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1

A new fluorometric method for anti-Leishmania drug screening on axenic amastigotes

100%
Le P. P., Pagniez F., Abdala-Valencia H.
Acta Parasitologica
|
2003
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tom 48
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nr 4
Primary screening of possible antileishmanial compounds is currently based either on the use of promastigotes, which are not the clinically relevant stage, or on the time-consuming intracellular amastigote test. With the aim of discovering new antileishmanial derivatives, a semi-automatized method using Leishmania axenic amastigotes and a fluorometric growth indicator (Alamar Blue®) was developed. This assay was evaluated in a comparative study of the susceptibility of promastigotes, axenic amastigotes and intracellular amastigotes of Leishmania mexicana with standard drugs used in antileishmanial therapy (meglumine antimoniate, amphotericin B, ketoconazole and allopurinol) and recently developed ether lipid compounds (edelfosine and miltefosine). The results showed that while inhibitory concentration 50s (IC₅₀s) of axenic and intracellular amastigotes were similar for all of the drugs tested, promastigotes and intracellular amastigotes IC₅₀s differed for three of the six compounds. In conclusion, this axenic amastigote model allowed us to combine the ease of in vitro drug screening on promastigote with the reliability of the IC₅₀ determination on intracellular amastigotes.
2

A new automatized fluorometric assay for anti-Leishmania drug screening

100%
Le P. P., Pagniez F., Abdala H.
Acta Parasitologica
|
2002
|
tom 47
|
nr 1
The therapeutic armentarium against leishmaniasis is very restricted, using mainly up to now drugs showing several side effects and resistance. Consequently, there is a real need to find new compounds as alternatives for the treatment of leishmaniasis. However, most of the classic antileishmanial primary screening assays are not suitable for measuring the cytotoxicity of large number of drug candidates because of the manipulations required. We have established a new assay that incorporate a fluorometric growth indicator based on the detection of a metabolic activity in culture medium after the chemical reduction of alamar Blue® by cells. This antileishmanial test was evaluated on amphotericin B, meglumine antimoniate, allopurinol, ketoconazole and edelfosine. The results reported show the advantages oj this fluorochrome on the tetrazolium salt 3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyltetrazolium bromide (MTT) for Leishmania cytotoxicity measurement. Moreover, this study is the first report of the use of alamar Blue® fluorogenic assay for activity assessment of potential antileishmanial drugs against promastigotes.
3

Activity of N-lutidinylarylcarboxamides against Leishmania donovani and L.braziliensis

88%
Le P. P., Abdala H., Pagniez F., Robert J. M., Le Baut G.
Acta Parasitologica
|
1999
|
tom 44
|
nr 3
Three arylcarboxamides issued from 2-amino- 4,6-dimethylpyridine, benzamide 1, furan-2-carboxamide 2 and 5-bromofuran-2-carboxamide 3 were evaluated against Leishmania promastigotes, at three doses, 0.5, 5, and 50 µM. Although benzamide 1 exerted but a moderate inhibition against cultured extracellular promastigotes at a concentration of 50 µM, furan-2-carboxamides 2 and 3 had potent activity at the same concentration. The IC₅₀ of 2 against L. donovani and L. braziliensis were 29.9 and 28.3 µM and those of 3 were 25.9 and 36.6 µM, respectively. In a BALB/c mice model of visceral leishmaniosis, an intraperitoneal administration of 10 mg/kg of 2, for 5 days, led to a consistent parasite burden reduction in the spleen smears (75.8 ± 5.7%) and in the microdilution spleen cultures (72.1 ± 0.6%). A very significant correlation (r = 0.96) was found between the two methods of spleen parasite burden quantification. These amides also exhibit potent antiinflammatory activity and it was previously stated that they inhibit arachidonic acid production by interfering in the PLA₂ activation. This suggests fact that they could disrupt Leishmania membrane lipid integrity by protein kinase C inhibition.
4

The effects of bistramides on rodent malaria

76%
Gautret P., Le P. P., Biard J. F., Menard D., Verbist J. F., Marjolet M.
Acta Parasitologica
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1998
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tom 43
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nr 1
Bistramide D and K were extracted from a New Caledonian marine colonial ascidian Lissoclinum bistratum and tested against Plasmodium berghei and P. vinckei petteri in mice. Bistramide D was able to reduce parasitaemia by almost 50% in P. berghei infected mice, but the ID₅₀ (>5 mg/kg) was very close to the LD₅₀ (8 mg/kg). In the same assay, bistramide K was less active than bistramide D. The mid-term trophozoite and the old trophozoite were shown to be the stages most sensitive to bistramide D in P. vinckei petteri infected mice. Therefore, bistramides are interesting experimental tools but do not present a major interest as potential antimalarial drugs.
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