Antiplasmodial and cytotoxic activity of galipinine and other tetrahydroquinolines from Galipea officinalis.
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 microg/ml for the chloroquine-sensitive strain (CQS) and from 0.09 to 38 microg/ml for the chloroquine-resistant strains (CQR). Galipinine yielded the best antimalarial effect (IC50: 0.09 - 0.9 microg/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 microg/ml.
Jacquemond-Collet
Ingrid
I
Laboratoire Pharmacophores Rédox, Phytochimie et Radiobiologie, Faculté des Sciences Pharmaceutiques, Toulouse, France.
Benoit-Vical
Françoise
F
Valentin
Alexis
A
Stanislas
Edouard
E
Mallié
Michèle
M
Fourasté
Isabelle
I
D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D024301:Plant Bark / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D027821:Rutaceae; D018675:Toxicity Tests; D014687:Venezuela
D000470:Alkaloids; D000962:Antimalarials; D010936:Plant Extracts; D011804:Quinolines; C452941:angustureine; C452940:galipeine; C452943:galipinine; C452942:cuspareine; D002738:Chloroquine