Both plants Sebastiania chamaelea from Niger and Chrozophora senegalensis from Senegal used in African traditional medicine in malaria treatment share a same active principle.

ETHNOPHARMACOLOGICAL RELEVANCE: Based on ethnobotanical data obtained from Nigerien and Senegalese traditional healers, two Euphorbiaceae plants, Sebastiania chamaelea and Chrozophora senegalensis, traditionally used to treat malaria, were selected for further investigations. MATERIALS AND METHODS: Plant extracts were prepared with different solvents and tested both in vitro on several strains of Plasmodium falciparum, and in vivo to evaluate their antiplasmodial properties and isolate their active principles. RESULTS: With IC50 values around 6.5µg/ml and no significant cytotoxicity (>50µg/ml), the whole plant aqueous extract from S. chamaelea showed the best in vitro results. In vitro potentiation assays showed strong synergistic activity of S. chamaelea extract with the antiplasmodial drug chloroquine on the chloroquine-resistant P. falciparum strain W2-Indochina. In other respects, the aqueous crude extract of C. senegalensis leaves showed the most significant antiplasmodial activity in vitro (IC50 values less than 2µg/ml). We also demonstrated the prophylactic activity of C. senegalensis in vivo in a murine malaria model. Bioassay-guided fractionation of aqueous extracts of these plants enabled the isolation and identification of ellagic acid (EA, 1) as the main compound responsible for their antiplasmodial activity. Together with EA, other derivatives belonging to different chemical groups were isolated but showed moderate antimalarial activity: gallic acid (2), brevifolin carboxylic acid (3), protocatechuic acid (4), corillagin (5), rutin (6) and 3,4,8,9,10-pentahydroxy-dibenzo(b,d)pyran-6-one (7). The structures were determined by the usual spectroscopic methods and by comparison with published data. Furthermore, we report here the quantification of compound 1 (EA) by RP-HPLC in the dried extracts of these plants, reported for the first time in both these species, and possessing the highest in vitro antiplasmodial activity with IC50 values from 180 to 330nm. CONCLUSIONS: These in vitro and in vivo results support the traditional use in Africa of crude extracts of both S. chamaelea and C. senegalensis as an antimalarial treatment and prove the significant antiplasmodial property of EA.

Evaluation of Senegalese plants used in malaria treatment: focus on Chrozophora senegalensis.

An ethnobotanical study was conducted in the Dakar area of Senegal to investigate the species used in the treatment of malaria. Seven plants are principally used: Cissampelos mucronata, Maytenus senegalensis, Terminalia macroptera, Bidens engleri, Ceratotheca sesamoides, Chrozophora senegalensis and Mitracarpus scaber. From a bibliographic study, it had been shown that the Cissampelos mucronata, Maytenus senegalensis and Terminalia macroptera have already been studied by several authors, and so only Bidens engleri, Ceratotheca sesamoides, Chrozophora senegalensis and Mitracarpus scaber were evaluated in the present study. For each plant, extracts were prepared with different solvents and tested in vitro on two chloroquine-resistant Plasmodium falciparum strains. Crude extracts from the leaves and the stems of Chrozophora senegalensis showed the best in vitro results. The IC(50) value of an aqueous extract of Chrozophora senegalensis was 1.6 microg/ml without cytotoxicity. The in vivo antiplasmodial activity of Chrozophora extracts was determined by both the oral and the intraperitoneal ways. The stages of Plasmodium cycle targeted by Chrozophora were then studied in vitro. These results could justify the traditional use of this plant in malaria treatment.

In vitro and in vivo antiplasmodial activity of Momordica balsamina alone or in a traditional mixture.

BACKGROUND: Because of the dramatic situation of malaria in Africa, there is an urgent need to find new and cheap drugs, such as herbal medicines. Here we report the study of the in vitro and in vivo antimalarial activity of Momordica balsamina alone or in a traditional mixture used in Niger. METHODS: Extracts were obtained with different solvents and tested in vitro on Plasmodium falciparum and in vivo on Plasmodium vinckei. RESULTS: The best extracts are methanolic and present promising results in vivo by intraperitoneal and oral administration. CONCLUSION: The antimalarial activity of M. balsamina, traditionally used in Niger, is confirmed in vitro and in vivo without any toxicity in healthy mice.

Semisynthesis of D-ring modified taxoids: novel thia derivatives of docetaxel.

Two novel 5(20)-thia analogues of docetaxel have been synthesized from 10-deacetylbaccatin III or taxine B and isotaxine B. The key step of these syntheses is the concomitant thietane ring formation and acetylation of the tertiary alcohol at C-4. Both compounds are less cytotoxic than docetaxel but have divergent activity on microtubule disassembly.

Neutral and basic taxoid contents in the needles of Taxus species.

The concentrations of paclitaxel, 10-deacetylbaccatin III (10-DAB III), basic taxoids (= "total alkaloids", TA), taxine B and isotaxine B (= "taxines B", TBS) in the dried needles of 127 trees belonging to 30 Taxus cultivars and species were determined by HPLC. Neutral and basic taxoid contents varied in individual trees within species as well as among varieties and species. The objective of this large analysis was to select the highest-yielding trees for each metabolite.