ABSTRACT
The methanolic extract of dried, powdered Cissampelos mucronata roots possesses significant in vitro activity against Plasmodium falciparum. In order to enable further pharmacological testing, the substances responsible for the observed activity were purified, mainly by HPLC, using various stationary and mobile phases. The active principles were determined to be a series of bisbenzylisoquinoline alkaloids, a group of natural products for which one of the first routine preparative HPLC separation methods is described.
Subject(s)
Alkaloids/isolation & purification , Alkaloids/pharmacology , Antimalarials/isolation & purification , Benzylisoquinolines , Cissampelos/chemistry , Isoquinolines/isolation & purification , Isoquinolines/pharmacology , Plant Roots/chemistry , Animals , Antimalarials/pharmacology , Cells, Cultured , Chromatography, High Pressure Liquid , Molecular Structure , Plasmodium falciparum/drug effectsABSTRACT
Seven plant species, belonging to different families, were collected in the eastern part of the Republic of Congo (Kivu) based on ethnopharmacological information. Their dichloromethane and methanolic extracts were tested for biological activity. Five of the seven collected plants exhibited antiplasmodial activity with IC(50) values ranging from 1.1 to 9.8 microg/ml. The methanolic extract of Cissampelos mucronata was the most active one showing activity against chloroquine sensitive (D6) and chloroquine resistant (W2) Plasmodium falciparum strains with IC(50) values of 1.5 and 1.1 microg/ml, respectively. Additionally, this extract significantly inhibited the enzyme tyrosine kinase p56(lck) (TK). The dichloromethane extract of Amorphophallus bequaertii inhibited the growth of Mycobacterium tuberculosis with a MIC of 100 microg/ml and the methanolic extract of Rubus rigidus inhibited the activity of both enzymes HIV1-reverse transcriptase (HIV1-RT) and TK p56(lck).
