ORBi: Frederich Michel - Antiplasmodial activity of alkaloids from various Strychnos species

Reference : Antiplasmodial activity of alkaloids from various Strychnos species


	Document type :	Scientific journals : Article
	Discipline(s) :	Engineering, computing & technology : Chemical engineering Physical, chemical, mathematical & earth Sciences : Chemistry Life sciences : Phytobiology (plant sciences, forestry, mycology...)
	To cite this reference:	http://hdl.handle.net/2268/13896

Title :	Antiplasmodial activity of alkaloids from various Strychnos species
Language :	English
Author, co-author :	Frederich, Michel [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
	Jacquier, M. J. [> > > >]
	Thepenier, P. [> > > >]
	De Mol, Patrick [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Microbiologie médicale et virologie médicale]
	Tits, Monique [Université de Liège - ULg > Département de pharmacie > Phytochimie et phytothérapie >]
	Philippe, Geneviève [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
	Delaude, Clément [Université de Liège - ULg > > Relations académiques et scientifiques (Sciences) >]
	Angenot, Luc [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
	Zeches-Hanrot, M. [> > > >]
Publication date :	Oct-2002
Journal title :	Journal of Natural Products
Publisher :	American Chemical Society
Volume :	65
Issue/season :	10
Pages :	1381-1386
Audience :	International
ISSN :	0163-3864
e-ISSN :	1520-6025
City :	Washington
Abstract :	[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.
Permalink :	http://hdl.handle.net/2268/13896

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