Antiprotozoal Compounds from Asparagus africanus

Abstract

Two antiprotozoal compounds have been isolated from the roots of Asparagus africanus Lam. (Liliaceae), a new sapogenin, 2β,12α-dihydroxy-(25R)-spirosta-4,7-dien-3-one (1), which was named muzanzagenin, and the lignan (+)-nyasol (2), (Z)-(+)-4,4‘-(3-ethenyl-1-propene-1,3-diyl)bisphenol. The structure of the sapogenin was elucidated by MS and by 1D and 2D NMR methods and established by a single crystal X-ray analysis. (+)-Nyasol potently inhibits the growth of Leishmania major promastigotes, the IC50 being 12 μM, and moderately inhibits Plasmodium falciparum schizonts with the IC50 49 μM. These concentrations only moderately affect the proliferation of human lymphocytes. Muzanzagenin showed a moderate in vitro activity in all three tests, the IC50 against leishmania promastigotes was 70 μM, and against four different malaria schizont strains the IC50 values were 16, 163, 23, and 16 μM, respectively.