Antileishmanial anthraquinones from the rhyzomes of Rumex abyssinicus Jacq (Polygonaceae).

Phytochemical investigation of the rhyzomes of Rumex abyssinicus (Polygonaceae) afforded six anthraquinones viz chrysophanol (1), physcion (2), emodin (3), mixture of physcion-8-O-ß,D-glucopyranoside (4) and chrypsophanol-8-O-ß,D-glucopyranoside (5), and emodin-8-O-ß,D-glucopyranoside (6). All the compounds were characterised and identified by comparison of their MS and NMR data with available literature data. The isolated compounds were evaluated for their antileishmanial activity. Emodin (3) was the most active compounds with IC50 13.82 and 0.26 µg/mL against Leishmania donovani amastigotes and promastigotes, respectively. Emodin-8-O-ß,D-glucopyranoside (6) also showed a moderate activity with IC50 27.53 and 37.08 µg/mL. This is the first report of antileishmanial compounds from R. abyssinicus and the antileishmanial activities of compounds 2, 4, 5 and 6 are here reported for the first time.

Extracts from Annona Muricata L. and Annona Reticulata L. (Annonaceae) Potently and Selectively Inhibit Plasmodium Falciparum.

The aim of this work was to screen extracts from Annona muricata and Annona reticulata in vitro against Plasmodium falciparum. Crude ethanolic extracts, methylene chloride fractions, aqueous fractions, subfractions and isolated compounds (stigmasterol-3-O-ß-d-glucopyranoside, lichexanthone, gallic acid and ß-sitosterol-3-O-ß-d-glucopyranoside) were tested for cytotoxicity on erythrocytes and Human Foreskin Fibroblasts cells and against the W2 strain of P. falciparum in culture. Results indicated that none of the extracts was cytotoxic at concentrations up to 10 µg/mL. Most of the extracts, fractions and subfractions inhibited the growth of P. falciparum with IC50 values ranging from 0.07 to 3.46 µg/mL. The most potent was the subfraction 30 from A. muricata stem bark (IC50 = 0.07 µg/mL) with a selectivity index of ˃ 142. Subfraction 3 from A. muricata root also exhibited very good activity (IC50 = 0.09 µg/mL) with a high selectivity index (SI ˃ 111). Amongst the isolated compounds, only gallic acid showed activity with IC50 of 3.32 µg/mL and SI > 10. These results support traditional claims for A. muricata and A. reticulata in the treatment of malaria. Given their limited cytotoxicity profile, their extracts qualify as promising starting points for antimalarial drug discovery.