Possible artefacts in the in vitro determination of antimalarial activity of natural products that incorporate into lipid bilayer: apparent antiplasmodial activity of dehydroabietinol, a constituent of Hyptis suaveolens
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Possible artefacts in the in vitro determination of antimalarial activity of natural products that incorporate into lipid bilayer : apparent antiplasmodial activity of dehydroabietinol, a constituent of Hyptis suaveolens. / Ziegler, Hanne Lindvig; Jensen, Thomas Høgh; Christensen, Jette; Stærk, Dan; Hägerstrand, Henry; Sittie, Archibald A; Olsen, Carl Erik; Staalsø, Trine; Ekpe, Patrick; Jaroszewski, Jerzy W.
In: Planta Medica, Vol. 68, 2002, p. 547-549.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Possible artefacts in the in vitro determination of antimalarial activity of natural products that incorporate into lipid bilayer
T2 - apparent antiplasmodial activity of dehydroabietinol, a constituent of Hyptis suaveolens
AU - Ziegler, Hanne Lindvig
AU - Jensen, Thomas Høgh
AU - Christensen, Jette
AU - Stærk, Dan
AU - Hägerstrand, Henry
AU - Sittie, Archibald A
AU - Olsen, Carl Erik
AU - Staalsø, Trine
AU - Ekpe, Patrick
AU - Jaroszewski, Jerzy W.
N1 - Keywords: Animals; Antimalarials; Artifacts; Biological Products; Cell Size; Chloroquine; Diterpenes; Diterpenes, Abietane; Erythrocytes; Humans; Inhibitory Concentration 50; Lamiaceae; Lipid Bilayers; Microscopy, Electron; Plasmodium falciparum; Sesquiterpenes; Tumor Cells, Cultured
PY - 2002
Y1 - 2002
N2 - Dehydroabietinol isolated from Hyptis suaveolens (L.) Poit. was found to inhibit growth of chloroquine-sensitive as well as chloroquine-resistant strains of Plasmodium falciparum cultivated in erythrocytes in vitro (IC 50 26-27 microM). However, erythrocytes exposed to dehydroabietinol were transformed in a dose-dependent manner towards spherostomatocytic forms with concomitant formation of endovesicles, as disclosed by transmission electron microscopy. The erythrocyte shape alterations caused by dehydroabietinol correlated well with its apparent IC 50 value. Thus, dehydroabietinol incorporates into the erythrocyte membrane, and since invasion and survival of Plasmodium parasites is known to depend on the function of the erythrocyte membrane, the observed antiplasmodial effect of dehydroabietinol is presumably an indirect effect on the host cell. Because of these findings, microscopic investigations should be generally used to support claims of antimalarial effects of apolar natural products.
AB - Dehydroabietinol isolated from Hyptis suaveolens (L.) Poit. was found to inhibit growth of chloroquine-sensitive as well as chloroquine-resistant strains of Plasmodium falciparum cultivated in erythrocytes in vitro (IC 50 26-27 microM). However, erythrocytes exposed to dehydroabietinol were transformed in a dose-dependent manner towards spherostomatocytic forms with concomitant formation of endovesicles, as disclosed by transmission electron microscopy. The erythrocyte shape alterations caused by dehydroabietinol correlated well with its apparent IC 50 value. Thus, dehydroabietinol incorporates into the erythrocyte membrane, and since invasion and survival of Plasmodium parasites is known to depend on the function of the erythrocyte membrane, the observed antiplasmodial effect of dehydroabietinol is presumably an indirect effect on the host cell. Because of these findings, microscopic investigations should be generally used to support claims of antimalarial effects of apolar natural products.
U2 - 10.1055/s-2002-32548
DO - 10.1055/s-2002-32548
M3 - Journal article
C2 - 12094303
VL - 68
SP - 547
EP - 549
JO - Planta Medica
JF - Planta Medica
SN - 0032-0943
ER -
ID: 17274513