mersalyl

Summary

Summary: A toxic thiol mercury salt formerly used as a diuretic. It inhibits various biochemical functions, especially in mitochondria, and is used to study those functions.

Top Publications

  1. Kowaltowski A, Vercesi A, Castilho R. Mitochondrial membrane protein thiol reactivity with N-ethylmaleimide or mersalyl is modified by Ca2+: correlation with mitochondrial permeability transition. Biochim Biophys Acta. 1997;1318:395-402 pubmed
    ..content of mitochondrial membrane protein thiol groups accessible to react with the monofunctional thiol reagents mersalyl or N-ethylmaleimide (NEM) was determined using Ellman's reagent...
  2. Agani F, Semenza G. Mersalyl is a novel inducer of vascular endothelial growth factor gene expression and hypoxia-inducible factor 1 activity. Mol Pharmacol. 1998;54:749-54 pubmed
    ..We report here that the organomercurial compound mersalyl induced expression of VEGF and enolase 1 mRNA, as well as HIF-1 activity, in cultured cells...
  3. Silva P, Epstein F, Solomon R. The effect of mercury on chloride secretion in the shark (Squalus acanthias) rectal gland. Comp Biochem Physiol C. 1992;103:569-75 pubmed
    ..3. Two organic mercurials, mersalyl and meralluride, that are effective diuretics in the mammalian kidney, and p-chloromercuribenzoyl sulfonic acid (..
  4. García N, Martínez Abundis E, Pavón N, Chávez E. On the opening of an insensitive cyclosporin A non-specific pore by phenylarsine plus mersalyl. Cell Biochem Biophys. 2007;49:84-90 pubmed
    ..To meet this proposal phenylarsine oxide (PHA) and mersalyl were employed as tools to induce permeability transition and CSA to inhibit it...
  5. Ventura H. History of heart failure. Congest Heart Fail. 2006;12:178 pubmed
  6. Belogurov G, Turkina M, Penttinen A, Huopalahti S, Baykov A, Lahti R. H+-pyrophosphatase of Rhodospirillum rubrum. High yield expression in Escherichia coli and identification of the Cys residues responsible for inactivation my mersalyl. J Biol Chem. 2002;277:22209-14 pubmed
    ..had no effect on the activity of H(+)-PPase but decreased its sensitivity to the sulfhydryl modifying reagent, mersalyl. H(+)-PPase lacking all three Cys residues was completely resistant to the effects of mersalyl...
  7. Lalitha K, Rani P. Mitochondrial selenium-75 uptake and regulation revealed by kinetic analysis. Biol Trace Elem Res. 1995;49:21-42 pubmed
    ..Thiol interactive 75Se uptake was confirmed by the inhibition mediated by mersalyl and NEM up to 50-70%...
  8. Manon S, Guerin M. Modifications of oxidative phosphorylations in mitochondria isolated from a mutant of Saccharomyces cerevisiae. Possible alterations of the phosphate transport. Eur J Biochem. 1988;172:205-11 pubmed
    ..to reach a maximal state 3 of respiration; (d) phosphate transport, as measured by swelling experiments, was mersalyl-insensitive and, consequently, state 3 of the respiration and ATP synthesis remained less mersalyl-sensitive than ..
  9. Atlante A, Passarella S, Pierro P, Quagliariello E. Proline transport in rat kidney mitochondria. Arch Biochem Biophys. 1994;309:139-48 pubmed
    ..Discussion is also made of the possible role of such translocators in proline metabolism and in the putative proline/glutamate shuttle. ..

More Information

Publications62

  1. Gallina F, Gerez De Burgos N, Burgos C, Coronel C, Blanco A. The lactate/pyruvate shuttle in spermatozoa: operation in vitro. Arch Biochem Biophys. 1994;308:515-9 pubmed
    ..6, 1.28, and 1.6 for mouse, rat, and rabbit organelles, respectively. The shuttle is inhibited by 0.6 mM mersalyl, a blocker of lactate transport...
  2. Manon S, Guerin M. Investigation of the effects of Zn2+ and Cu2+ on the K+ transport in yeast mitochondria. Evidences for the involvement of a Zn(2+)-binding protein in the K+/H+ exchange. Biochem Mol Biol Int. 1995;35:585-93 pubmed
    ..iii) The thiol reagent mersalyl prevented the inhibition by Zn2+ whereas N-ethylmaleimide and 5,5'-dithiobis(2-nitrobenzoate) prevented the ..
  3. Joseph S, Ryan S, Pierson S, Renard Rooney D, Thomas A. The effect of mersalyl on inositol trisphosphate receptor binding and ion channel function. J Biol Chem. 1995;270:3588-93 pubmed
    ..At 4 degrees C, the organomercurial thiol-reactive agent mersalyl markedly stimulates (3-4fold) [3H]IP3 binding to permeabilized hepatocytes...
  4. Ellis D, Tran S, Eagon P, Avner E. Reversible inhibition of cytosolic glucocorticoid receptors by mercurial agents. Application in the measurement of total and unoccupied receptors. J Recept Res. 1987;7:761-74 pubmed
    ..Experiments defined the conditions whereby two sulfhydryl-binding agents, p-hydroxymercuribenzoate (PHMB) and mersalyl, completely inhibited binding of the glucocorticoid receptor to ligand in mouse renal cytosol...
  5. Ligeti E, Fonyo A. Phosphate transport protein of rat heart mitochondria: location of its SH-groups and exploration of their environment. Biochim Biophys Acta. 1989;973:170-5 pubmed
    ..It is suggested that the amino-acid sequence around the NEM-reactive cysteine (i.e., Lys-41 - Cys-42 - Arg-43) does not participate in substrate binding. ..
  6. Alcantara R, Lopez Corcuera B, Aragon C. Group-selective reagent modification of the sodium- and chloride-coupled glycine transporter under native and reconstituted conditions. Biochim Biophys Acta. 1991;1067:64-70 pubmed
    ..SH groups display a similar reactivity for p-chloromercuribenzenesulfonate (pCMBS) and mersalyl in synaptosomal membrane vesicles and proteoliposomes reconstituted with the solubilized transporter...
  7. Atlante A, Passarella S, Quagliariello E, Moreno G, Salet C. Carrier thiols are targets of Photofrin II photosensitization of isolated rat liver mitochondria. J Photochem Photobiol B. 1990;7:21-32 pubmed
    ..The ability of the thiol reagent mersalyl (an inhibitor of phosphate, dicarboxylate and oxodicarboxylate carriers) to protect these carriers against ..
  8. Zara V, Dietmeier K, Palmisano A, Vozza A, Rassow J, Palmieri F, et al. Yeast mitochondria lacking the phosphate carrier/p32 are blocked in phosphate transport but can import preproteins after regeneration of a membrane potential. Mol Cell Biol. 1996;16:6524-31 pubmed
  9. Bobba A, Amadoro G, Petragallo V, Calissano P, Atlante A. Dissecting the molecular mechanism by which NH2htau and A?1-42 peptides impair mitochondrial ANT-1 in Alzheimer disease. Biochim Biophys Acta. 2013;1827:848-60 pubmed publisher
    ..and A?1-42 is due to an interplay between these two Alzheimer's peptides, ROS and ANT-1 thiols, use was made of mersalyl, a reversible alkylating agent of thiol groups that are oriented toward the external hydrophilic phase, to ..
  10. Siliprandi D, Toninello A, Dalla Via L. Bidirectional transport of spermine in rat liver mitochondria. Biochim Biophys Acta. 1992;1102:62-6 pubmed
    ..14C]spermine and [32P]phosphate, these components are released together into the surrounding medium by adding mersalyl or N-ethylmaleimide...
  11. Wang T, Hussey C, Hause L, Fobian J. Platelet aggregation induced by antilymphocyte serum. 2. Two modes of the aggregation mechanism. Am J Clin Pathol. 1976;65:680-9 pubmed
    ..Salyrgan (mersalyl) in the presence of ALS or bovine fibrinogen produced an aggregation response in unwashed platelets that ..
  12. Lanza Jacoby S, Feagins K, Bodine R, Reibel D. Impaired carnitine transport in the rat heart during E. coli sepsis. Circ Shock. 1991;35:159-63 pubmed
    ..Carnitine uptake in the presence of 0.05 M mersalyl acid was comparable in both groups of hearts at all perfusate carnitine concentrations indicating no change in ..
  13. Murakami E, Deppenmeier U, Ragsdale S. Characterization of the intramolecular electron transfer pathway from 2-hydroxyphenazine to the heterodisulfide reductase from Methanosarcina thermophila. J Biol Chem. 2001;276:2432-9 pubmed
    ..Fe-S cluster disruption by mersalyl acid inhibits heme reduction by HPhenH(2), suggesting that a 4Fe cluster is the initial electron acceptor from ..
  14. Paradies G, Ruggiero F. Effect of aging on the activity of the phosphate carrier and on the lipid composition in rat liver mitochondria. Arch Biochem Biophys. 1991;284:332-7 pubmed
    ..Inhibitor titrations with mersalyl provide no evidence for a lower content of functional phosphate translocase in mitochondria from aged rats...
  15. Sakr S, Lemoine R, Gaillard C, Delrot S. Effect of cutting on solute uptake by plasma membrane vesicles from sugar beet (Beta vulgaris L.) leaves. Plant Physiol. 1993;103:49-58 pubmed
    ..in fresh discs was sensitive to N-ethylmaleimide (NEM), to p-chloromercuribenzenesulfonic acid (PCMBS), and to mersalyl acid (MA)...
  16. Amores M, Hortelano P, Garcia Salguero L, Lupianez J. Metabolic adaptation of renal carbohydrate metabolism. V. In vivo response of rat renal-tubule gluconeogenesis to different diuretics. Mol Cell Biochem. 1994;137:117-25 pubmed
    We have studied the effects of the diuretics mersalyl, furosemide and ethacrynic acid on renal gluconeogenesis is isolated rat-kidney tubules and on the activities of the most important gluconeogenic and glycolytic enzymes in both fed and ..
  17. Herick K, Kramer R. Kinetic and energetic characterization of solute flux through the reconstituted aspartate/glutamate carrier from beef heart mitochondria after modification with mercurials. Biochim Biophys Acta. 1995;1238:63-71 pubmed
    ..The consequence of these results for understanding the transport function of the aspartate/glutamate carrier in the slippage mode (uniport) is discussed in energetic and kinetic terms. ..
  18. Tikhonova I, Andreyev AYu -, Antonenko YuN -, Kaulen A, Komrakov AYu -, Skulachev V. Ion permeability induced in artificial membranes by the ATP/ADP antiporter. FEBS Lett. 1994;337:231-4 pubmed
    ..b>Mersalyl treatment of ANT-bacteriorhodopsin proteoliposomes causes further increase in the delta pH dissipation rate due ..
  19. Quesada A, McGivan J. A rapid method for the functional reconstitution of amino acid transport systems from rat liver plasma membranes. Partial purification of System A. Biochem J. 1988;255:963-9 pubmed
    ..By using this reconstitution procedure, System A transport activity was partially purified by lectin-affinity chromatography...
  20. Ackley D, Yokel R. Aluminum transport out of brain extracellular fluid is proton dependent and inhibited by mersalyl acid, suggesting mediation by the monocarboxylate transporter (MCT1). Toxicology. 1998;127:59-67 pubmed
    ..Organomercurial thiol reagents, such as mersalyl acid, inhibit MCT1 but not MCT2...
  21. Silvestroni L, Menditto A, Modesti A, Scarpa S. Zinc uptake in human seminal spermatozoa: characterization and effects on cell membranes. Arch Androl. 1989;23:97-103 pubmed
    ..The failure of nonpermeant SH reagent mersalyl to modify zinc uptake indicates that functional membrane sulfhydryl groups are not involved in the process...
  22. Palmieri F, Passarella S, Stipani I, Quagliariello E. Mechanism of inhibition of the dicarboxylate carrier of mitochondria by thiol reagents. Biochim Biophys Acta. 1974;333:195-208 pubmed
    ..1) Mersalyl and p-hydroxymercuribenzoate increase the Km without changing the V of malonate/Pi exchange, when they are added ..
  23. Peterson F, Holtzman J, Crankshaw D, Mason R. Two sites of azo reduction in the monooxygenase system. Mol Pharmacol. 1988;34:597-603 pubmed
    ..620 V; sulfonazo III, E = -0.265 V versus normal hydrogen electrode). The organic mercurial mersalyl converted cytochrome P-450 to cytochrome P-420 (68%) and markedly decreased NADPH-cytochrome P-450(c) reductase ..
  24. Goeger D, Riley R. Interaction of cyclopiazonic acid with rat skeletal muscle sarcoplasmic reticulum vesicles. Effect on Ca2+ binding and Ca2+ permeability. Biochem Pharmacol. 1989;38:3995-4003 pubmed
    ..SR vesicles (in the presence of ruthenium red) when compared to either untreated vesicles or those treated with mersalyl acid, a mercurial which also inhibits the Ca2+-ATPase and is known to induce Ca2+ release by both ruthenium red-..
  25. Yagel S, Parhar R, Jeffrey J, Lala P. Normal nonmetastatic human trophoblast cells share in vitro invasive properties of malignant cells. J Cell Physiol. 1988;136:455-62 pubmed
    ..b>Mersalyl, a compound known to activate collagenase, stimulated invasion by all cell lines tested, including under ..
  26. Moreno G, Poussin K, Ricchelli F, Salet C. The effects of singlet oxygen produced by photodynamic action on the mitochondrial permeability transition differ in accordance with the localization of the sensitizer. Arch Biochem Biophys. 2001;386:243-50 pubmed
    ..Interestingly, this inducing effect is inhibited when TMP-treated mitochondria are irradiated after addition of mersalyl, a specific reagent protecting thiol groups of the inner mitochondrial membrane that are oriented toward the ..
  27. Beavis A. The mitochondrial inner-membrane anion channel possesses two mercurial-reactive regulatory sites. Eur J Biochem. 1989;185:511-9 pubmed
    ..In this paper, evidence is provided that mersalyl and p-chloromercuribenzene-sulfonate each interact with this uniporter at two distinct sites...
  28. Atlante A, Seccia T, Marra E, Minervini G, Vulpis V, Pirrelli A, et al. Carrier-mediated transport controls hydroxyproline catabolism in heart mitochondria from spontaneously hypertensive rat. FEBS Lett. 1996;396:279-84 pubmed
    ..by the occurrence of both saturation kinetics and the inhibition shown by phenylsuccinate and the thiol reagent mersalyl. In any case, hydroxyproline transport was found to limit the rate of mitochondrial hydroxyproline catabolism...
  29. Hapgood J, von Holt C. Steroid-affinity purification of the rat liver glucocorticoid hormone receptor complex. J Steroid Biochem. 1987;28:769-77 pubmed
    ..The use of denaturing and sulfhydryl modifying reagents (NaSCN, DMSO, Mersalyl) during elution led to partial or complete irreversible loss of steroid-binding activity of the unoccupied ..
  30. Tsuchiya N, Ochi T. Mechanism for the decrease in the accumulation of cadmium (Cd) in Cd-resistant Chinese hamster V79 cells. Arch Toxicol. 1994;68:325-31 pubmed
    ..The Km values were 31.95 microM for Cdr cells and 3.15 microM for Cds cells. Mersalyl acid, a sulfhydryl (SH) blocker to which cells are impermeable, inhibited the uptake of Cd by Cds cells at ..
  31. Gettings S, Reeve J, King L. Possible role of intracellular Ca2+ in the toxicity of phenformin. Biochem Pharmacol. 1988;37:281-9 pubmed
    ..g. 2-oxoglutarate dehydrogenase) due to alteration in mitochondrial calcium content, is proposed. ..
  32. Pastore D, Laus M, Di Fonzo N, Passarella S. Reactive oxygen species inhibit the succinate oxidation-supported generation of membrane potential in wheat mitochondria. FEBS Lett. 2002;516:15-9 pubmed
    ..It does not involve mitochondrial thiol groups sensitive to either mersalyl or N-ethylmaleimide and might involve both protein residues and/or membrane lipids, as suggested by the mixed ..
  33. Brustovetsky N, Klingenberg M. The reconstituted ADP/ATP carrier can mediate H+ transport by free fatty acids, which is further stimulated by mersalyl. J Biol Chem. 1994;269:27329-36 pubmed
    ..P. (1991) FEBS Lett. 294, 158-162). Mersalyl treatment of the AAC-COX proteoliposomes resulted in an increase of the AAC-mediated protonophoric action of FFA...
  34. Tischler M, Rosenberg S, Satarug S, Henriksen E, Kirby C, Tome M, et al. Different mechanisms of increased proteolysis in atrophy induced by denervation or unweighting of rat soleus muscle. Metabolism. 1990;39:756-63 pubmed
    ..3-Methyladenine, which inhibits phagosome formation, increased latency similarly in all muscles tested. Mersalyl, a thiol protease inhibitor, and 8-(diethylamino)octyl-3,4,5-trimethoxybenzoate hydrochloride (TMB-8), which ..
  35. Szewczyk A, Wojcik G, Lobanov N, Nalecz M. Modification of the mitochondrial sulfonylurea receptor by thiol reagents. Biochem Biophys Res Commun. 1999;262:255-8 pubmed
    ..Similar effects were observed with membrane permeable (N-ethylmaleimide) and non-permeable (mersalyl) thiol modifying agents...
  36. Park C, Doh P, Lee C, Han D, Carraway R, Miller T. Cellular mechanism of stimulation of renin secretion by the mercurial diuretic mersalyl. J Pharmacol Exp Ther. 1991;257:219-24 pubmed
    The aim of the present study was to elucidate the cellular mechanism by which the mercurial diuretic mersalyl stimulates renin secretion in rabbit renal cortical slices in vitro...
  37. Huang S, Klingenberg M. Chloride channel properties of the uncoupling protein from brown adipose tissue mitochondria: a patch-clamp study. Biochemistry. 1996;35:16806-14 pubmed
    ..Fatty acids, pH, divalent cations (Ca2+ and Mg2+), and mersalyl do not influence these Cl- currents...
  38. Roberg B, Torgner I, Kvamme E. Glutamine transport in rat brain synaptic and non-synaptic mitochondria. Neurochem Res. 1999;24:383-90 pubmed
    ..The uptake is inversely correlated to medium osmolarity, temperature-dependent, saturable and inhibited by mersalyl, and glutamine is upconcentrated in the mitochondria...
  39. Rubtsov A, Murphy A. Caffeine interaction with the Ca-release channels of heavy sarcoplasmic reticulum. Evidence that 170 kD Ca-binding protein is a caffeine receptor of the Ca-channels. Biochem Biophys Res Commun. 1988;154:462-8 pubmed
    ..The 170 kD Ca-binding protein which is eluted by caffeine is the most probable candidate for the caffeine receptor of the Ca-channels. ..
  40. Oppedisano F, Galluccio M, Indiveri C. Inactivation by Hg2+ and methylmercury of the glutamine/amino acid transporter (ASCT2) reconstituted in liposomes: Prediction of the involvement of a CXXC motif by homology modelling. Biochem Pharmacol. 2010;80:1266-73 pubmed publisher
    The effect of HgCl(2), methylmercury and mersalyl on the glutamine/amino acid (ASCT2) transporter reconstituted in liposomes has been studied...
  41. Wisniewski E, Kunz W, Gellerich F. Phosphate affects the distribution of flux control among the enzymes of oxidative phosphorylation in rat skeletal muscle mitochondria. J Biol Chem. 1993;268:9343-6 pubmed
    ..This indicates that under the conditions of intermediate state respiration, all of the other reactions have a negligible controlling influence on oxidative phosphorylation in skeletal muscle mitochondria. ..
  42. Trumper L, Schonfeld P, Augustin W. Flux control coefficients for Pi- and adenine nucleotide translocator in rat liver mitochondria after Fe2+/ascorbate induced oxidative stress. Biomed Biochim Acta. 1989;48:S44-7 pubmed
    ..The data show that the predominant step in the control of oxidative phosphorylation at the site of the consumers must be attributed to the ATP/ADP-exchanger. ..
  43. Genchi G, Petrone G, De Palma A, Cambria A, Palmieri F. Interaction of phenylisothiocyanates with the mitochondrial phosphate carrier. I. Covalent modification and inhibition of phosphate transport. Biochim Biophys Acta. 1988;936:413-20 pubmed
    ..Preincubation with mersalyl protects the carrier protein against the inactivation by p-sulfoPITC but not against PITC...
  44. Huang R, Lee T. Cellular uptake of trivalent arsenite and pentavalent arsenate in KB cells cultured in phosphate-free medium. Toxicol Appl Pharmacol. 1996;136:243-9 pubmed
    ..when cells were grown in phosphate-free RPMI medium, As(V) uptake was dose-dependently inhibited by phosphate, mersalyl acid (a membrane sulfhydryl agent), and energy poisons, such as sodium azide and potassium cyanide...
  45. Laus M, Soccio M, Trono D, Cattivelli L, Pastore D. Plant inner membrane anion channel (PIMAC) function in plant mitochondria. Plant Cell Physiol. 2008;49:1039-55 pubmed publisher
  46. Doussiere J, Vignais P. Diphenylene iodonium as an inhibitor of the NADPH oxidase complex of bovine neutrophils. Factors controlling the inhibitory potency of diphenylene iodonium in a cell-free system of oxidase activation. Eur J Biochem. 1992;208:61-71 pubmed
  47. Mariano A, Valente C, Cadena S, Rocha M, de Oliveira M, Carnieri E. Sensitivities of the alternative respiratory components of potato tuber mitochondria to thiol reagents and Ca2+. Plant Physiol Biochem. 2005;43:61-7 pubmed
    ..b>Mersalyl inhibited the externally located NADH dehydrogenase and had no effect on AOX activity...
  48. Samartsev V, Chezganova S, Polishchuk L, Paydyganov A, Vidyakina O, Zeldi I. Temperature dependence of rat liver mitochondrial respiration with uncoupling of oxidative phosphorylation by fatty acids. Influence of inorganic phosphate. Biochemistry (Mosc). 2003;68:618-26 pubmed
    ..b>Mersalyl (10 nmol/mg protein), an inhibitor of the phosphate carrier, similarly to phosphate, suppresses the uncoupling ..
  49. Boot J. Hepatotoxic effects of SH-reagents in human and rat hepatocyte cultures and in situ perfused rat livers. Cell Struct Funct. 1996;21:221-9 pubmed
    Effects organic mercurials (PCMBS, PCMB, mersalyl) an alkylating reagent (NEM), disulphide reagents (DTP, CPDS) and the dithiocarbamate agent DSF (disulfiram) were studied in hepatocyte culture...
  50. Gooding J, Shayeghi M, Saggerson E. Membrane transport of fatty acylcarnitine and free L-carnitine by rat liver microsomes. Eur J Biochem. 2004;271:954-61 pubmed
    ..This process, mediated either by a channel or a carrier, was inhibited by mersalyl but not by N-ethylmaleimide or sulfobetaine - properties that differentiate it from the mitochondrial inner ..
  51. Ng L, Selwyn M, Choo H. Inorganic phosphate is the major component of the thermostable cytoplasmic fraction which stimulates mitochondrial anion uniport. Biochim Biophys Acta. 1993;1183:180-4 pubmed
    ..b>Mersalyl blocks stimulation when added before, but not when added after, incubation with phosphate which shows that the ..
  52. Manon S, Guerin M. The ATP-induced K(+)-transport pathway of yeast mitochondria may function as an uncoupling pathway. Biochim Biophys Acta. 1997;1318:317-21 pubmed
    ..AT 5 mM phosphate, no uncoupling effect of K+ could be evidenced. These data suggest that the ATP-induced K(+)-transport pathway may, under certain conditions, function as an uncoupling pathway of oxidative phosphorylation. ..
  53. Bonanno J. Lactate-proton cotransport in rabbit corneal epithelium. Curr Eye Res. 1990;9:707-12 pubmed
    ..These inhibitors of lactate-H+ cotransport were reversible. Mersalyl acid (500 microM) inhibited proton flux from 10 mM lactate addition by nearly 100%, but was irreversible...