antimony potassium tartrate

Summary

Summary: A schistosomicide possibly useful against other parasites. It has irritant emetic properties and may cause lethal cardiac toxicity among other adverse effects.

Top Publications

  1. Wey H, Richards D, Tirmenstein M, Mathias P, Toraason M. The role of intracellular calcium in antimony-induced toxicity in cultured cardiac myocytes. Toxicol Appl Pharmacol. 1997;145:202-10 pubmed
    ..These results demonstrate that PAT disrupts [Ca2+]i handling and support a role for a calcium-dependent event, but do not support the necessity of events in PAT-induced cell death that are mediated by a large elevation in [Ca2+]i. ..
  2. Dieter M, Jameson C, Elwell M, Lodge J, Hejtmancik M, Grumbein S, et al. Comparative toxicity and tissue distribution of antimony potassium tartrate in rats and mice dosed by drinking water or intraperitoneal injection. J Toxicol Environ Health. 1991;34:51-82 pubmed
    b>Antimony potassium tartrate (APT) is a complex salt that until recently was used worldwide as an antischistosomal drug...
  3. Lynch B, Capen C, Nestmann E, Veenstra G, Deyo J. Review of subchronic/chronic toxicity of antimony potassium tartrate. Regul Toxicol Pharmacol. 1999;30:9-17 pubmed
    Subchronic/chronic toxicity studies on antimony potassium tartrate (APT) have been reviewed. One of the older studies (H. A. Schroeder et al., 1970, J. Nutr...
  4. Naredi P, Heath D, Enns R, Howell S. Cross-resistance between cisplatin, antimony potassium tartrate, and arsenite in human tumor cells. J Clin Invest. 1995;95:1193-8 pubmed
    ..two head and neck carcinoma cell lines selected for DDP resistance were found to be cross-resistant to antimony potassium tartrate, which contains trivalent antimony...
  5. Ferreira Pinto K, Miranda Vilela A, Anacleto C, Fernandes A, Abdo M, Petrillo Peixoto M, et al. Leishmania (V.) guyanensis: isolation and characterization of glucantime-resistant cell lines. Can J Microbiol. 1996;42:944-9 pubmed
    ..These cell lines showed cross resistance to heavy metals but were sensitive to puromycin, vinblastine, and pentostam. ..
  6. Sun H, Yan S, Cheng W. Interaction of antimony tartrate with the tripeptide glutathione implication for its mode of action. Eur J Biochem. 2000;267:5450-7 pubmed
    ..Such facile exchange may be important in the transport of Sb(III) in various biofluids and tissues in vivo. Our spin-echo 1H-NMR data show that Sb(III) rapidly entered red blood cell walls and was complexed by intracellular glutathione. ..
  7. Holzmuller P, Sereno D, Lemesre J. Lower nitric oxide susceptibility of trivalent antimony-resistant amastigotes of Leishmania infantum. Antimicrob Agents Chemother. 2005;49:4406-9 pubmed
    ..Shared biochemical targets for SbIII and NO resistance in Leishmania are discussed. ..
  8. Takahashi S, Sato H, Kubota Y, Utsumi H, Bedford J, Okayasu R. Inhibition of DNA-double strand break repair by antimony compounds. Toxicology. 2002;180:249-56 pubmed
    ..The cells were first incubated with antimony trichloride or antimony potassium tartrate (both Sb(III)) for 2 h, and then irradiated with gamma-rays at a dose of 40 Gy...
  9. Carter K, Hutchison S, Boitelle A, Murray H, Sundar S, Mullen A. Sodium stibogluconate resistance in Leishmania donovani correlates with greater tolerance to macrophage antileishmanial responses and trivalent antimony therapy. Parasitology. 2005;131:747-57 pubmed
    ..These results indicate that SSG exposure may favour the emergence of more virulent strains. ..

More Information

Publications47

  1. Pathak M, Yi T. Sodium stibogluconate is a potent inhibitor of protein tyrosine phosphatases and augments cytokine responses in hemopoietic cell lines. J Immunol. 2001;167:3391-7 pubmed
    ..Our results provide novel insights into the pharmacological effects of the drug and suggest potential new therapeutic applications. ..
  2. Faghiri Z, Skelly P. The role of tegumental aquaporin from the human parasitic worm, Schistosoma mansoni, in osmoregulation and drug uptake. FASEB J. 2009;23:2780-9 pubmed publisher
    ..These experiments reveal a heretofore unrecognized role of the schistosome tegument in controlling water and drug movement into the parasites and highlight the importance of the tegument in parasite osmoregulation and drug uptake. ..
  3. Liarte D, Murta S. Selection and phenotype characterization of potassium antimony tartrate-resistant populations of four New World Leishmania species. Parasitol Res. 2010;107:205-12 pubmed publisher
    ..Although the protocol of induction was the same, the SbIII-resistant populations showed different degrees of tolerance, stability, infectivity in mice and cross-resistance to antileishmanial drugs, depending on the Leishmania species. ..
  4. Wijeratne A, Yang S, Gracia J, Armstrong D, Schug K. ESI-MS investigation of solvent effects on the chiral recognition capacity of tartar emetic towards neutral side-chain amino acids. Chirality. 2011;23:44-53 pubmed publisher
  5. Lorico A, Bertola A, Baum C, Fodstad O, Rappa G. Role of the Multidrug Resistance Protein 1 in protection from heavy metal oxyanions: investigations in vitro and in MRP1-deficient mice. Biochem Biophys Res Commun. 2002;291:617-22 pubmed
    ..have previously shown that mrp1(-/-) cells are hypersensitive to sodium arsenite, sodium arsenate, and antimony potassium tartrate. We now report that the retroviral vector-mediated overexpression of MRP1 and of the two subunits of ..
  6. Sarkar A, Saha P, Mandal G, Mukhopadhyay D, Roy S, Singh S, et al. Monitoring of intracellular nitric oxide in leishmaniasis: its applicability in patients with visceral leishmaniasis. Cytometry A. 2011;79:35-45 pubmed publisher
    ..Taken together, this study opens new perspectives of research regarding monocyte function and provides a real time approach for monitoring the effect of anti-leishmanial compounds. ..
  7. Rosenstein R, Peschel A, Wieland B, G tz F. Expression and regulation of the antimonite, arsenite, and arsenate resistance operon of Staphylococcus xylosus plasmid pSX267. J Bacteriol. 1992;174:3676-83 pubmed
    ..The three ars genes conferred arsenite resistance in E. coli and arsenite as well as arsenate resistance in Bacillus subtilis...
  8. Salerno M, Petroutsa M, Garnier Suillerot A. The MRP1-mediated effluxes of arsenic and antimony do not require arsenic-glutathione and antimony-glutathione complex formation. J Bioenerg Biomembr. 2002;34:135-45 pubmed
    ..Moreover for the three compounds 50% of the efflux is inhibited by 2 microM MK571. This led us to suggest that As- and Sb-containing species could be cotransported with GSH. ..
  9. Lecureur V, Le Thiec A, Le Meur A, Amiot L, Drenou B, Bernard M, et al. Potassium antimonyl tartrate induces caspase- and reactive oxygen species-dependent apoptosis in lymphoid tumoral cells. Br J Haematol. 2002;119:608-15 pubmed
    ..These data therefore suggest that PAT may deserve to be evaluated in the treatment of some lymphoid malignancies. ..
  10. Sudhandiran G, Shaha C. Antimonial-induced increase in intracellular Ca2+ through non-selective cation channels in the host and the parasite is responsible for apoptosis of intracellular Leishmania donovani amastigotes. J Biol Chem. 2003;278:25120-32 pubmed
  11. Brochu C, Haimeur A, Ouellette M. The heat shock protein HSP70 and heat shock cognate protein HSC70 contribute to antimony tolerance in the protozoan parasite leishmania. Cell Stress Chaperones. 2004;9:294-303 pubmed
    ..Our results are consistent with HSP70 and HSC70 being a first line of defense against SbIII until more specific and efficient resistance mechanisms take over. ..
  12. Tarabar A, Khan Y, Nelson L, Hoffman R. Antimony toxicity from the use of tartar emetic for the treatment of alcohol abuse. Vet Hum Toxicol. 2004;46:331-3 pubmed
    ..It is important to recognize that foreign alcohol therapies aversive therapy other than disulfiram may be used, the contents of such a foreign product should be identified. ..
  13. Ruan X, Bhattacharjee H, Rosen B. Cys-113 and Cys-422 form a high affinity metalloid binding site in the ArsA ATPase. J Biol Chem. 2006;281:9925-34 pubmed
  14. Tirmenstein M, Plews P, Walker C, Woolery M, Wey H, Toraason M. Antimony-induced oxidative stress and toxicity in cultured cardiac myocytes. Toxicol Appl Pharmacol. 1995;130:41-7 pubmed
    ..Our results also suggest that PAT interacts with thiol-containing compounds. ..
  15. Ait Oudhia K, Gazanion E, Sereno D, Oury B, Dedet J, Pratlong F, et al. In vitro susceptibility to antimonials and amphotericin B of Leishmania infantum strains isolated from dogs in a region lacking drug selection pressure. Vet Parasitol. 2012;187:386-93 pubmed publisher
    ..Moreover, our data showed that isolates belonging to the relatively rare zymodeme of L. infantum, MON-281, were less susceptible to antimony than MON-1, when at the same time there was no significant difference for amphotericin B...
  16. Duffin J, Campling B. Therapy and disease concepts: the history (and future?) of antimony in cancer. J Hist Med Allied Sci. 2002;57:61-78 pubmed
  17. Tirmenstein M, Mathias P, Snawder J, Wey H, Toraason M. Antimony-induced alterations in thiol homeostasis and adenine nucleotide status in cultured cardiac myocytes. Toxicology. 1997;119:203-11 pubmed
    ..Decreases in cellular ATP levels paralleled PAT toxicity put appeared to be secondary to other cellular changes initiated by PAT exposure. ..
  18. Roberts W, Berman J, Rainey P. In vitro antileishmanial properties of tri- and pentavalent antimonial preparations. Antimicrob Agents Chemother. 1995;39:1234-9 pubmed
    ..N-Acetylcysteine antagonized the antileishmanial effects of these three drugs against intracellular amastigotes; in contrast, it had minimal effects on the action of sodium stibogluconate. ..
  19. Chen Z, Mutoh M, Sumizawa T, Furukawa T, Haraguchi M, Tani A, et al. Reversal of heavy metal resistance in multidrug-resistant human KB carcinoma cells. Biochem Biophys Res Commun. 1997;236:586-90 pubmed
    ..BSO at 100 microM or PAK-104P at 10 microM enhanced the accumulation of antimony potassium tartrate in C-A120 cells to the level of that in KB-3-1 cells without the agents...
  20. Sereno D, Holzmuller P, Lemesre J. Efficacy of second line drugs on antimonyl-resistant amastigotes of Leishmania infantum. Acta Trop. 2000;74:25-31 pubmed
    ..These results confirmed that these two drugs (pentamidine and amphotericin B) are good candidates to treat pentavalent antimonial unresponsiveness. ..
  21. de Melo A, Silva Barcellos N, Demicheli C, Frezard F. Enhanced schistosomicidal efficacy of tartar emetic encapsulated in pegylated liposomes. Int J Pharm. 2003;255:227-30 pubmed
    ..The present work demonstrates that LCL reduce the acute toxicity of TA and effectively deliver this drug to S. mansoni during the late stages of parasite infection. ..
  22. Vernhet L, Séité M, Allain N, Guillouzo A, Fardel O. Arsenic induces expression of the multidrug resistance-associated protein 2 (MRP2) gene in primary rat and human hepatocytes. J Pharmacol Exp Ther. 2001;298:234-9 pubmed
    ..Finally, these results confirm that some metals strongly regulate expression of detoxifying proteins, including biliary drug transporters...
  23. Wyllie S, Fairlamb A. Differential toxicity of antimonial compounds and their effects on glutathione homeostasis in a human leukaemia monocyte cell line. Biochem Pharmacol. 2006;71:257-67 pubmed
    ..Collectively, these findings suggest that Sb(III) seriously compromises thiol homeostasis in THP-1 macrophages and that this may be an early defining event in the mode of action of antimonials against leukaemia cells. ..
  24. Naredi P, Heath D, Enns R, Howell S. Cross-resistance between cisplatin and antimony in a human ovarian carcinoma cell line. Cancer Res. 1994;54:6464-8 pubmed
    ..DDP-selected cells were 15-fold resistant to DDP and 4.4-fold cross-resistant to antimony potassium tartrate, whereas of the cations tested (Cd2+, Zn2+, Ni2+ and Co2+) cross-resistance was observed only for Cd2+ (..
  25. Maciel N, Reis P, Kato K, Vidal A, Guimarães H, Frezard F, et al. Reduced cardiovascular alterations of tartar emetic administered in long-circulating liposomes in rats. Toxicol Lett. 2010;199:234-8 pubmed publisher
    ..In conclusion, a liposomal formulation of TA showed a reduced cardiotoxic profile for TA when compared to the free form. ..
  26. Su J, Mansour J, Mansour T. Purification, kinetics and inhibition by antimonials of recombinant phosphofructokinase from Schistosoma mansoni. Mol Biochem Parasitol. 1996;81:171-8 pubmed
    ..Recombinant PFK is more sensitive to inhibition by the trivalent antimonials, antimony potassium tartrate and Stibophen, than is the mammalian heart muscle enzyme...
  27. Snawder J, Tirmenstein M, Mathias P, Toraason M. Induction of stress proteins in rat cardiac myocytes by antimony. Toxicol Appl Pharmacol. 1999;159:91-7 pubmed
  28. Lecureur V, Lagadic Gossmann D, Fardel O. Potassium antimonyl tartrate induces reactive oxygen species-related apoptosis in human myeloid leukemic HL60 cells. Int J Oncol. 2002;20:1071-6 pubmed
  29. Poon R, Chu I. Effects of potassium antimony tartrate on rat erythrocyte phosphofructokinase activity. J Biochem Mol Toxicol. 1998;12:227-33 pubmed
    ..The weak effect of Sb on glycolysis in erythrocytes may be due in part to the protective effect of hemoglobin and, to a lesser extent, glutathione on PFK. ..
  30. Norris M, Madafiglio J, Gilbert J, Marshall G, Haber M. Reversal of multidrug resistance-associated protein-mediated drug resistance in cultured human neuroblastoma cells by the quinolone antibiotic difloxacin. Med Pediatr Oncol. 2001;36:177-80 pubmed
    ..The data demonstrate that difloxacin can reverse drug resistance in unselected human neuroblastoma cells and is therefore a potential candidate for future clinical trials. ..
  31. Day T, Bennett J, Pax R. Serotonin and its requirement for maintenance of contractility in muscle fibres isolated from Schistosoma mansoni. Parasitology. 1994;108 ( Pt 4):425-32 pubmed
  32. Nam S, Yang C, An Y. Effects of antimony on aquatic organisms (Larva and embryo of Oryzias latipes, Moina macrocopa, Simocephalus mixtus, and Pseudokirchneriella subcapitata). Chemosphere. 2009;75:889-93 pubmed publisher
    ..In the present study, antimony potassium tartrate (APT), the trivalent inorganic forms of antimony, was selected as a test antimony compound due to its ..
  33. Gyurasics A, Koszorus L, Varga F, Gregus Z. Increased biliary excretion of glutathione is generated by the glutathione-dependent hepatobiliary transport of antimony and bismuth. Biochem Pharmacol. 1992;44:1275-81 pubmed
    ..b>Antimony potassium tartrate (25-100 mumol/kg, i.v.) and bismuth ammonium citrate (50-200 mumol/kg, i.v...
  34. Choudhury K, Zander D, Kube M, Reinhardt R, Clos J. Identification of a Leishmania infantum gene mediating resistance to miltefosine and SbIII. Int J Parasitol. 2008;38:1411-23 pubmed publisher
    ..Database mining and karyotyping experiments suggest that in L. infantum this gene is part of a 44-kbp duplicated region that is found on two separate chromosomes, CHR08 and CHR29...
  35. Genest P, Haimeur A, Legare D, Sereno D, Roy G, Messier N, et al. A protein of the leucine-rich repeats (LRRs) superfamily is implicated in antimony resistance in Leishmania infantum amastigotes. Mol Biochem Parasitol. 2008;158:95-9 pubmed publisher
    ..This work pinpoints a novel protein that can contribute to antimonial resistance in Leishmania. ..
  36. Mohamed M, Bakr I, El Hoseiny M, Arafa N, Hassan A, Ismail S, et al. HCV-related morbidity in a rural community of Egypt. J Med Virol. 2006;78:1185-9 pubmed
  37. Subramanian K, Poon R, Chu I, Connor J. Antimony in drinking water, red blood cells, and serum: development of analytical methodology using transversely heated graphite furnace atomization-atomic absorption spectrometry. Arch Environ Contam Toxicol. 1997;32:431-5 pubmed
    ..5 ml) of RBCs and serum derived from rats given Sb-supplemented drinking water. ..
  38. Walker J, Saravia N. Inhibition of Leishmania donovani promastigote DNA topoisomerase I and human monocyte DNA topoisomerases I and II by antimonial drugs and classical antitopoisomerase agents. J Parasitol. 2004;90:1155-62 pubmed
    ..Nevertheless, the potent direct inhibition of TOPI by SSG and the differential interactions of camptothecin with L. donovani and human TOPI support the possibility of developing parasite-specific derivatives. ..