Search

Annona senegalensis Pers. is a plant used in Burkina folkloric medicine for the treatment of epilepsy. The stem-bark, roots and leaves of A. senegalensis are used for an array of human disorders, including epilepsy. Previous studies have demonstrated some genuine effects of A. senegalensis fractions in vivo models of temporal lobe epilepsy. In the present work, we have compared the pharmacological profile of the most promising A. senegalensis fraction obtained up-to-date with anticonvulsant drugs targeting voltage-activated channels namely Carbamazepine (Na+ channels) and Retigabine (KCNQ Channels). In an in vitro model of temporal lobe epilepsy, we could observe a dose-dependent reduction of electrically evoked epileptiform bursts in the CA1 region of the rat hippocampus when applying carbamazepine, retigabine or the F4 fraction of A. senegalensis. The intrinsic excitability of CA1 pyramidal neurons was dose-dependently reduced by A. senegalensis. Since A. senegalensis effects could not anymore be observed when endogenous voltage-dependent sodium channels were blocked and intrinsic excitability restored with a dynamic clamp amplifier, it was concluded that A. senegalensis contains molecules that target voltage-dependent sodium channels. Key words: Hippocampus, epilepsy, Annona senegalensis, Burkina Faso plant extracts, sodium channel, KCNQ channel, M-current, retigabine, carbamazepine.

Six limonoids [kotschyienone A and B (1, 2), 7-deacetylgedunin (3), 7-deacetyl-7-oxogedunin (4), andirobin (5) and methyl angolensate (6)] were investigated for their trypanocidal and leishmanicidal activities using bloodstream forms of Trypanosoma brucei and promastigotes of Leishmania major. Whereas all compounds showed anti-trypanosomal activity, only compounds 1–4 displayed anti-leishmanial activity. The 50% growth inhibition (GI50) values for the trypanocidal and leishmanicidal activity of the compounds ranged between 2.5 and 14.9 μM. Kotschyienone A (1) was found to be the most active compound with a minimal inhibition concentration (MIC) value of 10 μM and GI50 values between 2.5 and 2.9 μM. Only compounds 1 and 3 showed moderate cytotoxicity against HL-60 cells with MIC and GI50 values of 100 μM and 31.5–46.2 μM, respectively. Compound 1 was also found to show activity against intracellular amastigotes of L. major with a GI50 value of 1.5 μM. The results suggest that limonoids have potential as drug candidates for the development of new treatments against trypanosomiasis and leishmaniasis.

Ethnopharmacological relevance Flowers of Inula montana L. (Asteraceae), commonly known as “Arnica de Provence”, are used in the traditional medicine of Provence in France with the same indication as Arnica montana, for the relief of bruises, as an anti-inflammatory agent. Aims of the study The aim of our study is to evaluate its anti-inflammatory properties and to justify its traditional uses. Its potential valorization is evaluated in order to propose Inula montana as an alternative to Arnica montana. Materials and methods Bio-guided fractionation of ethanolic extract allowed the isolation of compounds responsible of the inhibition of NO production. The fractionation was realized using chromatographic techniques and structure elucidation was conducted by ESI-MS and NMR spectral data. Anti-inflammatory effect of ethanolic extract, different fractions and isolated pure compounds was studied in vitro on immortalized mouse macrophages RAW 264.7. An analytical UHPLC-DAD-ESI-MS/MS method was developed for the identification of these compounds in the herbal drug. This UHPLC-DAD method was validated and was used to compare the phenolic profile and content in plant material from the two collection sites: Bonnieux and Merindol. Results Eleven compounds were identified by UHPLC-MS. Chlorogenic acid (1), Luteolin (2), Nepetin (3), 3,5-O-Dicaffeoylquinic acid (4), 1,5-O-Dicaffeoylquinic acid (5), Nepitrin (6), Hispiduloside (7) and Jaceosid (8) were isolated and identified by NMR. Compounds 9, 10 and 11 were confirmed to be 6-Hydroxykaempferol 3,7-dimethyl ether, Hispidulin and Chrysosplenol C, respectively by comparing retention times and MS/MS data with those of the authentic substances. Six compounds: 1 and 4–8 are reported for the first time in Inula montana L. Compounds 2–8 showed promising anti-inflammatory activity with the release of NO with IC50 value Conclusion Flowers extracts and isolated compounds present promising anti-inflammatory activity which provides a scientific basis for the traditional use of Inula montana and may be proposed in the same indications as Arnica montana. The developed and validated simple, accurate and rapid UHPLC method can be used for the quality control of the herbal drug.

International audience; Introduction: Drugs resistant Plasmodium falciparum is a recurring issue that threatens public health. New anti-plasmodial drugs are needed to overcome this problem. The aim of this study was to characterize in vitro an-tiplasmodial activity of Withania frutescens (Solanaceae) against chloroquine-resistant Plasmodium falciparum strain. Methods: The in vitro antiplasmodial activity of leaves and roots extracts from Withania frutescens was performed in 96 well plates and preliminary phytochemical analysis was performed for the active fractions. The toxicity of the plant extract against CHO (Chinese Hamster Ovary) cells was assessed using the tetrazolium salt MTT col-orimetric assay. The selectivity index (SI) was calculated as the ratio between the cytotoxic and antiparasitic activities. Results: The methanol extract of W. frutescens leaves showed a good antiplasmodial activity (CC 50 18.1 μg/ml). Furthermore, ethyl acetate and butanol fractions showed promising in vitro antiplasmodial activity with a se-lectivity index of 3.1 and 2.4, respectively. The roots of W. frutescens were found to be inactive with a CC 50 value > 80 μg/ml. Conclusion: The antiplasmodial activity of W. frutescens may in part be attributed to the presence of polyphenolic and flavonoid compounds. Based on our results, ethyl acetate and butanol leaves fractions could be considered as a promising source for the development of putative antiplasmodial drugs.

Ethnopharmacological relevance Stephania rotunda Lour. (Menispermaceae) is an important traditional medicinal plant that is grown in Southeast Asia. The stems, leaves, and tubers have been used in the Cambodian, Lao, Indian and Vietnamese folk medicine systems for years to treat a wide range of ailments, including asthma, headache, fever, and diarrhoea. Aim of the review: To provide an up-to-date, comprehensive overview and analysis of the ethnobotany, phytochemistry, and pharmacology of Stephania rotunda for its potential benefits in human health, as well as to assess the scientific evidence of traditional use and provide a basis for future research directions. Material and methods Peer-reviewed articles on Stephania rotunda were acquired via an electronic search of the major scientific databases (Pubmed, Google Scholar, and ScienceDirect). Data were collected from scientific journals, theses, and books. Results The traditional uses of Stephania rotunda were recorded in countries throughout Southeast Asia (Cambodia, Vietnam, Laos, and India). Different parts of Stephania rotunda were used in traditional medicine to treat about twenty health disorders. Phytochemical analyses identified forty alkaloids. The roots primarily contain l-tetrahydropalmatine (l-THP), whereas the tubers contain cepharanthine and xylopinine. Furthermore, the chemical composition differs from one region to another and according to the harvest period. The alkaloids exhibited approximately ten different pharmacological activities. The main pharmacological activities of Stephania rotunda alkaloids are antiplasmodial, anticancer, and immunomodulatory effects. Sinomenine, cepharanthine, and l-stepholidine are the most promising components and have been tested in humans. The pharmacokinetic parameters have been studied for seven compounds, including the three most promising compounds. The toxicity has been evaluated for liriodenine, roemerine, cycleanine, l-tetrahydropalmatine, and oxostephanine. Conclusion Stephania rotunda is traditionally used for the treatment of a wide range of ailments. Pharmacological investigations have validated different uses of Stephania rotunda in folk medicine. The present review highlights the three most promising compounds of Stephania rotunda , which could constitute potential leads in various medicinal fields, including malaria and cancer.

International audience; Contact irritant and non-contact repellent activities of β-caryophyllene oxide were evaluated against laboratory strains of female Aedes aegypti (USDA strain), a major arbovirus vector and Anopheles minimus (KU strain), a major malaria parasite vector, compared with the synthetic repellent DEET, using an excito-repellency test system. β-caryophyllene oxide and DEET were tested at concentrations of 0.1, 0.25, 0.5 and 1.0% (v/v). Anopheles minimus was found to be more sensitive to β-caryophyllene oxide than that of Ae. aegypti and exhibited high avoidance response rates (86–96% escape) at 0.5% and 1.0% concentrations in contact and non-contact trials compared with Ae. aegypti (22–59% escape). However, at the same concentrations, DEET displayed lower irritancy and repellency capacities against these two mosquito species (range 0–54% escape) compared to β-caryophyllene oxide. The analysis of escape responses showed significant differences between mosquito species at all concentrations (P

Ethnopharmacological relevance Stephania rotunda Lour. ( Menispermaceae ) is a creeper growing in many countries of Asia and commonly found in the mountainous areas of Cambodia. As a folk medicine, it has been mainly used for the treatment of fever and malaria. The pharmacological activity is mostly due to alkaloids. Thus the aim of this study is to isolate new bioactive alkaloids from Stephania rotunda and to evaluate their in vitro antiplasmodial activity. Materials and methods Alkaloids were isolated and identified from dichloromethane and aqueous extracts using a combination of flash chromatography, high performance liquid chromatography, mass spectrometry and nuclear magnetic resonance. The purified compounds were tested for in vitro antiplasmodial activity on chloroquine-resistant W2 strain of Plasmodium falciparum . Results A new aporphine alkaloid named vireakine ( 2 ) along with two known alkaloids stephanine ( 1 ) and pseudopalmatine ( 8 ), described for the first time in Stephania rotunda , and together five known alkaloids tetrahydropalmatine ( 3 ), xylopinine ( 4 ), roemerine ( 5 ) , cepharanthine ( 6 ) and palmatine ( 7 ) were isolated and identified. The structure of the new alkaloid was established on the basis of 1D and 2D NMR experiments and mass spectrometry. The compounds were evaluated for their in vitro antiplasmodial and cytotoxic activities. All tested compounds showed significant antiplasmodial activities with IC 50 ranged from 1.2 μM to 52.3 μM with a good selectivity index for pseudopalmatine with IC 50 of 2.8 μM against W2 strain of Plasmodium falciparum and IC 50 >25 μM on K562S cells. Conclusions This study provides evidence to support the use of Stephania rotunda for the treatment of malaria and/or fever by the healers. Alkaloids of the tuber exhibited antiplasmodial activity and particularly cepharanthine and pseudopalmatine.

Ethnopharmacological relevance Bark extracts of Nauclea latifolia, Nauclea diderrichii, Nauclea pobeguinii and Nauclea vandergutchii are used in traditional medicine in West and South Africa for the treatment of fevers, diarrhea and malaria. Aim of the study To estimate the possible long-term toxicity and genotoxicity of plant extracts (dichloromethane, methanol, water/methanol, water) and saponins. Materials and methods The clastogenicity of plant extracts and saponins was assessed by the micronucleus assay performed on Chinese Hamster Ovary cells. The DNA-damaging activity of saponin mixture was assessed by the comet assay on Chinese Hamster ovary cells. Results Hydromethanolic extracts from Nauclea latifolia, Nauclea diderrichii and Nauclea pobeguinii exhibited a significant clastogenic/aneugenic activity without S9 mix. The hydromethanolic extract from Nauclea diderrichii was the most clastogenic/aneugenic fraction with a Minimal Active Concentration (MAC) of 23.1 μg mL−1. It was submitted to a separation step leading to six main saponins identified as quinovic acid glycosides (saponins A, D, E, G, J, K). None of the isolated saponins exerted a significant clastogenic/aneugenic activity by the micronucleus assay, however a mixture made with equal quantities of each of the six saponins exhibited a direct genotoxic/clastogenic activity as assessed by both the micronucleus assay and the comet assay on Chinese Hamster Ovary cells. Conclusion Saponins present in the hydromethanolic extracts of Nauclea induced synergistic in vitro DNA-damage and chromosome mutations in mammalian cells. This genotoxic activity was probably due to the capacity of Nauclea saponins to reduce cell defense against oxidative stress through the inhibition of glutathione-S-transferase activity.

Together with apigenine dimethylether and piperchabamide A, a new amide alkaloid, Kaousine and the Z form of antiepilepsirine were isolated from the aerial part of Piper capense L.f (Piperaceae). Their structures were elucidated by spectrometric methods and their in vitro antiparasitic activities were evaluated on Plasmodium falciparum.

Gentiopicroside (1) is the major secoiridoid glucoside constituent of Cephalaria kotschyi roots. The mutagenicity, DNA-damaging capacities, and clastogenicity of this molecule were evaluated by the Salmonella typhimurium mutagenicity assay (Ames test) on tester strains TA97a, TA98, TA100, and TA102, the alkaline comet assay, and the micronucleus assay on CHO cells. All tests were performed with and without the metabolization mixture, S9 mix. In the Ames test, the mutagenicity of 1 was limited to TA102 without S9 mix (2.3 rev microg(-1)). The genotoxicity was more evident without S9 mix (0.78 OTMchi(2) units microg(-1) mL) than with the metabolic mixture (0.16 OTMchi(2) units microg(-1) mL) with the comet assay. Similarly, the clastogenicity without S9 mix was 0.99 MNC microg(-1) mL and 0.38 MNC microg(-1) mL with S9 mix in the micronucleus assay. The interaction of 1 with DNA is probably through the involvement of oxidative DNA lesions.

The aim of this study was to investigate the ability of α-hederin to improve the efficacy of widely prescribed 5-fluorouracil (5-FU) in a human colon adenocarcinoma model. Drug combinations of α-hederin and 5-FU using both fixed-concentration and combination index methods were performed in vitro in HT-29 cells. The results showed that α-hederin at sub-IC50 cytotoxic concentrations enhanced 5-FU cytotoxicity about 3.3-fold (p < 0.001). Simultaneous combination of α-hederin and 5-FU at their IC50 ratio showed either a synergistic effect at a moderate cytotoxic range (25% of cell growth inhibition) or an antagonistic effect at a high level of growth inhibition. The data indicate therefore that it is possible to optimize colorectal cancer cell sensitivity to 5-FU with α-hederin. Copyright © 2008 John Wiley & Sons, Ltd.

International audience; DIG, a liquid herbal preparation made from a mixture of diluted mother tinctures of Berberis vulgaris, Taraxacum officinale and Arctium lappa, was assessed for its antimutagenic properties against mitomycin C. The micronucleus assay on Chinese hamster ovary (CHO)-K1 cells was used to evaluate the in vitro anticlastogenic activity of DIG compared to those of separately diluted mother tinctures. The micronucleus assay was performed on mouse erythrocytes and the comet assay was performed on mouse liver, kidney, lung, brain and testicles to assess the protective effects of DIG (0.2 and 2 % at libitum) against an intraperitoneal injection of mitomycin C (1 mg Kg(-1)) in mice. DIG exerted a powerful anticlastogenic activity, under both pretreatment and simultaneous treatment conditions as assessed by the micronucleus assay in CHO-K1 cells. Its protective activity was greater than that observed for each mother tincture. DIG reduced micronuclei levels in mouse erythrocytes and suppressed \textgreater 80 % of DNA strand breaks in the liver, kidney, lung, brain and testicles of mice exposed to mitomycin C.

Diphyllin isolated from Haplophyllum bucharicum Litv. (Rutaceae), an endemic plant of Uzbekistan, displayed a moderate antiproliferative activity towards human monocytes (IC50 = 35.2 microM) and Leishmania promastigotes (IC50 = 14.4 microM), by a mechanism of action that involved interaction with macromolecules and resulted in cell cycle arrest in the S-phase and inhibition of protein synthesis. In the intracellular amastigote form of the parasite, diphyllin exerted a strong specific inhibitory activity (IC50 = 0.2 microM) resulting from the inhibition of parasite internalization within macrophages. This property was mainly due to modulation of macrophage phagocytosis and, to a lesser extent, it also involved interference with surface molecules of the promastigote membrane.

In Burkina Faso, most people in particular, in rural areas, use traditional medicine and medicinal plants to treat usual diseases. In the course of new antimalarial compounds, an ethnobotanical survey has been conducted in different regions. Seven plants, often cited by traditional practitioners and not chemically investigated, have been selected for an antiplasmodial screening: Pavetta crassipes (K. Schum), Acanthospermum hispidum (DC), Terminalia macroptera (Guill. et Perr), Cassia siamea (Lam), Ficus sycomorus (L), Fadogia agrestis (Schweinf. Ex Hiern) and Crossopteryx febrifuga (AFZ. Ex G. Don) Benth. Basic, chloroform, methanol, water-methanol and aqueous crude extracts have been prepared and tested on Plasmodium falciparum chloroquine-resistant W2 strain. A significant activity has been observed with alkaloid extract of P. crassipes (IC(50)

Background New classes of anti-malarial drugs are needed to control the alarming Plasmodium falciparum resistance toward current anti-malarial therapy. The ethnopharmacological approach allows the discovery of original chemical structures from the vegetable biodiversity. Previous studies led to the selection of a bisbenzylisoquinoline, called cepharanthine and isolated from a Cambodian plant: Stephania rotunda. Cepharanthine could exert a mechanism of action different from commonly used drugs. Potential plasmodial targets are reported here. Methods To study the mechanism of action of cepharanthine, a combined approach using phenotypic and transcriptomic techniques was undertaken. Results Cepharanthine blocked P. falciparum development in ring stage. On a culture of synchronized ring stage, the comparisons of expression profiles showed that the samples treated with 5 μM of cepharanthine (IC90) were significantly closer to the initial controls than to the final ones. After a two-way ANOVA (p-value

Background: Stephania rotunda is used by traditional health practitioners in Southeast Asia to treat a wide range of diseases and particularly symptoms related to malaria. Cepharanthine (CEP) is an alkaloid isolated from this plant with potential innovative antiplasmodial activity. The analysis of interactions between antiplasmodial drugs is necessary to develop new drugs combinations to prevent de novo emergence of resistance. The objective of this study was to evaluate the anti-malarial activity of CEP in combination with usual anti-malarial compounds, both in vitro and in vivo. Methods: A fixed ratio method using the isotopic micro test was performed on the chloroquine-resistant plasmodial strain W2 to build isobolograms from eight CEP-based combinations with standard anti-malarial drugs. The efficacy of two combinations was then evaluated in the BALB/c mouse infected with Plasmodium berghei ANKA strain. Results: In vitro, efficiency gains were observed when CEP was combined with chloroquine (CQ), lumefantrine (LUM), atovaquone (ATO), piperaquine (PPQ) and particularly monodesethylamodiaquine (MdAQ), whereas an antagonistic interaction was observed with dihydroartemisinin (DHA) and mefloquine (MQ). In vivo ,t he combination of CEP with CQ or amodiaquine (AQ) improved significantly the survival of mice and extended the delay for parasitic recrudescence. Conclusion: All these observations suggest that CEP could be an interesting lead compound in the development of a combination therapy against malaria.

Crude extracts of Spanish plants (60 representing 12 species from 7 families) have been screened for antiparasitic activity against Leishmania infantum and Trichomonas vaginalis. 30% of the extracts showed activity against one of the parasites and 15% of the extracts were active against both tests organisms. The most promising extracts originate from plants used in traditional medicine, such as Inula montana L. (Asteraceae), Bupleurum rigidum L. (Apiaceae) and Scrophularia scorodonia L. (Scrophulariaceae).

International audience; The synthesis of beta-carbolines and their in vitro antiplasmodial and antileishmanial activities were described herein. These molecules have also been studied concerning their in vitro cytotoxicity toward the human cell line THP1, in order to calculate their respective selectivity indexes (SI). Among the 20 tested molecules, four exhibited significant antiplasmodial activity on the W2 multi-resistant Plasmodium falciparum strain (0.7 \textless IC50 \textless 1.7 mu M), in comparison with two references drugs (chloroquine and doxycycline), and a low cytotoxicity. These beta-carbolines were also evaluated concerning their in vitro antileshmanial activity on Leishmania donovani promastigotes, permitting to identify an antileshmanial hit compound, displaying quite promising activity (IC50 = 6.1 mu M) in comparison with amphotericin B and pentamidine chosen as reference drugs. Finally, structure-activity relationships were discussed, pointing out that molecules presenting a para-substituted phenyl moiety at position 1 of the beta-carboline ring displayed the best biological profile. (C) 2012 Elsevier Masson SAS. All rights reserved.

International audience; Aim of the study Antiplasmodial activity, inhibition of nitric oxide (NO) overproduction, and anti-proliferative activity were investigated in vitro to evaluate the bioactive potential of the traditional pharmacopoeia of the Mascarene Archipelago, which is known for its biodiversity and for the richness of its endemic flora. Materials and methods A total of 45 methanol (MeOH) and dichloromethane (DCM) extracts were prepared from 19 plant species collected on Réunion and Mauritius Islands. Ninety-six-well microplate assays were performed on chloroquine sensitive Plasmodium falciparum 3D7 strain, on LPS-stimulated Raw 264.7 murine macrophages and on A-549, DLD-1 and WS1 human cells. Activity was evaluated through spectrophotometric methods. Results Activity was attributed to plant extracts expressing IC50 \textless 50 μg/ml for antiplasmodial response, IC50 \textless 100 μg/ml for cytotoxicity, and IC50 \textless 130 μg/ml for anti-inflammatory reaction. The majority of the extracts tested (69%) exhibited potency in at least one of these three types of activity. This is the first report describing promising antiplasmodial activity (IC50 \textless 15 μg/ml) for Psiadia dentata DCM extract and Terminalia bentzoe MeOH bark extract. NO inhibition assay revealed seven interesting plants, described for the first time as anti-inflammatory: Aphloia theiformis, Buddleja salviifolia, Eupatorium riparium, Hiptage benghalensis, Psiadia arguta, Psiadia dentata, and Scutia commersonii. Finally, anti-proliferative activity was observed for two endemic species, Geniostoma borbonicum and Nuxia verticillata. Conclusion Using the criterion of endemism as part of the criteria for traditional medicinal use raises the chances of finding original active principles. In our case, 86% of the endemic plants tested displayed pharmacological interest.

A new iridoid diglycoside, scorodioside, has been isolated from Scrophularia scorodonia. The structure of this compound was elucidated by chemical and spectral analysis as 6-O-(3″-O- acetyl-2″ -O-trans- cinnamoyl )-α- l -rhamnopyranosylcatalpol . In addition, 8-O-cis-cinnamoylharpagide has been isolated.

An ethnobotanical study was conducted in Comores (Ngazidja) about plant species used traditionally for the treatment of various diseases, including malaria. Antimalarial activity of 76 vegetal extracts obtained from 17 species traditionally used to treat malaria symptoms, was evaluated in vitro using Plasmodium falciparum chloroquine-resistant strain (W2). Antiproliferative activity was evaluated on human monocytic THP1 cells and the selectivity index of the plant extracts was calculated. The results showed that 10 plant extracts had a moderate activity (5IC(50)or =10 microg/ml), and 6 a good in vitro activity with IC(50) valueor =5 microg/ml. The highest antiplasmodial activity was found for the MeOH/H(2)O leaves extract of Flueggea virosa (Roxb. Ex Willd.) Voigt subsp. virosa (Euphorbiaceae) (IC(50)=2 microg/ml), for roots decoction of Flueggea virosa (IC(50)=3 microg/ml) and for chloromethylenic roots extract of Vernonia colorata (Willd.) Drake subsp. grandis (DC.) C. Jeffrey (Asteraceae) (IC(50)=3 microg/ml). Three other extracts showed moderate antiplasmodial activity (IC(50)5 microg/ml): Vernonia colorata (aerial part), Piper capense L.f. (Piperaceae), and Leptadenia madagascariensis Decne (Asclepiadaceae) chloromethylenic extracts (IC(50)=6 microg/ml; 7 microg/ml and 9 microg/ml, respectively). All the plants tested displayed a low cytotoxicity on THP1 cells.

A reversed-phase high performance liquid chromatographic method has been developed for the determination of the main compounds (harpagoside, scorodioside, and verbascoside) from different samples of Scrophularia scorodonia. The chromatographic method has been validated and applied for quantitative determination of harpagoside. The results show the highest levels of harpagoside in the leaf extract. The purity and identity of peaks were controlled by diode-array detection and comparison with standards.

Seventy-seven crude extracts from leaves and stem barks of 15 Gabonese plants used in traditional medicine were evaluated for their cytotoxic, antileishmanial and antifungal activities. Most of the extracts exhibited cytotoxic activities toward human monocytes, and most particularly the hydromethanolic 50% (v/v) fraction of Ganophyllum giganteum leaves (IC(50)=1.3 microg/ml) as well as the methanolic extracts of Polyalthia suaveolens, Dioscorea preussii, Augouardia letestui leaves and Cola lizae stem barks (IC(50)5 microg/ml). The methanolic extract of Polyalthia suaveolens displayed a strong antiproliferative activity against the promastigote form of Leishmania infantum parasites and presented a good antifungal activity on all the tested strains (IC(50)1mg/ml). This extract was divided into six fractions: fraction F6 demonstrated a cytotoxic activity stronger than those of the crude extract (IC(50)=0.6 microg/ml), fractions F4 and F5 were devoid of cytotoxicity (IC(50)100 microg/ml) and displayed interesting antileishmanial activity against the intracellular amastigote form of the parasite (IC(50)=5.6 and 12.4 microg/ml), respectively. However, the antifungal activity observed for the crude extract could not be recovered in the corresponding fractions.

A new iridoid diglycoside, scorodioside, has been isolated from Scrophularia scorodonia. The structure of this compound was elucidated by chemical and spectral analysis as 6-O-(3″-O- acetyl-2″ -O-trans- cinnamoyl )-α- l -rhamnopyranosylcatalpol . In addition, 8-O-cis-cinnamoylharpagide has been isolated.

The plant genus Stephania Loureiro (1790: 608–609) (Menispermaceae) comprises about 60 species distributed in tropical and subtropical Asia, tropical Africa, and Oceania (Lo et al. 2008). Species of this genus are commonly used in folk medicine for the treatment of asthma, tuberculosis, dysentery, hyperglycemia, cancer, fever, and malaria (Semwal et al. 2010). Currently, active pharmacological research is being conducted on S. rotunda Loureiro (1790: 608), and particularly on its tubers. This species shows in addition to antioxidant and cytotoxic activities, a significant antiplasmodial activity (Bun et al. 2009, Baghdikian et al. 2013).

Two new triterpenoid saponins, glinosides A and B, isolated from the aerial parts of Glinus oppositifolius, have been characterized by 1D, 2D, NMR and high-resolution mass spectral (HRMS) techniques. Their structures were established respectively as 16-O-(beta-arabinopyranosyl)-3-oxo-12,16 beta,21 beta,22-tetrahydroxyhopane for glinoside A and 16-O-(beta-arabinopyranosyl)-3-oxo-12,16 beta,22-trihydroxyhopane for glinoside B. Results presented evidence that fractions had a better antiplasmodial activity (IC50 = 31.80 micrograms/ml) than pure glinoside A (IC50 = 42.30 micrograms/ml).

The study of the metabolism of iridoid glycosides from Harpagophytum procumbens and Harpagophytum zeyheri by human intestinal bacteria, was realized in order to elucidate compounds responsible for the pharmacological activities of Harpagophytum. Harpagide, harpagoside and 8-O-p-coumaroyl-harpagide were transformed into the pyridine monoterpene alkaloid aucubinine B by human fecal flora and by bacteria isolated from this flora. Aucubinine B was also prepared from harpagide, harpagoside and 8-O-p-coumaroylharpagide, by beta-glucosidase in the presence of NH4+.

The iridoids of Harpagophytum procumbens and Harpagophytum zeyheri were studied by CLHP. Harpagoside is the main iridoid for both drugs whereas 8-p-coumaroylharpagide is a representative iridoid of Harpagophytum zeyheri only. The ratio harpagoside/8-p-coumaroylharpagide can be used to distinguish chemically both species. For commercial dried aqueous extracts this ratio is intermediate because they are probably prepared from a mixture of H. procumbens and H. zeyheri drugs. The aqueous extracts of both drugs show similar analgesic and anti-inflammatory properties. Harpagophytum procumbens and Harpagophytum zeyheri should be accepted as sources for the drug Harpagophyti radix.

In most developing tropical countries, 80 per cent of the population use traditional medicine, in particular against parasitic diseases. Among these infections, malaria is very widespread. In most tropical countries, 500 million people are attacked annually by this disease, resulting in 1 million deaths in the world. In Africa the ethnobotanical studies show that in addition to the well known quinquina, different plants from the Rubiaceae family are used such as Gardenia ternifolia, Morinda lucida, Pavetta crassipes, Nauclea latifolia and Nauclea diderrichii. In the search to find new antimalarial compounds, we have studied Nauclea diderrichii (de Wild) Merr.

Two sesquiterpene alcohols, [11 R]-eudesm-4(14)-en-5s,11,12-triol ( 1 ) and [11R]-eudesm-4(14)-en-5a,11-12-triol ( 2 ), from Jasonia glutinosa aerial parts (Asteraceae), have been tested using an in vitro technique against Leishmania donovani (promastigote forms) and Plasmodium falciparum . Sesquiterpene 1 was not effective at the assayed concentrations. Sesquiterpene 2 was found to be active against Leishmania donovani and Plasmodium falciparum .