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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
1993-12-16
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pubmed:abstractText |
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 micrograms of Sb per ml; that of unfractionated sodium stibogluconate was 154 micrograms 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 micrograms/ml, a concentration equivalent to that present in unfractionated sodium stibogluconate at a concentration of 160 micrograms of Sb per ml. After ether extraction to remove m-chlorocresol, the IC50 of sodium stibogluconate was > 4,000 micrograms of Sb per ml. In contrast, when L. panamensis amastigotes were grown in macrophages, the IC50 of ether-extracted sodium stibogluconate was 10.3 micrograms 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 micrograms 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.
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pubmed:grant | |
pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-14325337,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-1775152,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-2104665,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-2173431,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-2844580,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-2845611,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-3002244,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-4453608,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-7403880,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8239593-8323020
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antimony Sodium Gluconate,
http://linkedlifedata.com/resource/pubmed/chemical/Antiprotozoal Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cresols,
http://linkedlifedata.com/resource/pubmed/chemical/Uracil,
http://linkedlifedata.com/resource/pubmed/chemical/chlorocresol
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0066-4804
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
37
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1842-6
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:8239593-Animals,
pubmed-meshheading:8239593-Antimony Sodium Gluconate,
pubmed-meshheading:8239593-Antiprotozoal Agents,
pubmed-meshheading:8239593-Cell Line,
pubmed-meshheading:8239593-Chromatography, Ion Exchange,
pubmed-meshheading:8239593-Cresols,
pubmed-meshheading:8239593-Leishmania,
pubmed-meshheading:8239593-Macrophages,
pubmed-meshheading:8239593-Mice,
pubmed-meshheading:8239593-Microbial Sensitivity Tests,
pubmed-meshheading:8239593-Spectrophotometry, Ultraviolet,
pubmed-meshheading:8239593-Uracil
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pubmed:year |
1993
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pubmed:articleTitle |
Antileishmanial activity of sodium stibogluconate fractions.
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pubmed:affiliation |
Department of Laboratory Medicine, Yale University, New Haven, Connecticut 06510.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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