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See detailChemical composition, cytotoxicity and in vitro antitrypanosomal and antiplasmodial activity of the essential oils of four Cymbopogon species from Benin.
Kpoviessi, Salome; Bero, Joanne; Agbani, Pierre et al

in Journal of ethnopharmacology (2014), 151

ETHNOPHARMACOLOGICAL RELEVANCE: Cymbopogon species are largely used in folk medicine for the treatment of many diseases some of which related to parasitical diseases as fevers and headaches. As part of ... [more ▼]

ETHNOPHARMACOLOGICAL RELEVANCE: Cymbopogon species are largely used in folk medicine for the treatment of many diseases some of which related to parasitical diseases as fevers and headaches. As part of our research on antiparasitic essential oils from Beninese plants, we decided to evaluate the in vitro antiplasmodial and antitrypanosomal activities of essential oils of four Cymbopogon species used in traditional medicine as well as their cytotoxicity. MATERIALS AND METHODS: The essential oils of four Cymbopogon species Cymbopogon citratus (I), Cymbopogon giganteus (II), Cymbopogon nardus (III) and Cymbopogon schoenantus (IV) from Benin obtained by hydrodistillation were analysed by GC/MS and GC/FID and were tested in vitro against Trypanosoma brucei brucei and Plasmodium falciparum respectively for antitrypanosomal and antiplasmodial activities. Cytotoxicity was evaluated in vitro against Chinese Hamster Ovary (CHO) cells and the human non cancer fibroblast cell line (WI38) through MTT assay to evaluate the selectivity. RESULTS: All tested oils showed a strong antitrypanosomal activity with a good selectivity. Sample II was the most active against Trypanosoma brucei brucei and could be considered as a good candidate. It was less active against Plasmodium falciparum. Samples II, III and IV had low or no cytotoxicity, but the essential oil of Cymbopogon citraus (I), was toxic against CHO cells and moderately toxic against WI38 cells and needs further toxicological studies. Sample I (29 compounds) was characterised by the presence as main constituents of geranial, neral, beta-pinene and cis-geraniol; sample II (53 compounds) by the presence of trans-p-mentha-1(7),8-dien-2-ol, trans-carveol, trans-p-mentha-2,8-dienol, cis-p-mentha-2,8-dienol, cis-p-mentha-1(7),8-dien-2-ol, limonene, cis-carveol and cis-carvone; sample III (28 compounds) by beta-citronellal, nerol, beta-citronellol, elemol and limonene and sample IV (41 compounds) by piperitone, (+)-2-carene, limonene, elemol and beta-eudesmol. CONCLUSIONS: Our study shows that essential oils of Cymbopogon genus can be a good source of antitrypanosomal agents. This is the first report on the activity of these essential oils against Trypanosoma brucei brucei, Plasmodium falciparum and analysis of their cytotoxicity. [less ▲]

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See detailTraditional plant-based remedies to control gastrointestinal disorders in livestock in the regions of Kamina and Kaniama (Katanga province, Democratic Republic of Congo)
Okombe Embeya, Victor; Lumbu Simbi, Jean-Baptiste; Stévigny, Caroline et al

in Journal of Ethnopharmacology (2014), 153(3), 686-693

Ethnopharmacological relevance: gastrointestinal parasitic diseases present one of the main constraints hindering the productivity of the livestock sector (goat and cattle). Due to the limited ... [more ▼]

Ethnopharmacological relevance: gastrointestinal parasitic diseases present one of the main constraints hindering the productivity of the livestock sector (goat and cattle). Due to the limited availability and affordability of deworming drugs, traditional herbal remedies are still frequently used. The study aims at collecting traditional knowledge on local plants and remedies used to treat gastrointestinal parasitoses in livestock in two adjacent territories (Haut-Lomami district). Material and methods: A field survey was carried out in a part of the Haut-Lomami district (province of Katanga). A semi-structured questionnaire was used to interview 44 people including farmers, traditional healers and livestock specialists (veterinarians and agronomist), identified as using or practicing traditional medicine. To prepare botanically identified herbarium specimens, cited plants were collected with the participation of interviewed people. Results: Although interviewed people cannot precisely identify the etiology of gastrointestinal disorders/parasitoses in domestic animals, they treat the condition with herbals collected in their near environment. Nineteen different traditional remedies were collected and described; 9 plant species were identified as commonly used to treat gastrointestinal parasitic infections. From these, Vitex thomasii De Wild (Verbenaceae) appears as the plant most often used. Conclusion: this survey contributed to the establishment of an inventory of plants used in livestock parasitic treatment in this region of the Democratic Republic of Congo. Future studies are needed to confirm the efficacy and safety of these traditional remedies. [less ▲]

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See detailIn vivo antimalarial activity of Keetia leucantha twigs extracts and in vitro antiplasmodial effect of their constituents.
Bero, Joanne; Herent, Marie-France; Schmeda-Hirschmann, Guillermo et al

in Journal of Ethnopharmacology (2013), 149(1), 176-83

ETHNOPHARMACOLOGICAL RELEVANCE: The West African tree Keetia leucantha (Rubiaceae) is used in traditional medicine in Benin to treat malaria. The twigs dichloromethane extract was previously shown to ... [more ▼]

ETHNOPHARMACOLOGICAL RELEVANCE: The West African tree Keetia leucantha (Rubiaceae) is used in traditional medicine in Benin to treat malaria. The twigs dichloromethane extract was previously shown to inhibit in vitro Plasmodium falciparum growth with no cytotoxicity (>100microg/ml on human normal fibroblasts). MATERIALS AND METHODS: The dichloromethane and aqueous extracts of twigs of K. leucantha were evaluated in vivo against Plasmodium berghei NK 173 by the 4-day suppressive test and in vitro against a chloroquine-sensitive strain of Plasmodium falciparum (3D7) using the measurement of the plasmodial lactate dehydrogenase activity. Bioguided fractionations were realized and compounds were structurally elucidated using extensive spectroscopic analysis. RESULTS: The in vivo antimalarial activity of K. leucantha dichloromethane and aqueous twigs extracts were assessed in mice at the dose of 200mg/kg/day. Both extracts exhibited significant effect in inhibiting parasite growth by 56.8% and 53.0% (p<0.0001) on day 7-postinfection. An LC-MS analysis and bioguided fractionations on the twigs dichloromethane extract led to the isolation and structural determination of scopoletin (1), stigmasterol (2), three phenolic compounds: vanillin (3), hydroxybenzaldehyde (4) and ferulaldehyde (5), eight triterpenic esters (6-13), oleanolic acid and ursolic acid. The antiplasmodial activity of the mixture of the eight triterpenic esters showed an antiplasmodial activity of 1.66+/-0.54microg/ml on the 3D7 strain, and the same range of activity was observed for isolated isomers mixtures. CONCLUSIONS: This is the first report on the in vivo activity of K. leucantha extracts, the isolation of thirteen compounds and analysis of their antiplasmodial activity. The results obtained may partially justify the traditional use of K. leucantha to treat malaria in Benin. [less ▲]

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See detailAntiparasitic activities of two sesquiterpenic lactones isolated from Acanthospermum hispidum D.C
Ganfon; Bero, Joanne; Tchinda Tiabou, Alembert ULg et al

in Journal of Ethnopharmacology (2012), 141(0), 411-417

Ethnopharmacological relevance : Aerial parts of Acanthospermum hispidum D.C. are often used by traditional healers in Benin for various diseases and especially for malaria Aim of the study : Identify ... [more ▼]

Ethnopharmacological relevance : Aerial parts of Acanthospermum hispidum D.C. are often used by traditional healers in Benin for various diseases and especially for malaria Aim of the study : Identify active compounds from extracts of Acanthospermum hispidum D.CV. leaves previously shown to possess antimalarial properties and analyse in vivo activity and toxicity of crude extracts. Materials and methods : Compounds were isolated from aerial part of A. hispidum D.C. and structurally elucidated using extensive spectroscopic analysis. Antiplasmodial activity was evaluated in vitro against a chloroquinosensitive strain of Plasmodium falciparum (3D7) using the measurement of the plasmodial lactate dehydrogenase activity and in vivo against P. berghei berghei by the 4-days suppressive test. Selectivity of extract and purified compounds on Plasmodium parasites were evaluated by using MTT test on J774 macrophage like murine cells and WI38 human normal fibroblasts and also against two other parasites: Trypanosoma brucei brucei and Leishmania mexicana mexicana. Acute and sub-acute toxicities of a crude extract were evaluated on mice. Results : Two known sesquiterpenic lactones were isolated: 1 (15-acetoxy-8β-[(2-methylbutyryloxy)]-14-oxo-4, 5-cis-acanthospermolide) and 2 (9α-acetoxy-15-hydroxy-8β-(2-methylbutyryloxy) -14-oxo-4, 5-trans-acanthospermolide). 1 and 2 showed in vitro antiplasmodial activity against the chloroquino-sensitive strain (3D7) with IC50 of 2.9 ± 0.5 and 2.23 ± 0.09 μM respectively. Only 2 showed a high selectivity index (SI: 18.4) on Plasmodium compared to cytotoxicity against human fibroblasts cell line (WI38). 1 and 2 also showed interesting antiparasitic activities in vitro against Trypanosoma brucei brucei (IC50 of 2.45 ± 0.49 and 6.36 ± 1.42 μM respectively) and Leishmania mexicana mexicana (IC50 of 0.94 ± 0.05 and 2.54 ± 0.19 μM respectively). Furthermore, crude acidic water extract and fractions containing one of the two isolated compounds displayed a weak in vivo antimalarial activity against P. berghei berghei with a long half-life causing a delayed effect. In vivo acute (2000 mg/kg) and sub-acute (1000 mg/kg) toxicity tests on the crude acidic water extract did not show toxicity. Conclusion : Crude acidic water extract, fractions and pure isolated compounds from A.hispidum showed promising in vitro antiplasmodial activity. Despite our study did not show in vivo acute and subacute toxicities of the crude acidic water extract, its weak in vivo antimalarial activity and the in vitro cytoxicity of pure compounds and enriched extracts containing 1 and 2 indicate that the aerial parts of A. hispidum should be used with caution for malaria treatments. [less ▲]

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See detailAntiplasmodial, anti-inflammatory and cytotoxic activities of various plant extracts from the Mascarene Archipelago.
Jonville, Marie ULg; Kodja, H.; Strasberg, D. et al

in Journal of Ethnopharmacology (2011), 136

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 ... [more ▼]

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 Reunion 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 IC(50)<50mug/ml for antiplasmodial response, IC(50)<100mug/ml for cytotoxicity, and IC(50)<130mug/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 (IC(50)<15mug/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. [less ▲]

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See detailMetabolomic investigation of the ethnopharmacological use of Artemisia afra with NMR Spectroscopy and Multivariate Data Analysis.
Liu, N. Q.; Cao, Martine ULg; Frederich, Michel ULg et al

in Journal of Ethnopharmacology (2010), 128

Ethnopharmacological relevance: Artemisia afra has been used as an infusion to treat malaria throughout the southern parts of Africa, in much the same way as the antimalarial plant Artemisia annua in ... [more ▼]

Ethnopharmacological relevance: Artemisia afra has been used as an infusion to treat malaria throughout the southern parts of Africa, in much the same way as the antimalarial plant Artemisia annua in China. The antiplasmodial activity of purified components from an apolar fraction of A. afra has been shown in the past. No data on the efficacy of the tea infusion prepared from A. afra are however available. OBJECTIVE: To investigate the antiplasmodial activity of various extracts of A. afra including an ethnopharmacological prepared sample. To identify polar metabolites in A. afra and A. annua and by using multivariate data analysis investigate the metabolic differences between these species. Materials and methods: The antiplasmodial activity of A. afra and A. annua extracts were tested for activity against Plasmodiam falciparum 3D7 (chloroquine-sensitive strain) with chloroquine, quinine and artemisinin as positive controls. Hydrophilic metabolites in A. afra and A. annua were identified directly from the crude extracts through 1D- and 2D-NMR spectra. The NMR spectra were also used to differentiate between the two species using principal component analysis (PCA) for quality control purposes. RESULTS: The apolar fractions of both A. afra and A. annua showed activity against P. falciparum while activity was only found in the tea infusion of A. annua. Metabolomic studies using 1D- and 2D-NMR spectroscopy identified 24 semi-polar components in A. afra including three new phenylpropanoids for this species: caffeic acid, chlorogenic acid and 3,5-dicaffeoyl quinic acid. PCA analysis conducted on the samples yielded good separation between the polar extracts of A. afra and A. annua. CONCLUSION: These findings shows that there are no in vitro activity in the tea infusion of A. afra and lists the identified metabolites causing the metabolic differences between A. afra and A. annua for quality control purposes. [less ▲]

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See detailEvaluation of 13 selected medicinal plants from Burkina Faso for their antiplasmodial properties.
Jansen, Olivia ULg; Angenot, Luc ULg; Tits, Monique ULg et al

in Journal of Ethnopharmacology (2010), 130

AIM OF THE STUDY: The aim of this study was to evaluate the antiplasmodial properties of 13 plants used against malaria in traditional medicine in Burkina Faso. MATERIALS AND METHODS: In vitro ... [more ▼]

AIM OF THE STUDY: The aim of this study was to evaluate the antiplasmodial properties of 13 plants used against malaria in traditional medicine in Burkina Faso. MATERIALS AND METHODS: In vitro antiplasmodial activity of dichloromethane, methanol and aqueous crude extracts obtained from vegetal samples collected in Burkina Faso was first evaluated on the Plasmodium falciparum 3D7 chloroquine-sensitive strain using a colorimetric method. RESULTS: Thirteen extracts obtained from 8 different species were found to exhibit antiplasmodial activity (IC(50)<50mug/ml). Five species demonstrated a moderate activity (15mug/ml<IC(50)<50mug/ml): Boswellia dalzielii (leaves), Waltheria indica (roots and aerial parts), Bergia suffruticosa (whole plant), Vitellaria paradoxa (bark) and Jatropha gossypiifolia (leaves). The best results were obtained with extracts from the Dicoma tomentosa whole plant, from Psorospermum senegalense leaves and from Gardenia sokotensis leaves. These extracts found to display promising antiplasmodial activity, with IC(50) values ranging from 7.0 to 14.0mug/ml. The most active plant extracts were then tested for in vitro activity on the Plasmodium falciparum W2 chloroquine-resistant strain and also for in vitro cytotoxicity on normal human fibroblasts (WI-38) in order to determine the selectivity index. CONCLUSIONS: Dicoma tomentosa (Asteraceae) and Psorospermum senegalense (Clusiaceae) appeared to be the best candidates for further investigation of their antiplasmodial properties, reported for the first time by this study. [less ▲]

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See detailIn vitro and in vivo antimalarial and cytotoxic activity of five plants used in Congolese traditional medicine.
Lusakibanza, M.; Mesia, G.; Tona, G. et al

in Journal of Ethnopharmacology (2010), 129

AIM OF THE STUDY: The in vitro antiplasmodial activity and cytotoxicity of methanolic and dichloromethane extracts from five Congolese plants were evaluated. The plants were selected following an ... [more ▼]

AIM OF THE STUDY: The in vitro antiplasmodial activity and cytotoxicity of methanolic and dichloromethane extracts from five Congolese plants were evaluated. The plants were selected following an ethnobotanical survey conducted in D.R. Congo and focusing on plants used traditionally to treat malaria. The in vivo antimalarial activity of aqueous and methanolic extracts active in vitro was also determined in mice infected by Plasmodium berghei berghei. MATERIALS AND METHODS: The growth inhibition of Plasmodium falciparum strains was evaluated using the measurement of lactate dehydrogenase activity. The extracts (aqueous, CH(3)OH, EtOH and CH(2)Cl(2)) were prepared by maceration and tested in vitro against the 3D7 (chloroquine sensitive) and W2 (chloroquine resistant) strains of Plasmodium falciparum and against the human normal fetal lung fibroblasts WI-38 to determine the selectivity index. Some extracts were also used at the dose of 300mg/kg to evaluate their activity in mice infected since 4 days by Plasmodium berghei. RESULTS: Two plants presented a very high activity (IC(50)<3mug/ml). These plants were Strychnos icaja roots bark (MeOH and CH(2)Cl(2)) and Physalis angulata leaves (MeOH and CH(2)Cl(2)). One plant (Anisopappus chinensis whole plant, MeOH and CH(2)Cl(2)) presented a high activity (IC50<15mug/ml). The extracts of Anisopappus chinensis and Physalis angulata showed also a good inhibition of parasitemia in vivo. Flavonoids, phenolic acids and terpenes were identified in these plants by a general phytochemical screening method. CONCLUSION: Three plants showed a very interesting antiplasmodial activity (Anisopappus chinensis, Physalis angulata and Strychnos icaja) and one of them showed a good selectivity index (>10, Anisopappus chinensis). Anisopappus chinensis and Physalis angulata were also active in vivo. [less ▲]

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See detailAntiplasmodial and cytotoxic activities of Rwandan medicinal plants used in the treatment of malaria.
Muganga, R.; Angenot, Luc ULg; Tits, Monique ULg et al

in Journal of Ethnopharmacology (2010), 128

AIM OF THE STUDY: In our study, methanol, dichloromethane and aqueous extracts of 13 Rwandan medicinal plants used in the treatment of malaria were tested for in vitro antiplasmodial activity. MATERIALS ... [more ▼]

AIM OF THE STUDY: In our study, methanol, dichloromethane and aqueous extracts of 13 Rwandan medicinal plants used in the treatment of malaria were tested for in vitro antiplasmodial activity. MATERIALS AND METHODS: The growth inhibition of chloroquine-sensitive Plasmodium falciparum strain (3D7) was evaluated using the measurement of lactate dehydrogenase activity. The active extracts were also tested against the chloroquine-resistant Plasmodium falciparum strain (W2) and for cytotoxicity assay using human normal foetal lung fibroblasts (WI-38). RESULTS: The majority of the plants tested showed an antiplasmodial activity and the best results were observed with dichloromethane leaf and flower extracts of Tithonia diversifolia, leaf extract of Microglossa pyrifolia and root extract of Rumex abyssinicus, methanol leaf extract of Fuerstia africana, root bark extracts of Zanthoxylum chalybeum and methanol bark extract of Terminalia mollis. Those extracts were active (IC(50)<15mug/ml) on both chloroquine-sensitive and resistant strains of Plasmodium falciparum. Zanthoxylum chalybeum, Solanecio mannii and Terminalia mollis presented the best selectivity index. CONCLUSIONS: The traditional use of most of the plant evaluated was confirmed by the antiplasmodial test. This study revealed for the first time the antiplasmodial activity of two plants: Terminalia mollis and Rumex abyssinicus. [less ▲]

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See detailIn vitro antiplasmodial activity of plants used in Benin in traditional medicine to treat malaria
Bero, Joanne; Ganfon, Habib; Jonville, Marie ULg et al

in Journal of Ethnopharmacology (2009), 122

Aim of the study: The aim of the studywas to evaluate the in vitro antiplasmodial activity of crude extracts of 12 plant species traditionally used in Benin for the treatment of malaria in order to ... [more ▼]

Aim of the study: The aim of the studywas to evaluate the in vitro antiplasmodial activity of crude extracts of 12 plant species traditionally used in Benin for the treatment of malaria in order to validate their use. Materials and methods: For each species, dichloromethane, methanol and total aqueous extracts were tested. The antiplasmodial activity of extracts was evaluated using the measurement of the plasmodial lactate dehydrogenase activity on chloroquine-sensitive (3D7) and resistant (W2) strains of Plasmodium falciparum. The selectivity of the different extractswas evaluated using the MTT test on J774 macrophagelike murine cells and WI38 human normal fibroblasts. Results: The best growth inhibition of both strains of Plasmodium falciparum was observed with the dichloromethane extracts of Acanthospermum hispidum DC. (Asteraceae) (IC50 =7.5 g/ml on 3D7 and 4.8 g/ml on W2), Keetia leucantha (K. Krause) Bridson (syn. Plectronia leucantha Krause) (Rubiaceae) leaves and twigs (IC50 = 13.8 and 11.3 g/ml on 3D7 and IC50 = 26.5 and 15.8 g/ml on W2, respectively), Carpolobia lutea G.Don. (Polygalaceae) (IC50 = 19.4 g/ml on 3D7 and 8.1 g/ml on W2) and Strychnos spinosa Lam. (Loganiaceae) leaves (IC50 = 15.6 g/ml on 3D7 and 8.9 g/ml on W2). All these extracts had a low cytotoxicity. Conclusion: Our study gives some justifications for the traditional uses of some investigated plants. [less ▲]

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See detailScreening of medicinal plants from Reunion Island for antimalarial and cytotoxic activity.
Jonville, Marie ULg; Kodja, H.; Humeau, L. et al

in Journal of Ethnopharmacology (2008), 120(3), 382-6

AIM OF THE STUDY: Nine plants from Reunion Island, selected using ethnopharmacology and chemotaxonomy, were investigated for their potential antimalarial value. MATERIALS AND METHODS: Thirty-eight ... [more ▼]

AIM OF THE STUDY: Nine plants from Reunion Island, selected using ethnopharmacology and chemotaxonomy, were investigated for their potential antimalarial value. MATERIALS AND METHODS: Thirty-eight extracts were prepared by maceration using CH(2)Cl(2) and MeOH, and were tested for in vitro activity against the 3D7 and W2 strain of Plasmodium falciparum. The most active extracts were then tested for in vitro cytotoxicity on human WI-38 fibroblasts to determine the selectivity index. Those extracts were also investigated in vivo against Plasmodium berghei infected mice. RESULTS: Most active of the extracts tested were the dichloromethane leaves extracts of Nuxia verticillata Lam. (Buddlejaceae), Psiadia arguta Voigt. (Asteraceae), Lantana camara L. (Verbenaceae), the methanol extracts from Aphloia theiformis (Vahl) Benn. (Aphloiaceae) bark, and Terminalia bentzoe L. (Combretaceae) leaves displaying in vitro IC(50) values ranging from 5.7 to 14.1mug/ml. Extracts from Psiadia, Aphloia at 200mg/(kgday) and Teminalia at 50mg/(kgday) also exhibited significant (p<0.0005) parasite inhibition in mice: 75.5%, 65.6% and 83.5%, respectively. CONCLUSION: Two plants showed interesting antimalarial activity with good selectivity: Aphloia theiformis and Terminalia bentzoe. Nuxia verticillata still needs to be tested in vivo, with a new batch of plant material. [less ▲]

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See detailPhytochemical and pharmacological study of roots and leaves of Guiera senegalensis JF Gmel (Combretaceae)
Fiot, Julien; Sanon, Souleymane; Azas, Nadine et al

in Journal of Ethnopharmacology (2006), 106(2), 173-178

The chemical composition of total alkaloids from leaves and roots of Guiera senegalensis was investigated. Three beta-carboline alkaloids were purified: in addition to harman and tetrahydroharman, known ... [more ▼]

The chemical composition of total alkaloids from leaves and roots of Guiera senegalensis was investigated. Three beta-carboline alkaloids were purified: in addition to harman and tetrahydroharman, known in roots and leaves. harmalan (dihydroharman) was isolated for the first time from roots of Guiera senegalensis. Guieranone A, a naphthyl butenone, was also purified from leaves and roots. The in vitro antiplasmodial activity and the cytotoxicity of extracts and pure compounds were evaluated. Each total alkaloid extract and beta-carboline alkaloids presented an interesting antiplasmodial activity associated with a low cytotoxicity. Harmalan was less active than harman and tetrahydroharman. Guieranone A showed a strong antiplasmodial activity associated with a high cytotoxicity toward human monocytes. Its cytotoxicity was performed against two cancer cell lines and normal skin fibroblasts in order to study its anticancer potential: guieranone A presented a strong cytotoxicity against each cell strains. Finally, we evaluated the potent synergistic antimalarial interaction between Guiera senegalensis and two plants commonly associated in traditional remedies: Mitragyna inermis and Pavetta crassipes. Three associations evaluated were additive. A synergistic effect was shown between total alkaloids extracted from leaves of Guiera senegalensis and those of Mitragyna inermis. This result justified the traditional use of the plants in combination to treat malaria. (c) 2006 Elsevier Ireland Ltd. All rights reserved. [less ▲]

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See detailScreening of 14 alkaloids isolated from Haplophyllum A. Juss. for their cytotoxic properties
Jansen, Olivia ULg; Akhmedjanova, Valentina; Angenot, Luc ULg et al

in Journal of Ethnopharmacology (2006), 105(1-2), 241-245

Further to a systematic chemotaxonomic study of Uzbek Haplophyllum A. Juss. plants selected on ethnopharmacological data, 14 alkaloids were screened for their cytotoxic properties. As a first selection ... [more ▼]

Further to a systematic chemotaxonomic study of Uzbek Haplophyllum A. Juss. plants selected on ethnopharmacological data, 14 alkaloids were screened for their cytotoxic properties. As a first selection for interesting compounds, each alkaloid was tested against two human cancer cell lines (HeLa and HCT-116), using WST-1 reagent. Of the 14 alkaloids, 5 were cytotoxic when tested against the HeLa line with an IC50 < 100 microM. These five compounds consisted of three furoquinolines: skimmianine; haplopine and gamma-fagarine and two pyranoquinolones: flindersine and haplamine. Only haplamine was active against the HCT-116 line. The cytotoxic properties of these five alkaloids were further investigated against five additional human cancer cell lines. Their structure-activity relationships will be discussed. Of these five pre-selected alkaloids, only haplamine showed significant cytotoxic activity against all the tested cell lines. This is the first report of the cytotoxic activity of haplamine. Finally, this pyranoquinolone alkaloid was tested here against 14 different cancer cell lines and against normal skin fibroblasts. [less ▲]

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See detailChemical and biological investigations of a toxic plant from Central Africa, Magnistipula butayei subsp montana
Karangwa, Charles; Esters, Virginie ULg; Frederich, Michel et al

in Journal of Ethnopharmacology (2006), 103(3), 433-438

Magnistipida butayei subsp. montana (Chrysobalanaceae) is known, in the Great Lakes Region, to possess toxicological properties. In this paper, we investigated the acute toxicity (dose levels 50-1600 mg ... [more ▼]

Magnistipida butayei subsp. montana (Chrysobalanaceae) is known, in the Great Lakes Region, to possess toxicological properties. In this paper, we investigated the acute toxicity (dose levels 50-1600 mg/kg) of its aqueous extract, administered orally to adult Wistar rats. This study demonstrated that the freeze-dried aqueous extract (5%, w/w) possesses high toxicity. The extract caused hypothermia, neurological disorders, including extensor reflex of maximal convulsive induced-seizures at about 2h after the administered dose, and death occurred (LD50 = 370 mg/kg) in a dose dependent manner. Blood parameter evaluation revealed slight variations, but these might not have clinical relevance. Histological examination of internal organs (lungs, liver, heart and kidneys) did not reveal any abnormality in the treated group compared to the control. Therefore, it can be concluded that Magnistipida butayei subsp. montana aqueous extract, given orally, is toxic and that its target is the central nervous system. General phytochemical screening revealed that the plant did not contain significant amounts of products known to be toxic, such as alkaloids or cardioactive glycosides, but only catechic tannins, amino acids, saponins and other aphrogen principles in the three parts of the species (fruit, leave and bark). (c) 2005 Elsevier Ireland Ltd. All rights reserved. [less ▲]

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See detailBiologically active bisbenzylisoquinoline alkaloids from the root bark of Epinetrum villosum
Otshudi, A. L.; Apers, S.; Pieters, L. et al

in Journal of Ethnopharmacology (2005), 102(1), 89-94

Methanol and water extracts of the root of Epinetrum villosum (Exell) Troupin (Menispermaceae) were found to exhibit antimicrobial and antiplasmodial activities. Investigation of the active methanol ... [more ▼]

Methanol and water extracts of the root of Epinetrum villosum (Exell) Troupin (Menispermaceae) were found to exhibit antimicrobial and antiplasmodial activities. Investigation of the active methanol fraction led to the isolation of four bisbenzylisoquinoline alkaloids, i.e., cycleanine, cycleanine N-oxide, isochondodendrine and cocsoline. Structures were established by spectroscopic methods. Cocsoline displayed antibacterial and antifungal activities (MIC values of 1000-15.62 and 31.25 mu g/ml, respectively). Isochondodendrine was found to have the most potent antiplasmodial activity (IC50 = 0- 10 mu g/ml), whereas the IC50 on HCT-116 human colon carcinoma cells was 17.5 mu g/ml (selectivity index 175). Cycleanine acted against HIV-2 (EC50 = 1.83 mu g/ml) but was at least 10-fold less active against HIV-1. Cycleanine N-oxide showed no activity towards all tested microorganisms. (C) 2005 Elsevier Ireland Ltd. All rights reserved. [less ▲]

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See detailRecent developments in the field of arrow and dart poisons
Philippe, Geneviève ULg; Angenot, Luc ULg

in Journal of Ethnopharmacology (2005), 100(1-2), 85-91

Arrow and dart poisons, considered as conventional natural sources for future drug discovery, have already provided numerous biologically active molecules used as drugs in therapeutic applications or in ... [more ▼]

Arrow and dart poisons, considered as conventional natural sources for future drug discovery, have already provided numerous biologically active molecules used as drugs in therapeutic applications or in pharmacological research. Plants containing alkaloids or cardiotonic glycosides have generally been the main ingredients responsible for the efficacy of these poisons, although some animals, such as frogs, have also been employed. This paper, without being exhaustive, reports the greater strides made during the past 15 years in the understanding of the chemical nature and biological properties of arrow and dart poison constituents. Examples both of promising biological properties shown by these molecules and of crucial discoveries achieved by their use as pharmacological tools are given. Further studies of these toxic principles are likely to enable scientists to find new valuable lead compounds, useful in many fields of research, like oncology, inflammation and infectious diseases. 2005 Elsevier Ireland Ltd. All rights reserved. [less ▲]

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See detailIn vitro screening of some Strychnos species for antiplasmodial activity
Philippe, Geneviève ULg; Angenot, Luc ULg; De Mol, Patrick ULg et al

in Journal of Ethnopharmacology (2005), 97(3), 535-539

The antiplasmodial activity of crude extracts of 19 species of Strychnos (Loganiaceae) was assessed in vitro against a chloroquine-susceptible strain of Plasmodium falciparum. For each species, ethyl ... [more ▼]

The antiplasmodial activity of crude extracts of 19 species of Strychnos (Loganiaceae) was assessed in vitro against a chloroquine-susceptible strain of Plasmodium falciparum. For each species, ethyl acetate (EtOAc) extracts were analysed and, for the most active species, methanolic (MeOH) extracts were also tested. Among them, Strychnos variabilis De Wild. seemed to be very promising (inhibitory concentration 50% (IC50) < 5 microg/ml) whereas two other species, Strychnos gossweileri Exell and Strychnos mellodora S. Moore, could be interesting (IC50 < 15 microg/ml) in further antimalarial studies. [less ▲]

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See detailIsolation and pharmacological activity of phenylpropanoid esters from Marrubium vulgare
Sahpaz, S.; Garbacki, Nancy ULg; Tits, Monique ULg et al

in Journal of Ethnopharmacology (2002), 79(3), 389-392

The isolation and identification of major phenylpropanoid esters from Marrubium vulgare: (+) (E)-caffeoyl-L-malic acid 1, acteoside 2, forsythoside B 3, arenarioside 4, ballotetroside 5, as well as their ... [more ▼]

The isolation and identification of major phenylpropanoid esters from Marrubium vulgare: (+) (E)-caffeoyl-L-malic acid 1, acteoside 2, forsythoside B 3, arenarioside 4, ballotetroside 5, as well as their anti-inflammatory activity are reported for the first time, We evaluated the inhibitory effects of these five compounds on cyclooxygenase (Cox) catalysed prostaglandin biosynthesis activity. Only the glycosidic phenylpropanoid esters showed an inhibitory activity towards the Cox-2 enzyme and three of them: acteoside 2, forsythoside B 3, arenarioside 4, exhibited higher inhibitory potencies on Cox-2 than on Cox-1. These results are of interest, as Cox-2 is mainly associated with inflammation and the Cox-1 inhibition with adverse side effects often observed with non-steroidal anti-inflammatory drugs. The occurence of these phenylpropanoid esters could also explain some other pharmacological properties of M. vulgare. (C) 2002 Elsevier Science Ireland Ltd. All rights reserved. [less ▲]

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See detailAnti-Inflammatory and Immunological Effects of Centaurea Cyanus Flower-Heads
Garbacki, Nancy ULg; Gloaguen, Vincent; Damas, Jacques ULg et al

in Journal of Ethnopharmacology (1999), 68(1-3), 235-41

Centaurea cyanus flower-heads are used in European phytotherapy for the treatment of minor ocular inflammations. Different pharmacological experiments (inhibition of carrageenan, zymosan and croton oil ... [more ▼]

Centaurea cyanus flower-heads are used in European phytotherapy for the treatment of minor ocular inflammations. Different pharmacological experiments (inhibition of carrageenan, zymosan and croton oil-induced oedemas, inhibition of plasma haemolytic activity, induction of anaphylatoxin activity) showed that polysaccharides extracted from C. cyanus flower-heads had anti-inflammatory properties and interfered with complement. Moreover, these polysaccharides were found to be mainly composed of galacturonic acid, arabinose, glucose, rhamnose and galactose. [less ▲]

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