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Chemical Compound Review

Protostib     hydroxy-dioxo-stiborane; (2R,3R,4R,5S)-6...

Synonyms: Glucantime, CHEMBL239129, LS-71364, AC1L22AB, AC1Q5B7H, ...
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Disease relevance of meglumine


High impact information on meglumine

  • Glibenclamide reduced the rate of lesion growth in BALB/c mice infected with Leishmania (Leishmania) mexicana, the effect was dose dependent, and the highest dose proved more effective than glucantime [6].
  • We report that amastigotes of Leishmania infantum cultured under axenic conditions were poorly susceptible to meglumine [Glucantime; an Sb(V)], unlike those growing inside THP-1 cells (50% inhibitory concentrations [IC50s], about 1.8 mg/ml and 22 microg/ml, respectively) [7].
  • The effect of camptothecin, an inhibitor of topoisomerase, and additive-free meglumine antimoniate (Glucantime) on the stabilization of cleavable DNA-protein complexes associated with the inhibition of topoisomerase was assessed in the human promonocytic cell line U-937, promastigotes of L [8].
  • Sinefungin was significantly suppressive against both L. donovani and L. braziliensis panamensis infections in hamsters when compared with meglumine antimonate (Glucantime) [9].
  • The resistance to glucantime was reverted by buthionine sulfoximine (BSO) and chlorambucil (CLB); however, thiol analyses by HPLC of wild-type and GLU-R10 cell lines, in the presence or absence of the drug, showed no differences between these two cell lines [3].

Chemical compound and disease context of meglumine


Biological context of meglumine

  • The resistant cell lines were partially characterized by their in vitro response to glucantime, the stability of resistance phenotype, cross resistance to a range of drugs, and also by the analysis of total DNA fragments generated by restriction endonucleases and blot hybridization [13].
  • A gene amplification from a glucantime-resistant Leishmania (Viannia) guyanensis cell line was characterised in an attempt to understand the mechanism of metal resistance in this pathogenic species [14].
  • The 50% effective dose (ED50) of pharmaceutical and additive-free formulations of Glucantime were determined based on the kinetics of the response of Leishmania Viannia to SbV in vitro [15].
  • During GLUCANTIME-treatment the following adverse reactions could be observed: general weakness, reduced food intake up to anorexia, vomiting and diarrhoea [16].
  • CONCLUSIONS: By itself, increased access to Glucantime is unlikely to increase usage of the drug and to reduce its frequent premature discontinuance unless public health planners accommodate the health and illness world views of local populations [17].

Anatomical context of meglumine

  • Elimination of the parasite burden by glucantime therapy restored responsiveness of lymphocytes to parasite antigens [18].
  • We also studied the capacity of CP-elicited peritoneal macrophages of C57Bl/6 mice cultured alone or in combination with Glucantime and/or lymphokine to eliminate intracellular L. donovani amastigotes [19].
  • Glucantime inhibited the growth of Leishmania cultured in complex medium but did not affect parasite growth when added to cells cultured in defined or semi-defined media [20].
  • A significant increase in alphabeta T cells was seen in glucantime-treated patients (62.4% +/-7.6), when compared to the untreated patients (55.7% +/-5.5) and controls (55.1% +/-9.6) [21].
  • Our data represent evidence for the reversibility of the abnormal HLA-DR expression by keratinocytes in ACL after Glucantime therapy or spontaneous scar formation, demonstrating that this expression is restricted to the period of active lesions [22].

Associations of meglumine with other chemical compounds


Gene context of meglumine

  • In contrast, glucantime therapy led to a Th2-type response in the control group with a lower level of IL-2 [27].
  • However, a combination of garlic and glucantime treatment was more effective than either treatment alone, and resulted in a Th1-type response similar to that which developed with garlic treatment [27].
  • Likewise, the pattern of immunoblot change after the patients were treated and apparently cured with meglumine antimoniate (Glucantime) was studied by evaluating sera pretreatment and 1 year posttreatment [28].
  • AIM: To evaluate the efficacy of combined cryotherapy and intralesional meglumine antimoniate (MA) (Glucantime, Specia, Paris, France) for the treatment of CL [29].
  • Immunopathology of American cutaneous leishmaniasis. Modulation of MHC class II gene products by keratinocytes before and after glucantime therapy [22].

Analytical, diagnostic and therapeutic context of meglumine

  • Control groups consisted of untreated mice and mice treated with a pentavalent antimonial (Glucantime) [30].
  • Patients were treated with conventional chemotherapy by using pentavalent antimonium salts (Glucantime) for 3 weeks [31].
  • In mice, it was found that immunostimulation of animals prophylactically, therapeutically, or both enhanced the effects of the antimonial drug (Glucantime) administered more than 1 week after a challenge of BALB/c and C57BL/6 mice [32].
  • Its efficacy by oral administration was approximately four to eight times that by intramuscular administration and four times that of the positive control drug Glucantime by intramuscular administration [33].
  • After glucantime therapy, immunoblotting profiles with LCL sera were reduced both in intensity and in the range of antigens detected; a 104-kDa antigen was newly detected with post-treatment LCL sera [34].


  1. Glucantime-resistant visceral leishmaniasis in immunocompromised patients. Verdejo, J., Alvar, J., Polo, R.M., González-Lahoz, J.M. Am. J. Med. (1988) [Pubmed]
  2. Efficacy of orally administered 2-substituted quinolines in experimental murine cutaneous and visceral leishmaniases. Nakayama, H., Loiseau, P.M., Bories, C., Torres de Ortiz, S., Schinini, A., Serna, E., Rojas de Arias, A., Fakhfakh, M.A., Franck, X., Figadère, B., Hocquemiller, R., Fournet, A. Antimicrob. Agents Chemother. (2005) [Pubmed]
  3. Involvement of thiol metabolism in resistance to glucantime in Leishmania tropica. Arana, F.E., Pérez-Victoria, J.M., Repetto, Y., Morello, A., Castanys, S., Gamarro, F. Biochem. Pharmacol. (1998) [Pubmed]
  4. Short report: efficacy of pentavalent antimony for treatment of colombian cutaneous leishmaniasis. Soto, J., Toledo, J., Vega, J., Berman, J. Am. J. Trop. Med. Hyg. (2005) [Pubmed]
  5. Cell-mediated immunity in localized cutaneous leishmaniasis patients before and after treatment with immunotherapy or chemotherapy. Castes, M., Moros, Z., Martinez, A., Trujillo, D., Castellanos, P.L., Rondon, A.J., Convit, J. Parasite Immunol. (1989) [Pubmed]
  6. Glibenclamide, a Blocker of K+ATP Channels, Shows Antileishmanial Activity in Experimental Murine Cutaneous Leishmaniasis. Serrano-Mart??n, X., Payares, G., Mendoza-Le??n, A. Antimicrob. Agents Chemother. (2006) [Pubmed]
  7. Axenically grown amastigotes of Leishmania infantum used as an in vitro model to investigate the pentavalent antimony mode of action. Sereno, D., Cavaleyra, M., Zemzoumi, K., Maquaire, S., Ouaissi, A., Lemesre, J.L. Antimicrob. Agents Chemother. (1998) [Pubmed]
  8. Sensitivity of Leishmania viannia panamensis to pentavalent antimony is correlated with the formation of cleavable DNA-protein complexes. Lucumi, A., Robledo, S., Gama, V., Saravia, N.G. Antimicrob. Agents Chemother. (1998) [Pubmed]
  9. Molecular target of the antileishmanial action of sinefungin. Nolan, L.L. Antimicrob. Agents Chemother. (1987) [Pubmed]
  10. Comparison of meglumine antimoniate and pentamidine for peruvian cutaneous leishmaniasis. Andersen, E.M., Cruz-Saldarriaga, M., Llanos-Cuentas, A., Luz-Cjuno, M., Echevarria, J., Miranda-Verastegui, C., Colina, O., Berman, J.D. Am. J. Trop. Med. Hyg. (2005) [Pubmed]
  11. The effect of intravenous or subcutaneous administration of meglumine antimonate (Glucantime) in dogs with leishmaniasis. A randomized clinical trial. Slappendel, R.J., Teske, E. The Veterinary quarterly. (1997) [Pubmed]
  12. Effect of combination therapy with systemic glucantime and pentoxifylline in the treatment of cutaneous leishmaniasis. Sadeghian, G., Nilforoushzadeh, M.A. International journal of dermatology. (2006) [Pubmed]
  13. Leishmania (V.) guyanensis: isolation and characterization of glucantime-resistant cell lines. Ferreira-Pinto, K.C., Miranda-Vilela, A.L., Anacleto, C., Fernandes, A.P., Abdo, M.C., Petrillo-Peixoto, M.L., Moreira, E.S. Can. J. Microbiol. (1996) [Pubmed]
  14. Structural and functional analysis of an amplification containing a PGPA gene in a glucantime-resistant Leishmania (Viannia) guyanensis cell line. Anacleto, C., Abdo, M.C., Ferreira, A.V., Murta, S.M., Romanha, A.J., Fernandes, A.P., Moreira, E.S. Parasitol. Res. (2003) [Pubmed]
  15. Sensitivity to Glucantime of Leishmania viannia isolated from patients prior to treatment. Robledo, S.M., Valencia, A.Z., Saravia, N.G. J. Parasitol. (1999) [Pubmed]
  16. Clinical follow-up examination after treatment of canine leishmaniasis. Moritz, A., Steuber, S., Greiner, M. Tokai J. Exp. Clin. Med. (1998) [Pubmed]
  17. The traditional and conventional medical treatment of cutaneous leishmaniasis in rural Ecuador. Weigel, M.M., Armijos, R.X. Rev. Panam. Salud Publica (2001) [Pubmed]
  18. Immunosuppression associated with visceral leishmaniasis of hamsters. Nickol, A.D., Bonventre, P.F. Parasite Immunol. (1985) [Pubmed]
  19. Enhancement of Glucantime therapy of murine Leishmania donovani infection by a synthetic immunopotentiating compound (CP-46,665-1). Adinolfi, L.E., Bonventre, P.F. Am. J. Trop. Med. Hyg. (1985) [Pubmed]
  20. Glucantime susceptibility of Leishmania promastigotes under variable growth conditions. Moreira, E.S., Soares, R.M., Petrillo-Peixoto, M.d.e. .L. Parasitol. Res. (1995) [Pubmed]
  21. Expansion of gammadelta T Cells in patients infected with cutaneous leishmaniasis with and without glucantime therapy. Darabi, H., Abolhassani, M., Kariminia, A., Alimohammadian, M.H. The Brazilian journal of infectious diseases : an official publication of the Brazilian Society of Infectious Diseases. (2002) [Pubmed]
  22. Immunopathology of American cutaneous leishmaniasis. Modulation of MHC class II gene products by keratinocytes before and after glucantime therapy. Pirmez, C., Oliveira-Neto, M.P., Grimaldi Júnior, G., Savino, W. Mem. Inst. Oswaldo Cruz (1990) [Pubmed]
  23. Isolation of a taxol-resistant Leishmania donovani promastigote mutant that exhibits a multidrug-resistant phenotype. Kapoor, P., Ghosh, A., Madhubala, R. FEMS Microbiol. Lett. (1999) [Pubmed]
  24. Value of Western blotting in the clinical follow-up of canine leishmaniasis. Fernández-Pérez, F.J., Méndez, S., de la Fuente, C., Cuquerella, M., Gómez, M.T., Alunda, J.M. J. Vet. Diagn. Invest. (1999) [Pubmed]
  25. Efficacy of 8-bromoguanosine against murine cutaneous leishmaniasis induced with Leishmania amazonensis. Barão, S.C., Giorgio, S. Chemotherapy. (2003) [Pubmed]
  26. Ultrastructural changes in parasites induced by nanoparticle-bound pentamidine in a Leishmania major/mouse model. Fusai, T., Boulard, Y., Durand, R., Paul, M., Bories, C., Rivollet, D., Astier, A., Houin, R., Deniau, M. Parasite (1997) [Pubmed]
  27. Garlic induces a shift in cytokine pattern in Leishmania major-infected BALB/c mice. Ghazanfari, T., Hassan, Z.M., Ebtekar, M., Ahmadiani, A., Naderi, G., Azar, A. Scand. J. Immunol. (2000) [Pubmed]
  28. Immunoblot analysis of Leishmania panamensis antigens in sera of patients with American cutaneous leishmaniasis. Isaza, D.M., Restrepo, M., Mosca, W. J. Clin. Microbiol. (1997) [Pubmed]
  29. Comparative study of the efficacy of combined cryotherapy and intralesional meglumine antimoniate (Glucantime) vs. cryotherapy and intralesional meglumine antimoniate (Glucantime) alone for the treatment of cutaneous leishmaniasis. Asilian, A., Sadeghinia, A., Faghihi, G., Momeni, A. International journal of dermatology. (2004) [Pubmed]
  30. Therapy of visceral leishmaniasis due to Leishmania infantum: experimental assessment of efficacy of AmBisome. Gangneux, J.P., Sulahian, A., Garin, Y.J., Farinotti, R., Derouin, F. Antimicrob. Agents Chemother. (1996) [Pubmed]
  31. Antimonial therapy induces circulating proinflammatory cytokines in patients with cutaneous leishmaniasis. Kocyigit, A., Gur, S., Gurel, M.S., Bulut, V., Ulukanligil, M. Infect. Immun. (2002) [Pubmed]
  32. Synergistic effect of glucantime and a liposome-encapsulated muramyl dipeptide analog in therapy of experimental visceral leishmaniasis. Adinolfi, L.E., Bonventre, P.F., Vander Pas, M., Eppstein, D.A. Infect. Immun. (1985) [Pubmed]
  33. Leishmania donovani: oral efficacy and toxicity of formycin B in the infected hamster. Berman, J.D., Keenan, C.M., Lamb, S.R., Hanson, W.L., Waits, V.B. Exp. Parasitol. (1983) [Pubmed]
  34. Immunological selection for Leishmania (Viannia) braziliensis antigens. Cuba Cuba, C.A., Ogunkolade, W., Howard, M.K., Miles, M.A. Ann. Trop. Med. Parasitol. (2001) [Pubmed]
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