Different effects of oxytetracycline and doxycycline on mitochondrial protein synthesis in rat liver after long-term treatment.


:The tetracyclines inhibit specifically mitochondrial (mt) and bacterial protein synthesis when they are present in low concentrations (2-10 micrograms/ml). There is no difference between the various members of this group of antibiotics in this respect. In the present study, however, it is shown that the inhibitory effect of doxycycline on mt-protein synthesis in rat liver is partially lost after continuous treatment for more than 1 week, whereas oxytetracycline continues to inhibit mt-protein synthesis effectively after 1 week of treatment. To find an explanation for this difference between doxycycline and oxytetracycline, a detailed study was made of the distribution and the effects on mt-protein synthesis of both tetracyclines under various conditions in rat liver. The results of the studies lead to the hypothesis that doxycycline treatment induces the formation of a doxycycline complex, and thus to a reduced amount of free doxycycline. This may explain the loss of effective inhibition of mt-protein synthesis.


Biochem Pharmacol


Biochemical pharmacology


van den Bogert C,Holtrop M,Melis TE,Roefsema PR,Kroon AM




Has Abstract


1987-05-01 00:00:00














  • Broad specificity of human phosphoglycerate kinase for antiviral nucleoside analogs.

    abstract::Nucleoside analogs used in antiviral therapies need to be phosphorylated to their tri-phospho counterparts in order to be active on their cellular target. Human phosphoglycerate kinase (hPGK) was recently reported to participate in the last step of phosphorylation of cytidine L-nucleotide derivatives [Krishnan PGE, La...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gallois-Montbrun S,Faraj A,Seclaman E,Sommadossi JP,Deville-Bonne D,Véron M

    更新日期:2004-11-01 00:00:00

  • Potentiating effects of clofibrate on prostaglandin-dependent and -independent pathways of human platelet activation: evidence for involvement of cyclic AMP.

    abstract::Although clofibrate has been shown to inhibit platelet aggregation that is caused by thrombin, ADP and epinephrine, by blocking the release of arachidonic acid from platelet phospholipids [8], here we have demonstrated that clofibrate enhanced platelet aggregation by arachidonic acid and PLC and reversed the effects o...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Huzoor-Akbar,Witiak DT,Newman HA,Fertel RH,Feller DR

    更新日期:1982-06-01 00:00:00

  • Jingzhaotoxin-II, a novel tarantula toxin preferentially targets rat cardiac sodium channel.

    abstract::Naturally occurring toxins are invaluable tools for exploration of the structure and function relationships of voltage-gated sodium channels (VGSCs). In this study, we isolated and characterized a novel VGSC toxin named jingzhaotoxin-II (JZTX-II) from the tarantula Chilobrachys jingzhao venom. JZTX-II consists of 32 a...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wang M,Liu Q,Luo H,Li J,Tang J,Xiao Y,Liang S

    更新日期:2008-12-15 00:00:00

  • Bromodomains: Structure, function and pharmacology of inhibition.

    abstract::Bromodomains are epigenetic readers of histone acetylation involved in chromatin remodeling and transcriptional regulation. The human proteome comprises 46 bromodomain-containing proteins with a total of 61 bromodomains, which, despite highly conserved structural features, recognize a wide array of natural peptide lig...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Ferri E,Petosa C,McKenna CE

    更新日期:2016-04-15 00:00:00

  • Castanospermine-glucosides as selective disaccharidase inhibitors.

    abstract::Castanospermine (CS) is a potent but non-selective inhibitor of many glycohydrolases including the intestinal disaccharidases. Several CS-glucosides were synthesized to investigate the effect of an attached glucopyranosyl residue on the potency and selectivity of CS toward inhibition of intestinal disaccharidases. 8 a...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Rhinehart BL,Robinson KM,King CH,Liu PS

    更新日期:1990-05-15 00:00:00

  • Use of comprehensive screening methods to detect selective human CAR activators.

    abstract::The so-called human xenosensors, constitutive androstane receptor (hCAR), pregnane X receptor (hPXR) and aryl hydrocarbon receptor (hAhR), participate in drug metabolism and transport as well as in several endogenous processes by regulating the expression of their target genes. While the ligand specificities for hPXR ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Küblbeck J,Laitinen T,Jyrkkärinne J,Rousu T,Tolonen A,Abel T,Kortelainen T,Uusitalo J,Korjamo T,Honkakoski P,Molnár F

    更新日期:2011-12-15 00:00:00

  • The prodigiosins, proapoptotic drugs with anticancer properties.

    abstract::The family of natural red pigments, called prodigiosins (PGs), characterised by a common pyrrolylpyrromethene skeleton, are produced by various bacteria. Some members have immunosuppressive properties and apoptotic effects in vitro and they have also displayed antitumour activity in vivo. Understanding the mechanism o...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Pérez-Tomás R,Montaner B,Llagostera E,Soto-Cerrato V

    更新日期:2003-10-15 00:00:00

  • 5,6-Epoxy-cholesterols contribute to the anticancer pharmacology of tamoxifen in breast cancer cells.

    abstract::Tamoxifen (Tam) is a selective estrogen receptor modulator (SERM) that remains one of the major drugs used in the hormonotherapy of breast cancer (BC). In addition to its SERM activity, we recently showed that the oxidative metabolism of cholesterol plays a role in its anticancer pharmacology. We established that thes...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Segala G,de Medina P,Iuliano L,Zerbinati C,Paillasse MR,Noguer E,Dalenc F,Payré B,Jordan VC,Record M,Silvente-Poirot S,Poirot M

    更新日期:2013-07-01 00:00:00

  • Evidence for separate effects of U73122 on phospholipase C and calcium channels in human platelets.

    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

    pub_type: 杂志文章


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

    更新日期:1998-12-01 00:00:00

  • Halysin, an antiplatelet Arg-Gly-Asp-containing snake venom peptide, as fibrinogen receptor antagonist.

    abstract::By means of Sephadex G-75 and CM-Sephadex C-50 column chromatography and reverse-phase HPLC, a low molecular weight (Mr = 7500), cysteine-rich peptide, halysin, was purified from Agkistrodon halys (mamushi) snake venom. Halysin is a potent platelet aggregation inhibitor that concentration-dependently inhibited human p...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Huang TF,Liu CZ,Ouyang CH,Teng CM

    更新日期:1991-08-22 00:00:00

  • Role of cytochrome P450 1A2 in bilirubin degradation Studies in Cyp1a2 (-/-) mutant mice.

    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

    pub_type: 杂志文章


    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

  • The dispositional enantioselectivity of indobufen in man.

    abstract::The plasma pharmacokinetics and urinary elimination of the enantiomers of indobufen (2-[p-(1-oxo-2-isoindolinyl)-phenyl]butyric acid), a novel platelet aggregation inhibitor, have been studied in male healthy volunteers given either the racemic compound or the S-enantiomer (200 mg racemate, 100 mg S-enantiomer). Enant...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Strolm Benedetti M,Frigerio E,Tamassia V,Noseda G,Caldwell J

    更新日期:1992-05-08 00:00:00

  • Regulation of eicosanoid biosynthesis in the macrophage. Involvement of protein tyrosine phosphorylation and modulation by selective protein tyrosine kinase inhibitors.

    abstract::The protein tyrosine kinase (PTK) inhibitor genistein has been demonstrated to inhibit platelet-activating factor-stimulated prostaglandin E2 (PGE2) production in lipopolysaccharide (LPS)-primed P388D1 macrophage-like cells (Glaser et al., J Biol Chem 265: 8658-8664, 1990). Therefore, the role of PTK in eicosanoid bio...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Glaser KB,Sung A,Bauer J,Weichman BM

    更新日期:1993-02-09 00:00:00

  • Is there a future for andrographolide to be an anti-inflammatory drug? Deciphering its major mechanisms of action.

    abstract::Andrographis paniculata has long been part of the traditional herbal medicine system in Asia and in Scandinavia. Andrographolide was isolated as a major bioactive constituent of A. paniculata in 1951, and since 1984, andrographolide and its analogs have been scrutinized with modern drug discovery approach for anti-inf...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Tan WSD,Liao W,Zhou S,Wong WSF

    更新日期:2017-09-01 00:00:00

  • Role of ion channels and intraterminal calcium homeostasis in the action of deltamethrin at presynaptic nerve terminals.

    abstract::Using a continuous perfusion system, synaptosomes prepared from rat brain released [3H]norepinephrine in a Ca2+-dependent manner when pulse depolarized by briefly elevating external potassium concentrations. Tetrodotoxin (10(-7) M), a sodium channel blocker, inhibited 48% of this pulsed release, and D595 (10(-5) M), a...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Clark JM,Brooks MW

    更新日期:1989-07-15 00:00:00

  • Platelet-mediated vascular contractions. Inhibition by flunarizine, a calcium-entry blocker.

    abstract::Flunarizine, a calcium (Ca2+)-entry blocker, selective for vascular tissues, inhibits in a concn-dependent way the contraction of isolated rat caudal artery preparations induced by mediators derived from thrombin-stimulated rat platelets. This inhibition is slow in onset and is of prolonged duration. Specific measurem...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: De Clerck F,Van Nueten JM

    更新日期:1983-03-01 00:00:00

  • Microsomal epoxide hydrolase in different rat strains.

    abstract::Epoxide hydrolase activity was determined in hepatic microsomes of adult males of 22 rat strains. The specific activity varied between 4.3 and 12.7 nmole styrene glycol/mg protein per min. The enzyme in F344, DA and Sprague--Dawley rats, strains with low, high and intermediate activity, respectively, was studied in mo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Oesch F,Zimmer A,Glatt HR

    更新日期:1983-06-01 00:00:00

  • Melatonin fine-tunes intracellular calcium signals and eliminates myocardial damage through the IP3R/MCU pathways in cardiorenal syndrome type 3.

    abstract::Cardiorenal syndrome type-3 (CRS-3) is characterized by acute cardiac injury induced by acute kidney injury. Here, we investigated the causes of CRS-3 by analyzing cardiac function after renal ischemia-reperfusion injury (IRI) using echocardiography and evaluation of pro-inflammatory markers, calcium balance, mitochon...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wang J,Toan S,Li R,Zhou H

    更新日期:2020-04-01 00:00:00

  • Inhibition of tumour-induced lipolysis in vitro and cachexia and tumour growth in vivo by eicosapentaenoic acid.

    abstract::Stimulation of lipolysis in murine adipocytes in response to a lipid-mobilizing factor produced by a cachexia-inducing murine adenocarcinoma was inhibited by eicosapentaenoic acid (EPA) with a Ki value of 104 microM. The inhibitory effect was strictly structurally specific, since other related fatty acids of both the ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Tisdale MJ,Beck SA

    更新日期:1991-01-01 00:00:00

  • Differential regulation of a fibroblast growth factor-binding protein by receptor-selective analogs of retinoic acid.

    abstract::We have demonstrated earlier that a secreted fibroblast growth factor-binding protein (FGF-BP) can enhance angiogenesis and promote tumor growth in vivo. Furthermore, we found that FGF-BP expression in squamous cell carcinoma (SCC) is reduced by concentrations of retinoids that are effective in the treatment of SCC an...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Boyle BJ,Harris VK,Liaudet-Coopman ED,Riegel AT,Wellstein A

    更新日期:2000-12-01 00:00:00

  • Zardaverine as a selective inhibitor of phosphodiesterase isozymes.

    abstract::The pyridazinone derivative zardaverine has recently been introduced as a potent bronchodilator in vivo and in vitro. In addition, zardaverine exerts a positive inotropic action on heart muscle in vitro. The actions of zardaverine are thought to be mediated via inhibition of phosphodiesterase (PDE) activity. Recent da...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Schudt C,Winder S,Müller B,Ukena D

    更新日期:1991-06-21 00:00:00

  • Cellular pharmacokinetics of carboplatin and cisplatin in relation to their cytotoxic action.

    abstract::We have studied the cellular pharmacokinetics of carboplatin (CBDCA), as part of the evaluation of the antitumor activity of CBDCA in cancers limited to the peritoneal cavity in comparison with cisplatin (cDDP). The uptake of CBDCA into L1210 (lymphosarcoma), CC531 (colonic carcinoma), COV413.B (human ovarian carcinom...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Los G,Verdegaal E,Noteborn HP,Ruevekamp M,de Graeff A,Meesters EW,ten Bokkel Huinink D,McVie JG

    更新日期:1991-07-05 00:00:00

  • The inhibitory effect of HOE 731 in isolated rabbit gastric glands.

    abstract::HOE 731, a substituted thienoimidazole derivative, was studied on [14C] aminopyrine uptake and oxygen consumption in isolated rabbit gastric glands. HOE 731 caused a concentration-dependent inhibition of [14C]aminopyrine uptake during histamine and dbcAMP stimulation. The inhibition during dbcAMP stimulation was in ac...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Herling AW,Becht M,Lang HJ,Scheunemann KH,Weidmann K,Scholl T,Rippel R

    更新日期:1990-10-15 00:00:00

  • In search of the Holy Grail: Folate-targeted nanoparticles for cancer therapy.

    abstract::Targeted drug therapy or "smart" drug delivery, potentially combined with simultaneous imaging modalities to monitor the delivery of drugs to specific tissues, is arguably the "holy grail" of pharmacology. Therapeutic approaches that exploit nanoparticles to deliver drugs selectively to cancer cells are currently cons...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Garcia-Bennett A,Nees M,Fadeel B

    更新日期:2011-04-15 00:00:00

  • Expression of fibronectin and interstitial collagen genes in smooth muscle cells: modulation by low molecular weight heparin fragments and serum.

    abstract::The effect of low M(r) heparin fragments (CY222) and fetal calf serum (FCS) on the level of fibronectin and fibrillar collagen mRNAs was investigated in smooth muscle cells (SMC) in culture. In the absence of FCS, addition of CY222 (100 micrograms/10(6) cells) to postconfluent early passage SMC resulted in a decrease ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Asselot-Chapel C,Combacau L,Labat-Robert J,Kern P

    更新日期:1995-03-01 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

  • In vivo evidence that insulin does not inhibit hepatic tryptophan pyrrolase activity in rats.

    abstract::Previous reports have indicated that insulin administration triggers an early increase in plasma tryptophan (TRP) levels in fasted rats. Then, the present study was undertaken to investigate the putative role of liver tryptophan pyrrolase (TPO) in this short-term effect of insulin. In 24 hr fasted rats, doses of insul...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Broqua P,Baudrie V,Laude D,Guezennec Y,Chaouloff F

    更新日期:1990-08-15 00:00:00

  • Selective modifications in the de novo biosynthesis of retinal phospholipids and glycerides by propranolol or phentolamine.

    abstract::The effects of propranolol or phentolamine on the metabolism of phospholipids, diacylglycerol, and triacylglycerol were studied in the bovine retina in vitro. Lipid labeling was followed during short-term incubation of intact bovine retinas with [U-14C]glycerol and [1-14C]palmitic acid. Each of these precursors was re...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: de Boschero MG,Bazan NG

    更新日期:1982-03-15 00:00:00

  • Function, diversity and therapeutic potential of the N-terminal domain of human chemokine receptors.

    abstract::Chemokines and their receptors play fundamental roles in many physiological and pathological processes such as leukocyte trafficking, inflammation, cancer and HIV-1 infection. Chemokine-receptor interactions are particularly intricate and therefore require precise orchestration. The flexible N-terminal domain of human...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Szpakowska M,Fievez V,Arumugan K,van Nuland N,Schmit JC,Chevigné A

    更新日期:2012-11-15 00:00:00

  • New proteins in the rat CYP2B subfamily: presence in liver microsomes of the constitutive CYP2B3 protein and the phenobarbital-inducible protein product of alternatively spliced CYP2B2 mRNA.

    abstract::The rat CYP2B gene subfamily includes CYP2B1, CYP2B2 and CYP2B3. Translation of an alternatively spliced hepatic CYP2B2 mRNA would generate a CYP2B2 variant, CYP2B2v, having eight additional amino acid residues inserted between CYP2B2 positions 274 and 275. The presence of CYP2B3 and CYP2B2v in rat liver has yet to be...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Desrochers M,Christou M,Jefcoate C,Belzil A,Anderson A

    更新日期:1996-10-25 00:00:00