THE 1ST PROTOBERBERINE ALKALOID ANALOG WITH IN-VIVO ANTIMALARIAL ACTIVITY

2,3,11,12-Tetramethoxyberbinium chloride at very low doses causes a ma rked reduction of parasitaemia produced by Plasmodium chabaudi infecti on in mice. The 2,3,10,11 and 13-amino-2,3,10,11-tetramethoxy analogue s are inactive in this test system at the same dose levels, despite al l three compounds having marked in vitro activity against P. falciparu m. This is the first time that in vivo antimalarial activity of a prot oberberine alkaloid analogue has been demonstrated. The parent alkaloi d berberine also has activity in vivo against P. chabaudi, in contrast to its reported lack of activity against P. berghei in mice.