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Chemical Compound Review

CID456326     oxo-oxostibanyloxy-stibane; 2,3,4,5,6...

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Disease relevance of LS-2383

  • Pentostam, a Sb(V)-containing drug that is one of the first-line therapeutic agents for treatment of leishmaniasis, inhibited uptake after reaction with GSH [1].
  • Also, in promastigotes of both wild-type L. donovani and the Pentostam-resistant mutant L. donovani Ld1S.20, Sb(V) inhibited the toxicity of Sb(III) but not of As(III) [2].
  • In the present report, the oral antifungal agent ketoconazole (600 mg/day for 28 days) was compared to a recommended regimen of intramuscular Pentostam (20 mg antimony/kg, with a maximum of 850 mg antimony/day, for 20 days) in a randomized study of the treatment of Panamanian cutaneous leishmaniasis due to Leishmania braziliensis panamensis [3].
  • Thirty-five golden hamsters infected with Leishmania donovani were treated with Pentostam and followed up to determine the effect of treatment on the development of secondary amyloidosis [4].
  • In a model of visceral leishmaniasis, infected mice were treated with ineffective concentrations of rIFN-gamma (10(4) U) plus suboptimal doses of Pentostam (10 or 50 mg/kg) [5].

High impact information on LS-2383

  • We report that treatment with interleukin 12 (IL-12), in combination with the antimony-based leishmanicidal drug Pentostam, induces healing in L. major-infected mice and that healing is associated with a switch from a Th2 to a Th1 response [6].
  • Switch from a type 2 to a type 1 T helper cell response and cure of established Leishmania major infection in mice is induced by combined therapy with interleukin 12 and Pentostam [6].
  • Transfection of LmAQP1 in a Pentostam-resistant field isolate also sensitized the parasite in the macrophage-associated amastigote form [7].
  • Leishmania major LmACR2 is a pentavalent antimony reductase that confers sensitivity to the drug pentostam [8].
  • An IFN-secreting T cell line derived from the spleen of a chronically infected mouse, after boosting with leishmanial Ag and treatment with Pentostam to kill residual parasites, was able to activate macrophages to kill amastigotes in vitro [9].

Chemical compound and disease context of LS-2383


Biological context of LS-2383


Anatomical context of LS-2383

  • Partial or complete activation of macrophages as judged by killing of tumor cells significantly enhanced the efficacy of sodium antimony gluconate (Pentostam) [19].
  • The PENT0400 and PENT03200 cell lines were isolated after prolonged exposure to 0.4 mg/ml and 3.2 mg/ml Pentostam (Sb concentration), respectively [20].
  • Concentration of Pentostam in human breast milk [21].
  • In Pentostam-treated cultures, some organisms exhibited diminished definition of mitochondrial and other membranes, while other organisms had completely disintegrated [22].

Associations of LS-2383 with other chemical compounds


Gene context of LS-2383

  • In order to investigate the role of the expanding parasite population on the Th2 response, mice infected for 2 weeks with L. major, which exhibited a Th2-like cytokine profile, were treated with a leishmanicidal agent (Pentostam) and/or various doses of anti-IL-4 antibody [28].
  • However, in 8 of 10 mice treated with this dose of anti-IL-4 antibody plus Pentostam lesion development was arrested and lesions were either controlled or eventually healed [28].
  • Activities of hexadecylphosphocholine (miltefosine), AmBisome, and sodium stibogluconate (Pentostam) against Leishmania donovani in immunodeficient scid mice [29].
  • Synergism of IL-2-stimulated splenocytes and Pentostam enhances the killing of Leishmania donovani in vitro [30].
  • A complicated case of ACL, which showed feverish and widely disseminated ulcers over the face was successfully treated with systemic antibiotic and pentostam as intralesional injections [31].

Analytical, diagnostic and therapeutic context of LS-2383


  1. An ATP-dependent As(III)-glutathione transport system in membrane vesicles of Leishmania tarentolae. Dey, S., Ouellette, M., Lightbody, J., Papadopoulou, B., Rosen, B.P. Proc. Natl. Acad. Sci. U.S.A. (1996) [Pubmed]
  2. Novel Intracellular SbV reducing activity correlates with antimony susceptibility in Leishmania donovani. Shaked-Mishan, P., Ulrich, N., Ephros, M., Zilberstein, D. J. Biol. Chem. (2001) [Pubmed]
  3. Efficacy of ketoconazole against Leishmania braziliensis panamensis cutaneous leishmaniasis. Saenz, R.E., Paz, H., Berman, J.D. Am. J. Med. (1990) [Pubmed]
  4. The effect of treatment of the associated disease on the development of amyloidosis in the experimental animal. Kennedy, J.S., Anderson, J.D. J. Pathol. (1983) [Pubmed]
  5. Immunochemotherapy for intracellular Leishmania donovani infection: gamma interferon plus pentavalent antimony. Murray, H.W., Berman, J.D., Wright, S.D. J. Infect. Dis. (1988) [Pubmed]
  6. Switch from a type 2 to a type 1 T helper cell response and cure of established Leishmania major infection in mice is induced by combined therapy with interleukin 12 and Pentostam. Nabors, G.S., Afonso, L.C., Farrell, J.P., Scott, P. Proc. Natl. Acad. Sci. U.S.A. (1995) [Pubmed]
  7. Drug uptake and modulation of drug resistance in Leishmania by an aquaglyceroporin. Gourbal, B., Sonuc, N., Bhattacharjee, H., Legare, D., Sundar, S., Ouellette, M., Rosen, B.P., Mukhopadhyay, R. J. Biol. Chem. (2004) [Pubmed]
  8. Leishmania major LmACR2 is a pentavalent antimony reductase that confers sensitivity to the drug pentostam. Zhou, Y., Messier, N., Ouellette, M., Rosen, B.P., Mukhopadhyay, R. J. Biol. Chem. (2004) [Pubmed]
  9. Isolation of protective T cells from BALB/cJ mice chronically infected with Leishmania donovani. Holaday, B., Sadick, M.D., Pearson, R.D. J. Immunol. (1988) [Pubmed]
  10. Sodium stibogluconate (Pentostam) potentiates oxidant production in murine visceral leishmaniasis and in human blood. Rais, S., Perianin, A., Lenoir, M., Sadak, A., Rivollet, D., Paul, M., Deniau, M. Antimicrob. Agents Chemother. (2000) [Pubmed]
  11. Axenically cultured amastigote forms as an in vitro model for investigation of antileishmanial agents. Sereno, D., Lemesre, J.L. Antimicrob. Agents Chemother. (1997) [Pubmed]
  12. A comparison of three dosage regimens of sodium stibogluconate in the treatment of visceral leishmaniasis in Kenya. Chulay, J.D., Bhatt, S.M., Muigai, R., Ho, M., Gachihi, G., Were, J.B., Chunge, C., Bryceson, A.D. J. Infect. Dis. (1983) [Pubmed]
  13. Comparison of generic to branded pentavalent antimony for treatment of new world cutaneous leishmaniasis. Soto, J., Valda-Rodriquez, L., Toledo, J., Vera-Navarro, L., Luz, M., Monasterios-Torrico, H., Vega, J., Berman, J. Am. J. Trop. Med. Hyg. (2004) [Pubmed]
  14. Clinical, haematological and parasitological response to treatment of visceral leishmaniasis in Kenya. A study of 64 patients. Kager, P.A., Rees, P.H., Manguyu, F.M., Bhatt, K.M., Wellde, B.T., Hockmeyer, W.T., Lyerly, W.H. Tropical and geographical medicine. (1984) [Pubmed]
  15. Pentostam induces resistance to antimony and the preservative chlorocresol in Leishmania donovani promastigotes and axenically grown amastigotes. Ephros, M., Waldman, E., Zilberstein, D. Antimicrob. Agents Chemother. (1997) [Pubmed]
  16. Antileishmanial effect of 3-aminooxy-1-aminopropane is due to polyamine depletion. Singh, S., Mukherjee, A., Khomutov, A.R., Persson, L., Heby, O., Chatterjee, M., Madhubala, R. Antimicrob. Agents Chemother. (2007) [Pubmed]
  17. Herpes zoster and lymphopenia associated with sodium stibogluconate therapy for cutaneous leishmaniasis. Wortmann, G.W., Aronson, N.E., Byrd, J.C., Grever, M.R., Oster, C.N. Clin. Infect. Dis. (1998) [Pubmed]
  18. Pharmacokinetics of pentavalent antimony (Pentostam) in hamsters. Berman, J.D., Gallalee, J.F., Gallalee, J.V. Am. J. Trop. Med. Hyg. (1988) [Pubmed]
  19. Efficacy of combined immunostimulation and chemotherapy in experimental visceral Leishmaniasis. Haidaris, C.G., Bonventre, P.F. Am. J. Trop. Med. Hyg. (1983) [Pubmed]
  20. Leishmania donovani: isolation and characterization of sodium stibogluconate (Pentostam)-resistant cell lines. Ullman, B., Carrero-Valenzuela, E., Coons, T. Exp. Parasitol. (1989) [Pubmed]
  21. Concentration of Pentostam in human breast milk. Berman, J.D., Melby, P.C., Neva, F.A. Trans. R. Soc. Trop. Med. Hyg. (1989) [Pubmed]
  22. Fine-structural alterations in Leishmania tropica within human macrophages exposed to antileishmanial drugs in vitro. Langreth, S.G., Berman, J.D., Riordan, G.P., Lee, L.S. J. Protozool. (1983) [Pubmed]
  23. Gene amplification in Leishmania tarentolae selected for resistance to sodium stibogluconate. Haimeur, A., Ouellette, M. Antimicrob. Agents Chemother. (1998) [Pubmed]
  24. Sodium stibogluconate (Pentostam) inhibition of glucose catabolism via the glycolytic pathway, and fatty acid beta-oxidation in Leishmania mexicana amastigotes. Berman, J.D., Gallalee, J.V., Best, J.M. Biochem. Pharmacol. (1987) [Pubmed]
  25. Drug resistance in leishmaniasis: its implication in systemic chemotherapy of cutaneous and mucocutaneous disease. Grogl, M., Thomason, T.N., Franke, E.D. Am. J. Trop. Med. Hyg. (1992) [Pubmed]
  26. Activity of oral drugs against Leishmania tropica in human macrophages in vitro. Berman, J.D., Lee, L.S. Am. J. Trop. Med. Hyg. (1983) [Pubmed]
  27. Bifunctional role of the leishmanial antimonate reductase LmACR2 as a protein tyrosine phosphatase. Zhou, Y., Bhattacharjee, H., Mukhopadhyay, R. Mol. Biochem. Parasitol. (2006) [Pubmed]
  28. Depletion of interleukin-4 in BALB/c mice with established Leishmania major infections increases the efficacy of antimony therapy and promotes Th1-like responses. Nabors, G.S., Farrell, J.P. Infect. Immun. (1994) [Pubmed]
  29. Activities of hexadecylphosphocholine (miltefosine), AmBisome, and sodium stibogluconate (Pentostam) against Leishmania donovani in immunodeficient scid mice. Escobar, P., Yardley, V., Croft, S.L. Antimicrob. Agents Chemother. (2001) [Pubmed]
  30. Synergism of IL-2-stimulated splenocytes and Pentostam enhances the killing of Leishmania donovani in vitro. Eslami, Z., Gaucher, D., Tanner, C.E. Clin. Immunol. Immunopathol. (1996) [Pubmed]
  31. A case of complicated anthroponotic cutaneous leishmaniasis in Al Baha, Saudi Arabia. Morsy, T.A., Faris, R.M. Journal of the Egyptian Society of Parasitology. (1991) [Pubmed]
  32. Intralesional therapy of cutaneous leishmaniasis with sodium stibogluconate antimony. Sharquie, K.E., Al-Talib, K.K., Chu, A.C. Br. J. Dermatol. (1988) [Pubmed]
  33. Treatment of visceral leishmaniasis with sodium stibogluconate in Sudan: management of those who do not respond. Khalil, E.A., el Hassan, A.M., Zijlstra, E.E., Hashim, F.A., Ibrahim, M.E., Ghalib, H.W., Ali, M.S. Ann. Trop. Med. Parasitol. (1998) [Pubmed]
  34. The use of Pentostam liposomes in the chemotherapy of experimental leishmaniasis. Black, C.D., Watson, G.J., Ward, R.J. Trans. R. Soc. Trop. Med. Hyg. (1977) [Pubmed]
  35. Efficacy of cryotherapy and intralesional pentostam in treatment of cutaneous leishmaniasis. Gurei, M.S., Tatli, N., Ozbilge, H., Erel, O., Seyrek, A., Kocyigit, A., Ulukanligil, M. Journal of the Egyptian Society of Parasitology. (2000) [Pubmed]
  36. Treatment of cutaneous leishmaniasis with Pentostam or cryosurgery. Morsy, T.A., Abdel Rahman, E.G., Ahmed, M.M. Journal of the Egyptian Society of Parasitology. (1989) [Pubmed]
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