RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: 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. MATERIALS AND METHODS: Mice received mitraphylline once a day for 3 days at 30 mg/kg/day by oral route. Then, they were subjected to bacterial lipopolysaccharide (LPS) endotoxin (15 mg/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 100 µM was monitored by XTT-colorimetric assay. RESULTS AND CONCLUSIONS: 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, 1ß, 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 100 µM.
Assuntos
Anti-Inflamatórios/farmacologia , Unha-de-Gato , Alcaloides Indólicos/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Citocinas/sangue , Feminino , Lipopolissacarídeos , Macrófagos Peritoneais/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos BALB C , Oxindóis , Casca de Planta/químicaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The study of traditional remedies used by the Chayahuita, an ethnic group from the Peruvian Amazonia, has prompted us to investigate in detail the ethanolic extract of Pseudelephantopus spicatus (Juss. ex Aubl.) C.F. Baker, which has demonstrated strong biological activity towards Leishmania amazonensis. Our goal was to discover the active compound of this plant-based remedy. MATERIALS AND METHODS: A bioguided fractionation of the crude extract was undertaken based on the biological activity recorded against Leishmania amazonensis axenic amastigotes in in vitro bioassays. RESULTS: Three strongly to moderately active compounds were isolated: two hirsutinolides (the 8,13-diacetyl-piptocarphol and the 8-acetyl-13-O-ethyl-piptocarphol) and ursolic acid. IC(50) against Leishmania amazonensis axenic amastigotes are respectively 0.2, 0.37 and 0.99 µM (while IC(50) of amphotericin B is 0.41 µM). These compounds have never been isolated from this plant species, and germacranolides have never been identified as potential antileishmanial agents. CONCLUSIONS: The compounds isolated from Pseudelephantopus spicatus account for the antileishmanial activity of the plant, thus giving support to its use by the Chayahuita in Peru.
Assuntos
Asteraceae , Lactonas/farmacologia , Leishmania/efeitos dos fármacos , Extratos Vegetais/farmacologia , Sesquiterpenos/farmacologia , Tripanossomicidas/farmacologia , Anfotericina B/farmacologia , Asteraceae/química , Fracionamento Químico , Relação Dose-Resposta a Droga , Humanos , Indígenas Sul-Americanos , Concentração Inibidora 50 , Lactonas/química , Lactonas/isolamento & purificação , Leishmania/crescimento & desenvolvimento , Medicina Tradicional , Peru , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Triterpenos/farmacologia , Tripanossomicidas/química , Tripanossomicidas/isolamento & purificação , Ácido UrsólicoRESUMO
AIM OF THE STUDY: 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. MATERIALS AND METHODS: 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. RESULTS: 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/mlAssuntos
Conhecimentos, Atitudes e Prática em Saúde
, Leishmania/efeitos dos fármacos
, Leishmaniose/tratamento farmacológico
, Leishmaniose/etnologia
, Medicina Tradicional
, Humanos
, Testes de Sensibilidade Microbiana/métodos
, Peru/etnologia
, Fitoterapia
, Plantas Medicinais
RESUMO
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.
Assuntos
Antimaláricos/uso terapêutico , Países em Desenvolvimento , Malária/prevenção & controle , Medicina Tradicional , Etnobotânica , Humanos , Malária/tratamento farmacológico , Plantas Medicinais , PesquisaRESUMO
AIM OF THE STUDY: 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. MATERIAL AND METHODS: A colorimetric method based on the reduction of tetrazolium salt (MTT) was used to measure the viability of Leishmania amazonensis promastigote and amastigote stages. RESULTS AND CONCLUSIONS: 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.
Assuntos
Antiprotozoários/farmacologia , Leishmania mexicana/efeitos dos fármacos , Plantas Medicinais/química , Anfotericina B/farmacologia , Animais , Colorimetria , Avaliação Pré-Clínica de Medicamentos , Etnobotânica , Etnofarmacologia , Humanos , Indígenas Sul-Americanos , Indicadores e Reagentes , Leishmania mexicana/crescimento & desenvolvimento , Meglumina/farmacologia , Peru , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/classificação , Sais de Tetrazólio , TiazóisRESUMO
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.
Assuntos
Etnofarmacologia , Medicina Tradicional , Farmácia/instrumentação , Quassia , Madeira/análise , Cromatografia Líquida de Alta Pressão , História do Século XIX , História do Século XX , Humanos , Teste de Materiais , Medicina Tradicional/história , Microscopia , SurinameRESUMO
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.
Assuntos
Antimaláricos/farmacologia , Bebidas , Dessecação , Malária/tratamento farmacológico , Plasmodium falciparum/efeitos dos fármacos , Plasmodium yoelii , Quassia/crescimento & desenvolvimento , Animais , Antimaláricos/química , Antimaláricos/normas , Antimaláricos/uso terapêutico , Cromatografia Líquida de Alta Pressão , Guiana Francesa , Malária/parasitologia , Camundongos , Testes de Sensibilidade Parasitária , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/crescimento & desenvolvimento , Controle de Qualidade , Quassia/química , Quassinas/análiseRESUMO
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.
Assuntos
Antimaláricos/farmacologia , Fitoterapia , Plasmodium falciparum/efeitos dos fármacos , Quassia/química , Quassinas/química , Quassinas/farmacologia , Animais , Antimaláricos/química , Bebidas , Guiana Francesa , Medicina Tradicional , Estrutura Molecular , Roedores/parasitologiaRESUMO
Antimalarial activity of 10 vegetal extracts (9 ethanolic extracts and 1 crude alkaloid extract), obtained from eight species traditionally used in Colombia to treat malaria symptoms, was evaluated in culture using Plasmodium falciparum chloroquine resistant (FcB2) strain and in vivo on rodent malaria Plasmodium berghei. The activity on ferriprotoporphyrin biomineralization inhibition test (FBIT) was also assessed. Against Plasmodium falciparum, eight extracts displayed good activity Abuta grandifolia (Mart.) Sandwith (Menispermaceae) leaves, Acacia farnesiana (L.) Willd. (Mimosaceae) leaves, Acnistus arborescens (L.) Schltdl. (Solanaceae) aerial part, Croton leptostachyus Kunth (Euphorbiaceae) aerial part, Piper cumanense Kunth (Piperaceae) fruits and leaves, Piper holtonii C. DC. (Piperaceae) aerial part and Xylopia aromatica (Lam.) Mart. (Annonaceae) bark with IC(50) values ranging from <1 to 2.1 microg/ml, while in the in vivo model only Abuta grandifolia alkaloid crude extract exhibits activity, inhibiting 66% of the parasite growth at 250 mg/kg/day. In the FBIT model, five extracts were active (Abuta grandifolia, Croton leptostachyus, Piper cumanense fruit and leaves and Xylopia aromatica).
Assuntos
Antimaláricos/farmacologia , Malária/tratamento farmacológico , Plantas Medicinais , Plasmodium berghei , Plasmodium falciparum/efeitos dos fármacos , Animais , Antimaláricos/uso terapêutico , Colômbia , Hemina/metabolismo , Testes de Sensibilidade Parasitária , Extratos Vegetais/farmacologia , Plasmodium/efeitos dos fármacos , Plasmodium/metabolismo , Plasmodium falciparum/crescimento & desenvolvimento , RoedoresRESUMO
Zanthoxylum rhoifolium bark (Rutaceae) is a medicinal plant, traditionally used in French Guiana to treat and prevent malaria. Bioassay-guided extractions of Zanthoxylum rhoifolium bark have shown that antiplasmodial activity is concentrated in the alkaloid fraction. Further fractionation of this extract has yielded seven benzophenanthridine alkaloids, dihydroavicine 1, dihydronitidine 2, oxyavicine 3, oxynitidine 4, fagaridine 5, avicine 6 and nitidine 7. Antimalarial activity of the last five compounds has been evaluated, and nitidine was the most potent, displaying an IC(50)<0.27microM against Plasmodium falciparum. Investigation of the traditional remedy, a trunk bark decoction in water, has shown that fagaridine 5, avicine 6 and nitidine 7 are also present in the decoction, therefore justifying the traditional use of Zanthoxylumrhoifolium bark as antimalarial.