Related Experiment Videos
Antileishmanial activity of the ether phospholipid ilmofosine
S L Croft1, R A Neal, E A Thornton
1Department of Medical Parasitology, London School of Hygiene and Tropical Medicine, UK.
Abstract:
The ether phospholipid ilmofosine (BM 41.440) was active in vitro against amastigotes of Leishmania donovani and an antimony-resistant line of L. infantum in mouse peritoneal macrophages with ED50 values of 3.7 microM and 3.5 microM respectively. Ilmofosine was also active against L. donovani in BALB/c mice following oral and subcutaneous dosing, with an ED50 value of 10.5 mg/kg x 5 by the oral route.
Insights
Ilmofosine, an ether phospholipid, demonstrated potent in vitro activity against Leishmania parasites. This compound also showed efficacy in vivo against Leishmania donovani in mice, suggesting therapeutic potential.
Area of Science:
- Parasitology
- Pharmacology
- Drug Discovery
Background:
- Leishmaniasis remains a significant global health challenge, particularly in its visceral form.
- Antimony-resistant Leishmania strains necessitate the development of novel therapeutic agents.
- Ether phospholipids represent a class of compounds with potential antiparasitic properties.
Purpose of the Study:
- To evaluate the in vitro and in vivo efficacy of ilmofosine against Leishmania parasites.
- To determine the antiparasitic activity of ilmofosine against both wild-type and drug-resistant Leishmania strains.
Main Methods:
- In vitro assays using mouse peritoneal macrophages infected with Leishmania amastigotes.
- In vivo efficacy studies in BALB/c mice infected with Leishmania donovani.
- Determination of median effective dose (ED50) values for oral and subcutaneous administration.
Main Results:
- Ilmofosine exhibited significant in vitro activity against Leishmania donovani and an antimony-resistant Leishmania infantum line (ED50 values of 3.7 microM and 3.5 microM, respectively).
- In vivo, ilmofosine demonstrated efficacy against Leishmania donovani in mice, with an ED50 of 10.5 mg/kg following oral administration over 5 days.
Conclusions:
- Ilmofosine displays promising antileishmanial activity both in vitro and in vivo.
- The compound's efficacy against antimony-resistant strains warrants further investigation for potential clinical application in treating leishmaniasis.