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Interaction between lumefantrine and monodesbutyl-benflumetol in Plasmodium falciparum in vitro

Interaktion zwischen Lumefantrin und Monodesbutyl-Benflumetol bei Plasmodium falciparum in vitro

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Zusammenfassung

Die pharmakodynamische Interaktion zwischen Lumefantrin und seinem Monodesbutyl-Analog (DBB) wurde bei 35 frischen Isolaten von Plasmodium falciparum untersucht. Beide Substanzen zeigten signifikante Wirkungskorrelation. Die geometrischen Mittelwerte für volle Hemmung der Schizontenreifung (GMCOC) lagen bei 536,8 nM für Lumefantrin, 246,0 nM für DBB, 235,5 nM für LUM-DBB 999:1, und 155,2 nM für LUM-DBB 995:5, mit signifikanten Unterschieden zwischen Lumefantrin und DBB sowie den LUM-DBB Kombinationen. Die Summen der fraktionellen Hemmwerte nach Berenbaum (SFIC) lagen für LUM-DBB 995:5 im Bereich von klarem Synergismus, wobei der Interaktionsgrad mit der effektiven Hemmkonzentration stieg.

Summary

The pharmacodynamic interaction between lumefantrine and its monodesbutyl analogue (DBB) has been investigated in 35 fresh isolates of Plasmodium falciparum. Both compounds showed highly significant activity correlation. The geometric mean values for complete inhibition of schizont maturation (GMCOC) were 536,8 nM for lumefantrine, 246.0 nM for DBB, 235,5 nM for LUM-DBB 999:1, and 155,2 nM for LUM-DBB 995:5, with significant activity differences between lumefantrine and DBB as well as the LUM-DBB combinations. For the combination of lumefantrine and DBB 995:5 the sums of the fractional inhibitory concentrations according to Berenbaum (SFIC) indicated marked synergism, the intensity of interaction rising with the effective inhibitory concentrations.

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Authors and Affiliations

  1. Institute of Specific Prophylaxis and Tropical Medicine, Centre for Physiology and Pathophysiology, Medical University of Vienna, Austria

    Peter Starzengruber, Herwig Kollaritsch & Walther H. Wernsdorfer

  2. Bureau of Vector Borne Diseases, Ministry of Public Health, Nonthaburi, Thailand

    Jeeraphat Sirichaisinthop & Kanungnit Congpuong

  3. Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand

    Gunther Wernsdorfer & Walther H. Wernsdorfer

Authors
  1. Peter Starzengruber
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  2. Herwig Kollaritsch
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  3. Jeeraphat Sirichaisinthop
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  4. Gunther Wernsdorfer
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  5. Kanungnit Congpuong
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  6. Walther H. Wernsdorfer
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Correspondence to Peter Starzengruber.

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Starzengruber, P., Kollaritsch, H., Sirichaisinthop, J. et al. Interaction between lumefantrine and monodesbutyl-benflumetol in Plasmodium falciparum in vitro. Wien Klin Wochenschr 120 (Suppl 4), 85–89 (2008). https://doi.org/10.1007/s00508-008-1080-8

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  • DOI: https://doi.org/10.1007/s00508-008-1080-8

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