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1.
Molecules ; 28(14)2023 Jul 11.
Artículo en Inglés | MEDLINE | ID: mdl-37513210

RESUMEN

The alkaloids isolated from Zanthoxylum rhoifolium have demonstrated great pharmacological potential; however, the toxic profiles of these extracts and fractions are still not well elucidated. This study evaluated the toxicity of the ethanol extract (EEZR) and neutral (FNZR) and alkaloid (FAZR) fractions. Chemical characterization was performed by chromatographic methods: thin-layer chromatography (TLC) and high-performance liquid chromatography coupled with diode array detection (HPLC-DAD). The cytotoxicity of the samples was evaluated in human hepatocellular carcinoma (HepG2) cells using the cell viability method (MTT) and mutagenicity by the Allium cepa assay (ACA). Alkaloids isolated from the species were selected for toxicity prediction using preADMET and PROTOX. The molecular docking of the topoisomerase II protein (TOPOII) was used to investigate the mechanism of cell damage. In the EEZR, FNZR, and FAZR, the presence of alkaloids was detected in TCL and HPLC-DAD analyses. These samples showed a 50% inhibitory concentration (IC50) greater than 400 µg/mL in HepG2 cells. In ACA, time- and concentration-dependent changes were observed, with a significant reduction in the mitotic index and an increase in chromosomal aberrations for all samples. Nuclear sprouts and a micronucleus of the positive control (PC) were observed at 10 µg/mL and in the FAZR at 30 µg/mL; a chromosomal bridge in FNZR was observed at 105 µg/mL, CP at a concentration of 40 µg/mL, and nuclear bud and mitotic abnormalities in the EEZR were observed at 170 µg/mL. The alkaloids with a benzophenanthridine were selected for the in silico study, as structural alterations demonstrated certain toxic effects. Molecular docking with topo II demonstrated that all alkaloids bind to the protein. In summary, the fractionation of Z. rhoifolium did not interfere with toxicity; it seems that alkaloids with a benzophenanthridine nucleus may be involved in this toxicity.


Asunto(s)
Alcaloides , Zanthoxylum , Humanos , Extractos Vegetales/toxicidad , Extractos Vegetales/química , Zanthoxylum/química , Simulación del Acoplamiento Molecular , Benzofenantridinas , Alcaloides/química , Etanol
2.
Molecules ; 28(14)2023 Jul 20.
Artículo en Inglés | MEDLINE | ID: mdl-37513429

RESUMEN

From Eleutherine plicata, naphthoquinones, isoeleutherine, and eleutherol were isolated, and previous studies have reported the antioxidant activity of these metabolites. The present work evaluated the role of oxidative changes in mice infected with Plasmodium berghei and treated with E. plicata extract, fraction, and isolated compounds, as well as to verify possible oxidative changes induced by these treatments. E. plicata extracts were prepared from powder from the bulbs, which were submitted to maceration with ethanol, yielding the extract (EEEp), which was fractionated under reflux, and the dichloromethane fraction (FDMEp) was submitted for further fractionation, leading to the isolation of isoeleutherine, eleutherine, and eleutherol. The antimalarial activity was examined using the suppressive test, evaluating the following parameters of oxidative stress: trolox equivalent antioxidant capacity (TEAC), thiobarbituric acid reactive substances (TBARS), and reduced glutathione (GSH). Furthermore, the molecular docking of naphthoquinones, eleutherol, eleutherine, and isoeleutherine interactions with antioxidant defense enzymes was investigated, which was favorable for the formation of the receptor-ligand complex, according to the re-rank score values. Eleutherine and isoeleutherine are the ones with the lowest binding energy for catalase (CAT), glutathione reductase (GR), and glutathione peroxidase (GPx1), showing themselves as possible targets of these molecules in the involvement of redox balance. Data from the present study showed that treatments with E. plicata stimulated an increase in antioxidant capacity and a reduction in oxidative stress in mice infected with P. berghei, with naphthoquinones being responsible for reducing oxidative changes and disease severity.


Asunto(s)
Antioxidantes , Naftoquinonas , Ratones , Animales , Antioxidantes/farmacología , Antioxidantes/metabolismo , Simulación del Acoplamiento Molecular , Estrés Oxidativo , Naftoquinonas/química , Catalasa/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/química , Glutatión/metabolismo , Glutatión Peroxidasa/metabolismo , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismo , Superóxido Dismutasa/metabolismo
3.
Nutrients ; 15(8)2023 Apr 21.
Artículo en Inglés | MEDLINE | ID: mdl-37111226

RESUMEN

Docosahexaenoic acid (DHA), also known as omega-3 (n-3) polyunsaturated fatty acid (PUFA), is a natural compound that has demonstrated pharmacological activity against several malignant neoplasms. Available cancer treatments cause side effects, affect healthy cells, reduce the quality of life of patients and may cause resistance to antineoplastics. For these reasons, the search for new therapies is continuous. This narrative review aimed to compile information on in vitro experiments that study the cytotoxic effect of DHA or molecules derived from DHA in tumor and nontumor cells. This was performed to highlight the potential of DHA as a strategy for cancer therapy and to gather information, which will help researchers plan experimental designs and develop research to discover effective therapies against cancer. In addition, studies were presented that demonstrate the dose of DHA that can treat patients with cancer. Thus, a search was conducted for articles on the SCOPUS and Web of Science platforms, published until 2022, that analyzed the action of DHA against breast, lung, colorectal, prostate, stomach and liver cancers. Cytotoxic effects were observed in tumor and nontumor cell lines, and these results varied with the type of cell line studied, drug concentration, incubation time and treatment combination, i.e., with DHA alone, combined with other drugs and with molecules derived from DHA. In patients with cancer, in all analyzed studies, DHA intake was associated with eicosapentaenoic acid (EPA) and/or proteins to aid chemotherapy, and with this procedure, tumor reduction, chemotherapy tolerance and muscle mass gain were obtained. This work contributes to the community by demonstrating the possible applicability of DHA in the pharmaceutical area of oncological therapies.


Asunto(s)
Antineoplásicos , Ácidos Grasos Omega-3 , Neoplasias , Masculino , Humanos , Ácidos Docosahexaenoicos , Calidad de Vida , Ácidos Grasos Omega-3/farmacología , Ácido Eicosapentaenoico/metabolismo , Antineoplásicos/farmacología , Neoplasias/tratamiento farmacológico
4.
Sci Rep ; 12(1): 8662, 2022 05 23.
Artículo en Inglés | MEDLINE | ID: mdl-35606396

RESUMEN

This study evaluated the morphological changes caused by fractions and subfractions, obtained from barks of Aspidosperna nitidum, against L. (L.) amazonensis promastigotes. The ethanolic extract (EE) obtained through the maceration of trunk barks was subjected to an acid-base partition, resulting the neutral (FN) and the alkaloid (FA) fractions, and fractionation under reflux, yielded hexane (FrHEX), dichloromethane (FrDCL), ethyl acetate (FrACoET), and methanol (FrMEOH) fractions. The FA was fractionated and three subfractions (SF5-6, SF8, and SF9) were obtained and analyzed by HPLC-DAD and 1H NMR. The antipromastigote activity of all samples was evaluated by MTT, after that, scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for the active fractions were performed. Chromatographic analyzes suggest the presence of alkaloids in EE, FN, FA, and FrDCL. The fractionation of FA led to the isolation of the indole alkaloid dihydrocorynantheol (SF8 fractions). The SF5-6, dihydrocorynantheol and SF-9 samples were active against promastigotes, while FrDCL was moderately active. The SEM analysis revealed cell rounding and changes in the flagellum of the parasites. In the TEM analysis, the treated promastigotes showed changes in flagellar pocket and kinetoplast, and presence of lipid inclusions. These results suggest that alkaloids isolated from A. nitidum are promising as leishmanicidal.


Asunto(s)
Alcaloides , Antiprotozoarios , Aspidosperma , Leishmania , Alcaloides/farmacología , Antiprotozoarios/química , Aspidosperma/química , Alcaloides Indólicos , Extractos Vegetales/química
5.
Molecules ; 28(1)2022 Dec 27.
Artículo en Inglés | MEDLINE | ID: mdl-36615425

RESUMEN

Cancer is a multifactorial organic dysfunction for which great efforts are being devoted in searching for new treatments and therapeutic adjuvants. Annona muricata is a fruit that has promising activity against several types of cancer, as it contains acetogenins, the metabolite group associated with this action. Thus, the objective of this study was to evaluate, in experimental models, the toxic behavior of an extract and fraction rich in acetogenins from A. muricata seeds and study the acetogenin, Annonacin, in silico. Phytochemical characterization was made by thin layer chromatography, spectroscopy in the infrared region and nuclear magnetic resonance. Toxicity was evaluated by tests of Allium cepa and Artemia salina, and in silico studies using the SwissDock servers DockThor, PharmMapper, ADMETLab, PreADME, Osiris and ProTox. The extract and fraction showed genotoxic activity against meristematic cells of A. cepa, reducing the mitotic index; however, the extract produced great deleterious effects on the system, even causing cell necrosis. In A. Saline, the extract was more toxic than the fraction, but both samples were considered toxic. Annonacin was effectively linked to complex I, and presented different activities regarding toxicity. Thus, the results of this study are promising, highlighting the anticancer potential of acetogenins.


Asunto(s)
Acetogeninas , Annona , Acetogeninas/farmacología , Acetogeninas/química , Annona/química , Semillas/química , Extractos Vegetales/química
6.
Sci Rep ; 11(1): 18283, 2021 09 14.
Artículo en Inglés | MEDLINE | ID: mdl-34521944

RESUMEN

This study investigated the acute and subacute toxicity of the ethanolic extract (EE) and alkaloid fraction (FA) from A. nitidum. The EE was obtained from trunk bark with ethanol, FA was obtained from the fractionation of EE. To test the acute toxicity, mice were divided into four groups, and the negative controls received water or aqueous solution of dimethyl sulfoxide, whereas the others received EE or FA (2000 mg/kg, orally, single dose). The same controls were used in the subacute trial. However, the animals were treated for 28 days, and the dose used was 1000 mg/kg per day of EE and FA. Daily clinical evaluations of the animals were performed. At the end of the experiment, hematological, biochemical, and histopathological assessments (liver, lung, heart, and kidney) were performed. In the acute and subacute toxicity studies, mice treated with EE and FA did not show any clinical changes, there were no changes in weight gain, hematological and biochemical parameters compared to the control groups (p > 0.05). In the histopathological examination, there was no abnormality in the organs of the treated animals. Therefore, EE and FA did not produce toxic effects in mice after acute and subacute treatment.


Asunto(s)
Alcaloides/toxicidad , Aspidosperma/toxicidad , Corteza de la Planta/toxicidad , Extractos Vegetales/toxicidad , Alcaloides/administración & dosificación , Alcaloides/aislamiento & purificación , Animales , Aspidosperma/química , Cromatografía Líquida de Alta Presión/métodos , Etanol , Masculino , Ratones , Ratones Endogámicos BALB C , Corteza de la Planta/química , Extractos Vegetales/administración & dosificación , Extractos Vegetales/aislamiento & purificación
7.
Toxicol Rep ; 8: 1480-1487, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34401358

RESUMEN

Eleutherine plicata has been shown to be a promising medicinal plant, and its activity has been associated with naphthoquinones. The present study aimed at evaluating the cytotoxicity, genotoxicity, and oral toxicity of the ethanol extract (EEEp), dichloromethane fraction (FDMEp) of E. plicata, and isoeleutherin. For the cytotoxicity evaluation, the viability test (MTT) was used. Genotoxicity was accessed through the Comet assay (alkaline version), acute and subacute oral toxicities were also evaluated. The antioxidant capacity of the samples in the wells where the cells were treated with E. plicata was evaluated. Furthermore, the participation of caspase-8 in the possible mechanism of action of isoeleutherin, eleutherin, and eleutherol was also investigated through a docking study. FDMEp and isoeleutherin were cytotoxic, with higher rates of DNA fragmentation observed for FDMEp and isoeleutherin, and all samples displayed higher antioxidant potential than the control. In the acute oral toxicity test, EEEp, FDMEp, and isoeleutherin did not cause significant clinical changes. In the subacute toxicity assay, EEEp and FDMEp also did not cause clinical, hematological, or biochemical changes. The three compounds bound similarly to caspase-8. Despite the results of cytotoxicity, in vitro studies demonstrated that the use of EEEp appears to be safe and cell death may involve its binding to caspase-8.

8.
Oxid Med Cell Longev ; 2020: 2360872, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33101584

RESUMEN

Parkinson's disease (PD) occurs in approximately 1% of the population over 65 years of age and has become increasingly more common with advances in age. The number of individuals older than 60 years has been increasing in modern societies, as well as life expectancy in developing countries; therefore, PD may pose an impact on the economic, social, and health structures of these countries. Oxidative stress is highlighted as an important factor in the genesis of PD, involving several enzymes and signaling molecules in the underlying mechanisms of the disease. This review presents updated data on the involvement of oxidative stress in the disease, as well as the use of antioxidant supplements in its therapy.


Asunto(s)
Antioxidantes/farmacología , Estrés Oxidativo/efectos de los fármacos , Enfermedad de Parkinson/patología , Animales , Antioxidantes/uso terapéutico , Humanos , Enfermedad de Parkinson/tratamiento farmacológico , Fenoles/farmacología , Fenoles/uso terapéutico , Especies Reactivas de Oxígeno/metabolismo , Superóxido Dismutasa/metabolismo , Terpenos/farmacología , Terpenos/uso terapéutico , Ubiquinona/análogos & derivados , Ubiquinona/farmacología , Ubiquinona/uso terapéutico
9.
Molecules ; 24(4)2019 Feb 21.
Artículo en Inglés | MEDLINE | ID: mdl-30795632

RESUMEN

Chemotherapy is limited in the treatment of leishmaniasis due to the toxic effects of drugs, low efficacy of alternative treatments, and resistance of the parasite. This work assesses the in vitro activity of flavopereirine on promastigote cultures of Leishmania amazonensis. In addition, an in silico evaluation of the physicochemical characteristics of this alkaloid is performed. The extract and fractions were characterized by thin-layer chromatography and HPLC-DAD, yielding an alkaloid identified by NMR. The antileishmanial activity and cytotoxicity were assayed by cell viability test (MTT). The theoretical molecular properties were calculated on the Molinspiration website. The fractionation made it possible to isolate a beta-carboline alkaloid (flavopereirine) in the alkaloid fraction. Moreover, it led to obtaining a fraction with greater antileishmanial activity, since flavopereirine is very active. Regarding the exposure time, a greater inhibitory effect of flavopereirine was observed at 24 h and 72 h (IC50 of 0.23 and 0.15 µg/mL, respectively). The extract, fractions, and flavopereirine presented low toxicity, with high selectivity for the alkaloid. Furthermore, flavopereirine showed no violation of Lipinski's rule of five, showing even better results than the known inhibitor of oligopeptidase B, antipain, with three violations. Flavopereirine also interacted with residue Tyr-499 of oligopeptidase B during the molecular dynamics simulations, giving a few insights of a possible favorable mechanism of interaction and a possible inhibitory pathway. Flavopereirine proved to be a promising molecule for its antileishmanial activity.


Asunto(s)
Antiprotozoarios/farmacología , Apocynaceae/química , Carbolinas/farmacología , Alcaloides Indólicos/aislamiento & purificación , Leishmania mexicana/efectos de los fármacos , Proteínas Protozoarias/antagonistas & inhibidores , Serina Endopeptidasas/química , Antipaína/química , Antipaína/farmacología , Antiprotozoarios/química , Antiprotozoarios/aislamiento & purificación , Carbolinas/química , Carbolinas/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Humanos , Alcaloides Indólicos/química , Alcaloides Indólicos/clasificación , Concentración 50 Inhibidora , Leishmania mexicana/crecimiento & desarrollo , Estadios del Ciclo de Vida/efectos de los fármacos , Estadios del Ciclo de Vida/fisiología , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Corteza de la Planta/química , Extractos Vegetales/química , Proteínas Protozoarias/química , Células THP-1
10.
Artículo en Inglés | MEDLINE | ID: mdl-28286535

RESUMEN

This study aimed to evaluate the leishmanicidal activity of ethanol extract, fractions, and isolated substance from Handroanthus serratifolius against Leishmania amazonensis. Furthermore, this activity was related to cytotoxicity, and the selectivity index was determined. The ethanol extract was obtained by maceration of the stem powder, and the extract was subjected to fractionation on chromatographic column. The lapachol was obtained by acid base extraction followed by purification in chromatographic column. The antipromastigote activity and cytotoxicity tests were carried out by the cell viability method (MTT). Modified THP-1 cells were infected with L. amazonensis promastigotes and treated for 24 h with different concentrations of the extract, fractions, and lapachol. The ethanol extract, dichloromethane, and ethyl acetate fractions were not active against promastigotes (IC50 > 200 µg/mL) or cytotoxic (CC50 > 500 µg/mL), and the selectivity index (SI) was greater than 2.5. The ethyl acetate fraction was active only in promastigotes; it is not cytotoxic (CC50 > 500 µg/mL, SI > 5). The lapachol was selectively active only against amastigote (IS > 2.5, CC50 > 500 µg/mL). In summary, lapachol and ethyl acetate fraction are promising against amastigote and promastigote forms, respectively.

11.
Artículo en Inglés | MEDLINE | ID: mdl-28194218

RESUMEN

The present study describes the use of the traditional species Copaifera for treating wounds, such as ulcers scarring and antileishmanial wounds. It also relates phytochemical studies, evaluation of the leishmanicidal activity, and toxicity. The species of Copaifera with a higher incidence in the Amazon region are Copaifera officinalis, Copaifera reticulata, Copaifera multijuga Hayne. The copaiba oil is used in the Amazon's traditional medicine, especially as anti-inflammatory ingredient, in ulcers healing, and in scarring and for leishmaniasis. Chemical studies have shown that these oils contain diterpenes and sesquiterpenes. The copaiba oil and terpenes isolated have antiparasitic activity, more promising in the amastigote form of L. amazonensis. This activity is probably related to changes in the cell membrane and mitochondria. The oil showed low cytotoxicity and genotoxicity. Furthermore, it may interfere with immune response to infection and also has a healing effect. In summary, the copaiba oil is promising as leishmanicidal agent.

12.
Acta amaz ; 46(1): 69-72, jan./mar. 2016. ilus
Artículo en Inglés | LILACS, VETINDEX | ID: biblio-1455283

RESUMEN

Endophytic fungi are fungi that colonize internal tissues of plants. There are few studies of compounds isolated from endophytic fungi of Amazon plants. Thus, the aim this study was the isolation and structural identification of sitosterol (1), stigmasterol (2), sitostenone (3), squalene (4), ergosterol (5) and ergosterol peroxide (6) from fungus Colletotrichum gloeosporioidesisolated as endophytic from Virola michelli, a typical Amazon plant, used in folk medicine against skin infection. Compounds were isolated by chromatography column on silica and identified by 1H and 13C NMR and MS. The presence of phytosterols in fungi is rare and this is the first report of the isolation of the phytosterols sitosterol, stigmasterol and sitostenone from the genus Colletotrichum.


Fungos endofíticos são fungos que colonizam os tecidos internos das plantas. Existem poucos estudos de compostos isolados de fungos endofíticos de plantas da Amazônia. Assim, o objetivo deste estudo foi o isolamento e identificação estrutural de sitosterol (1), estigmasterol (2), sitostenona (3), esqualeno (4), ergosterol (5) e peroxido de ergosterol (6) do fungo Colletotrichum gloeosporioidesisolado como endofítico de Virola michelli, uma planta típica da Amazônia, usada na medicina popular no combate a infecções de pele. Os compostos foram isolados por cromatografia em coluna de sílica e identificados por RMN 1H e 13C e EM. A presença de fitoesteróis em fungos é rara e este é o primeiro relato do isolamento dos fitoesteróides sitosterol, estigmasterol e sitostenona do gêreno Colletotrichum.


Asunto(s)
Animales , Colletotrichum/química , Endófitos , Fitosteroles/aislamiento & purificación , Myristicaceae , Esteroides , Hongos
13.
Malar J ; 14: 202, 2015 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-25971771

RESUMEN

BACKGROUND: Malaria infection can cause high oxidative stress, which could lead to the development of severe forms of malaria, such as pulmonary malaria. In recent years, the role of reactive oxygen species in the pathogenesis of the disease has been discussed, as well as the potential benefit of antioxidants supplementation. The aim of this study was to investigate the effects of N-acetyl cysteine (NAC) or mushroom Agaricus sylvaticus supplementation on the pulmonary oxidative changes in an experimental model of malaria caused by Plasmodium berghei strain ANKA. METHODS: Swiss male mice were infected with P. berghei and treated with NAC or AS. Samples of lung tissue and whole blood were collected after one, three, five, seven or ten days of infection for the assessment of thiobarbituric acid reactive substances (TBARS), trolox equivalent antioxidant capacity (TEAC), nitrites and nitrates (NN) and to assess the degree of parasitaemia. RESULTS: Although parasitaemia increased progressively with the evolution of the disease in all infected groups, there was a significant decrease from the seventh to the tenth day of infection in both antioxidant-supplemented groups. Results showed significant higher levels of TEAC in both supplemented groups, the highest occurring in the group supplemented with A. sylvaticus. In parallel, TBARS showed similar levels among all groups, while levels of NN were higher in animals supplemented with NAC in relation to the positive control groups and A. sylvaticus, whose levels were similar to the negative control group. CONCLUSION: Oxidative stress arising from plasmodial infection was attenuated by supplementation of both antioxidants, but A. sylvaticus proved to be more effective and has the potential to become an important tool in the adjuvant therapy of malaria.


Asunto(s)
Acetilcisteína/farmacología , Agaricus/química , Suplementos Dietéticos/análisis , Malaria/dietoterapia , Estrés Oxidativo/efectos de los fármacos , Plasmodium berghei/fisiología , Acetilcisteína/administración & dosificación , Animales , Modelos Animales de Enfermedad , Pulmón/efectos de los fármacos , Malaria/parasitología , Masculino , Ratones , Parasitemia/dietoterapia , Parasitemia/parasitología
14.
Cell Mol Neurobiol ; 35(5): 595-614, 2015 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-25616523

RESUMEN

The risk of chronic diseases such as Alzheimer's disease is growing as a result of the continuous increasing average life span of the world population, a syndrome characterized by the presence of intraneural neurofibrillary tangles and senile plaques composed mainly by beta-amyloid protein, changes that may cause a number of progressive disorders in the elderly, causing, in its most advanced stage, difficulty in performing normal daily activities, among other manifestations. Therefore, it is important to understand the underlying pathogenic mechanisms of this syndrome. Nevertheless, despite intensive effort to access the physiopathological pathways of the disease, it remains poorly understood. In that context, some hypotheses have arisen, including the recent oxidative stress hypothesis, theory supported by the involvement of oxidative stress in aging, and the vulnerability of neurons to oxidative attack. In the present revision, oxidative changes and redox mechanisms in Alzheimer's disease will be further stressed, as well as the grounds for antioxidant supplementation as adjuvant therapy for the disease will be addressed.


Asunto(s)
Enfermedad de Alzheimer/tratamiento farmacológico , Enfermedad de Alzheimer/patología , Antioxidantes/uso terapéutico , Estrés Oxidativo , Enfermedad de Alzheimer/fisiopatología , Péptidos beta-Amiloides/metabolismo , Animales , Antioxidantes/farmacología , Suplementos Dietéticos , Humanos , Modelos Biológicos , Estrés Oxidativo/efectos de los fármacos
15.
Planta Med ; 80(5): 378-86, 2014 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-24590399

RESUMEN

Several plant species belonging to the genus Aspidosperma are traditionally used in Brazil and other Meso- and South American countries for the treatment of malaria and fevers. These traditional uses were motivation for this review. A literature survey completed for this review has identified scientific bibliographical references to the use of 24 Aspidosperma species to treat malaria/fevers and to 19 species that have had their extracts and/or alkaloids evaluated, with good results, for in vitro and/or in vivo antimalarial activity. Indole alkaloids are typical constituents of Aspidosperma species. However, only 20 out of more than 200 known indole alkaloids isolated from this genus have been assayed for antimalarial activity. These data support the potential of Aspidosperma species as sources of antimalarials and the importance of research aimed at validating their use in the treatment of human malaria.


Asunto(s)
Antimaláricos/farmacología , Aspidosperma/química , Medicina Tradicional , Extractos Vegetales/farmacología , Humanos , América del Sur
16.
An Acad Bras Cienc ; 84(4): 899-910, 2012 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-23207699

RESUMEN

Ethnomedicinal informations point to some Aspidosperma species (Apocynaceae) as antimalarial plants in Brazil and have motivated the evaluation of six species which were collected in the state of Minas Gerais: A. cylindrocarpon Müll. Arg., A. parvifolium A. DC., A. olivaceum Müll. Arg., A. ramiflorum Müll. Arg., A. spruceanum Benth. ex Müll. Arg. and A. tomentosum Mart.. A total of 23 extracts of different plant parts in different solvents were assayed in vitro against chloroquine-resistant (W2) and chloroquine-sensitive (3D7) strains of Plasmodium falciparum. All the extracts were shown to be active with IC50 values in the range of 5.0 ± 0 2.8 µg/mL to 65.0 ± 4.2 µg/mL. TLC profile of the extracts revealed the presence of alkaloids in the six species assayed. These results seem to confirm the popular use of Aspidosperma species to treat human malaria in Brazil and seem point to alkaloids as the putative active compounds of the assayed species.


Asunto(s)
Antimaláricos/farmacología , Aspidosperma/química , Extractos Vegetales/farmacología , Plasmodium falciparum/efectos de los fármacos , Aspidosperma/clasificación , Humanos , Concentración 50 Inhibidora , Pruebas de Sensibilidad Parasitaria
17.
J Ethnopharmacol ; 142(3): 679-83, 2012 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-22659195

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: From seeds of Carapa guianensis the Amazon native people extracts the andiroba oil, which is traditionally used as febrifuge, anti-malarial, insecticidal and repellant. The non-saponifiable fraction separated from the oil is rich in limonoids, which assigns its pharmacological effects. MATERIALS AND METHODS: The andiroba oil and its limonoid-rich fraction were submitted to in vitro antiplasmodial bioassay using W(2) and Dd(2) strains of Plasmodium falciparum. The acute toxicity of andiroba oil was evaluated. The limonoid-rich fraction was subjected to fractionation and identified its major constituents. RESULTS: Andiroba oil and its limonoid-rich fraction inhibited the growth of W(2) clone in 100%, between 24 and 72 h, at concentrations of 8.2 µg/mL and 3.1 µg/mL, respectively. Under the same conditions, the parasitaemia of Dd(2) clone provoked by the andiroba oil showed inhibition of 31% (IC(50) >82 µg/mL) with a time-dependent relationship of 24h and inhibition of 88% (IC(50) 8.4 µg/mL) after 72 h, while for the limonoid-rich fraction the inhibition of Dd(2) clone was 56% (IC(50) 2.8µg/mL) at 24h and 82% (IC(50) 0.4 µg/mL) after 72 h. Andiroba oil in acute toxicity test with a fixed dose (LD(50) >2000 mg/kg) was not toxic The limonoids identified in the oil were gedunin, 6α-acetoxygedunin, 7-deacetoxy-7-oxogedunin, 7-deacetylgedunin, 1,2-dihydro-3ß-hydroxy-7-deacetoxy-7-oxogedunin and andirobin. Gedunin and derivatives has been reputed as anti-malarials. CONCLUSION: The results support the traditional use of andiroba oil as antiplasmodial, which additionally proved not to be toxic in bioassays conducted with mice.


Asunto(s)
Antimaláricos/farmacología , Limoninas/farmacología , Meliaceae , Aceites de Plantas/farmacología , Animales , Antimaláricos/química , Antimaláricos/toxicidad , Eritrocitos/microbiología , Femenino , Limoninas/análisis , Limoninas/toxicidad , Ratones , Aceites de Plantas/química , Aceites de Plantas/toxicidad , Plasmodium falciparum/efectos de los fármacos
18.
Acta amaz ; 41(3): 431-434, 2011. ilus, tab
Artículo en Portugués | LILACS, VETINDEX | ID: lil-595563

RESUMEN

Montrichardia linifera é uma planta aquática de amplo uso na medicina tradicional amazônica. Entretanto, muito pouco se conhece sobre a sua composição química, e sua atividade biológica ainda não foi comprovada. Na busca de substância(s) biologicamente ativa(s), este trabalho realizou um estudo fitoquímico biomonitorado no qual foram testados os extratos hexânico e etanólico obtidos do caule desta espécie, dos quais apenas o extrato etanólico foi selecionado para o fracionamento cromatográfico por ter apresentado toxicidade contra a Artemia salina e atividade contra o Plasmodium falciparum, parasita causador da malária. As atividades biológicas concentraram-se na fração diclorometânica que apresentou alta toxicidade contra A. salina (DL50<31µg mL-1) e alta atividade antiplasmódica (IC50<10 µg mL-1), mostrando promissora atividade antimalárica. Desta fração, o composto aromático p-hidroxibenzaldeído foi isolado pela primeira vez nesta planta.


Montrichardia linifera is an aquatic plant widely use in Amazon folkmedicine. However, very little is known about the chemical composition and biological activity. In search of biologically active (s) substance (s) phytochemical bioassay-guided study was conducted evaluating hexane extract and ethanol extract obtained from stems of this species. Since only the ethanol extract presented toxicity against Artemia salina and activity against Plasmodium falciparum, this extract was selected for chromatographic fractionation. The biological activities were concentred in dichloromethane fraction which showed high toxicity against A. saline (LD50< µg mL-1) and high antiplasmodial activity (IC50 <10 µg mL-1), showing promising antimalarial activity. Of this fraction, the aromatic compound p-hydroxybenzaldehyde was isolated for the first time in this plant.


Asunto(s)
Toxicidad
19.
Rev. cuba. plantas med ; 15(2): 66-74, abr.-jun. 2010.
Artículo en Español | LILACS | ID: lil-585077

RESUMEN

INTRODUCIÓN: de acuerdo con la Secretaria Municipal de Economía, la ciudad de Belém, Pará, Brasil, tiene 53 establecimientos entre mercadillos y mercados, distribuidos en diferentes barrios y distritos. De estos, 22 de gran escala, 10 de mediana y 16 de pequeña. Por otra parte, 13 están en distritos distantes del centro de la ciudad, en Icoaraci, Outeiro y Mosqueiro. OBJETIVO: se evaluaron las condiciones de la comercialización de las plantas medicinales en estos mercados y mercadillos. MÉTODOS: se visitaron 15 mercados y(o) mercadillos; después de visitados, 7 fueron excluidos porque no tenían las tiendas de comercialización de las plantas medicinales, por lo tanto, apenas 8 quedaron como muestra de la investigación. Se caracterizaron de acuerdo con su estructura fisica y condiciones higiénico-sanitarias. RESULTADOS: de los mercados y(o) mercadillos estudiados, en relación con la estructura física, la mayor parte (85 por ciento) era de madera. En lo referente a las condiciones higiénico-sanitarias, se observó: bancas al lado de las alcantarillas (25 por ciento), en los lugares cuya basura fue exhibida después y(o) debajo a los tableros (50 por ciento); al lado de los tableros que comercializaron la carne (14 por ciento); próximos a la preparación de las comidas (6 por ciento); y uso de agua contaminada para mojar los vegetales (74 por ciento). También se observó la incidencia fuerte de la luz en las plantas (14 por ciento), el condicionamiento en las botellas reaprovechables de productos industrializados (99 por ciento). Además, las plantas se mezclaron entre sí (61 por ciento), así como con productos de otros orígenes (100 por ciento). CONCLUSIONES: se considera que existe un riesgo potencial para estos productos.


INTRODUCTION: according to Economy Municipal Secretariat, the city of Belem, Pará, Brazil has 53 setting ups between flea markets and markets, distributed in different areas and districts. From these, 22 on a large scale, 10 on middle scale and 16 on a small scale. Besides, 13 are located in districts far away from the town center in Icoaraci, Outeiro and Mosqueiro. OBJECTIVE: marketing conditions of medicinal plants in these flea markets and markets were assessed. METHODS: authors went visiting 15 markets and /or flea markets after this visit 7 were ruled out due to the lack of suitable medicinal plant marketing shops, thus, only remained 8 as a research sample. They were characterized according its physical structure and hygienic-sanitary conditions. RESULTS: from the study markets and/or flea markets related to the physical structure, most (85 percent) was of wooden. In relation to the hygienic-sanitary conditions there were benches besides the sewers (25 percent) in places where garbage was at sight and/or under the boards (50 percent); besides the boards for meat marketing (14 percent); close to the food preparation (6 percent) and use of polluted water to wash the vegetables (74 percent). Also, there was a strong light incidence on the plants (14 percent), the conditioning in the reusable bottles of industrial products (99 percent). Also, the plants were mixed each other (61 percent), as well as with products of different origins (100 percent). CONCLUSIONS: there is a potential risk for these products.

20.
Rev. bras. farmacogn ; 19(4): 834-838, out.-dez. 2009. tab
Artículo en Portugués | LILACS | ID: lil-542696

RESUMEN

O presente trabalho descreve os resultados do estudo farmacognóstico, estudo fitoquímico preliminar, toxicidade em Artemia salina e atividade antiplasmódica contra cepa de Plasmodium falciparum resistente a cloroquina (W2) do extrato etanólico obtido do pó das folhas de Montrichardia linifera (Arruda) Schott, Araceae. Para realização dos estudos farmacognósticos utilizou-se as metodologias descritas na Farmacopéia Brasileira. A prospecção fitoquímica foi realizada pelos métodos descritos por Mattos. No ensaio antiplasmódico foi utilizado o microteste tradicional e no ensaio de Artemia salina. Os resultados obtidos nos estudos farmacognósticos do pó das folhas de M. linifera demonstraram tratar-se de um pó moderadamente grosso, com teores de água e cinzas totais dentro dos limites aceitáveis, baixa densidade (0,324 e 0,339 g/mL), pH próximo de neutro (6,69±0,02). A análise fitoquímica preliminar evidenciou a presença de alcaloides, flavonoides, taninos, triterpenos e esteroides. O extrato etanólico das folhas de M. linifera apresentou moderada atividade antiplasmódica e baixa toxicidade para a Artemia salina.


The present paper describes results of a pharmacognostic, a preliminary phytochemical study, brine shrimp toxicity and antiplasmodic activity in a strain of Plasmodium falciparum that is resistant to chloroquine (W2) using ethanolic extract obtained from powder of the leaves of Montrichardia linifera (Arruda) Schott, Araceae. To perform the pharmacognostic studies methodologies employed in the Brazilian Pharmacopoea were utilized. The methods described by Mattos were utilized for phytochemical prospecting. In the antiplasmodic test the traditional microtest was employed, as well as in the test with brine shrimp. The results obtained in the pharmacognostic studies with the powder from M. linifera leaves showed that it was a moderate thick powder, with water and ash totals within acceptable limits, low density (0.324 and 0.339 g/mL), pH close to neutral (6.69 ± 0.02). Preliminary phytochemical analysis showed the presence of alkaloids, flavonoids, tannins, triterpenes and esters. The ethanolic extract from M. linifera leaves presented moderate antiplasmodic activity and low brine shrimp toxicity. To summarize, the powder used in preparing the extract presented good quality in pharmacognostic terms.

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