Isolation of Bis-Indole Alkaloids with Antileishmanial and Antibacterial Activities from Perschiera van heurkii (Syn. Tabernaemontana van heurkii)

V. Muñoz; C. Moretti; M. Sauvain; C. Caron; A. Porzel; G. Massiot; B. Richard; L. Le Men-Olivier

doi:10.1055/s-2006-959531

Planta Med 1994; 60(5): 455-459
DOI: 10.1055/s-2006-959531

Paper

Isolation of Bis-Indole Alkaloids with Antileishmanial and Antibacterial Activities from Perschiera van heurkii (Syn. Tabernaemontana van heurkii)

V. Muñoz¹ , C. Moretti¹ ^, ² ^, ³ , M. Sauvain¹ ^, ² , C. Caron³ , A. Porzel³ , G. Massiot³ , B. Richard³ , L. Le Men-Olivier³

¹Insituto Boliviano de Biologia de Altura (IBBA), CP 717, La Paz, Bolivia
²Institut Français de Recherche Scientifique pour le Développement en Coopération (ORSTOM), Département Santé, 213 rue La Fayette, F-75480 Paris Cedex 10, France
³Laboratoire de Pharmacognosie, associé au CNRS - URA 492, Faculté de Pharmacie, 51 rue Cognacq Jay, F-51096 - Reims Cedex, France

Abstract

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Abstract

Extracts from leaves and stem bark of Peschiera van heurkii (Muell. Arg.) L. Allorge (syn. Tabernaemontana van heurkii Muell. Arg., Apocynaceae) have been assayed for antileishmanial and antibacterial activities. The activities were concentrated in the alkaloid fractions which yielded 20 indole and bis-indole alkaloids. The strongest leishmanicidal and antibacterial activities were observed with the dimeric alkaloids conodurine (1), N-demethylconodurine (= gabunine) (2), and conoduramine (3). Weak toxicity towards macrophage host cells and strong activity against the intracellular amastigote form of Leishmania were observed for compounds 1 and 2. In vivo, 1 was less active than glucantime (= N-methylglucamine antimonate), the drug of reference, while 2 was devoid of activity at l00 mg/kg.

Key words

Peschiera van heurkii - Tabernaemontana - Apocynaceae - bis-indole alkaloids - conodurine - gabunine - conoduramine - leishmanicidal - antibacterial activities - Leishmania amazonensis - Leishmania braziliensis

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