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Girardot M.,CNRS Laboratory of Communication Molecules and Adaptation of Microorganisms | Deregnaucourt C.,CNRS Laboratory of Communication Molecules and Adaptation of Microorganisms | Deville A.,CNRS Laboratory of Communication Molecules and Adaptation of Microorganisms | Dubost L.,CNRS Laboratory of Communication Molecules and Adaptation of Microorganisms | And 4 more authors.
Phytochemistry | Year: 2012

Four vobasinyl-iboga bisindole and one 2-acyl monomeric indole alkaloids were isolated from the stem bark of Muntafara sessilifolia along with eleven known compounds. Their structures and relative stereochemistry were elucidated on the basis of spectroscopic data including 1D and 2D NMR and mass spectrometry (MS). All isolated compounds were evaluated in vitro for antiplasmodial activity against the chloroquine-resistant strain FcB1 of Plasmodium falciparum, and for cytotoxicity against the human lung cell line MRC-5 and the rat skeletal muscle cell line L-6. 3′-Oxo-tabernaelegantine A exhibited antiplasmodial activity (4.4 μM IC 50) associated with non-significant cytotoxicity (selectivity index of 48). Tabernaelegantine B and D displayed the highest cytotoxicity with IC 50 values of 0.47 and 1.89 μM on MRC-5 cells, and 0.42 and 2.7 μM on L-6 cells, respectively. © 2011 Elsevier Ltd. All rights reserved.


Willcox M.,Research Initiative on Traditional Antimalarial Methods RITAM | Willcox M.,University of Oxford | Benoit-Vical F.,Research Initiative on Traditional Antimalarial Methods RITAM | Benoit-Vical F.,CNRS Coordination Chemistry | And 12 more authors.
Malaria Journal | Year: 2011

Background: Over 1200 plant species are reported in ethnobotanical studies for the treatment of malaria and fevers, so it is important to prioritize plants for further development of anti-malarials. Methods. The RITAM score was designed to combine information from systematic literature searches of published ethnobotanical studies and laboratory pharmacological studies of efficacy and safety, in order to prioritize plants for further research. It was evaluated by correlating it with the results of clinical trials. Results and discussion. The laboratory efficacy score correlated with clinical parasite clearance (r s=0.7). The ethnobotanical component correlated weakly with clinical symptom clearance but not with parasite clearance. The safety component was difficult to validate as all plants entering clinical trials were generally considered safe, so there was no clinical data on toxic plants. Conclusion: The RITAM score (especially the efficacy and safety components) can be used as part of the selection process for prioritising plants for further research as anti-malarial drug candidates. The validation in this study was limited by the very small number of available clinical studies, and the heterogeneity of patients included. © 2011 Willcox et al; licensee BioMed Central Ltd.


Beniddir M.A.,CNRS Natural Product Chemistry Institute | Grellier P.,CNRS Laboratory of Communication Molecules and Adaptation of Microorganisms | Rasoanaivo P.,Institute Malgache Of Recherches Appliquees | Loiseau P.M.,University Paris - Sud | And 4 more authors.
European Journal of Organic Chemistry | Year: 2012

Eight new diarylheptanoid glucosides 1-8 have been isolated from the leaves of Pyrostria major (A. Rich & DC.) Cavaco [syn. Canthium major (A. Rich & DC.)] Cavaco. Their structures were determined by 1D and 2D NMR spectroscopic and HRMS analyses. The absolute configurations of the diarylheptanoids 1-4 were determined to be 3S and 5S by the application of the CD exciton chirality method to the corresponding 3,5-bis(p-bromobenzoyl) (1-3) and 3,5-bis(p-dimethylaminobenzoyl) (4) derivatives. Their antiparasitic activities against Plasmodium falciparum, Leishmania donovani (amastigote forms), and Trypanosoma brucei (trypomastigote bloodstream forms) as well as their cytotoxic activities against the HL-60, KB, and MRC5 cell lines of naturally occurring diarylheptanoid glucosides and their derivatives are reported. A story of serendipity: biologically inactive natural diarylheptanoid glucosides have been isolated from Pyrostria major. Their absolute configurations were determined to be 3S and 5S by the application of the CD exciton chirality method to the corresponding benzoyl derivatives. The study led to the discovery of new compounds possessing selective antiprotozoal activity. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Girardot M.,CNRS Laboratory of Communication Molecules and Adaptation of Microorganisms | Gadea A.,CNRS Laboratory of Communication Molecules and Adaptation of Microorganisms | Deregnaucourt C.,CNRS Laboratory of Communication Molecules and Adaptation of Microorganisms | Deville A.,CNRS Laboratory of Communication Molecules and Adaptation of Microorganisms | And 5 more authors.
European Journal of Organic Chemistry | Year: 2012

Bioassay-guided fractionation of the stem bark of Muntafara sessilifolia has led to the isolation of six new vobasinyl-iboga bisindole alkaloids, tabernaelegantinals A, B and E, and (3'R)-hydroxytabernaelegantines A, C and D, together with six known monomeric indole and two bisindole alkaloids. The structures of these alkaloids were established by NMR and MS analysis. The bisindole alkaloids demonstrated cytotoxicity against the human lung MRC-5 and rat skeletal muscle L-6 cell lines whereas only one monomeric indole alkaloid was found to be cytotoxic. Tabernaemontanine acetate was found to be selectively antiplasmodial against the chloroquine-resistant strain FcB1 of Plasmodium falciparum (5.3 μM IC 50) over mammalian cell lines (selectivity index > 45). The tabernaelegantinals share an unprecedented α-amino aldehyde moiety, the biosynthetic origin of which is discussed. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Maggi F.,University of Camerino | Randriana R.F.,University of Antananarivo | Rasoanaivo P.,University of Antananarivo | Rasoanaivo P.,Institute Malgache Of Recherches Appliquees | And 8 more authors.
Chemistry and Biodiversity | Year: 2013

Vepris macrophylla is an evergreen tree occurring in sub-humid forest of Madagascar and traditionally used in the Island to treat several complaints as well as to prepare aromatic teas and alcoholic drinks. In the present work, the essential oil distilled from the leaves was analyzed for the first time by gas chromatography (GC-FID) and gas chromatography/mass spectrometry (GC/MS). The major compounds were citral (56.3%), i.e., mixture of neral (23.1%) and geranial (33.2%), citronellol (14.5%), and myrcene (8.3%). The essential oil exhibited antimicrobial activity against S. aureus, P. aeruginosa, and C. albicans as determined by vapor-diffusion assay, supporting the traditional use of the plant for preparing steam bath for the treatment of infectious diseases. The essential oil was evaluated for cytotoxic activity on human tumor cell lines by MTT (=3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) assay, showing inhibitory effects comparable to those of cisplatin, notably on MDA-MB 231 (human breast adenocarcinoma) and HCT116 (human colon carcinoma) cell lines. Finally, the essential oil was also subjected to screening for its antioxidant activity and the free radical scavenging capacity. Copyright © 2013 Verlag Helvetica Chimica Acta AG, Zürich.

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