In Vitro Antimalarial Activity and Chloroquine Potentiating Action of Two Bisbenzylisoquinoline Enantiomer Alkaloids Isolated from Strychnopsis thouarsii and Spirospermum penduliflorum

S. Ratsimamanga-Urverg; P. Rasoanaivo; L. Ramiaramanana; R. Milijaona; H. Rafatro; F. Verdier; A. Rakoto-Ratsimamanga; J. Le Bras

doi:10.1055/s-2006-961545

Planta Med 1992; 58(6): 540-543
DOI: 10.1055/s-2006-961545

Papers

In Vitro Antimalarial Activity and Chloroquine Potentiating Action of Two Bisbenzylisoquinoline Enantiomer Alkaloids Isolated from Strychnopsis thouarsii and Spirospermum penduliflorum

S. Ratsimamanga-Urverg¹ ^, ² , P. Rasoanaivo¹ , L. Ramiaramanana² , R. Milijaona¹ , H. Rafatro¹ , F. Verdier³ , A. Rakoto-Ratsimamanga¹ , J. Le Bras⁴

¹Institut Malgache de Recherches Appliquees, B.P.3833, Antananarivo, Madagascar
²Ecole pratique des Hautes Etudes, Laboratoiro de Nutrition tropicale. Institut de Médecine et d'Epidémiologie Africaines et Tropicales (IMEAT), F-75944, Paris, France
³INSERM U13/IMEAT, F-75944, Paris, France
⁴Centra National de Référence Chimiosensibilité du Paludisme (IMEAT) and Laboratoiro de Parasitologie, Université R. Descartes, F-75270 Paris, France

Abstract

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Abstract

The bisbenzylisoquinolines 7-O-deme-thyltetrandrine and limacine, respectively, isolated from Strychnopsis thouarsii Baill. and Spirospermum penduliflorum Thou, were evaluated for their intrinsic anti-malarial activity in vitro and chloroquine potentiating action against the chloroquine-resistant Plasmodium falciparum FCM 29 originating from Cameroon. They both showed significant antiplasmodial potency in vitro with very similar IC₅₀ values of respectively, 740 nM and 789 nM (IC₅₀ = 214 nM for chloroquine used as standard drug), which demonstrated that the stereochemistry of the C-1 and C-1′ configuration likely plays a role in the chloroquine potentiating effect of these drugs. If confirmed in vivo, these results may account for the traditional use of the two plants as antimalarials and adjuvant to chloroquine in Madagascan folklore remedies.

Key words

Strychnopsis thouarsii - Spirospermum penduliflorum - Menispermaceae - 7-O-demethyltetrandrine - limacine - in vitro tests - Plasmodium falciparum

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