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ABSTRACT: Uncaria tomentosa (Willd. ex Roem. & Schult.) DC. (Rubiaceae) is widely used by populations living in South America to treat many ailments associated with inflammatory disorders. Mitraphylline was shown to be the major pentacyclic oxindolic alkaloid present in the bark chloroformic extract of this plant. Its activity against cytokines involved in inflammation process was tested in a murine model in vivo.
Mice received mitraphylline once a day for 3 days at 30mg/kg/day by oral route. Then, they were subjected to bacterial lipopolysaccharide (LPS) endotoxin (15mg/kg) and the LPS-induced production of 16 different cytokines was determined by Elisa multiplex. Control group received dexamethasone orally at 2mg/kg/day. Toxicity on K565 cells and murine peritoneal macrophages, in vitro, at doses up to 100μM was monitored by XTT-colorimetric assay.
For the first time mitraphylline was tested in vivo against a large range of cytokines that play a crucial role in inflammation. Mitraphylline inhibited around 50% of the release of interleukins 1α, 1β, 17, and TNF-α. This activity was similar to dexamethasone. It also reduced almost 40% of the production of interleukin 4 (IL-4) while the corticoid did not. Lastly it did not show any toxicity on K565 cells nor murine macrophages at doses up to 100μM.
Journal of ethnopharmacology 07/2012; 143(3):801-4. · 2.32 Impact Factor
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N Cachet,
F Hoakwie,
S Bertani,
G Bourdy, E Deharo,
D Stien,
E Houel,
H Gornitzka,
J Fillaux,
S Chevalley,
A Valentin,
V Jullian
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ABSTRACT: We report the isolation and identification of a new quassinoid named simalikalactone E (SkE), extracted from a widely used Amazonian antimalarial remedy made out of Quassia amara L. (Simaroubaceae) leaves. This new molecule inhibited the growth of Plasmodium falciparum cultured in vitro by 50%, in the concentration range from 24 to 68 nM, independently of the strain sensitivity to chloroquine. We also showed that this compound was able to decrease gametocytemia with a 50% inhibitory concentration sevenfold lower than that of primaquine. SkE was found to be less toxic than simalikalactone D (SkD), another antimalarial quassinoid from Q. amara, and its cytotoxicity on mammalian cells was dependent on the cell line, displaying a good selectivity index when tested on nontumorogenic cells. In vivo, SkE inhibited murine malaria growth of Plasmodium vinckei petteri by 50% at 1 and 0.5 mg/kg of body weight/day, by the oral or intraperitoneal routes, respectively. The contribution of quassinoids as a source of antimalarial molecules needs therefore to be reconsidered.
Antimicrobial Agents and Chemotherapy 09/2009; 53(10):4393-8. · 4.84 Impact Factor
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ABSTRACT: A knowledge attitude and practice study centred on leishmaniasis and its treatment was performed among the Chayahuita, an Amazonian Peruvian ethnic group living in an endemic area. This study documents traditional Chayahuita plant's use and disease concepts. Also, activity of some medicinal plants used by the Chayahuita is highlighted and discussed.
Ninety-three Chayahuita people were interviewed, following a semi-structured questionnaire focussed on disease knowledge and perception, personal attitude and healing practices. Simultaneously, a collection of plants was performed in different ecotopes, in order to make an extensive inventory of the pharmacopoeia.
For the Chayahuita, cutaneous (CL) and muco-cutaneous leishmaniasis (MCL) are considered as diseases of their own, with specific names, aetiologies, mode of transmission. Regarding CL, Chayahuita people consider that the humid characteristic of the skin ulcer is a discriminative fact orienting the diagnostic forTa'ta' (leishmaniasis). Forty-six different species were designated useful against LC and /or MCL (29 species by means of the questionnaire and 27 species when collecting in different ecotopes). Thirty-seven extracts corresponding to 31 species used medicinally were screened in vitro against Leishmania amazonensis axenic amastigotes, assessing their viability by the reduction of tetrazolium salt (MTT). Six species displayed a good activity (10 microg/ml<IC50<20 microg/ml): an undetermined hemi-epiphytic Clusiaceae, Cybianthus anthuriophyllus Pipoly (Myrsinaceae), two Piper, Piper sanguineispicum Trel., and Piper loretoanum Trel. (Piperaceae), Desmodium axillare Sw. DC. (Fabaceae), and Clibadium sylvestre (Aubl.) Baill. (Asteraceae).
Perception of leishmaniasis, attitude, treatments and diet prohibitions still largely reflects traditional Chayahuita cosmovision, even if some tentative of bio-medical re-interpretation is arising.
Journal of ethnopharmacology 07/2009; 126(1):149-58. · 2.32 Impact Factor
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ABSTRACT: New treatments are urgently needed to curb and eradicate malaria in developing countries. As most people living in malarial endemic areas use traditional medicine to fight this disease, why have new treatments not emerged recently from ethnopharmacology-oriented research? The rationale and limitations of the ethnopharmacological approach are discussed in this paper, focusing on ethnopharmacology methodologies and techniques used for assessing botanical samples for their antimalarial properties. Discrepancies often observed between strong ethnopharmacological reputation and laboratory results are discussed, as well as new research perspectives.
International Journal for Parasitology 02/2008; 38(1):33-41. · 3.39 Impact Factor
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ABSTRACT: A total of 27 ethanolic plant extracts from 27 species were screened for leishmanicidal activity in vitro against Leishmania amazonensis. Most of the selected species (19) are traditionally used by the Chayahuitas, an Amazonian Peruvian ethnic group, to treat skin affections and/or leishmaniasis.
A colorimetric method based on the reduction of tetrazolium salt (MTT) was used to measure the viability of Leishmania amazonensis promastigote and amastigote stages.
Only the leaves of two species of the Piperaceae family (Piper hispidum Sw., and Piper strigosum Trel.) showed good leishmanicidal activities (IC(50)<10 microg/ml against amastigotes). Roots of Tabernaemontana sananho Ruiz & Pav. (Apocynaceae), together with bark of Vismia tomentosa Ruiz & Pav. (Clusiaceae), fruits of Solanum straminifolium var straminifolium Jacq. (Solanaceae), and stems of Zamia lindenii Regel ex André (Cycadaceae) showed low activity against amastigote stage (IC(50) around 50 microg/ml). Of those only Tabernaemontana sananho displayed also good activity on promastigotes (IC(50)<10 microg/ml). Results are discussed herein, in relation with the traditional use of the plants and compared with other data from the relevant literature.
Journal of Ethnopharmacology 11/2007; 114(2):254-9. · 3.01 Impact Factor
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ABSTRACT: Methylene blue (MB) is the oldest synthetic antimalarial. It is not used anymore as antimalarial but should be reconsidered. For this purpose we have measured its impact on both chloroquine sensitive and resistant Plasmodium strains. We showed that around 5 nM of MB were able to inhibit 50% of the parasite growth in vitro and that late rings and early trophozoites were the most sensitive stages; while early rings, late trophozoites and schizonts were less sensitive. Drug interaction study following fractional inhibitory concentrations (FIC) method showed antagonism with amodiaquine, atovaquone, doxycycline, pyrimethamine; additivity with artemether, chloroquine, mefloquine, primaquine and synergy with quinine. These results confirmed the interest of MB that could be integrated in a new low cost antimalarial combination therapy.
Parasite (Paris, France) 07/2007; 14(2):135-40. · 1.00 Impact Factor
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ABSTRACT: In French Guiana, Quassia amara L. (Simaroubaceae) leaf tea is a well-known widely used traditional antimalarial remedy. Impact of the vegetal sampling condition on in vivo and in vitro antimalarial activity was assessed. Traditional infusions were prepared with juvenile or mature leaves, both either fresh or dried. Results showed that growing stage and freshness of vegetal material exert a striking effect on antimalarial activity, both in vitro and in vivo. By far, leaf tea made from fresh juvenile (FJ) Quassia amara leaves was the most active. In vitro, active component (simalikalactone D) concentration correlates biological activities, although unexplained subtle variations were observed. In vivo, tea made with dried juvenile (DJ) leaves displays a peculiar behavior, meaning that some components may help simalikalactone D delivery or may be active in vivo only, therefore enhancing the expected curative effect of the traditional preparation.
Journal of Ethnopharmacology 05/2007; 111(1):40-2. · 3.01 Impact Factor
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ABSTRACT: In the main markets of Paramaribo (Suriname), many stands offer what is locally called "Bitter-cups", or "Kwasi bita beker", small footed-cups, roughly carved from a whitish wood. The use of these cups is strictly medicinal and it seems to be restricted to Suriname, as they are not found in neighbouring countries (Guyana, French Guiana). The aim of this study was to identify the botanical origin of Bitter-cups still in use in the Saramaka traditional medicine (as information from field people was controversial), and document the ethnopharmacology of this original galenical artefact. Microscopic and high performance liquid chromatography (HPLC) analyses were carried out on Bitter-cup, and anatomical criteria (marginal parenchyma band, size of intervessel and vessel-ray pits, rays width and rays composition, vessels clustering, frequency and size of parenchyma pits) together with HPLC profiles of the macerates showed that the wood cup was similar to Quassia amara L. (Simaroubaceae) wood. Ethnopharmacological investigation indicates that the use of these cups is simply due to the pharmacological properties attributed to "bitters", and is strongly linked to tradition and cultural attitudes. This study also emphasizes the long lasting use of these cups, now restricted to Suriname only, with almost no variation over one century.
Journal of Ethnopharmacology 04/2007; 110(2):318-22. · 3.01 Impact Factor
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ABSTRACT: French Guiana (North-East Amazonia) records high malaria incidence rates. The traditional antimalarial remedy most widespread there is a simple tea made out from Quassia amara L. leaves (Simaroubaceae). This herbal tea displays an excellent antimalarial activity both in vitro and in vivo. A known quassinoid, simalikalactone D (SkD), was identified as the active compound, with an IC(50) value of 10nM against FcB1 Plasmodium falciparum chloroquine resistant strain in vitro. Lastly, it inhibits 50% of Plasmodium yoelii yoelii rodent malaria parasite at 3.7 mg/kg/day in vivo by oral route. These findings confirm the traditional use of this herbal tea.
Journal of Ethnopharmacology 12/2006; 108(1):155-7. · 3.01 Impact Factor
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ABSTRACT: Chabirenia cayennensis n. g., n. sp. (Nematoda: Rhabdiasidae) is described from the teiid lizard Ameiva ameiva. A total of 139 worms were recovered, all females, from the mucous glands of the buccal cavity. The worm has a free-living phase in a homogonic life-cycle. Infective larvae are enclosed in a sheath with chequered ornamentation and composed of two exuviae. The new genus is distinct from the five known genera of the family, Pneumonema Johnston, 1916, Acanthorhabdias Pereira, 1927, Entomelas Travassos, 1930, Rhabdias Stiles and Hassall, 1905 and Neoentomelas Hasagawa, 1989, in the following characters: helical habitus, longitudinal cuticular crests, very tiny buccal cavity without thick walls and three oesophageal onchia. Several characters of this new rhabdiasid suggest the Strongylida.
Systematic Parasitology 11/2005; 62(2):151-60. · 1.25 Impact Factor
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ABSTRACT: A "knowledge attitudes and practices" study about malaria treatments was undertaken in French Guiana, along with an ethnopharmacological study. One hundred and seventeen people from five different groups and nationalities (Creole, Palikur, Galibi, Brazilian, and European) answered the questionnaire. The results were analysed using univariate and multivariate statistical analysis. First, we evaluated the overall knowledge about malaria from the interviewed people. According to bio-medical concepts, we noticed that they have a good knowledge of this illness. Secondly, we studied the treatment used by sick people during their last malaria attack. We demonstrated that, although bio-medical treatment is available in this area, people use both modern drugs and traditional remedies. Finally, preventive attitudes have been examined. One-third of the interviewed people drink regularly some herbal remedy to prevent febrile illnesses and malaria, thus displaying a strong concern about this disease. The ethnopharmacological study highlighted the frequent use of traditional remedies, along with their mode of preparation and administration. A total of 34 different species (both from flora and fauna) have been registered as antimalarial. Twenty-seven are used for curative purposes, 20 as preventive and 13 of them are used for both purposes. Quassia amara (Simaroubaceae) whose antimalarial activity has already been demonstrated was the species most frequently used as antimalarial for curative and preventive purposes.
Journal of Ethnopharmacology 05/2005; 98(3):351-60. · 3.01 Impact Factor
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ABSTRACT: In order to evaluate the antimalarial potential of traditional remedies used in French Guiana, 35 remedies were prepared in their traditional form and screened for blood schizonticidal activity in vitro on Plasmodium falciparum chloroquine re4sistant strain (W2). Some of these extracts were screened in vivo against Plasmodium yoelii rodent malaria. Ferriprotoporphyrin inhibition test was also performed. Four remedies, widely used among the population as preventives, were able to inhibit more than 50% of the parasite growth in vivo at around 100 mg/kg: Irlbachia alata (Gentiananceae), Picrolemma pseudocoffea (Simaroubaceae), Quassia amara (Simaroubaceae), Tinospora crispa (Menispermaceae) and Zanthoxylum rhoifolium (Rutaceae). Five remedies displayed an IC50 in vitro < 10 microg/ml: Picrolemma pseudocoffea, Pseudoxandra cuspidata (Annonaceae) and Quassia amara leaves and stem, together with a multi-ingredient recipe. Two remedies were more active than a Cinchona preparation on the ferriprotoporphyrin inhibition test: Picrolemma pseudocoffea and Quassia amara. We also showed that a traditional preventive remedy, made from Geissospermum argenteum bark macerated in rum, was able to impair the intrahepatic cycle of the parasite. For the first time, traditional remedies from French Guiana have been directly tested on malarial pharmacological assays and some have been shown to be active.
Journal of Ethnopharmacology 05/2005; 98(1-2):45-54. · 3.01 Impact Factor
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ABSTRACT: One hundred and seventy-eight ethanolic plant extracts from the pharmacopoeia of the Tacana, an ethnic group from Bolivia, were screened for immunomodulatory activity using complement cascade inhibition and ADP-induced platelet aggregation inhibition assays. Six impaired both complement pathways (classical and alternative): stem bark from Astronium urundeuvea (Anacardiaceae), Cochlospermum vitifolium (Cochlospermaceae), Terminalia amazonica (Combretaceae), Triplaris americana (Polygonaceae), Uncaria tomentosa (Rubiaceae) and Euterpe precatoria (Arecaceae) roots. Inhibition of complement cascade was independent of essential ion complexation, and was not due to direct hemolytic activity on target red blood cells. For A. urundeuvea, C. vitifolium, and T. amazonica, anti-inflammatory activity relied on cyclo-oxygenase inhibition. Four of these species (A. urundeuva, T. americana, U. tomentosa and E. precatoria) are used traditionally to treat inflammatory processes.
Phytomedicine 10/2004; 11(6):516-22. · 3.27 Impact Factor
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ABSTRACT: Seventy-seven plant extracts (corresponding to 62 different species) traditionally used by the Isoceño-Guaraní, a native community living in the Bolivian Chaco, were screened for antimalarial activity in vitro on Plasmodium falciparum chloroquine sensitive strain (F32), and on ferriprotoporphyrin (FP) IX biocrystallisation inhibition test (FBIT). Among these extracts, seven displayed strong in vitro antimalarial activity, and 25 were active in the FBIT test. Positive results on both tests were recorded for six extracts: Argemone subfusiformis aerial part, Aspidosperma quebracho-blanco bark, Castela coccinea leaves and bark, Solanum argentinum leaves and Vallesia glabra bark. Results are discussed in relation with Isoceño-Guaraní traditional medicine. Further studies to be undertaken in relation with these results are also highlighted.
Journal of Ethnopharmacology 09/2004; 93(2-3):269-77. · 3.01 Impact Factor
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ChemInform 05/2003; 34(21).
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Pharmazie 02/2003; 58(1):68-9. · 1.01 Impact Factor
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ABSTRACT: Intraerythrocytic malaria parasites produce large amounts of toxic ferriprotoporphyrin IX (FP) during their digestion of host cell haemoglobin. The inhibition of biomineralisation of FP to haemozoin (or beta-haematin) by antimalarial drugs underlies their mode of action. We have developed an in vitro microassay for testing the inhibition of biomineralisation by drugs. It is based on the detection by optical density measurement of solubilised beta-haematin remaining after contact with drugs. The assay uses a 192-microM haemin chloride solution in dimethyl sulfoxide, 96-well filtration microplates as well as normal microplates; it lasts 18-24h and requires a spectrophotometer. We determined by this assay the IC(50) of chloroquine phosphate (28microM) and quinine base (324microM) and showed that unlike previous methods it is insensitive to inorganic anions. We also determined the activity of synthetic dyes and plant extract to determinate the interference of coloured compounds on the accuracy of the test. We found that methylene blue, thionine (IC(50) 38 and 87microM, respectively), and an extract of plants that contains quinoline derivatives, inhibited the biomineralisation of FP regardless of their intrinsic colour.
Experimental Parasitology 05/2002; 100(4):252-6. · 2.12 Impact Factor
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ABSTRACT: In our search for therapeutical alternatives for antiprotozoal chemotherapy, we collected a selection of 44 plants from western Colombia upon ethnopharmacological and chemotaxonomic considerations. Polar and apolar extracts of these species were examined for antimalarial activity using in vitro tests with two clones of Plasmodium falciparum. Leishmanicidal and trypanocidal activity were determined in vitro using promastigote and amastigote forms of several strains of Leishmania sp. and epimastigotes of Trypanosoma cruzi. Among the selected plants, the 15 following species showed good or very good antiprotozoal activity in vitro: Aspidosperma megalocarpon, Campnosperma panamense, Conobea scoparioides, Guarea polymera, Guarea guidonia, Guatteria amplifolia, Huberodendron patinoi, Hygrophila guianensis, Jacaranda caucana, Marila laxiflora, Otoba novogranatensis, Otoba parviflora, Protium amplium, Swinglea glutinosa and Tabernaemontana obliqua. Cytotoxicity was assessed in U-937 cells and the ratio of cytotoxicity to antiprotozoal activity was determined for the active extracts. Ten extracts from eight species showed selectivity indexes > or = 10. Among the extracts that showed leishmanicidal activity, the methylene chloride extract of leaves from C. scoparioides showed a selectivity index in the same range that the one of the Glucantime control. Several of the active leishmanicidal plants are traditionally used against leishmaniasis by the population of the concerned area.
Journal of Ethnopharmacology 01/2002; 78(2-3):193-200. · 3.01 Impact Factor
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ABSTRACT: We report the anti-Chagasic activity of the natural dihydrostilbenoid isonotholaenic acid and several simple derivatives, as well as that of some representative compounds of related synthetic series, with basic structures of benzalphthalides, dihydrostilbamides, isoindoles, phthalazin-1-ones, imidazo[2,1-a]isoindoles and pyrimido[2,1-a]isoindoles. The evaluation was performed in vitro on cultures of epimastigote and trypomastigote forms of Trypanosoma cruzi. Some of the tested compounds resulted to be as potent as benznidazole (epimastigotes), and others were shown to be more active than gentian violet (trypomastigotes), used as reference drugs.
Bioorganic & Medicinal Chemistry Letters 11/2001; 11(20):2755-7. · 2.55 Impact Factor
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ABSTRACT: One hundred and twenty-five extracts of 122 different plant species traditionally used by the Tacana, a native community living in lowland forest at the base of the last foothills of the Cordillera Oriental of the Bolivian Andes, were screened for antimalarial activity in vitro on Plasmodium falciparum chloroquine resistant (D2) and sensitive strains (F32), and were evaluated in vivo on rodent malaria Plasmodium berghei. Five ethanolic stembark extracts showed marked activity either in vitro or in vivo, and only one of them, Bowdichia virgilioides being traditionally used against malaria, was active in vitro (IC50=1 microg/ml on both strains) and in vivo (51% at 100 mg/kg). Other active extracts were from Caesalpinia pluviosa bark displaying activity in vitro against chloroquine resistant strain (IC50 8.3 microg/ml), traditionally used against dysentery; two Lauraceae bark extracts, Nectandra aff. hihua and Licaria canella respectively used for construction purposes and against stomach ache, both displaying activity in vitro against P. falciparum sensible and resistant strains (IC50 around 4 microg/ml); finally, the bark of a strongly aromatic Burseraceae, Protium glabrescens exuding an anti-inflammatory and analgesic resin, was active in vivo only (61% at 100 mg/kg). Results are discussed in relation with Tacana traditional medicine.
Journal of Ethnopharmacology 10/2001; 77(1):91-8. · 3.01 Impact Factor
