In vitro antimalarial activity and chloroquine potentiating action of two bisbenzylisoquinoline enantiomer alkaloids isolated from Strychnopsis thouarsii and Spirospermum penduliflorum.
The bisbenzylisoquinolines 7-O-demethyltetrandrine and limacine, respectively, isolated from Strychnopsis thouarsii Baill. and Spirospermum penduliflorum Thou. were evaluated for their intrinsic antimalarial activity in vitro and chloroquine potentiating action against the chloroquine-resistant Plasmodium falciparum FCM 29 originating from Cameroon. They both showed significant antiplasmodial potency in vitro with very similar IC50 values of respectively, 740 nM and 789 nM (IC50 = 214 nM for chloroquine used as standard drug), which demonstrated that the stereochemistry of the C-1 and C-1' configuration likely plays a role in the chloroquine potentiating effect of these drugs. If confirmed in vivo, these results may account for the traditional use of the two plants as antimalarials and adjuvant to chloroquine in Madagascan folklore remedies.
Ratsimamanga-Urverg
S
S
Institut Malgache de Recherches Appliquees, Antananarivo, Madagascar.
Rasoanaivo
P
P
Ramiaramanana
L
L
Milijaona
R
R
Rafatro
H
H
Verdier
F
F
Rakoto-Ratsimamanga
A
A
Le Bras
J
J
D000470:Alkaloids / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000302:isolation & purification / Q000494:pharmacology*; D044182:Benzylisoquinolines; D002738:Chloroquine / Q000494:pharmacology*; D004357:Drug Synergism; D010946:Plants, Medicinal / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects*
D000470:Alkaloids; D000962:Antimalarials; D044182:Benzylisoquinolines; D002738:Chloroquine; C060802:fangchinoline