Antileishmanial activity of sodium stibogluconate fractions

W. L. Roberts, P. M. Rainey

Research output: Contribution to journalArticlepeer-review

60 Scopus citations

Abstract

Sodium stibogluconate, a pentavalent antimony derivative produced by the reaction of stibonic and gluconic acids, is the drug of choice for the treatment of leishmaniasis. It has been reported to be a complex mixture rather than a single compound. We separated sodium stibogluconate into 12 fractions by anion-exchange chromatography. One fraction accounted for virtually all the leishmanicidal activity of the fractionated material against Leishmania panamensis promastigotes, with a 50% inhibitory concentration (IC50) of 12 μg of Sb per ml; that of unfractionated sodium stibogluconate was 154 μg of Sb per ml. Further analysis of this active fraction revealed that a major component was m-chlorocresol, which had been included in the sodium stibogluconate formulation as a preservative. The IC50 of pure m-chlorocresol was 1.6 μg/ml, a concentration equivalent to that present in unfractionated sodium stibogluconate at a concentration of 160 μg of Sb per ml. After ether extraction to remove m-chlorocresol, the IC50 of sodium stibogluconate was >4,000 μg of Sb per ml. In contrast, when L. panamensis amastigotes were grown in macrophages, the IC50 of ether-extracted sodium stibogluconate was 10.3 μg of Sb per ml. The 12 fractions of ether-extracted sodium stibogluconate obtained by anion-exchange chromatography had IC50s of 10.1 to 15.4 μg of Sb per ml. We conclude that preservative-free sodium stibogluconate has little activity against L. panamensis promastigotes but is highly active against L. panamensis amastigotes in macrophages. This activity is associated with multiple chemical species.
Original languageEnglish (US)
Pages (from-to)1842-1846
Number of pages5
JournalAntimicrobial Agents and Chemotherapy
Volume37
Issue number9
DOIs
StatePublished - Jan 1 1993
Externally publishedYes

Bibliographical note

Generated from Scopus record by KAUST IRTS on 2023-09-20

ASJC Scopus subject areas

  • Infectious Diseases
  • Pharmacology
  • Pharmacology (medical)

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