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

Hanne Lindvig Ziegler; Thomas Høgh Jensen; Jette Christensen; Dan Stærk; Henry Hägerstrand; Archibald A Sittie; Carl Erik Olsen; Trine Staalsø; Patrick Ekpe; Jerzy W. Jaroszewski

doi:10.1055/s-2002-32548

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

Hanne Lindvig Ziegler, Thomas Høgh Jensen, Jette Christensen, Dan Stærk, Henry Hägerstrand, Archibald A Sittie, Carl Erik Olsen, Trine Staalsø, Patrick Ekpe, Jerzy W. Jaroszewski

Department of Immunology and Microbiology

31 Citations (Scopus)

21 Downloads (Pure)

Abstract

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.

Original language	English
Journal	Planta Medica
Volume	68
Pages (from-to)	547-549
Number of pages	3
ISSN	0032-0943
DOIs	https://doi.org/10.1055/s-2002-32548
Publication status	Published - 2002

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Ziegler, H. L., Jensen, T. H., Christensen, J., Stærk, D., Hägerstrand, H., Sittie, A. A., Olsen, C. E., Staalsø, T., Ekpe, P., & Jaroszewski, J. W. (2002). 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. Planta Medica, 68, 547-549. https://doi.org/10.1055/s-2002-32548

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 et al.

In: Planta Medica, Vol. 68, 2002, p. 547-549.

Research output: Contribution to journal › Journal article › Research › peer-review

Ziegler, HL, Jensen, TH, Christensen, J, Stærk, D, Hägerstrand, H, Sittie, AA, Olsen, CE, Staalsø, T, Ekpe, P & Jaroszewski, JW 2002, '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', Planta Medica, vol. 68, pp. 547-549. https://doi.org/10.1055/s-2002-32548

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title = "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",

abstract = "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.",

author = "Ziegler, {Hanne Lindvig} and Jensen, {Thomas H{\o}gh} and Jette Christensen and Dan St{\ae}rk and Henry H{\"a}gerstrand and Sittie, {Archibald A} and Olsen, {Carl Erik} and Trine Staals{\o} and Patrick Ekpe and Jaroszewski, {Jerzy W.}",

note = "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",

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doi = "10.1055/s-2002-32548",

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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

SN - 0032-0943

VL - 68

SP - 547

EP - 549

JO - Planta Medica

JF - Planta Medica

ER -