Dorstenia barteri and D. convexa extracts and some isolated components of the former were investigated for effectiveness against Trichomonas gallinarum and compared with quercetin and quercitrin. The antioxidant activity of the extracts/compounds was also determined. The minimum lethal concentrations (MLCs) for the extract of D. barteri leaves and twigs at 24 h were found to be 15.625 and 15.625 µg/ml, respectively. However, the MLCs of the leaf and twig extract of D. convexa were 125 and 437.5 µg/ml, respectively. The prenylated and geranylated chalcones were as active as the prenylated flavones, 6-prenylapigenin and the diprenylated derivative 6,8-diprenyleridictyol. The order of the antitrichomonal activity of the compounds at 24 h was: quercetin (0.121 µg/ml) > quercitrin (0.244 µg/ml) ≥ bartericin B (0.244 µg/ml) > bartericin A (0.73 µg/ml) > stigmasterol (0.98 µg/ml) > 6,8-diprenyleridictyol = isobavachalcone = dorsmanin F (31.25 µg/ ml). D. barteri extracts, quercitrin, and bartericin A, and the prenylated flavonoids had potent antioxidant properties. The twig extract of D. barteri was more potent than the leaf extract. Moderate (EC 50 >50 µg/ ml) and high (EC 50 <50 µg/ml) antioxidant activities were detected in the leaf and twig extracts of D. barteri and the prenylated flavonoids. Prenylated flavonoids and the isolated compounds with antioxidant properties described here may account for the anti-inflammatory action of these extracts. The antitrichomonal and antioxidant activities shown by the extracts and compounds in this study are consistent with the ethnomedicinal and local use of the Dorstenia species studied.
In efforts to find new bioactive beta-lactamase inhibitors, this study investigated 16 Cameroonian plants belonging to 10 families which were evaluated for anti-beta-lactamase activity. The investigation showed that extracts 2, 6, 3 and 5 of the 16 plants investigated presented interesting in vitro beta-lactamase inhibition (over 90%), respectively, of the beta-lactamases TEM-1, OXA-10, IMP-1 and P99. These extracts were from Mammea africana (all beta-lactamases), Garcinia lucida, G. kola (OXA-10, IMP-1 and P99), Bridelia micrantha (OXA-10, P99), Ochna afzelii (OXA-10, P99), Prunus africana (IMP-1) and Adenia lobata (TEM-1). After elimination of tannins (according to the European Pharmacopoeia) the extracts from B. micrantha, G. lucida and M. africana were tested further for their anti-beta-lactamase activity. The extracts from B. micrantha and G. lucida exhibited potent inhibitory activity, respectively, of beta-lactamase OXA-10 (IC(50) = 0.02 mg/mL) and P99 (IC(50) = 0.01 mg/mL). The anti-beta-lactamase activity of M. africana extract was weak. The isolation and the structural elucidation of the active constituents of G. lucida and B. micrantha will provide useful leads in the development of beta-lactamase inhibitors.
A minor novel 1,7-naphthyridine alkaloid with an unprecedented skeleton, named anisopusine (1), was isolated from the CH2Cl2 soluble materials of an acetone extract of the bark of Anisopus mannii (Asclepiadaceae) together with four known compounds 5α-hydroxy-lup-20(29)-en-3β-yl eicosanoate (2), [6]-gingerdione (3), [6]-dehydrogingerdione (4), and ferulic acid (5). Their structures were determined on the basis of spectroscopic data, including 1D and 2D NMR, HR-EI-MS. Compounds (2–5) were characterized for the first time from this genus.
The ever widening level of Plasmodium falciparum resistance to antimalarials has led to the search of alternative therapies. In this context, any resources that can help alleviate the burden of the deadly malaria; including the search for new plant-derived biologically active ingredients are worthy of investigation. Amongst these, naturally occurring and synthetic chalcones have demonstrated promising potencies. In the present study, two diprenylated chalcones Bartericin A 1 and B 2, and four known natural products, stipulin 3, 4-hydroxylonchocarpin 4, isobavachalcone 5 and kanzonol B 6 were isolated from the twigs of Dorstenia barteri var. subtriangularis (Moraceae) by means of chromatographic methods. The structures of the purified compounds were elucidated by spectroscopic methods, mainly 1D and 2D-NMR spectroscopy. These compounds (1-6) were evaluated in culture against the W2 strain of P. falciparum. The evaluated compounds were found to be active in vitro against P. falciparum, 1, 3 and 4 demonstrating particular potencies with relatively low IC 50 values (2.15 µM, 5.13 µM and 3.36 µM respectively). The observed activities confirmed the chalcones as potential leads for the development of antimalarials.
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