Document Detail

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.
MedLine Citation:
PMID:  7479655     Owner:  NLM     Status:  MEDLINE    
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.
I S Shin; H Tanifuji; Y Arata; Y Morizawa; T Nakayama; Y Wataya
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Parasitology research     Volume:  81     ISSN:  0932-0113     ISO Abbreviation:  Parasitol. Res.     Publication Date:  1995  
Date Detail:
Created Date:  1995-12-14     Completed Date:  1995-12-14     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8703571     Medline TA:  Parasitol Res     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  622-6     Citation Subset:  IM    
Faculty of Pharmaceutical Sciences, Okayama University, Japan.
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MeSH Terms
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*
Mice, Inbred BALB C
Time Factors
Reg. No./Substance:
0/Antiprotozoal Agents; 117517-20-1/3'-deoxy-3'-fluoroinosine; 58-63-9/Inosine

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