Reference : Antiplasmodial activity of alkaloids from various Strychnos species
Scientific journals : Article
Engineering, computing & technology : Chemical engineering
Physical, chemical, mathematical & earth Sciences : Chemistry
Life sciences : Phytobiology (plant sciences, forestry, mycology...)
http://hdl.handle.net/2268/13896
Antiplasmodial activity of alkaloids from various Strychnos species
English
Frederich, Michel mailto [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
Jacquier, M. J. [> > > >]
Thepenier, P. [> > > >]
De Mol, Patrick mailto [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Microbiologie médicale et virologie médicale]
Tits, Monique mailto [Université de Liège - ULg > Département de pharmacie > Phytochimie et phytothérapie >]
Philippe, Geneviève mailto [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
Delaude, Clément [Université de Liège - ULg > > Relations académiques et scientifiques (Sciences) >]
Angenot, Luc mailto [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
Zeches-Hanrot, M. [> > > >]
Oct-2002
Journal of Natural Products
American Chemical Society
65
10
1381-1386
Yes (verified by ORBi)
International
0163-3864
1520-6025
Washington
[en] The in vitro antiplasmodial activities of 69 alkaloids from various Strychnos species were evaluated against chloroquine-resistant and chloroquine-sensitive lines of Plasmodium falciparum. The compounds, comprising mainly indolomonoterpenoid alkaloids, exhibited a wide range of biological potencies in the antiplasmodial assays. The most active alkaloids were also tested for cytotoxicity against HCT-116 colon cancer cells to determine their antiplasmodial selectivity. As a result of these studies, structure-activity relationships for these alkaloids have begun to emerge. Alkaloids presenting four types of bisindole skeleton exhibited potent and selective activities against Plasmodium. They were sungucine-type (IC(50) values ranging from 80 nM to 10 microM), longicaudatine-type (IC(50) values ranging from 0.5 to 10 microM), matopensine-type (IC(50) values ranging from 150 nM to 10 microM), and usambarine-type alkaloids. Within the last structural type, isostrychnopentamine (49) and ochrolifuanine A (46) were found to be active against chloroquine-sensitive and -resistant strains (IC(50) values of 100-150 and 100-500 nM, respectively), and dihydrousambarensine (51) exhibited a 30-fold higher activity against the chloroquine-resistant strain (IC(50) = 32 nM) than against the chloroquine-sensitive one.
http://hdl.handle.net/2268/13896

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