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Author Kulke, Daniel ♦ Krücken, Jürgen ♦ Demeler, Janina ♦ Harder, Achim ♦ Mehlhorn, Heinz ♦ Samson Himmelstjerna, Georg
Source SpringerLink
Content type Text
Publisher Springer-Verlag
File Format PDF
Copyright Year ©2012
Language English
Subject Domain (in DDC) Technology ♦ Medicine & health
Subject Keyword Medical Microbiology ♦ Microbiology ♦ Immunology
Abstract The present study investigates the in vitro efficacy of derivatives of the cyclooctadepsipeptides and the aminophenylamidines, which are promising candidates for the evaluation of the treatment of human soil-transmitted helminthiases. The effects of emodepside and PF1022A as well as of amidantel, deacylated amidantel and tribendimidine were evaluated in a concentration range between 0.01 and 100 μg/ml against third-stage larvae (L3) and adult worms of Nippostrongylus brasiliensis and first-stage larvae (L1) of Trichinella spiralis. Furthermore, drug combinations of PF1022A plus deacylated amidantel or tribendimidine and of tribendimidine plus levamisole were tested for any potential additive or even synergistic interactions. Emodepside had a significantly lower EC50 value than PF1022A in the T. spiralis (0.02788 vs. 0.05862 μg/ml) and the N. brasiliensis (0.06188 vs. 0.1485 μg/ml) motility assays but not in the acetylcholine esterase secretion assay with adult N. brasiliensis (0.05650 vs. 0.06886 μg/ml). While amidantel showed only minimal or at best partial inhibition of nematode motility and acetylcholine esterase secretion, tribendimidine was nearly as potent as deacylated amidantel. Whereas deacylated amidantel had a significantly lower EC50 than tribendimidine in the N. brasiliensis L3 motility assay (0.05492 vs. 0.2080 μg/ml), differences were not significant in the T. spiralis L1 motility assay (0.7766 vs. 1.145 μg/ml). Surprisingly, none of the combinations showed improved efficacy when compared to the individual drugs including levamisole/tribendimidine, which have previously been reported to act synergistically against Ancylostoma ceylanicum.
ISSN 09320113
Age Range 18 to 22 years ♦ above 22 year
Educational Use Research
Education Level UG and PG
Learning Resource Type Article
Publisher Date 2012-10-02
Publisher Place Berlin/Heidelberg
e-ISSN 14321955
Journal Parasitology Research
Volume Number 112
Issue Number 1
Page Count 11
Starting Page 335
Ending Page 345

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Source: SpringerLink