after they we...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Murata K,Takano F,Fushiya S,Oshima Y

    更新日期:1999-11-15 00:00:00

  • Redox modulation of the DNA damage response.

    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

    pub_type: 杂志文章,评审


    authors: Caputo F,Vegliante R,Ghibelli L

    更新日期:2012-11-15 00:00:00

  • Binding of dihydrodigitoxin to beef and human cardiac (Na+ + K+)-ATPase: evidence for two binding sites in cell membranes.

    abstract::The specific binding of three cardiac glycosides, 3H-ouabain, 3H-digitoxin and 3H-dihydrodigitoxin, to beef cardiac (Na+ + K+)-ATPase was compared. Non-specific binding was defined as that in the presence of 0.1 mM unlabelled compound, or in the absence of ligands. The dissociation constants (KD-values) calculated fro...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Brown L,Erdmann E

    更新日期:1983-11-01 00:00:00

  • Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor.

    abstract::Inflammation-induced microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal enzyme that synthesizes prostaglandin E(2) (PGE(2)) downstream of cyclooxygenase-2 (COX-2). The efficacy of nonsteroidal anti-inflammatory drugs and COX-2 inhibitors in the treatment of the signs and symptoms of osteoarthritis, rheuma...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Mbalaviele G,Pauley AM,Shaffer AF,Zweifel BS,Mathialagan S,Mnich SJ,Nemirovskiy OV,Carter J,Gierse JK,Wang JL,Vazquez ML,Moore WM,Masferrer JL

    更新日期:2010-05-15 00:00:00

  • In vivo induction of cytochrome P450 CYP3A expression in rat leukocytes using various inducers.

    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

    pub_type: 杂志文章


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

    更新日期:1996-06-14 00:00:00

  • Cellular pharmacology of deferrioxamine B and derivatives in cultured rat hepatocytes in relation to iron mobilization.

    abstract::Two radiolabelled derivatives of deferrioxamine B (DF) have been synthesized: methyl-DF and acetyl-DF. Both derivatives are non cytotoxic and stable in cell culture but they are degraded in human plasma and more extensively in rat plasma. Methyl-DF, acetyl-DF and DF mobilize radioiron to the same extent from hepatocyt...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Laub R,Schneider YJ,Octave JN,Trouet A,Crichton RR

    更新日期:1985-04-15 00:00:00

  • Inhibition of squalene synthase in vitro by 3-(biphenyl-4-yl)-quinuclidine.

    abstract::Squalene synthase (SQS) catalyses a step following the final branch in the pathway of cholesterol biosynthesis. Inhibition of this enzyme, therefore, is an approach for the treatment of atherosclerosis with the potential for low side effects. We have characterised the inhibition of rat liver microsomal SQS by 3-(biphe...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ward WH,Holdgate GA,Freeman S,McTaggart F,Girdwood PA,Davidson RG,Mallion KB,Brown GR,Eakin MA

    更新日期:1996-06-14 00:00:00

  • Targeting the epidermal growth factor receptor for therapy of carcinomas.

    abstract::As a group, the carcinomas represent a substantial proportion of all human malignancies, but, with relatively few exceptions, current treatments are ineffective. Modification of existing chemotherapeutic agents has not led to significant improvements in the survival of carcinoma patients, and development of new therap...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Davies DE,Chamberlin SG

    更新日期:1996-05-03 00:00:00

  • Antioxidant effects of 2,3-dihydro-5-hydroxy-4,6-di-tert-butyl-2,2-dipentylbenzofuran and alpha-tocopherol in hyperlipidemic mice as evaluated by hydroxyoctadecadienoic acid and 7-hydroxycholesterol.

    abstract::It has been hypothesized that oxidative modification of low density lipoprotein plays a key role in the pathogenesis of atherosclerosis. In order to elucidate the role of lipid oxidation and its inhibition in vivo, apolipoprotein E and alpha-tocopherol (alphaT) transfer protein double knockout (ApoE(-/-)alpha-TTP(-/-)...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yoshida Y,Hayakawa M,Itoh N,Habuchi Y,Inoue R,Chen ZH,Cao J,Cynshi O,Jishage K,Niki E

    更新日期:2007-10-01 00:00:00

  • Identification of dual mTORC1 and mTORC2 inhibitors in melanoma cells: prodigiosin vs. obatoclax.

    abstract::The PI3K/AKT/mTOR signaling pathway regulates cell proliferation, survival and angiogenesis. The mammalian target of rapamycin (mTOR) is a protein kinase ubiquitously expressed within cells that regulates cell growth and survival by integrating nutrient and hormonal signals. mTOR exists in two complexes, mTORC1 and mT...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Espona-Fiedler M,Soto-Cerrato V,Hosseini A,Lizcano JM,Guallar V,Quesada R,Gao T,Pérez-Tomás R

    更新日期:2012-02-15 00:00:00

  • Effects of hypophysectomy and thyroxine on the expression of hepatic oestrogen, hydroxysteroid and phenol sulphotransferases.

    abstract::Sulphation in rats, and other mammals, is carried out by a family of sulphotransferase isoenzymes, which can be further subdivided into oestrogen, hydroxysteroid and phenol sulphotransferases. We have examined the effects of hypophysectomy on the activity and expression of representative members of the three major sul...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Borthwick EB,Voice MW,Burchell A,Coughtrie MW

    更新日期:1995-05-17 00:00:00

  • Mouse N-acetyltransferase type 2, the homologue of human N-acetyltransferase type 1.

    abstract::There is increasing evidence that human arylamine N-acetyltransferase type 1 (NAT1, EC, although first identified as a homologue of a drug-metabolising enzyme, appears to be a marker in human oestrogen receptor positive breast cancer. Mouse Nat2 is the mouse equivalent of human NAT1. The development of mouse ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Kawamura A,Westwood I,Wakefield L,Long H,Zhang N,Walters K,Redfield C,Sim E

    更新日期:2008-04-01 00:00:00

  • Effect of repeated administration of 11-hydroxy-delta 8-tetrahydrocannabinol, an active metabolite of delta 8-tetrahydrocannabinol, on the hepatic microsomal drug-metabolizing enzyme system of mice.

    abstract::The effects of delta 8-tetrahydrocannabinol (delta 8-THC) and its major and active metabolite, 11-hydroxy-delta 8-tetrahydrocannabinol (11-OH-delta 8-THC), on the hepatic microsomal drug-metabolizing enzyme system were studied in mice. The repeated administration of 11-OH-delta 8-THC (5 mg/kg/day, i.v.) for 3 or 7 day...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Watanabe K,Arai M,Narimatsu S,Yamamoto I,Yoshimura H

    更新日期:1986-06-01 00:00:00

  • Gimatecan and other camptothecin derivatives poison Leishmania DNA-topoisomerase IB leading to a strong leishmanicidal effect.

    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

    pub_type: 杂志文章


    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

  • Inhibition of nitric oxide-guanylate cyclase-dependent and -independent signaling contributes to impairment of beta-adrenergic vasorelaxations by cyclosporine.

    abstract::This study investigated the role of endothelium- and smooth muscle-dependent mechanisms in the interaction of cyclosporine (CyA), an immunosuppressant drug, with beta-adrenoceptor (isoprenaline)-mediated relaxations in isolated rat aortas precontracted with phenylephrine. CyA effects were assessed in the absence and p...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: El-Mas MM,Sharabi FM,El-Gowilly SM,El-Din MM

    更新日期:2007-02-01 00:00:00

  • Inhibitory effect of ionized free intracellular calcium enhanced by ruthenium red and m-chloro-carbonylcyanide phenyl hydrazon on the evoked release of acetylcholine.

    abstract::In order to understand the relationship between the free ionized calcium concentration in the axon terminals and the transmitter release we have investigated the effect of ruthenium red (RuR) and m-chloro-carbonylcyanide phenyl hydrazon (CCCP), mitochondrial uncoupler agents on the liberation of acetylcholine from mye...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Bernath S,Vizi ES

    更新日期:1987-11-01 00:00:00

  • Colchicine biotransformation by human liver microsomes. Identification of CYP3A4 as the major isoform responsible for colchicine demethylation.

    abstract::Colchicine disposition involves both active biliary and renal excretion of parent drug, and at least in mammals a substantial fraction undergoes hepatic demethylation prior to excretion. We investigated the biotransformation of [3H]colchicine in a panel of microsomal preparations obtained from sixteen human liver samp...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Tateishi T,Soucek P,Caraco Y,Guengerich FP,Wood AJ

    更新日期:1997-01-10 00:00:00