Antiprotozoal activities of Millettia richardiana (Fabaceae) from Madagascar.

With at least 60% of the Millettia species (Fabaceae) being in medicinal use, we found it relevant to assess the potential antiprotozoal and antifungal activities of Millettia richardiana. Water and methanol crude extracts of the stem barks from M. richardiana and the six fractions resulting from the fractionation of the methanol extract were tested. The dichloromethane extracted fraction showed the best in vitro antiprotozoal activities (IC50=5.8 µg/mL against Plasmodium falciparum, 11.8 µg/mL against Leishmania donovani and 12.8 µg/mL against Trypanosoma brucei brucei) as well as low cytotoxicity on several cell lines. The phytochemical analysis showed this selected fraction to be rich in terpenoids and alkaloids, which could explain its antiparasitic activity. A phytochemical study revealed the presence of lonchocarpenin, betulinic acid, ß-amyrin, lupeol, palmitic acid, linoleic acid and stearic acid, among which betulinic acid and lupeol could be the compounds responsible of these antiprotozoal activities. By contrast, neither the crude extracts nor the fractions showed antifungal activity against Candida. These results confirm the importance of the genus Millettia in Malagasy ethnomedicine, its potential use in antiparasitic therapy, and the interest of developing a sustainable exploitation of this plant. Moreover, both molecules betulinic acid and lupeol appeared as very relevant molecules for their antiprotozoal properties.

Antiplasmodial activity and cytotoxicity of plants used in West African traditional medicine for the treatment of malaria.

Eighteen plants originating from Ivory Coast were selected by ethnobotanical survey as plants commonly used by traditional healers for the treatment of malaria. Extracts of these plants were tested on two strains of Plasmodium falciparum: FcM29-Cameroon (chloroquine-resistant strain) and a Nigerian chloroquine-sensitive strain. The powdered plants were used to prepare three kinds of extracts: by decoction in water, in ethanol (95%) and in pentane. A radioactive micromethod allowed the evaluation of the antiplasmodial in vitro activity of the extracts on P. falciparum. Concentrations inhibiting 50% of the parasite growth (IC50) ranged from 18 microg/ml to more than 500 microg/ml for aqueous and ethanol extracts and from 4.3 microg/ml to more than 500 microg/ml for pentane extracts. Cytotoxicity was estimated on A375 melanoma cells and a cytotoxicity/antiplasmodial index (CAR) was calculated for each extract, ranging from 1 to 10. The pentane extracts of Cola caricaefolia and Uvaria afzelii, which revealed the strongest antiplasmodial activity had CAR values of about 10.

Pyranocoumarin and triterpene from Millettia richardiana.

From the stem bark of a Madagascan endemic plant, Millettia richardiana Baill., lonchocarpenin and betulinic acid were isolated and their structures established by spectroscopic methods. The analysis of dichloromethane fractions suggested the presence of beta-amyrin, lupeol, palmitic acid, linoleic acid and stearic acid. Except for beta-amyrin and lupeol, these compounds are described for the first time for the Millettia genus.

Cogniauxia podolaena: bioassay-guided fractionation of defoliated stems, isolation of active compounds, antiplasmodial activity and cytotoxicity.

COGNIAUXIA PODOLAENA Baill. (Cucurbitaceae) is traditionally used in Congo Brazzaville for the treatment of malaria. We assessed the antiplasmodial activity of the plant and isolated some of the compounds responsible for this activity. It was the first time that a chemical study of this plant has been undertaken. Three triterpenes were isolated: cucurbitacin B ( 1), cucurbitacin D ( 2) and 20-epibryonolic acid ( 3) and their structures were assigned from spectroscopic evidence and comparison with published data. The crystallographic structure of 3 was determined. All fractions and compounds obtained in this study were assayed for antiplasmodial activity (on FcM29, a chloroquine-resistant strain of P. FALCIPARUM) and cytotoxicity (on KB and Vero cell lines). The IC50 values of 1, 2 and 3 are 1.6, 4 and 2 microg/mL on FcM29. Both 1 and 2 have a high cytotoxicity whereas 3 shows a better selectivity index.