Interaction of the Antimalarial Agents Halofantrine and Lumefantrine with Lipid Bilayers

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概要

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• The effects of antimalarial drugs halofantrine and lumefantrine on the fluoresence anisotropy of diphenyl-hexatriene (DPH)-containing phospholipid vesicles have been examined. Lumefantrine increases DPH anisotropy, indicating a condensing effect on bilayers of dipalmitoylphosphatidyl choline (DPPC), dioleoylphos-phatidylcholine (DOPC), egg lecithin and mouse erythrocyte membranes (including membranes isolated from plasmodial-infected mice). Its condensing effect is more pronounced in bilayers of lower microviscosity. In contrast, increases or decreases in DPH anisotropy are observed with halofantrine, depending on the nature of the lipid. Decreases in anisotropy, which reflect a perturbing effect, are observed in bilayers of high microviscosity (for example, gel state of DPPC bilayers). Increases in anisotropy are observed in bilayers of low microviscosity (such as DOPC and egg lecithin bilayers). The perturbing effect of halofantrine is further confirmed by the increases in permeability of calcein-conning DPPC vesicles in the presence of the drug. However the perturbative effects of halofantrine are observed to the same magnitude in uninfected and plasmodial-infected erythrocyte membranes, and may not be relevant to the antimalarial action of the drug. In contrast, the condensing ef-fect of lumefantrine is significantly greater in infected erythrocyte membranes and may contribute to its anti-malarial action.

• 公益社団法人日本薬学会の論文
• 2003-03-01

著者

• Go M‐l

  Department Of Pharmacy National Uneversity Of Sengapore

• GO Mei-Lin

  Department of Pharmacy, National Uneversity of Sengapore

• LI Qui-Tian

  Department of Biochemistry, National University of Singapore

• Go Mei-lin

  Department Of Pharmacy National University Of Singapore

• Li Qui-tian

  Department Of Biochemistry National University Of Singapore

関連論文

• Interaction of the Antimalarial Agents Halofantrine and Lumefantrine with Lipid Bilayers
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• The Antimalarial Agent Halofantrine Perturbs Phosphatidylcholine and Phosphatidylethanolamine Bilavers : a Differential Scanning Calorimetric Study
• Structure-Hydrolyzability Relationships in a Series of Piperidinyl and Tropinyl Esters with Antimuscarinic Activity
• Halofantrine-Phospholipid Interactions : Monolayer Studies
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• Thermodynamics of Partitioning of the Antimalarial Drug Mefloquine in Phospholipid Bilayers and Bulk Solvents
• A Differential Scanning Calorimetry Study of the Interaction of the Antimalarial Agent Halofanthrine with Dipalmitoyl Phosphatidyl Choline Bilayers
• Thermodynamics of the Partitioning of 7-Chloro-4-(4'-methoxy)antilinoquinoline and Its Cyclized Analog in Octanol-Buffer and Liposome Systems

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