ORBi: Frederich Michel - In vitro and in vivo antimalarial properties of isostrychnopentamine, an indolomonoterpenic alkaloid from Strychnos usambarensis

Reference : In vitro and in vivo antimalarial properties of isostrychnopentamine, an indolomonoterpe...


	Document type :	Scientific journals : Article
	Discipline(s) :	Human health sciences : Pharmacy, pharmacology & toxicology Physical, chemical, mathematical & earth Sciences : Chemistry Life sciences : Phytobiology (plant sciences, forestry, mycology...)
	To cite this reference:	http://hdl.handle.net/2268/14042

Title :	In vitro and in vivo antimalarial properties of isostrychnopentamine, an indolomonoterpenic alkaloid from Strychnos usambarensis
Language :	English
Author, co-author :	Frederich, Michel [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
	Tits, Monique [Université de Liège - ULg > Département de pharmacie > Phytochimie et phytothérapie >]
	Goffin, Eric [Université de Liège - ULg > > Chimie pharmaceutique >]
	Philippe, Geneviève [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
	Grellier, P. [> > > >]
	De Mol, Patrick [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Microbiologie médicale et virologie médicale]
	Hayette, Marie-Pierre [Université de Liège - ULg > > Microbiologie médicale >]
	Angenot, Luc [Université de Liège - ULg > Département de pharmacie > Pharmacognosie >]
Publication date :	Jun-2004
Journal title :	Planta Medica
Publisher :	Georg Thieme Verlag Kg
Volume :	70
Issue/season :	6
Pages :	520-525
Audience :	International
ISSN :	0032-0943
City :	Stuttgart
Keywords :	[en] Plasmodium falciparum ; Plasmodium berghei ; Plasmodium vinckei ; isostrychnopentamine ; Strychnos usambarensis ; loganiaceae
Abstract :	[en] Isostrychnopentamine (ISP) is an asymmetric indolomonoterpenic alkaloid isolated from the leaves of Strychnos usambarensis. The in vitro antiplasmodial activities against five Plasmodium falciparum cell lines were evaluated: ISP possessed an in vitro IC (50) near 0.1 microM against all P. falciparum cell lines tested (chloroquine-resistant and chloroquine-sensitive lines) and showed antiplasmodial selectivity compared to cytotoxicity on human cell lines. The stage-dependent susceptibility to a short exposure of ISP was then investigated. The ring stage was shown to be the most sensitive one, but all stages were affected by ISP treatment. By means of fluorescence microscopy, it was shown that ISP was not accumulated inside the food vacuole of the parasite. Finally, the in vivo antimalarial activities against the P. berghei NK173 and P. vinckei petteri murine strains were determined. The ED (50) in vivo was about 30 mg/kg/day by the intraperitoneal route (after 4 days treatment).
Permalink :	http://hdl.handle.net/2268/14042

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