Pentosan polysulfate to control hepcidin expression in vitro and in vivo.


:Hepcidin peptide is crucial in the regulation of systemic iron availability controlling its uptake from the diet and its release from the body storage tissues. Hepcidin dysregulation causes different human disorders ranging from iron overload (e.g. hemochromatosis) to iron deficiency (e.g. anemia). Hepcidin excess is common in the Anemia of Chronic Diseases or Anemia of Inflammation and in the genetic form of anemia named IRIDA; the pharmacological downregulation of hepcidin in these disorders could improve the anemia. Commercial heparins were shown to be strong inhibitors of hepcidin expression, by interfering with BMP6/SMAD pathway. The non-anti-coagulant heparins, modified to abolish the anti-thrombin binding site, were equally potent and could be used to improve iron status. To perform its anti-hepcidin activity heparin needs 2O- and 6O-sulfation and an average molecular weight (MW) up to 4000-8000 Dalton, depending on the sulfation level. The pentosane polysulfate (PPS), which shares with heparin a high degree of sulfation, is a compound with low anti-coagulant activity that is already in use for pharmaceutical treatment. In the present work we analyzed the anti-hepcidin activity of PPS in vitro and in vivo. We found that it acts as a strong inhibitor of hepcidin expression in HepG2 cells with an effect already visible after 2-3 h of treatment. It also suppressed hepcidin in mice in a dose dependent manner after 3 h and with a significant redistribution of systemic iron without evident side effects. PPS is also able to abolish the LPS dependent hepcidin upregulation similarly to that showed for heparin derivatives. These results suggest PPS as an interesting compound to control hepcidin in vivo.


Biochem Pharmacol


Biochemical pharmacology


Asperti M,Denardo A,Gryzik M,Castagna A,Girelli D,Naggi A,Arosio P,Poli M




Has Abstract


2020-05-01 00:00:00












  • Stimulation of drug and carcinogen metabolism by prolonged oral tobacco consumption.

    abstract::Oral administration of tobacco to rats for 21 days caused remarkable stimulation of the metabolism of phenacetin, aniline and benzo[a]pyrene, a carcinogen, by hepatic microsomal mixed function oxidases (MFO). Such treatment for 6 days resulted in a small increase in the activities of phenacetin O-dealkylase and aromat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Kaur S,Ali B

    更新日期:1982-04-15 00:00:00

  • Enhancement of the functional stability of solubilized nucleoside transporters by substrates and inhibitors.

    abstract::Purification of functional nucleoside transporters has been hampered by the instability of detergent-solubilized proteins. The present study was undertaken to determine if the presence of specific transporter ligands in the solubilization medium could enhance the functional stability of the isolated proteins. Ehrlich ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hammond JR

    更新日期:1997-03-07 00:00:00

  • The measurement of polyglutamate metabolites of the thymidylate synthase inhibitor, ICI D1694, in mouse and human cultured cells.

    abstract::A method is described for the measurement of the polyglutamates of the quinazoline thymidylate synthase inhibitor, N-(5-[N-(3,4-dihydro-2-methyl-4-oxoquinazolin- 6-ylmethyl)-N-methylamino]-2-theonyl)-L-glutamic acid (ICI D1694). This involved incubation of cells with [5-3H]ICI D1694, extraction of the polyglutamates a...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gibson W,Bisset GM,Marsham PR,Kelland LR,Judson IR,Jackman AL

    更新日期:1993-02-24 00:00:00

  • Ins and outs of dietary phytochemicals in cancer chemoprevention.

    abstract::A voluminous number of evidence suggests that an increased consumption of fruit and vegetables is a relatively easy and practical strategy to reduce significantly the incidence of chronic diseases, such as cancer, cardiovascular diseases and other aging-related pathologies. This review will critically discuss the appl...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Russo GL

    更新日期:2007-08-15 00:00:00

  • Catalase expression in MCF-7 breast cancer cells is mainly controlled by PI3K/Akt/mTor signaling pathway.

    abstract::Catalase is an antioxidant enzyme that catalyzes mainly the transformation of hydrogen peroxide into water and oxygen. Although catalase is frequently down-regulated in tumors the underlying mechanism remains unclear. Few transcription factors have been reported to directly bind the human catalase promoter. Among them...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Glorieux C,Auquier J,Dejeans N,Sid B,Demoulin JB,Bertrand L,Verrax J,Calderon PB

    更新日期:2014-05-15 00:00:00

  • Serine protease inhibition and mitochondrial dysfunction associated with cisplatin resistance in human tumor cell lines: targets for therapy.

    abstract::Indicators of mitochondrial function were studied in two different cell culture models of cis-diamminedichloroplatinum-II (CDDP) resistance: the intrinsically resistant human ovarian cancer cell line CI-80-13S, and resistant clones (HeLa-S1a and HeLa-S1b) generated by stable expression of the serine protease inhibitor...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Dong Y,Berners-Price SJ,Thorburn DR,Antalis T,Dickinson J,Hurst T,Qiu L,Khoo SK,Parsons PG

    更新日期:1997-06-01 00:00:00

  • MicroRNA: A new generation therapeutic target in diabetic nephropathy.

    abstract::Diabetic nephropathy (DN) is one of the most prevalent lethal complications of diabetes that leads to end stage renal disease. Although several clinical approaches exist to attenuate DN, there is not curative treatment to date. DN is complicated, as it involves several simultaneous molecular pathways. Some natural and...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Dewanjee S,Bhattacharjee N

    更新日期:2018-09-01 00:00:00

  • Desensitization of neurotensin-induced phosphoinositide hydrolysis in transfected CHO cells.

    abstract::The regulation of neurotensin-induced phosphoinositide turnover was studied in transfected CHO cells expressing the rat neurotensin receptor. Stimulation of these cells with neurotensin resulted in an important, but transient, increase in inositol phosphate cell content. Preincubation of the cells with neurotensin dra...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hermans E,Maloteaux JM

    更新日期:1996-06-28 00:00:00

  • Protection by phosphodiesterase inhibitors against endotoxin-induced liver injury in galactosamine-sensitized mice.

    abstract::Phosphodiesterase inhibitors were used as a tool to manipulate cellular nucleotide levels in vitro and in vivo. The lipopolysaccharide (LPS)-induced release of tumor necrosis factor alpha (TNF-alpha) from mouse peritoneal macrophages was inhibited by prostaglandin E2 with an IC50 of 0.05 microM and by dibutyryl-cAMP w...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Fischer W,Schudt C,Wendel A

    更新日期:1993-06-22 00:00:00

  • Novel modified adenosine 5'-triphosphate analogues pharmacologically characterized in human embryonic kidney 293 cells highly expressing rat brain P2Y(1) receptor: Biotinylated analogue potentially suitable for specific P2Y(1) receptor isolation.

    abstract::Rat brain P2Y(1) (rP2Y(1)) receptor-transfected human embryonic kidney cells (HEK 293) were recently shown to have enhanced reactivity to both ATP and ADP (Vöhringer C, Schäfer R, Reiser G. Biochem Pharmacol 2000;59:791-800). Here, we demonstrated the usefulness of this cell line as a system for further studying novel...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Zündorf G,Schäfer R,Vöhringer C,Halbfinger E,Fischer B,Reiser G

    更新日期:2001-05-15 00:00:00

  • The cystic fibrosis mutation G1349D within the signature motif LSHGH of NBD2 abolishes the activation of CFTR chloride channels by genistein.

    abstract::Cystic fibrosis (CF) is a common lethal genetic disease caused by autosomal recessive mutations of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel that belongs to the ATP-Binding Cassette (ABC) family of transporters. The class III CF mutations G551D and G1349D are located within the "s...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Melin P,Thoreau V,Norez C,Bilan F,Kitzis A,Becq F

    更新日期:2004-06-15 00:00:00

  • Histamine H1 receptor-induced Ca2+ mobilization and prostaglandin E2 release in human gingival fibroblasts. Possible role of receptor-operated Ca2+ influx.

    abstract::Stimulation of human gingival fibroblasts with histamine elicited an increase in the intracellular concentration of free calcium ([Ca2+]i) and the formation of inositol 1,4,5-trisphosphate (InsP3) in a concentration- and time-dependent manner. The histamine-induced increase in [Ca2+]i was attenuated completely by chlo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Niisato N,Ogata Y,Furuyama S,Sugiya H

    更新日期:1996-10-11 00:00:00

  • Inhibition of microsomal biotransformation by a series of nitrogen and oxygen heterocyclic histamine H2-antagonists.

    abstract::A homologous series of potent, long-lasting thiazolo-pyrimidone-pyridine histamine H2-antagonists were examined for their inhibitory effects on rat hepatic ethylmorphine N-demethylation. Inhibitory potency increased in the order: 2-pyridinyl less than 3-pyridinyl less than 4-pyridinyl histamine H2-antagonist. Substitu...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lindstrom TD,Whitaker GW,Pioch RP

    更新日期:1987-05-15 00:00:00

  • Alkannin induces cytotoxic autophagy and apoptosis by promoting ROS-mediated mitochondrial dysfunction and activation of JNK pathway.

    abstract::Naphthoquinone derivatives and metabolites are widely dispersed molecules in nature. Alkannin, a natural naphthoquinone compound, induces excellent cytotoxicity in cancer cells. However, the detailed mechanism by which alkannin inhibits cancer cell survival remains unclear. In the present study, we isolated alkannin f...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Zheng Q,Li Q,Zhao G,Zhang J,Yuan H,Gong D,Guo Y,Liu X,Li K,Lin P

    更新日期:2020-10-01 00:00:00

  • The mitochondrial uncoupler dicumarol disrupts the MTT assay.

    abstract::Dicumarol is routinely added to the 3-[4,4-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay to study the role of NAD(P)H:quinone oxido-reductase in drug activation and detoxification. We assessed the direct impact of dicumarol (a mitochondrial uncoupler) on the MTT assay. Mouse mammary tumor (EMT6) an...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Collier AC,Pritsos CA

    更新日期:2003-07-15 00:00:00

  • Species differences in the pharmacokinetics of cefadroxil as determined in wildtype and humanized PepT1 mice.

    abstract::PepT1 (SLC15A1) is a high-capacity low-affinity transporter that is important in the absorption of digested di/tripeptides from dietary protein in the small intestine. PepT1 is also crucial for the intestinal uptake and absorption of therapeutic agents such as the β-lactam aminocephalosporins and antiviral prodrugs. S...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hu Y,Smith DE

    更新日期:2016-05-01 00:00:00

  • The intracellular phosphorylation of (-)-2'-deoxy-3'-thiacytidine (3TC) and the incorporation of 3TC 5'-monophosphate into DNA by HIV-1 reverse transcriptase and human DNA polymerase gamma.

    abstract::(-)-2'-deoxy-3'-thiacytidine (3TC) has been shown to be a potent, selective inhibitor of HIV replication in vitro, which requires phosphorylation to its 5'-triphosphate for antiviral activity. The intracellular concentration of 3TC 5'-triphosphate in phytohaemagglutinin (PHA)-stimulated peripheral blood lymphocytes (P...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gray NM,Marr CL,Penn CR,Cameron JM,Bethell RC

    更新日期:1995-09-28 00:00:00

  • Effects of five anion channel blockers on thrombin- and ionomycin-activated platelet functions.

    abstract::The inhibitory effects of anion channel blockers were evaluated on aggregation, intracellular Ca2+ rises, and the production of arachidonic acid metabolites in human platelets. Inhibitors included five anion channel blockers: phloretin, probenecid, pyridoxal phosphate, 4,4'-diisothiocyano-2,2'-disulfonic acid stilbene...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ozaki Y,Matsumoto Y,Yatomi Y,Higashihara M,Kariya T,Shoji K

    更新日期:1989-07-01 00:00:00

  • Radiolabelling of the human 5-HT2A receptor with an agonist, a partial agonist and an antagonist: effects on apparent agonist affinities.

    abstract::Previous work has shown that 5-hydroxytryptamine (5-HT)2A receptors can be radiolabelled with various radioligands, including partial agonists, such as [125I]-DOI and [3H]-DOB, and antagonists, such as [3H]-ketanserin and [3H]-spiperone. Because 5-HT has high affinity for the 5-HT2A receptor when displacing [3H]-DOB, ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sleight AJ,Stam NJ,Mutel V,Vanderheyden PM

    更新日期:1996-01-12 00:00:00

  • Re-examining osteoarthritis therapy from a developmental biologist's perspective.

    abstract::Osteoarthritis is the most prevalent musculoskeletal disorder and one for which there is no disease modifying therapy available at present. Our current understanding of the disease mechanism of osteoarthritis is limited owing to a lacuna of knowledge about the development and maintenance of articular cartilage that is...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Jaswal AP,Bandyopadhyay A

    更新日期:2019-07-01 00:00:00

  • HeLa cell RNA and protein syntheses. Effects of long-term treatment with 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB).

    abstract::The population growth rate of HeLa cells treated with 60 microM 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB) in reinforced Eagle's minimum essential medium was directly related to the concentration of fetal bovine serum in the range from 5 to 30%. Control cells proliferated at a maximal rate (doubling time: ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Tamm I

    更新日期:1984-02-15 00:00:00

  • Characterization of beta 1- and beta 2-adrenoceptors in rat skeletal muscles.

    abstract::Binding studies with (-)-[125I]cyanopindolol (ICYP) were conducted to characterize beta-adrenoceptors in plantaris and soleus muscles of rats (male, 250-300 g). The distribution of beta 1- and beta 2-adrenoceptors in different muscle fiber types, identified in serial sections by succinic dehydrogenase (SDH) staining, ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Kim YS,Sainz RD,Molenaar P,Summers RJ

    更新日期:1991-10-09 00:00:00

  • Role of the endocannabinoid system in the control of mouse myometrium contractility during the menstrual cycle.

    abstract::Cannabis and cannabinoids are known to affect female reproduction. However, the role of the endocannabinoid system in mouse uterine contractility in the dioestrus and oestrus phases has not been previously investigated. The present study aimed at filling this gap. Endocannabinoid (anandamide and 2-arachidonoylglycerol...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Pagano E,Orlando P,Finizio S,Rossi A,Buono L,Iannotti FA,Piscitelli F,Izzo AA,Di Marzo V,Borrelli F

    更新日期:2017-01-15 00:00:00

  • Substrates for arachidonic acid co-oxidation with peroxidase/hydrogen peroxide. Further evidence for radical intermediates.

    abstract::We tested the ability of a wide variety of organic compounds, including benzene and phenol derivatives, aromatic amines, pyrazoline derivatives and other non-steroidal anti-inflammatory drugs, to act as cosubstrates during the horseradish peroxidase/hydrogen peroxide-mediated oxygenation of arachidonic acid. Structura...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lehmann FM,Bretz N,von Bruchhausen F,Wurm G

    更新日期:1989-04-15 00:00:00

  • Metabolism and mode of selective inhibition of human immunodeficiency virus replication by 3'-azido-2',3'-dideoxy-5-iodouridine and 3'-azido-2',3'-dideoxy-5-bromouridine.

    abstract::3'-Azido-2',3'-dideoxy-5-iodouridine (AzIdUrd) and 3'-azido-2',3'-dideoxy-5-bromouridine (AzBdUrd), previously shown to be potent and selective inhibitors of human immunodeficiency virus replication in vitro were minimally toxic to the uninfected human lymphoid cell line H9 (IC50 = 197 and 590 microM, respectively). B...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: August EM,Qian HY,Birks EM,Thombre UA,Lin TS,Prusoff WH

    更新日期:1993-01-07 00:00:00

  • Anti-fibrotic and anti-inflammatory properties of melatonin on human gingival fibroblasts in vitro.

    abstract::Melatonin (MEL) has been proposed as a therapeutic agent for the oral cavity, due to its antioxidant and anti-inflammatory effects since periodontal diseases are aggravated by free radicals, and by disproportionate immunological response to plaque microorganism. In addition, MEL promotes bone formation. This study aim...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gómez-Florit M,Ramis JM,Monjo M

    更新日期:2013-12-15 00:00:00

  • Studies on substrate specificity of the hog liver flavin-containing monooxygenase. Anionic organic sulfur compounds.

    abstract::The influence of anionic groups on interaction of nucleophilic sulfur compounds with the purified hog liver flavin-containing monooxygenase was evaluated from kinetic constants obtained with various dithiobenzoates, thiolbenzoates, and thiolalkylcarboxylic acids. All compounds tested bearing a single negative charge l...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Taylor KL,Ziegler DM

    更新日期:1987-01-01 00:00:00

  • Studies on inhibitors of mammalian DNA polymerase alpha and beta: sulfolipids from a pteridophyte, Athyrium niponicum.

    abstract::Three sulfolipid compounds, 1, 2, and 3, have been isolated from a higher plant, a pteridophyte, Athyrium niponicum, as potent inhibitors of the activities of calf DNA polymerase alpha and rat DNA polymerase beta. The inhibition by the sulfolipids was concentration dependent, and almost complete inhibition of DNA poly...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Mizushina Y,Watanabe I,Ohta K,Takemura M,Sahara H,Takahashi N,Gasa S,Sugawara F,Matsukage A,Yoshida S,Sakaguchi K

    更新日期:1998-02-15 00:00:00

  • Superoxide anion mediates the L-selectin down-regulation induced by non-steroidal anti-inflammatory drugs in human neutrophils.

    abstract:UNLABELLED:Non-steroidal anti-inflammatory drugs (NSAIDs) induce the shedding of L-selectin in human neutrophils through a mechanism still not well understood. In this work we studied both the functional effect of NSAIDs on the neutrophils/endothelial cells dynamic interaction, and the potential involvement of reactive...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Domínguez-Luis M,Herrera-García A,Arce-Franco M,Armas-González E,Rodríguez-Pardo M,Lorenzo-Díaz F,Feria M,Cadenas S,Sánchez-Madrid F,Díaz-González F

    更新日期:2013-01-15 00:00:00

  • Gs alpha availability to cholera toxin-catalysed ADP-ribosylation is decreased in membranes of retinoic acid-treated leukemic cell lines HL-60 and THP-1. A posttranslational effect.

    abstract::Retinoic acid (RA) induces HL-60 and THP-1 leukemic cell lines to differentiate into granulocyte-like and monocyte-like cells. Limited data are available concerning the effects of RA on components of the cyclic AMP pathway in human myeloid leukemic cells. We showed previously a decrease in adenylate cyclase activity i...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: de Cremoux P,Zimber A,Calvo F,Lanotte M,Mercken L,Abita JP

    更新日期:1991-11-06 00:00:00