A screening of Sudanese medicinal plants for antiprotozoal activities revealed that the chloroform and water fractions of the ethanolic root extract of
Haplophyllum tuberculatum exhibited appreciable bioactivity against
Leishmania donovani. The antileishmanial activity was tracked by HPLC-based activity profiling, and eight compounds
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A screening of Sudanese medicinal plants for antiprotozoal activities revealed that the chloroform and water fractions of the ethanolic root extract of
Haplophyllum tuberculatum exhibited appreciable bioactivity against
Leishmania donovani. The antileishmanial activity was tracked by HPLC-based activity profiling, and eight compounds were isolated from the chloroform fraction. These included lignans tetrahydrofuroguaiacin B (
1), nectandrin B (
2), furoguaiaoxidin (
7), and 3,3′-dimethoxy-4,4′-dihydroxylignan-9-ol (
10), and four cinnamoylphenethyl amides, namely dihydro-feruloyltyramine (
5), (
E)-
N-feruloyltyramine (
6),
N,
N′-diferuloylputrescine (
8), and 7′-ethoxy-feruloyltyramine (
9). The water fraction yielded steroid saponins
11–
13. Compounds
1,
2, and
5–
13 are reported for the first time from
Haplophyllum species and the family Rutaceae. The antiprotozoal activity of the compounds plus two stereoisomeric tetrahydrofuran lignans—fragransin B
2 (
3) and fragransin B
1 (
4)—was determined against
Leishmania donovani amastigotes,
Plasmodium falciparum, and
Trypanosoma brucei rhodesiense bloodstream forms, along with their cytotoxicity to rat myoblast L6 cells. Nectandrin B (
2) exhibited the highest activity against
L. donovani (IC
50 4.5 µM) and the highest selectivity index (25.5).
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