Antiplasmodial and Cytotoxic Activity of Galipinine and other Tetrahydroquinolines from Galipea officinalis

 

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Abstract

The antimalarial and toxicological properties of four tetrahydroquinoline alkaloids from Galipea officinalis trunk bark were studied. Crude extracts and pure alkaloids were tested for in vitro antimalarial activity on Plasmodium falciparum. The IC₅₀ were evaluated after 24 and 72 h contact between compounds and the parasite culture, and ranged from 1.8 to 40 μg/ml for the chloroquine-sensitive strain (CQS) and from 0.09 to 38 μg/ml for the chloroquine-resistant strains (CQR). Galipinine yielded the best antimalarial effect (IC₅₀: 0.09 - 0.9 μg/ml on CQR strain) and this compound interacted particularly between the 32^nd and the 40^th hour of the P. falciparum erythrocytic cycle. The cytotoxicity of the extracts and pure tetrahydroquinoline alkaloids was assessed on the HeLa cell line and showed IC₅₀ values ranging from 5.8 to above 50 μg/ml.

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Dr. Alexis Valentin

Laboratoire d’Immunologie et Parasitologie

UFR Sciences Pharmaceutiques

15, avenue Charles Flahault

F-34060 Montpellier Cedex 02

France

Email: valentin@iup.pharma.univ-montp1.fr

Fax: +33 4-67-41-16-17