Beneficial effects of L-carnitine in myoblastic C2C12 cells. Interaction with zidovudine.

Abstract:

:L-Carnitine is a key molecule in the transfer of fatty acid across mitochondrial membranes. Bioavailable L-carnitine is either provided by an endogeneous biosynthesis or after intestinal absorption of dietary items containing L-carnitine. After intestinal absorption or hepatic biosynthesis, L-carnitine is transferred to organs whose metabolism is dependent upon fatty acid oxidation, such as skeletal muscle. To cross the muscle plasma membrane, there are several transporters involved. Among those transporters, OCTN2 is actually the only one to have been clearly characterized. Zidovudine is a commonly used inhibitor of human immunodeficiency virus (HIV) replication. Zidovudine has many side effects, including induction of myopathy characterized by a metabolic mitochondria dysfunction and a diminution of the muscle L-carnitine content. In this study, we described the characteristics of L-carnitine transport in C2C12 cells. We also demonstrated that zidovudine inhibited the L-carnitine transporter. This inhibition led to a significant reduction of the muscle cell growth. In C2C12 cells, the supplementation of L-carnitine prevented the effects of zidovudine and restored the normal cell growth.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Georges B,Galland S,Rigault C,Le Borgne F,Demarquoy J

doi

10.1016/s0006-2952(03)00110-2

subject

Has Abstract

pub_date

2003-05-01 00:00:00

pages

1483-8

issue

9

eissn

0006-2952

issn

1873-2968

pii

S0006295203001102

journal_volume

65

pub_type

杂志文章
  • An indirubin derivative, E804, exhibits potent angiosuppressive activity.

    abstract::Angiogenesis, the development of neovessels from pre-existing vessels, is obligatory for solid tumors survival, growth, invasion, and metastasis. Many anti-angiogenic agents are small molecules originated from natural sources. Recently, angiosuppressive effects of indirubin and its derivatives, the active components i...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2011.12.003

    authors: Chan YK,Kwok HH,Chan LS,Leung KS,Shi J,Mak NK,Wong RN,Yue PY

    更新日期:2012-03-01 00:00:00

  • CYP2C19 polymorphisms account for inter-individual variability of drug metabolism in cynomolgus macaques.

    abstract::CYP2C19 (formerly known as CYP2C75), highly homologous to human CYP2C19, has been identified in cynomolgus and rhesus macaques, non-human primate species widely used in drug metabolism studies. CYP2C19 is predominantly expressed in liver and encodes a functional drug-metabolizing enzyme. Genetic variants in human CYP2...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2014.07.004

    authors: Uno Y,Matsushita A,Shukuya M,Matsumoto Y,Murayama N,Yamazaki H

    更新日期:2014-09-15 00:00:00

  • RACking up ceramide-induced islet β-cell dysfunction.

    abstract::The International Diabetes Federation predicts that by 2045 the number of individuals afflicted with diabetes will increase to 629 million. Furthermore, ∼352 million individuals with impaired glucose tolerance are at increased risk for developing diabetes. Several mechanisms have been proposed for the onset of metabol...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2018.04.026

    authors: Kowluru A,Kowluru RA

    更新日期:2018-08-01 00:00:00

  • Regulation on SIRT1-PGC-1α/Nrf2 pathway together with selective inhibition of aldose reductase makes compound hr5F a potential agent for the treatment of diabetic complications.

    abstract::(R,E)-N-(3-(2-acetamido-3-(benzyloxy) propanamido)propyl)-2-cyano-3-(4-hydroxy phenyl)acrylamide (hr5F) was design-synthesized based on bioactivity focus strategy as a potential agent to treat diabetic complicates. With in vitro enzyme assay, it is confirmed that hr5F is an effective ALR2 inhibitor with IC50 value of ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2018.01.034

    authors: Wang Z,Yuan S,Li Y,Zhang Z,Xiao W,Tang D,Ye K,Liu Z,Wang C,Zheng Y,Nie H,Chen H

    更新日期:2018-04-01 00:00:00

  • Inhibition of heart mitochondrial lipid peroxidation by non-toxic concentrations of carvedilol and its analog BM-910228.

    abstract::Carvedilol, a non-selective beta-adrenoreceptor blocker, has been shown to possess a high degree of cardioprotection in experimental models of myocardial damage. Reactive oxygen species have been proposed to be implicated in such situations, and antioxidants have been demonstrated to provide partial protection to the ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(00)00522-0

    authors: Santos DJ,Moreno AJ

    更新日期:2001-01-15 00:00:00

  • Evidence for acyloxymethyl esters of pyrimidine 5'-deoxyribonucleotides as extracellular sources of active 5'-deoxyribonucleotides in cultured cells.

    abstract::Cells commonly resist growth inhibition by purine and pyrimidine bases and nucleosides by restricting intracellular formation of the corresponding 5'-mononucleotides. Nucleotide derivatives that can act as effective membrane-transport precursors of the poorly membrane-permeable nucleotides have not been identified so ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(89)90613-8

    authors: Freed JJ,Farquhar D,Hampton A

    更新日期:1989-10-01 00:00:00

  • Complex relationships of nicotinic receptor actions and cognitive functions.

    abstract::Nicotine has been shown in a variety of studies to improve cognitive function including learning, memory and attention. Nicotine both stimulates and desensitizes nicotinic receptors, thus acting both as an agonist and a net antagonist. The relative roles of these two actions for nicotine-induced cognitive improvement ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2013.07.021

    authors: Levin ED

    更新日期:2013-10-15 00:00:00

  • Comparison of the inducing effect of dehydroepiandrosterone on hepatic peroxisome proliferation-associated enzymes in several rodent species. A short-term administration study.

    abstract::The in-vivo effect of dehydroepiandrosterone (DHEA) on hepatic enzyme activities of rats, mice, hamsters and guinea pigs was investigated. After DHEA treatment (300 mg/kg body weight, per os, 14 days), the activities of peroxisomal beta-oxidation, catalase, carnitine acetyltransferase, carnitine palmitoyltransferase, ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(92)90502-a

    authors: Sakuma M,Yamada J,Suga T

    更新日期:1992-03-17 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

    doi:10.1016/0006-2952(94)90093-0

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

    更新日期:1994-07-19 00:00:00

  • Comparative effects of englitazone and glyburide on gluconeogenesis and glycolysis in the isolated perfused rat liver.

    abstract::Englitazone (CP 68,722, Pfizer) is a member of a family of drugs known as thiazolidinediones. One member of this family, troglitazone (Rezulin), is currently utilized in the treatment of Type 2 diabetes. Previous studies have focused on the ability of englitazone to increase insulin sensitivity in various tissues. How...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(98)00052-5

    authors: Adams MD,Raman P,Judd RL

    更新日期:1998-06-01 00:00:00

  • A novel biologically active seleno-organic compound--I. Glutathione peroxidase-like activity in vitro and antioxidant capacity of PZ 51 (Ebselen).

    abstract::a synthetic seleno-organic compound, 2-phenyl-1,2-benzoisoselenazol-3(2H)-one (PZ 51), exhibits GSH peroxidase-like activity in vitro, in contrast to its sulfur analog, PZ 25. In addition, PZ 51 behaves as an antioxidant shown by a temporary protection of rat liver microsomes against ascorbate/ADP-Fe-induced lipid per...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(84)90083-2

    authors: Müller A,Cadenas E,Graf P,Sies H

    更新日期:1984-10-15 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

    doi:10.1016/j.bcp.2015.12.005

    authors: Ferri E,Petosa C,McKenna CE

    更新日期:2016-04-15 00:00:00

  • Unequivocal synthesis and characterisation of dopamine 3- and 4-O-sulphates.

    abstract::The major metabolic products of the endogeneous catecholamine dopamine are its 3- and 4-O-sulphates which have also been implicated as intermediates in noradrenaline biosynthesis. Because of the unsatisfactory status of the literature concerning the synthesis, isolation, purity and characterisation of the dopamine O-s...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90115-0

    authors: Osikowska BA,Idle JR,Swinbourne FJ,Sever PS

    更新日期:1982-07-01 00:00:00

  • Discovery of a novel nicotinic receptor antagonist for the treatment of nicotine addiction: 1-(3-Picolinium)-12-triethylammonium-dodecane dibromide (TMPD).

    abstract::Limitations in efficacy and high relapse rates of currently available smoking cessation agents reveal the need for more efficacious pharmacotherapies. One strategy is to develop subtype-selective nicotinic receptor (nAChR) antagonists that inhibit nicotine-evoked dopamine (DA) release, the primary neurotransmitter inv...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2007.07.021

    authors: Dwoskin LP,Joyce BM,Zheng G,Neugebauer NM,Manda VK,Lockman P,Papke RL,Bardo MT,Crooks PA

    更新日期:2007-10-15 00:00:00

  • Targeted delivery of superoxide dismutase to macrophages via mannose receptor-mediated mechanism.

    abstract::Human recombinant superoxide dismutase (SOD) was modified into a mannosylated form (Man-SOD), and its cellular uptake and inhibitory effect on superoxide anion release were studied in vitro, using cultured mouse peritoneal macrophages. [111In]Man-SOD was taken up by the macrophages to a great extent, whereas no signif...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90485-5

    authors: Takakura Y,Masuda S,Tokuda H,Nishikawa M,Hashida M

    更新日期:1994-03-02 00:00:00

  • Effects of suramin on increases in cytosolic calcium and on inhibition of adenylate cyclase induced by adenosine 5'-diphosphate in human platelets.

    abstract::The effects of the P2-purinoceptor antagonist, suramin, on ADP-induced increases in human platelet cytosolic calcium concentration ([Ca2+]i) and inhibition of prostaglandin E1 (PGE1)-stimulated adenylate cyclase activity were investigated. Suramin (50-200 microM) acted as an antagonist of ADP-induced increases in [Ca2...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90412-x

    authors: Hall DA,Hourani SM

    更新日期:1994-03-15 00:00:00

  • A selective NaV1.1 activator with potential for treatment of Dravet syndrome epilepsy.

    abstract::Dravet syndrome (DS) is a catastrophic epileptic encephalopathy characterised by childhood-onset polymorphic seizures, multiple neuropsychiatric comorbidities, and increased risk of sudden death. Heterozygous loss-of-function mutations in one allele of SCN1A, the gene encoding the voltage-gated sodium channel 1.1 (NaV...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2020.113991

    authors: Chow CY,Chin YKY,Ma L,Undheim EAB,Herzig V,King GF

    更新日期:2020-11-01 00:00:00

  • Cytotoxicity and glutathione depletion by 1-methyl-2-nitrosoimidazole in human colon cancer cells.

    abstract::The biological effects of 1-methyl-2-nitrosoimidazole (INO), the 2 electron reduction product of biologically active 1-methyl-2-nitroimidazole, were examined in HT-29 human colon cancer cells by clonogenic assay and glutathione (GSH) determination. INO was very toxic towards HT-29 cells and was equally toxic under aer...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(89)90315-8

    authors: Mulcahy RT,Gipp JJ,Ublacker GA,Panicucci R,McClelland RA

    更新日期:1989-05-15 00:00:00

  • Inhibition of IgE-mediated release of histamine and peptide leukotriene from human basophils and mast cells by forskolin.

    abstract::Forskolin, a diterpene compound isolated from the roots of Coleus forskohlii, activates adenylate cyclase in membranes from a variety of mammalian tissues. We found that forskolin (10(-7) to 3 X 10(-5) M) caused a concentration-related inhibition of IgE-mediated release of histamine and peptide leukotriene C4 (LTC4) f...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(87)90377-7

    authors: Marone G,Columbo M,Triggiani M,Cirillo R,Genovese A,Formisano S

    更新日期:1987-01-01 00:00:00

  • Effect of various amounts of selenium on the metabolism of mercuric chloride in mice.

    abstract::Male ddY mice were given one injection of (1) mercury (mercuric chloride) simultaneously with various doses of selenium (sodium selenite), (2) mercury alone, or (3) various doses of selenium alone. The interaction between mercury and selenium in the liver and kidneys at 1, 5, 24, 120, and 240 hr after administration w...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(85)90572-6

    authors: Yamamoto I

    更新日期:1985-08-01 00:00:00

  • Cytosine arabinoside affects multiple cellular factors and induces drug resistance in human lymphoid cells.

    abstract::Continuous in vitro cultivation of human lymphoid H9 cells in the presence of 0.5microM arabinosyl-cytosine (araC) resulted in cell variant, H9-araC cells, that was >600-fold resistant to the drug and cross resistant to its analogs and other unrelated nucleosides, e.g. dideoxycytidine (5-fold), thiacytidine (2-fold), ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2005.05.014

    authors: Sarkar M,Han T,Damaraju V,Carpenter P,Cass CE,Agarwal RP

    更新日期:2005-08-01 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

    doi:10.1016/j.bcp.2007.05.007

    authors: Raddatz R,Schaffhauser H,Marino MJ

    更新日期:2007-08-01 00:00:00

  • Enzymatic and non-enzymatic activities of SHIP-1 in signal transduction and cancer.

    abstract::PI3K cascade is a central signaling pathway regulating cell proliferation, growth, differentiation, and survival. Tight regulation of the PI3K signaling pathway is necessary to avoid aberrant cell proliferation and cancer development. Together with SHIP-1, the inositol phosphatases PTEN and SHIP-2 are the gatekeepers ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2011.05.031

    authors: Condé C,Gloire G,Piette J

    更新日期:2011-11-15 00:00:00

  • PGE2 receptors in detrusor muscle: Drugging the undruggable for urgency.

    abstract::Overactive bladder (OAB) syndrome is a prevalent condition of the lower urinary tract that causes symptoms, such as urinary frequency, urinary urgency, urge incontinence, and nocturia, and disproportionately affects women and the elderly. Current medications for OAB merely provide symptomatic relief with considerable ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2020.114363

    authors: Hou R,Yu Y,Jiang J

    更新日期:2020-12-09 00:00:00

  • Effect of the digitoxigenin derivative, INCICH-D7, on Na+, K+-ATPase.

    abstract::Compound 14beta,17beta-cycloketoester-3beta-OH androstane (INCICH-D7) is a semisynthetic product of a structural modification of the digitoxigenin molecule. INCICH-D7 has a heterocyclic ketoester type fusion between positions C14 and C17 of the steroid nucleus, which confers this molecule stronger electronegativity th...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2005.06.020

    authors: Ramirez M,Del Valle L,Sanchez-Mendoza A,Tenorio FA,Zarco G,Pastelin G

    更新日期:2005-09-15 00:00:00

  • Potential of phytochemicals as immune-regulatory compounds in atopic diseases: A review.

    abstract::Atopic diseases (atopic dermatitis, asthma and allergic rhinitis) affects a huge number of people around the world and their incidence rate is on rise. Atopic dermatitis (AD) is more prevalent in paediatric population which sensitizes an individual to develop allergic rhinitis and asthma later in life. The complex pat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2019.113790

    authors: Sharma S,Naura AS

    更新日期:2020-03-01 00:00:00

  • Cudratricusxanthone G inhibits human colorectal carcinoma cell invasion by MMP-2 down-regulation through suppressing activator protein-1 activity.

    abstract::Cudratricusxanthone G (CTXG), a natural bioactive cudratricusxanthone extracted from C. tricuspidata, has shown anti-cancer properties. However, the function and mechanism of CTXG in tumor invasion have not been elucidated to date. In this study, we investigated the inhibitory effect of CTXG on the proliferation, migr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2011.02.017

    authors: Kuang L,Wang L,Wang Q,Zhao Q,Du B,Li D,Luo J,Liu M,Hou A,Qian M

    更新日期:2011-05-15 00:00:00

  • Pharmacological modulation of human platelet leukotriene C4-synthase.

    abstract::The aim of this study was to test if human platelet leukotriene C4-synthase (LTC4-S) is pharmacologically different from cloned and expressed LTC4-S and, in light of the significant homologies between 5-lipoxygenase activating protein (FLAP) and LTC4-S, if different potencies of leukotriene synthesis inhibitors acting...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(96)00819-2

    authors: Sala A,Folco G,Henson PM,Murphy RC

    更新日期:1997-03-21 00:00:00

  • Role of NADPH:cytochrome P450 reductase in the hypoxic accumulation and metabolism of BRU59-21, a technetium-99m-nitroimidazole for imaging tumor hypoxia.

    abstract::Nitroimidazoles labeled with technetium-99m are being investigated as non-invasive markers of tumor hypoxia. They are bioreductive compounds that require enzymatic reduction for retention in hypoxic cells, but little is known about the cellular factors affecting their accumulation in hypoxic cells. If the absolute acc...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(00)00373-7

    authors: Melo T,Ballinger JR,Rauth AM

    更新日期:2000-09-01 00:00:00

  • Rat liver kininase, a serine peptidase.

    abstract::A serine peptidase (RLK1) was partially purified from rat liver homogenates. Its molecular weight was 80,000, and its optimum pH was 7.5. Bz-Tyr-O-Et was hydrolyzed by the enzyme, which was inhibited by Ip2PF, PMSF and by Tos-Phe-CH2Cl. The bonds cleaved by the enzyme were Phe5-Ser6 and Phe8-Arg9, when bradykinin was ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90466-x

    authors: Da Graça M,Mazzacoratti N,Sampaio CA

    更新日期:1982-03-01 00:00:00