In vitro antiplasmodial, antiamoebic, and cytotoxic activities of a series of bisbenzylisoquinoline alkaloids

Abstract

Twenty-four bisbenzylisoquinoline alkaloids were screened for antiplasmoidal, antiamoebic, and cytotoxic activities by use of in vitro microtests. Eight of the alkaloids had antiplasmodial activity, with a 50% inhibitory concentration (IC50) of less than 1 microM against a multidrug-resistant strain of Plasmodium falciparum (chloroquine had an IC50 of 0.2 microM). The three alkaloids most active against Entamoeba histolytica, aromoline, isotrilobine, and insularine, had IC50s of 5 to 11.1 microM (metronidazole had an IC50 of 1.87 microM). None of the 24 bisbenzylisoquinoline alkaloids exhibited significant cytotoxicity against the KB cell line, the most toxic being berbamine, with an IC50 of 17.8 microM (the IC50 of podophyllotoxin was 0.008 microM). Bisbenzylisoquinoline alkaloids merit further investigation as potential novel antimalarial agents.

Antiprotozoal and cytotoxic screening of 45 plant extracts from Democratic Republic of Congo

“…That of Momordica charantia revealed the presence of alkaloids such as coosuline, efirine, gilletine, trigilletine, trigilletimine and tricordatine belonging to the bisbenzylisoquinoline alkaloid group as predominant constistuents (Tackie et al, 1973;Owusu et al, 1980), and triterpenes (Begun et al, 1997;Chang et al, 2006;Kimura et al, 2005). These compounds most likely are active constituents of this plant species since some of them have been previously reported to exhibit antiprotozoal activity at different extents against different protozoa (Marshall et al, 1994;Camacho et al, 2002). Unfortunately, no phytochemical and biological studies of Omphalocarpum glomerata were available in the literature.…”

In vitro antiprotozoal and cytotoxic activity of 33 ethonopharmacologically selected medicinal plants from Democratic Republic of Congo

“…and with appreciable selectivity. The activity of Triclisia dictyophylla leaves may be due to the presence of bisbenzylisoquinoline alkaloids, since these compounds isolated from other plant species have been shown to exhibit antiprotozoal activity (Marshall et al, 1994;Fournet et al, 1993Fournet et al, , 1997Fournet et al, , 2000Camacho et al, 2002;Longanga Otshudi et al, 2005;Murebwayire et al, 2008). The aqueous extract from Quassia africana stem bark displayed pronounced activity against Plasmodium falciparum (IC 50 = 1.27 g/ml; SI > 13.6) and was inactive against Leishmania infantum, this in slight contrast to the activity of the root bark extract.…”

Actividad in vitro de la mezcla de alcaloides de Ervatamia coronaria (Jacq) Staff. Apocynaceae sobre amastigotes de Leishmania braziliensis

“…Soares et al (2003) evaluaron la citotoxicidad del extracto obtenido a partir de la especie Tabernaemontana catharinensis, de la cual se cuantifi caron mediante cromatografía de gas los alcaloides coronaridina y voacristina, demostrando que no presentaron efectos tóxicos en macrófagos murinos de ratón. En estudios realizados con varios alcaloides (Marshall et al, 1994), se encontró que el más citotóxico, berbamina, con IC 50 de 17.8 M fue casi 2000 veces menos potente que la droga control, glucantime.…”