Antiprotozoal screening and cytotoxicity of extracts and fractions from the leaves, stem bark and root bark of Alstonia congensis.

ETHNOPHARMACOLOGICAL RELEVANCE: To evaluate the antiprotozoal activity and cytotoxicity of extracts and fractions from the leaves, root bark and stem bark of Alstonia congensis (Apocynaceae), used in traditional medicine against parasitic diseases. MATERIALS AND METHODS: The aqueous and 80% MeOH extracts, and a series of fractions and subfractions from the leaves, stem and root bark of Alstonia congensis were tested in vitro for their antiprotozoal activity against Trypanosoma brucei brucei, Trypanosoma cruzi, Lesihamania infantum and the chloroquine and pyrimethamine-resistant K1 strain of Plasmodium falciparum. Their cytotoxicity on MRC-5 cells (human lung fibroblasts) was evaluated as well. RESULTS: The aqueous and 80% MeOH extracts and a series of subfractions of each plant part exhibited pronounced antiprotozoal activity against the K1 strain of Plasmodium falciparum with IC50 values ranging from 2 to 5 µg/ml, and good activity against Trypanosoma brucei brucei and Trypanosoma cruzi with IC50 values ranging between 5 and 10 µg/ml. The residual 80% MeOH extract from the leaves, and the total alkaloid extract from stem and root bark were the only subfractions active against Leishmania infantum with IC50 values <10 µg/ml. None of the samples from the root bark was cytotoxic against MRC-cell lines (CC50>64 µg/ml). In general, the aqueous extract (traditional decoction) showed the highest selectivity, especially against Plasmodium falciparum. CONCLUSION: These results can partly support and justify the traditional use of these plant parts of Alstonina congensis as raw materials for the preparation of traditional remedies to treat parasitic diseases such as malaria and trypanosomiasis.

In vitro and in vivo antimalarial activity and cytotoxicity of extracts and fractions from the leaves, root-bark and stem-bark of Triclisia gilletii.

ETHNOPHARMACOLOGICAL RELEVANCE: To evaluate the in vitro antiplasmodial activity and cytotoxicity, and the in vivo activity of extracts and fractions from the leaves, root-bark and stem-bark of Triclisia gilletii (De Wild) Staner (Menispermaceae), used in traditional medicine against malaria. MATERIALS AND METHODS: The aqueous and 80% MeOH extracts, and a series of fractions and subfractions from the leaves, stem and root-bark of Triclisia gilletii were tested in vitro for their antiplasmodial activity against a Congolese-sensitive strain of Plasmodium falciparum, against the chloroquine and pyrimethamine-resistant K1 strain of Plasmodium falciparum, for cytotoxicity against MRC-5 cells, and in vivo in mice infected with Plasmodium berghei berghei. RESULTS: Many samples from the three plant parts exhibited pronounced activity against the Congolese chloroquine-sensitive strain of Plasmodium falciparum with some IC50 values <0.02 µg/ml, and against the K1 strain, with some IC50 <0.25; the selectivity was higher against the Congolese strain. At oral doses of 200 and 400mg/kg body weight in infected mice, the aqueous, 80% methanol and total alkaloid extracts from the three plant parts produced more than 65% and 75% chemosuppression, respectively. The antiplasmodial activity of these three plant parts of Triclisia gilletii can at least in part be attributed to bisbenzylisoquinoline alkaloids, and supports its use for the treatment of uncomplicated malaria in traditional medicine.

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

ETHNOPHARMACOLOGICAL RELEVANCE: The antiprotozoal and cytotoxic activity of the aqueous extracts from 33 medicinal plants, used by traditional healers for the treatment of various parasitic diseases and collected after an ethnopharmacological inventory conducted in the Bolongo area, Bandundu province in DR Congo, was evaluated. MATERIALS AND METHODS: Decoctions were prepared, lyophilized and evaluated for in vitro antiprotozoal activity against Trypanosoma b. brucei, Trypanosoma cruzi, Leishmania infantum, and the chloroquine- and pyrimethamine-resistant K1 strain of Plasmodium falciparum. Cytotoxicity against MRC-5 cells was included to assess selectivity of activity. RESULTS: Most of the tested extracts exhibited pronounced (IC(50)≤5µg/ml) or good (5

The spasmolytic activity of extracts and some isolated compounds from the leaves of Morinda morindoides (Baker) Milne-Redh. (Rubiaceae).

AIM: The study was aimed to evaluate the in vitro antispasmodic activity of Morinda morindoides leaves aqueous extract, its soluble fractions and isolated compounds to provide the pharmacological basis for its use for the treatment of constipation and diarrhoea in traditional medicine. METHODS: The antispasmodic activity of each sample was evaluated on acetylcholine (ACh) and the depolarized KCl solution induced contractions on guinea-pig isolated ileum suspended in Tyrode's solution. RESULTS: At a test concentration of 40mug/ml in organ bath, the aqueous extract and its petroleum ether soluble fraction showed a spasmogenic effect on both agonists. The diethylether, ethyl acetate, n-butanol and residual aqueous phase soluble fractions from the partition of the aqueous extract exhibited spasmolytic activity producing 47-100% inhibition of contractions induced by both agonists with IC(50) values ranged from 6 to 15 microg/ml according to the case. In addition, the n-butanol and residual aqueous phase soluble fractions showed an inhibitory effect of 75 and 66% respectively on low high [K(+)] (25 mM) and 65 and 60% respectively on high [K+] (80 mM). Crude flavonoids showed spasmolytic on both agonists while crude saponins only showed spasmolytic activity on ACh and displayed spasmogenic effect on KCl. Quercetin, quercitrin and rutin exhibited significant antispasmodic effect with IC(50) values <0.1 microg/ml. Epoxygaertneroside and gaertneroside showed good antispasmodic activity on both agonists (4