| 3'-Deoxy-3'-fluoroinosine as a potent antileishmanial agent. The metabolism and selective cytotoxic effect of 3'-deoxy-3'-fluoroinosine against Leishmania tropica and L. donovani in vitro and in vivo. | |
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MedLine Citation:
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PMID: 7479655 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We studied the antileishmanial activity of 3'-deoxy-3'-fluoroinosine (3'-FI) against Leishmania tropica and L. donovani. In in vitro cultivation, the EC50 values (the concentration of drug necessary to inhibit the growth rate of cells to 50% of the control value) obtained for 3'-FI against the promastigotes of L. tropica and L. donovani were 2.3 x 10(-7) and 1.0 x 10(-6) M, respectively. It was less toxic toward mouse mammary-tumor FM3A cells, a model host; the EC50 value was 1.9 x 10(-4) M. Leishmania promastigote metabolized 3'-FI to 3'-deoxy-3'-fluoroadenosine 5'-triphosphate (3'-FATP) but FM3A cells did not. 3'-FI was effective against L. donovani amastigotes in J774.1 cells in an in vitro cultivation system under conditions similar to those used in the in vivo assay. 3'-FI (50 mg/kg, given i.v.) showed a cytotoxic effect against the amastigotes of L. donovani in mice. |
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Authors:
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I S Shin; H Tanifuji; Y Arata; Y Morizawa; T Nakayama; Y Wataya |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Parasitology research Volume: 81 ISSN: 0932-0113 ISO Abbreviation: Parasitol. Res. Publication Date: 1995 |
Date Detail:
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Created Date: 1995-12-14 Completed Date: 1995-12-14 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8703571 Medline TA: Parasitol Res Country: GERMANY |
Other Details:
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Languages: eng Pagination: 622-6 Citation Subset: IM |
Affiliation:
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Faculty of Pharmaceutical Sciences, Okayama University, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antiprotozoal Agents / metabolism*, therapeutic use, toxicity* Chromatography, High Pressure Liquid Dose-Response Relationship, Drug Inosine / analogs & derivatives*, metabolism, therapeutic use, toxicity Leishmania donovani / drug effects*, growth & development Leishmania tropica / drug effects*, growth & development Leishmaniasis, Visceral / drug therapy* Male Mice Mice, Inbred BALB C Time Factors |
| Chemical | |
Reg. No./Substance:
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0/Antiprotozoal Agents; 117517-20-1/3'-deoxy-3'-fluoroinosine; 58-63-9/Inosine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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