In vitro antiplasmodial, antiamoebic, and cytotoxic activities of some monomeric isoquinoline alkaloids.
Twenty-one alkaloids have been assessed for activities against Plasmodium falciparum (multidrug- resistant strain K1) in vitro; 18 of these are reported for the first time. Two protoberberine alkaloids, dehydrodiscretine and berberine, were found to have antiplasmodial IC(50) values less than 1 M, while seven alkaloids-allocrytopine, columbamine, dehydroocoteine, jatrorrhizine, norcorydine, thalifendine, and ushinsunine-had values between 1 and 10 M. These results are discussed in the context of structure-activity relationships. Compounds were also assessed for antiamoebic and cytotoxic activities, but none was significantly active except for berberine, which was moderately cytotoxic.
Wright
C W
CW
The School of Pharmacy, University of Bradford, West Yorkshire, BD7 1DP, UK. c.w.wright@bradford.ac.uk
Marshall
S J
SJ
Russell
P F
PF
Anderson
M M
MM
Phillipson
J D
JD
Kirby
G C
GC
Warhurst
D C
DC
Schiff
P L
PL
D000470:Alkaloids / Q000737:chemistry / Q000494:pharmacology*; D000563:Amebicides / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D004748:Entamoeba histolytica / Q000187:drug effects; D007546:Isoquinolines / Q000737:chemistry / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
D000470:Alkaloids; D000563:Amebicides; D000962:Antimalarials; D007546:Isoquinolines