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Braz. arch. biol. technol ; 64: e21200163, 2021. tab, graf
Article in English | LILACS | ID: biblio-1153296


HIGHLIGHTS Isolate, fractionate and characterize extracts obtained from soursop leaves. Use of emerging green technologies such as microwave-ultrasound hybridization. The extracts contain kaempferol, procyanidins, catechin, and quercetin. The total ethanolic extract demonstrates cytotoxic effect on HeLa cells.

Abstract Cervical cancer is classified as the fourth most common malignancy in women. Natural compounds are a therapeutic alternative in cancer therapy. The aim of the study is to isolate, fractionate, and characterize extracts obtained from soursop leaves (Annona muricata L.) and determine their cytotoxic effect against HeLa cervical cancer cells and non-carcinogenic fibroblast 3T3 cells. The phytochemicals of soursop leaves were extracted through emerging green technologies such as the novel use of microwave-ultrasound hybridization and the use of environmentally friendly solvents (water and ethanol), in addition to the purification of extracts enriched in polyphenols by liquid chromatography with Amberlite XAD-16. Total aqueous and ethanolic extract were purified, as well as the fraction one of each extract. The extracts recovered from soursop leaves contained kaempferol and its isomers, procyanidins, catechin, and quercetin. The viability of the cells was determined with the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. HeLa and 3T3 cells were exposed to concentrations of 25, 50, 75, 100, 150, 200, and 250 ppm of a solution of soursop leaf extract powder. The MTT assay showed that soursop leaf extracts were toxic to both cell lines in general, however, the ethanolic extract at 25 and 50 ppm demonstrated inhibition in cell viability against the HeLa cancer line and low cytotoxicity for 3T3 fibroblast cells. In conclusion, the novel microwave-ultrasound hybridization technology allows the extraction of polyphenols that may have a potential cytotoxic effect on cancer cells.

Humans , Female , HeLa Cells , Annona/chemistry , Polyphenols/isolation & purification , Phytochemicals/pharmacology , Antineoplastic Agents, Phytogenic/isolation & purification , Plant Extracts/pharmacology , Catechin/chemistry , Chromatography, Liquid/methods , Ethanol , Antineoplastic Agents, Phytogenic/pharmacology
Rev. chil. nutr ; 47(2): 281-285, abr. 2020. tab
Article in English | LILACS | ID: biblio-1115499


Synthetic preservatives are widely present in processed foods, but most of them have carcinogenic potential, requiring the development of new natural alternatives such as fruit extracts, for microbial control. The objective of the study was to evaluate the chemical characterization, antioxidant, and antimicrobial activity of the sugar apple pulp (Annona squamosa L.). Physicochemical characteristics were evaluated, an extract was prepared, and its antioxidant activity by DPPH method and antimicrobial by disk diffusion. Minimal inhibitory concentration and minimum bactericidal concentration against strains of Salmonella typhimurium, Escherichia coli, Listeria monocytogenes, and Staphylococcus aureus were evaluated. The physicochemical analysis revealed that sugar apple pulp had 75.0% moisture, 3.0% ash, 4.0% protein, 0.2% lipids, 3.3% fibers, and 14.5% carbohydrates. The antioxidant activity of the extract by the DPPH method was 20.6%. The pulp extract from the sugar apple had inhibition zone for Staphylococcus aureus, satisfactory inhibitory effect against Staphylococcus aureus, Escherichia coli, Listeria monocytogenes, and Salmonella Typhimurium, but did not present a bactericidal effect. Sugar apple pulp presents adequate levels of nutrients and potential for food application due to its microbiological activity and antioxidant properties.

Los conservantes sintéticos están ampliamente presentes en los alimentos procesados, pero la mayoría tienen potencial carcinogénico, lo que requiere el desarrollo de nuevas alternativas naturales para el control microbiano, como los extractos de frutas. El objetivo del estudio fue evaluar la caracterización química, la actividad antioxidante y antimicrobiana de la pulpa de manzana de azúcar (Annona squamosa L.). Se evaluaron las características fisicoquímicas, y se evaluó su actividad antioxidante mediante el método DPPH y antimicrobiano por difusión en disco, concentración inhibitoria mínima y concentración bactericida mínima contra cepas de Salmonella Typhimurium, Escherichia coli, Listeria monocytogenes y Staphylococcus aureus. El análisis fisicoquímico reveló que la pulpa de manzana de azúcar tiene 75.0% de humedad, 3.0% de cenizas, 4.0% de proteínas, 0.2% de lípidos, 3.3% de fibras y 14.5% de carbohidratos. La actividad antioxidante del extracto por el método DPPH fue del 20.6%. El extracto de pulpa de la manzana de azúcar tenía zona de inhibición para Staphylococcus aureus, efecto inhibidor satisfactorio contra Staphylococcus aureus, Escherichia coli, Listeria monocytogenes y Salmonella Typhimurium, pero no presenta efecto bactericida. La pulpa de manzana de azúcar presenta niveles adecuados de nutrientes y potencial para la aplicación de alimentos debido a su actividad microbiológica y propiedades antioxidantes.

Plant Extracts/pharmacology , Annona/chemistry , Anti-Bacterial Agents/pharmacology , Antioxidants/pharmacology , Salmonella typhimurium/drug effects , Staphylococcus aureus/drug effects , Carbohydrates/analysis , Plant Extracts/chemistry , Proteins/analysis , Microbial Sensitivity Tests , Escherichia coli/drug effects , Lipids/analysis , Listeria monocytogenes/drug effects , Anti-Bacterial Agents/chemistry , Antioxidants/chemistry
Rev. Soc. Bras. Med. Trop ; 53: e20190139, 2020. graf
Article in English | LILACS | ID: biblio-1057288


Abstract INTRODUCTION: Leishmaniasis, a disease caused by a parasite endemic to large areas of tropical and subtropical countries, is a growing public health problem. METHODS: Male BALB/c mice were infected with Leishmania amazonensis and treated with extracts isolated from Annona mucosa. RESULTS: Treated groups had significantly reduced footpad swelling. The group treated intraperitoneally with hexane extract showed footpad swelling similar to groups treated with Pentamidine® and Glucantime®. Groups treated with dichloromethane extract and hexane extract presented the recovering phenotype associated with reduced parasite levels. CONCLUSIONS: Extracts of A. mucosa are promising sources of novel antileishmanial compounds.

Animals , Male , Plant Extracts/therapeutic use , Leishmaniasis, Cutaneous/drug therapy , Annona/chemistry , Leishmania/drug effects , Antiprotozoal Agents/therapeutic use , Leishmaniasis, Cutaneous/parasitology , Disease Models, Animal , Mice , Mice, Inbred BALB C , Antiprotozoal Agents/isolation & purification
Hig. aliment ; 31(272/273): 112-119, 30/10/2017.
Article in Portuguese | LILACS | ID: biblio-876334


Atualmente no Peru, o processamento para obter a polpa de cherimoia é muito delicado e complexo devido ao fato deste fruto precisar de condições específicas para evitar a sua deterioração durante a fabricação, pois a carga de micro-organismos não pode ser reduzida pela pasteurização por causar sérios problemas nas características sensoriais da polpa. Este trabalho apresenta e avalia oito novos tratamentos para o processo de polpa de cherimoia, com trocas focadas na etapa de descascamento termoquímico, a fim de melhorar sua qualidade microbiológica e manter suas características sensoriais. Os resultados mostraram que todos os tratamentos influenciaram na redução da carga dos micro-organismos indicadores de alteração, enquanto que coliformes totais, E. coli e Salmonella spp. não foram detectados nas amostras avaliadas, assegurando sua inocuidade. Nenhum dos tratamentos influenciou negativamente as características sensoriais, ficando conformes segundo as provas realizadas por um painel treinado e qualificado. Em relação aos processos com pasteurização, que geram alterações indesejáveis do sabor, cor e aroma na polpa de cherimoia, os novos processos com descascamento termoquímico apresentados nesta pesquisa conservaram a qualidade sensorial enquanto que melhoraram a qualidade microbiológica, representado assim boas alternativas na produção deste fruto a nível industrial.(AU)

Humans , Annona/chemistry , Food Production , Fruit , Food Industry , Food Preservation/methods , Pasteurization , Temperature
An. acad. bras. ciênc ; 89(3,supl): 2101-2111, 2017. tab, graf
Article in English | LILACS | ID: biblio-886796


ABSTRACT Annona glabra L. is a semi-deciduous tree that contains several active substances, including secondary metabolites, with antifungal activity. Phytopathogenic strains of the genus Pythium cause billion dollar losses all over the world on natural and crop species. Searching for eco-friendly algaecides and fungicides, we analyzed the effects of acetone extracts of A. glabra leaves on the algae Rhaphidocelis subcapitata (Korshikov) and on the oomycete Pythium aphanidermatum (Edson). We evaluated ten extract concentrations for each organism - 0 to 400 mg L-1 for algae and 0-1000 µg disc1 for oomycete. The results showed no effect on algae up to 75 mg L-1, but a significant inhibitory effect at 125 mg L-1 and above, which reduced the growth rate and the final biomass of the algae. Extract concentrations above 200 mg L-1 were completely inhibitory. The half maximal inhibitory concentration for 72 and 96 h of exposure to our crude extracts are comparable to those obtained with commercial fungicides and herbicides used in aquatic ecosystems. The P. aphanidermatum inhibition concentrations have effects comparable to fungicides as Cycloheximide and Bifonazole. Some substances isolated from the extracts are described as antifungals, which could explain part of anti-oomycete activity. Our results highlight the importance of searching bioactive compounds from plants.

Pythium/drug effects , Plant Extracts/pharmacology , Plant Leaves/drug effects , Annona/chemistry , Herbicides/pharmacology , Antifungal Agents/pharmacology , Microalgae
An. acad. bras. ciênc ; 89(3,supl): 2053-2073, 2017. tab, graf
Article in English | LILACS | ID: biblio-886784


ABSTRACT This study aimed to further investigate the cytotoxicity against tumor cell lines and several bacterial strains of Annona squamosa and its mode of action. Methanol extracts of A. squamosa leaves (ASL) and seeds (ASS) were used. ASL showed significant antibacterial activity against S. aureus, K. pneumoniae and E. faecalis with MIC values of 78, 78 and 39 µg/mL respectively. Moreover, ASL exhibited significant biofilm disruption, rapid time dependent kinetics of bacterial killing, increased membrane permeability and significantly reduced the cell numbers and viability. Regarding the cytotoxicity against tumor cell lines, ASS was more active against Jurkat and MCF-7 cells, with CI50 1.1 and 2.1 µg/mL, respectively. ASL showed promising activity against Jurkat and HL60, with CI50 4.2 and 6.4 µg/mL, respectively. Both extracts showed lower activity against VERO cells and reduced the clonogenic survival at higher concentrations (IC90) to MCF-7 and HCT-116 lineages. The alkaloids anonaine, asimilobine, corypalmine, liriodenine nornuciferine and reticuline were identified in extracts by UPLC-ESI-MS/MS analysis. This study reinforced that A. squamosa presents a remarkable phytomedicinal potential and revealed that its antimicrobial mechanism of action is related to bacterial membrane destabilization.

Humans , Animals , Staphylococcus aureus/drug effects , Plant Extracts/pharmacology , Enterococcus faecalis/drug effects , Annona/chemistry , Klebsiella pneumoniae/drug effects , Anti-Bacterial Agents/pharmacology , Microbial Sensitivity Tests , Cell Membrane/drug effects , Chlorocebus aethiops , Cell Line, Tumor/drug effects
Braz. j. biol ; 75(3): 685-691, Aug. 2015. tab
Article in English | LILACS | ID: lil-761574


AbstractThe antioxidant potential of fruit pulp and seeds of extracts of the Annona coriacea, and A. sylvatica(Annonaceae) were investigated, as well contents total phenolics, flavonoids, condensed tannins and ascorbic acid. Was used to determine the antioxidant activity the 1,1-diphenyl-1-picrylhydrazyl free radical (DPPH), β-carotene bleaching and ABTS radical cation method. The total phenol, total flavonoid, condensed tannin, and ascorbic acid contents were measured spectrophotometrically. In this study, the pulp and seeds of the fruits were extracted using methanol/water (8:2) for maceration. The seed extracts of A. coriacea demonstrated a moderate antioxidant effect with free radical scavenging activity of 31.53%, by the DPPH test, 51.59% by the β-carotene bleaching test and 159.50 µM trolx/g of extract in the ABTS assay. We found that the hydromethanolic seed extract of A. coriacea had high total phenol (147.08 ± 4.20 mg of GAE/g of extract) and flavonoid (131.18 ± 2.31 mg of QE/g of extract) content. This indicated that the antioxidant activity of the extracts was related to the contents of these constituents.

ResumoO potencial antioxidante de extratos da polpa e sementes de frutos da Annona coriacea e A. sylvatica(Annonaceae) foram investigados, bem como os teores de fenóis totais, flavonóides totais, ácido ascórbico total e taninos condensados. Os métodos utilizados para avaliação da atividade antioxidante foram o 1,1-difenil-2-picrilhidrazil (DPPH) branqueamento do β-caroteno e ensaio do radical ABTS. O teor de fenóis totais, flavonoides totais, taninos condensados e ácidos ascórbico foram determinados utilizando espectrofotômetro. A polpa e as sementes dos frutos foram extraídas por maceração com metanol/água (8:2). O extrato da semente de A. coriacea demonstrou moderado efeito antioxidante, com 31,53% no sequestro de radicais livres pelo ensaio do DPPH, 51,59% pelo teste do branqueamento do β-caroteno e pelo ensaio do ABTS com 159,50 µM trolox/g de extrato. Foi observado que o extrato hidrometanólico das sementes de A. coriacea obteve alto teor de fenóis totais (147,08 ± 4,20 mg of GAE/ g de extrato) e flavonóides totais (131,18 ± 2,31 mg of QE/ g de extrato). Isto indica que atividade antioxidante dos extratos pode estar relacionada com o teor destes constituintes.

Annona/chemistry , Antioxidants/metabolism , Fruit/chemistry , Species Specificity , Seeds/chemistry
Rev. Inst. Med. Trop. Säo Paulo ; 56(4): 333-340, Jul-Aug/2014. tab, graf
Article in English | LILACS | ID: lil-716414


Currently multiresistant Staphylococcus aureus is one common cause of infections with high rates of morbidity and mortality worldwide, which directs scientific endeavors in search for novel antimicrobials. In this study, nine extracts from Bidens pilosa (root, stem, flower and leaves) and Annona crassiflora (rind fruit, stem, leaves, seed and pulp) were obtained with ethanol: water (7:3, v/v) and their in vitro antibacterial activity evaluated through both the agar diffusion and broth microdilution methods against 60 Oxacillin Resistant S. aureus (ORSA) strains and against S. aureus ATCC6538. The extracts from B. pilosa and A. crassiflora inhibited the growth of the ORSA isolates in both methods. Leaves of B. pilosa presented mean of the inhibition zone diameters significantly higher than chlorexidine 0.12% against ORSA, and the extracts were more active against S. aureus ATCC (p < 0.05). Parallel, toxicity testing by using MTT method and phytochemical screening were assessed, and three extracts (B. pilosa, root and leaf, and A. crassiflora, seed) did not evidence toxicity. On the other hand, the cytotoxic concentrations (CC50 and CC90) for other extracts ranged from 2.06 to 10.77 mg/mL. The presence of variable alkaloids, flavonoids, tannins and saponins was observed, even though there was a total absence of anthraquinones. Thus, the extracts from the leaves of B. pilosa revealed good anti-ORSA activity and did not exhibit toxicity.

Atualmente Staphylococcus aureus multirresistente é causa comum de infecções com altas taxas de morbidade e mortalidade mundialmente, o que direciona esforços científicos na busca de novos antimicrobianos. Neste estudo, nove extratos de Bidens pilosa (raiz, caule, flor e folhas) e de Annona crassiflora (casca do fruto, caule, folha, semente e polpa) foram obtidos com etanol:água (7:3, v/v) e suas atividades antibacteriana in vitro avaliadas através de difusão em agar e microdiluição em caldo contra 60 cepas de Oxacillin Resistant S. aureus (ORSA) e contra S. aureus ATCC 6538. Os extratos de B. pilosa e A. crassiflora inibiram o crescimento dos isolados ORSA em ambos os métodos. O extrato da folha de B. pilosa apresentou média dos diâmetros dos halos de inibição significativamente maior que a clorexidina 0,12%, contra os isolados ORSA, e os extratos foram mais ativos contra S. aureus ATCC (p < 0,05). Paralelamente, teste de toxicidade pelo método MTT e triagem fitoquímica foram avaliadas, e três extratos (raiz e folha de B. pilosa e semente de A. crassiflora) não apresentaram toxicidade. Por outro lado, as concentrações citotóxicas (CC50 e CC90) para os outros extratos variaram de 2,06 a 10,77 mg/mL. Observou-se variável presença de alcalóides, flavonóides, taninos e saponinas, apesar de total ausência de antraquinonas. Portanto, os extratos das folhas de B. pilosa revelaram boa atividade anti-ORSA e não exibiram toxicidade.

Annona/chemistry , Anti-Bacterial Agents/pharmacology , Bidens/chemistry , Plant Extracts/pharmacology , Staphylococcus aureus/drug effects , beta-Lactam Resistance/drug effects , Dental Clinics , Environmental Microbiology , Microbial Sensitivity Tests , Staphylococcus aureus/isolation & purification
Indian J Exp Biol ; 2014 Jun; 52(6): 623-629
Article in English | IMSEAR | ID: sea-153741


The hexane extract of A. squamosa (ASHE) in 100 and 400 mg/kg body weight dose raised the insulin level when compared with Glimepiride (1 mg/kg) and also inhibited α-glucosidase activity when compared with Acarbose (10 mg/kg) in streptozotocin induced diabetic rats. The ASHE significantly reduced peak blood glucose (Gp30) and area under curve (AUC) in diabetic rats in oral glucose (OGTT) and oral sucrose (OSTT) tolerance test, but there was more reduction of Gp30 value than AUC in OSTT. Thus, it can be suggested that the ASHE, has hypoglycemic role at 2 levels, i.e. it acts as secretagogue and also inhibits the intestinal enzymes, responsible for glucose metabolism.

Animals , Annona/chemistry , Diabetes Mellitus, Experimental/blood , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/metabolism , Glycoside Hydrolase Inhibitors , Hexanes/chemistry , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/therapeutic use , Insulin/metabolism , Male , Plant Extracts/chemistry , Plant Extracts/therapeutic use , Rats
Rev. biol. trop ; 61(1): 419-427, Mar. 2013. tab
Article in English | LILACS | ID: lil-674091


The use of synthetic insecticides for insect control may lead to different kind of problems, such as vector resistance to insecticides. To avoid these problems, a new research area to study botanical products as possible disease vectors controls, has become a feasible alternative. The purpose of this research was to evaluate the biocide activity of the ethanol extract of seeds of Annona coriacea on Rhodnius neglectus (Chagas disease vector) nymphs and adults. For this, different concentrations extracts were evaluated: 25, 50, 100 and 200mg/ mL, and water in DMSO (20%) was used as control. The experimental design was completely randomized and we conducted the bioassay with nymphs and adults, with 10 nymphs and 10 adults (five males and five females) per treatment. Extract action was evaluated in both bioassays, in order to identify possible effects of mortality and life cycle interruption of nymphs and adults during a 28-day-period. The results obtained showed that the extract of A. coriacea was able to disrupt the development of nymphs and adults of R. neglectus, with a mortality rate of more than 90%, 36% and 100%, at the highest concentrations, respectively. There was also molting inhibition in nymphs, lower reproductive capacity in females, feeding deterrence and morphological changes in nymphs and adults. We concluded that the extract of A. coriacea has insecticide action on nymphs and adults of R. neglectus.

La enfermedad de Chagas se convirtió en un problema de salud debido a su importancia epidemiológica, es producida por el protista Trypanosoma cruzi, cuyos insectos vectores son del género Triatoma y Panstrongylus. El objetivo de este estudio fue evaluar la actividad biocida del extracto de Annona coriacea en las ninfas de Rhodnius neglectus y en sus adultos. Se evaluaron 14 concentraciones de 25, 50, 100 y 200mg/ml del extracto etanólico, así como el control, en este caso agua de DMSO (20%). Se utilizo un diseño completamente aleatorizado con tres repeticiones para el bioensayo con 10 ninfas y 10 adultos (cinco machos y cinco hembras) para cada tratamiento. La acción del extracto se observo durante 28 días en ambos bioensayos. Los resultados obtenidos mostraron que el extracto de A. coriacea fue capaz de interrumpir el desarrollo de las ninfas y adultos de R. neglectus, con una mortalidad de más del 90%, 36% y 100%, correspondiendo a las concentraciones más altas. También hubo inhibición de la muda de las ninfas, una menor capacidad reproductiva de las hembras, disuasión alimentaria y cambios morfológicos en las ninfas y adultos. Se concluye que el extracto de A. coriacea presentó acción insecticida en ninfas y adultos de R. neglectus.

Animals , Female , Male , Annona/chemistry , Insect Vectors , Insecticides , Plant Extracts , Rhodnius , Chagas Disease/transmission , Dose-Response Relationship, Drug , Insecticides/isolation & purification , Seeds/chemistry
Bol. latinoam. Caribe plantas med. aromát ; 11(2): 111-126, mar. 2012. tab
Article in Spanish | LILACS | ID: lil-647623


An antioxidant is a compound capable of inhibiting molecular oxidation and therefore of protecting biological molecules from reactive oxygen species or free radicals. Antioxidants can be synthesized by the body or obtained from a diet containing fruit, such as soursop. The aim of this project was to review the literature on antioxidant activity of the soursop and compounds that might be responsible for this activity. From the analysis of fourteen studies, we found that in most cases soursop did not contain high activity or concentration of antioxidants in fresh or frozen pulp, in comparison with highly consumed fruits in Colombia. The leaves, as well as the juice and wine from the plant, do not contain high activity or concentration of antioxidants. In-depth characterization of antioxidant activity and compounds in soursop is lacking; additional studies are required to identify the mechanisms of action of the compounds present in the whole fruit (peel and seed) for different varieties of this tropical fruit.

Los compuestos antioxidantes están en la capacidad de inhibir la oxidación de moléculas y por lo tanto actuar como protectores de moléculas biológicas contra especies reactivas de oxígeno o radicales libres. Muchos antioxidantes pueden ser sintetizados en el cuerpo u obtenidos a partir de una dieta basada en frutas, como la guanábana. El propósito del presente trabajo fue revisar las principales investigaciones relacionadas con el estudio de la capacidad antioxidante de la guanábana y los compuestos presentes que le otorgan dicha propiedad. A partir del análisis de catorce investigaciones halladas sobre el tema, se encontró que en la mayoría de los casos la guanábana no contiene concentraciones elevadas de actividad o compuestos antioxidantes en su pulpa fresca o congelada comparada con frutos de mayor consumo en Colombia. Sus hojas, al igual que sus jugos y vinos, no contienen concentraciones elevadas de actividad o compuestos antioxidantes. Sin embargo, el tema de investigación de compuestos antioxidantes en guanábana se ha realizado con poca profundidad, hace falta estudios adicionales con métodos que logren la identificación de los mecanismos de acción de los compuestos presentes en el fruto completo (cáscara y semilla) de las diferentes variedades que se conocen de este fruto tropical.

Ascorbic Acid/analysis , Annona/chemistry , Antioxidants/pharmacology , Plant Extracts/pharmacology , Phenols/analysis , Colombia
Rev. Soc. Bras. Med. Trop ; 44(6): 777-780, Nov.-Dec. 2011. tab
Article in English | LILACS | ID: lil-611762


INTRODUCTION: Fatty acids are abundant in vegetable oils. They are known to have antibacterial and antifungal properties. METHODS: Antifungal susceptibility was evaluated by broth microdilution assay following CLSI (formerly the NCCLS) guidelines against 16 fungal strains of clinical interest. RESULTS: In this work, fatty acid methyl esters (FAME) was able to inhibit 12 clinical strains of the pathogenic fungus Paracoccidioides brasiliensis and were also active in the bioautographic assay against Cladosporium sphaerospermum. CONCLUSIONS: FAME was a more potent antifungal than trimethoprim-sulfamethoxazole against P. brasiliensis under the experimental conditions tested.

INTRODUÇÃO: Os ácidos graxos são abundantes em óleos vegetais. Eles são conhecidos por suas propriedades antibacterianas e antifúngicas. MÉTODOS: A suscetibilidade a antifúngicos foi avaliada pelo ensaio de microdiluição em caldo de acordo com CLSI (anteriormente NCCLS) sobre 16 isolados de interesse clínico. RESULTADOS: Nesse trabalho, os ésteres metílicos de ácidos graxos (FAME) inibiram doze isolados clínicos do fungo patogênico Paracoccidioides brasiliensis, e também foi muito ativo no ensaio de bioautografia sobre o fungo Cladosporium sphaerospermum. CONCLUSÕES: FAME foi um antifúngico mais potente do que sulfametoxazol-trimetoprim contra P. brasiliensis, nas condições utilizadas no presente trabalho.

Annona/chemistry , Antifungal Agents/pharmacology , Fatty Acids/pharmacology , Methyl Ethers/pharmacology , Paracoccidioides/drug effects , Plant Extracts/pharmacology , Antifungal Agents/isolation & purification , Candida/classification , Candida/drug effects , Cryptococcus gattii/drug effects , Fatty Acids/isolation & purification , Microbial Sensitivity Tests , Methyl Ethers/isolation & purification , Seeds/chemistry
Rev. Soc. Bras. Med. Trop ; 44(5): 567-571, Sept.-Oct. 2011. ilus, tab
Article in English | LILACS | ID: lil-602898


INTRODUCTION: Visceral leishmaniasis is endemic in 88 countries, with a total of 12 million people infected and 350 million at risk. In the search for new leishmanicidal agents, alkaloids and acetogenins isolated from leaves of Annona squamosa and seeds of Annona muricata were tested against promastigote and amastigote forms of Leishmania chagasi. METHODS: Methanol-water (80:20) extracts of A. squamosa leaves and A. muricata seeds were extracted with 10 percent phosphoric acid and organic solvents to obtain the alkaloid and acetogenin-rich extracts. These extracts were chromatographed on a silica gel column and eluted with a mixture of several solvents in crescent order of polarity. The compounds were identified by spectroscopic analysis. The isolated compounds were tested against Leishmania chagasi, which is responsible for American visceral leishmaniasis, using the MTT test assay. The cytotoxicity assay was evaluated for all isolated compounds, and for this assay, RAW 264.7 cells were used. RESULTS: O-methylarmepavine, a benzylisoquinolinic alkaloid, and a C37 trihydroxy adjacent bistetrahydrofuran acetogenin were isolated from A. squamosa, while two acetogenins, annonacinone and corossolone, were isolated from A. muricata. Against promastigotes, the alkaloid showed an IC50 of 23.3 µg/mL, and the acetogenins showed an IC50 ranging from 25.9 to 37.6 µg/mL; in the amastigote assay, the IC50 values ranged from 13.5 to 28.7 µg/mL. The cytotoxicity assay showed results ranging from 43.5 to 79.9 µg/mL. CONCLUSIONS: These results characterize A. squamosa and A. muricata as potential sources of leishmanicidal agents. Plants from Annonaceae are rich sources of natural compounds and an important tool in the search for new leishmanicidal therapies.

INTRODUÇÃO: A leishmaniose visceral é uma enfermidade endêmica em 88 países, com um total de 12 milhões de pessoas infectadas e 350 milhões em risco. Na procura de novos agentes com ação leishmanicida, alcalóides e acetogeninas isoladas de Annona squamosa e Annona muricata, foram testados contra as formas promastigotas e amastigotas de Leishmania chagasi. MÉTODOS: Foram preparados extratos com metanol: água (80: 20) das folhas de A. squamosa e sementes de A. muricata que foram extraídos com solução de ácido fosfórico 10 por cento e solventes orgânicos, para obter extratos ricos em alcalóides e acetogeninas. Estes extratos foram cromatografados em coluna de sílica gel sendo eluídos com solventes de diferentes polaridades para o isolamento dos constituintes, e feita a determinação estrutural por análise espectroscópica. Os constituintes isolados foram testados contra Leishmania chagasi, responsável pela leishmaniose visceral, utilizando o teste MTT. Testes de toxicidade foram realizados em todos os compostos isolados, sendo utilizadas células RAW 264.7. RESULTADOS: Um alcalóide benzilisoquinolínico, O-metilarmepavina, e uma C37-triidróxi-acetogenina com anel bistetrahidrofurânico adjacente foram isolados de A. squamosa e duas acetogeninas annonacinona e corossolona da A. muricata. O alcalóide mostrou um índice de inibição médio (IC50) de 23,3µg/mL e as acetogeninas apresentaram IC50 variando entre 25,9 a 37,6µg/mL contra promastigotas, e no ensaio de amastigotas, o IC50 valores variaram entre 13,5 a 28,7 µg/mL. A toxicidade mostrou resultados que variaram entre 43,5 a 79,9µg/mL. CONCLUSÕES: Estes resultados caracterizam A. squamosa e A. muricata como fontes potenciais de agentes leishmanicidas.

Annona/chemistry , Leishmania infantum/drug effects , Plant Extracts/pharmacology , Trypanocidal Agents/pharmacology , /analogs & derivatives , /isolation & purification , /pharmacology , /toxicity , Acetogenins/isolation & purification , Acetogenins/pharmacology , Acetogenins/toxicity , Benzylisoquinolines/isolation & purification , Benzylisoquinolines/pharmacology , Benzylisoquinolines/toxicity , Chromatography, Gel , Furans/isolation & purification , Furans/pharmacology , Furans/toxicity , Mutagenicity Tests , Parasitic Sensitivity Tests , Plant Extracts/isolation & purification , Plant Leaves/chemistry , Seeds/chemistry , Trypanocidal Agents/isolation & purification , Trypanocidal Agents/toxicity
Article in English | IMSEAR | ID: sea-135735


Background & objectives: Mosquitoes transmit serious human diseases, causing millions of deaths every year and the development of resistance to chemical insecticides resulting in rebounding vectorial capacity. Plants may be alternative sources of mosquito control agents. The present study assessed the role of larvicidal activities of hexane, chloroform, ethyl acetate, acetone, and methanol dried leaf and bark extracts of Annona squamosa L., Chrysanthemum indicum L., and Tridax procumbens L. against the fourth instar larvae of malaria vector, Anopheles subpictus Grassi and Japanese encephalitis vector, Culex tritaeniorhynchus Giles (Diptera: Culicidae). Methods: Larvicidal activities of three medicinal plant extracts were studied in the range of 4.69 to 1000 mg/l in the laboratory bioassays against early 4th instar larvae of An. subpictus and Cx. tritaeniorhynchus. The mortality data were subjected to probit analysis to determine the lethal concentrations (LC50 and LC90) to kill 50 and 90 per cent of the treated larvae of the respective species. Results: All plant extracts showed moderate effects after 24 h of exposure; however, the highest toxic effect of bark methanol extract of A. squamosa, leaf ethyl acetate extract of C. indicum and leaf acetone extract of T. procumbens against the larvae of An. subpictus (LC50 = 93.80, 39.98 and 51.57 mg/l) and bark methanol extract of A. squamosa, leaf methanol extract of C. indicum and leaf ethyl acetate extract of T. procumbens against the larvae of Cx. tritaeniorhynchus (LC50 =104.94, 42.29 and 69.16 mg/l) respectively. Interpretation & Conclusions: Our data suggest that the bark ethyl acetate and methanol extract of A. squamosa, leaf ethyl acetate and methanol extract of C. indicum, acetone and ethyl acetate extract of T. procumbens have the potential to be used as an ecofriendly approach for the control of the An. subpictus, and Cx. tritaeniorhynchus.

Acetates/chemistry , Animals , Annona/chemistry , Anopheles/drug effects , Asteraceae/chemistry , Chrysanthemum/chemistry , Culex/drug effects , Dose-Response Relationship, Drug , Humans , Insecticides/chemistry , Insecticides/pharmacology , Larva/drug effects , Malaria/prevention & control , Methanol/chemistry , Plant Bark/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology
Braz. j. biol ; 71(1): 197-202, Feb. 2011. tab
Article in English | LILACS | ID: lil-578417


Although the use of medicinal plants or natural products has increased in recent decades all over the world, little information is available on their potential risk to health. Annona crassiflora Mart., a plant commonly known as araticum in Brazil, has been widely used in folk medicine for a long time since its seeds and leaves are often utilised in the treatment of cancer, snake bites, and venereal diseases, its fruits are consumed as tonic and astringent, and its bark powder has anti-fungal and anti-rheumatic properties. To evaluate the genotoxic and mutagenic properties induced by the ethanolic extract of araticum leaves, we performed the prophage λ induction (Inductest) and bacterial mutagenicity assays. We used Escherichia coli WP2s(λ) and RJF013 strains in the lysogenic induction test, whereas the mutagenic studies were carried out using Salmonella typhimurium histidine auxotroph strains TA97a, TA98, TA100, and TA102. Each experiment was performed three times in duplicate and included positive and negative controls. No statistically significant (p > 0.05) positive results were obtained for any of the strains tested, which suggests that the ethanolic extract of araticum leaves did not exhibit direct mechanisms of genotoxicity or mutagenicity that could be detected by the tests used in the present work.

Embora o uso de plantas medicinais ou de produtos naturais venha aumentando nas últimas décadas no mundo todo, existem poucas informações acerca de seu risco potencial para a saúde. Annona crassiflora Mart., uma planta comumente conhecida como araticum no Brasil, tem tido amplo uso em medicina popular há muito tempo, uma vez que suas sementes e folhas são frequentemente empregadas no tratamento de câncer, picadas de cobras e doenças venéreas, seus frutos são consumidos como tônico e adstringente, e o pó da casca de seu tronco apresenta propriedades antifúngicas e antirreumáticas. Para avaliar as propriedades genotóxica e mutagênica induzidas pelo extrato etanólico das folhas de araticum, utilizaram-se os testes de indução do profago λ (Induteste) e de mutagenicidade bacteriana. Foram empregadas as linhagens WP2s(λ) e RJF013 de Escherichia coli no teste de indução lisogênica, enquanto os estudos sobre mutagenicidade foram conduzidos utilizando as linhagens auxotróficas para histidina TA97a, TA98, TA100 e TA102 de Salmonella typhimurium. Cada experimento foi executado três vezes em duplicata, incluindo controles positivo e negativo. Não foram obtidos resultados positivos estatisticamente significativos (p > 0,05) para quaisquer das linhagens testadas, o que sugere que o extrato etanólico das folhas de araticum não apresentou mecanismos diretos de genotoxicidade ou mutagenicidade que pudessem ser detectados pelos testes usados no presente estudo.

Annona/chemistry , Escherichia coli/drug effects , Mutagenicity Tests/methods , Plant Extracts/toxicity , Salmonella typhimurium/drug effects , DNA Damage/drug effects , DNA Damage/genetics , Escherichia coli/genetics , Prophages/drug effects , Prophages/genetics , SOS Response, Genetics/drug effects , SOS Response, Genetics/genetics , Salmonella typhimurium/genetics
Rev. Inst. Med. Trop. Säo Paulo ; 52(3): 129-132, May-June 2010. tab, ilus
Article in English | LILACS | ID: lil-550351


Antibacterial effects of aqueous and ethanolic extracts of seeds of moringa (Moringa oleifera) and pods of soursop (Annona muricata) in the concentration of 1:5 and 1:10 in volumes 50, 100, 150 and 200 µL were examined against Staphylococcus aureus, Vibrio cholerae, Escherichia coli (isolated from the organism and the aquatic environment) and Salmonella Enteritidis. Antibacterial activity (inhibition halo > 13 mm) against S. aureus, V. cholerae and E. coli isolated from the whiteleg shrimp, Litopenaeus vannmaei, was detected in aqueous and ethanolic extracts of moringa. E. coli isolated from tilapiafish, Oreochromis niloticus, was sensitive to the ethanolic extract of moringa. The aqueous extracts of soursop showed an antibacterial effect against S. aureus and V. cholerae, but the antibacterial activity by the ethanol extracts of this plant was not demonstrated.

Para avaliação do efeito bactericida frente à Staphylococcus aureus, Vibrio cholerae, Escherichia coli (isolada de pescados e ambiente aquático) e Salmonella Enteretidis, foram testados extratos aquosos e etanólicos de sementes de moringa (Moringa oleifera) e casca de graviola (Annona muricata) na concentração de 1:5 e 1:10, nos volumes de 50, 100, 150 e 200 µL. Os resultados mostraram efeito antibacteriano (halo de inibição > 13mm) dos extratos aquosos e etanólicos de moringa frente a S. aureus, V. cholerae e E. coli isoladas de camarão cinza Litopenaeus vannmaei. A cepa de E. coli isolada do pescado Oreochromis niloticus apresentou sensibilidade frente ao extrato etanólico de moringa. Os extratos aquosos de graviola apresentaram efeito bactericida frente a S. aureus e V. cholerae, entretanto, os extratos etanólicos dessa planta não mostraram atividade antibacteriana.

Animals , Annona/chemistry , Anti-Bacterial Agents/pharmacology , Gram-Negative Bacteria/drug effects , Moringa oleifera/chemistry , Plant Extracts/pharmacology , Staphylococcus aureus/drug effects , Cichlids/microbiology , Escherichia coli/drug effects , Escherichia coli/isolation & purification , Gram-Negative Bacteria/isolation & purification , Microbial Sensitivity Tests , Penaeidae/microbiology , Salmonella enteritidis/drug effects , Salmonella enteritidis/isolation & purification , Staphylococcus aureus/isolation & purification , Vibrio cholerae/drug effects , Vibrio cholerae/isolation & purification
Biol. Res ; 43(2): 165-168, 2010. ilus
Article in English | LILACS | ID: lil-567530


Extracts prepared from seeds of Manilkara zapota, Anona squamosa, and Tamarindus indica were screened for their antibacterial activity by disc diffusion and broth dilution methods. Acetone and methanol extracts of T. indica seeds were found active against both gram-positive and gram-negative organisms. MIC values of potent extracts against susceptible organisms ranged from 53-380 μg/mL. Methanol extract of T. indica and acetone extract of M. zapota seeds were found to be bactericidal.

Annona/chemistry , Anti-Bacterial Agents/pharmacology , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Manilkara/chemistry , Plant Extracts/pharmacology , Tamarindus/chemistry , Anti-Bacterial Agents/isolation & purification , Microbial Sensitivity Tests/methods , Seeds/chemistry
An. acad. bras. ciênc ; 80(2): 271-277, June 2008. ilus, tab
Article in English | LILACS | ID: lil-482881


Annona squamosa seeds extracts showed anthelmintic activity against Haemonchus contortus, the main nematode of sheep and goat in Northeastern Brazil. A compound 1 was isolated from ethyl acetate extract and inhibited the egg hatching of H. contortus at 25 mg ml-1. The structure of 1 was determined as a C37 trihydroxy adjacent bistetrahydrofuran acetogenin based on spectroscopic analysis.

Extratos das sementes de Annona squamosa demonstraram atividade anti-helmíntica contra Haemonchus contortus, o principal nematódeo de ovinos e caprinos no Nordeste do Brasil. O composto 1 foi isolado do extrato acetato de etila e inibiu a eclosão dos ovos de H. contortus a 25 mg ml-1. A estrutura de 1 foi determinada como uma acetogenina C37 tri-hidroxi bis-tetrahydrofurano adjacente, baseando-se nos dados espectrais.

Animals , Acetogenins/pharmacology , Annona/chemistry , Anthelmintics/pharmacology , Haemonchus/drug effects , Ovum/drug effects , Acetogenins/chemistry , Acetogenins/isolation & purification , Anthelmintics/chemistry , Anthelmintics/isolation & purification , Parasitic Sensitivity Tests , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Spectrum Analysis , Seeds/chemistry
Braz. j. biol ; 68(1): 141-147, Feb. 2008. tab
Article in English | LILACS | ID: lil-482195


A typical Brazilian plant, araticum (Annona crassiflora Mart.), is widely used in humans as therapeutic medicine to treat several diseases such as diarrhea, rheumatism and syphilis. It contains acetogenins which present cytotoxic, antitumogenic, and antiparasitic properties. In this study, mutagenic, antimutagenic and cytotoxic effects of araticum leaves ethanolic extract were evaluated by micronucleus test in mice. To evaluate the mutagenic activity, animals were treated with ethanolic extract of araticum (EEA) using 10, 20, 50, 100 and 160 For all doses, micronucleated polychromatic erythrocytes (MNPCE) frequency was evaluated at 24, 48 and 72 hours after treatment. To evaluate the antimutagenic activity, animals were treated with 10, 20, 50 and 100 of EEA and 4 of MMC simultaneously. The frequency of MNPCE was evaluated 36 hours after exposure. Cytotoxicity was evaluated by the polychromatic and normochromatic erythrocytes ratio (PCE/NCE). In the mutagenicity assessment, all doses of EEA resulted in no significant increase of MNPCE (P > 0.05), compared to solvent- control group. Regarding administration time, no significant difference among three evaluation periods was observed (P > 0.05). Such results indicate that EEA did not exert mutagenic activity. Cytotoxicity was evident in doses of 50, 100 and 160 at 24 and 48 hours after exposure. Concerning antimutagenicity, except the 10 co-administered with 4 mg/kg of MMC, all doses reduced significantly the frequency of MNPCE compared to the positive control group (P < 0.05). These results, therefore, indicate an antimutagenic activity of the EEA. Cytotoxicity was significantly increased (P < 0.01) at 100 EEA doses co-administered with 4 of MMC.

O araticum (Annona crassiflora Mart.) é uma planta tipicamente brasileira, largamente utilizada em humanos como remédio para o tratamento de diversas doenças como diarréia, reumatismo e sífilis. Esta planta contém acetogeninas que apresentam propriedades citotóxica, antitumorigênica e antiparasitária. Neste estudo, foram avaliados os possíveis efeitos mutagênico, antimutagênico e citotóxico do extrato etanólico de folhas de araticum, pelo teste de micronúcleos em camundongos. Para a investigação da atividade mutagênica, os animais foram tratados com o extrato etanólico de araticum (EEA) utilizando 10, 20, 50, 100 e 160 Para todas as doses, as freqüências de eritrócidos policromáticos micronucleados (MNPCE) foram avaliadas em 24, 48 e 72 horas após o tratamento. Para a investigação da atividade antimutagênica, os animais foram tratados com 10, 20, 50 e 100 de EEA simultaneamente com 4 de MMC. A freqüência de MNPCE foi avaliada após 36 horas de exposição. A citotoxicidade foi avaliada pela razão de eritrócitos policromáticos e normocromáticos (PCE/NCE). Na avaliação da mutagenicidade, todas as doses de EEA não aumentaram significativamente o número de MNPCE (P > 0,05), comparativamente as do grupo solvente-controle. Em relação ao tempo de administração, não foi constatada diferença significativa entre os 3 períodos avaliados (P > 0,05). Esses resultados indicam que o EEA não exerceu atividade mutagênica.A citotoxicidade foi evidente nas doses de 50, 100 e 160 em 24 e 48 horas depois da exposição. Em relação à antimutagenicidade, exceto para a dose de 10 co-administrada com 4 de MMC, todas reduziram significativamente a freqüência de MNPCE, comparativamente as do grupo controle positivo (P < 0,05). Esses resultados, portanto, indicam uma atividade antimutagênica do EEA. A citotoxicidade foi significativamente aumentada (P < 0,01) na dose de 100 de EEA co-administrada com 4 de MMC.

Animals , Male , Mice , Annona/chemistry , Antimutagenic Agents/pharmacology , Bone Marrow/drug effects , Erythrocytes, Abnormal/drug effects , Plant Extracts/pharmacology , Antimutagenic Agents/isolation & purification , Dose-Response Relationship, Drug , Micronucleus Tests
Indian J Exp Biol ; 2007 May; 45(5): 480-5
Article in English | IMSEAR | ID: sea-63071


Antioxidant potential of leaves of three different species of Annona was studied by using different in vitro models eg., 1,1-diphenyl-2-picryl hydrazyl (DPPH), 2,2-azinobis-(3-ethylbenzothizoline-6-sulphonate) (ABTS), nitric oxide, superoxide, hydroxy radical and lipid peroxidation. The ethanolic extract of A. muricata at 500 microg/ml showed maximum scavenging activity (90.05%) of ABTS radical cation followed by the scavenging of hydroxyl radical (85.88%) and nitric oxide (72.60%) at the same concentration. However, the extract showed only moderate lipid peroxidation inhibition activity. In contrast, the extract of A. reticulata showed better activity in quenching DPPH (89.37%) and superoxide radical (80.88%) respectively. A.squamosa extract exhibited least inhibition in all in vitro antioxidant models excepting hydroxyl radical (79.79%). These findings suggest that the extracts of A. muricata possess potent in vitro antioxidant activity as compared to leaves of A. squamosa and A. reticulata suggesting its role as an effective free radical scavenger, augmenting its therapeutic

Animals , Annona/chemistry , Antioxidants/analysis , Biphenyl Compounds/metabolism , Free Radical Scavengers/pharmacology , Free Radicals/metabolism , Goats , Hydrazines/metabolism , Lipid Peroxidation/drug effects , Liver/chemistry , Osmolar Concentration , Plant Extracts/chemistry , Plant Leaves/chemistry