In vitro activities of glycoalkaloids from the Solanum lycocarpum against Leishmania infantum

ABSTRACT Leishmania infantum is an etiologic agent of visceral leishmaniasis. This disease is a neglected disease that can be fatal if not treated and additionally, the few therapeutic option present several drawbacks, including difficult route of administration and toxicity, which turn the search for new therapeutic alternatives necessary. Herein, we evaluated the leishmanicidal in vitro activity of the solanum extract from Solanum lycocarpum A. St.-Hil., Solanaceae, and the isolated alkaloids solasodine, solamargine and solasonine against promastigotes and intracellular amastigotes of L. infantum. Solasodine (IC50-pro = 4.7 µg/ml; IC50-ama = 10.8 µg/ml) and solamargine (IC50-pro = 8.1 µg/ml; IC50-ama = 3.0 µg/ml) exhibited interesting leishmanicidal ativity. Solasonine was approximately four-times (Selective Index 3.7) more selective to the parasite than to the host cells. This data suggest that solasonine might be considered as a potential drug candidate for leishmaniasis treatment.

Effects of the extract and glycoalkaloids of Solanum lycocarpum St. Hill on Giardia lamblia trophozoites.

BACKGROUND: Solanum lycocarpum has great importance for food and medicinal traditional use. Recently, it was also evidenced that extracts of S. lycocarpum St. Hill (Solanaceae) and its glycoalkaloids, solamargine (Sg) and solasonine (Sn), are active against flagellated protozoa. OBJECTIVE: The aim was to assess the effects of the extract of S. lycocarpum and its glycoalkaloids, Sn, and Sg, on Giardia lamblia trophozoites. MATERIALS AND METHODS: A crude extract (96%ethanol) (EB) of fruits of S. lycocarpum was prepared and fractionated by partition with 40%ethanol and n-hexane: Ethyl acetate. Glycoalkaloids, Sn, and Sg were recognized in the ethanol fraction (EF) and further isolated by column chromatography. EB, EF, the isolated Sn and Sg and a mixture (1:1) of both glycoalkaloids were tested on cultures of G. lamblia trophozoites and macrophages. RESULTS: EB, EF and glycoalkaloids of S. lycocarpum showed activity against Giardia (95.0 < Inhibitory concentration 50 [IC50] ≤120.3 µg/mL). The mixture of glycoalkaloids (1:1) was more active (IC50 = 13.23 µg/mL) than each one individually, suggesting a synergic effect. Moreover, the mixture is nontoxic to macrophage cells. CONCLUSION: Results are optimistic concerning the anti-Giardia potential of the mixture Sn + Sg. Further studies, in vitro and in vivo, will be required to consolidate the usefulness of the mixture of Sn + Sg in view of a new therapeutic strategy for giardiasis.

Phytochemical Characterization, Antimicrobial Activity, and Antioxidant Potential of Equisetum hyemale L. (Equisetaceae) Extracts.

Equisetum hyemale species is considered a medicinal plant used in the form of infusions to combat infectious or inflammation diseases and also diuretic effects, presenting several compounds related to these actions. In previous studies different species of Equisetum showed several phenolic compounds. The objective of this study was, for the first time, based on phytochemistry analysis to evaluate the antioxidant and antimicrobial activity. The 70% ethanolic and methanolic extracts of E. hyemale were characterized by spectrophotometric and high-performance liquid chromatography with pulsed amperometric detector analyses, as well as its antioxidant potential based on the scavenger activity of 2,2-diphenyl-1-picrylhydrazyl (DPPH). In addition was verified the antimicrobial activity by broth microdilution technique against bacteria and fungi. The extracts showed phytochemical similarity, which demonstrated the presence of phenolic compounds, the scavenging activity for free radicals was about 30% and was observed better antifungal activity against dermatophyte fungi, with minimum inhibitory concentration and minimum fungicidal concentration of 0.62 mg/mL to Trichophyton rubrum and Microsporum canis. The extracts exhibits great potential to therapeutic applications or product development, since both possess antifungal activity and antioxidant action associated with little difference in their phytochemical composition.

In vitro trypanocidal activity of solamargine and extracts from Solanum palinacanthum and Solanum lycocarpum of Brazilian cerrado.

The present investigation was to evaluate the potential trypanocidal activity of crude ethanolic extract of the fruits of Solanum palinacanthum, Solanum lycocarpum and the glycoalcaloid, solamargine. S. palinacanthum and S. lycocarpum fruit powders were submitted to exhaustively extraction with 96% ethanol and solamargine were isolated from the extract of S. palinacanthum. Both extracts and solamargine were analysed for trypanocidal activity by using MTT colorimetric assay. Extracts of S. palinacanthum showed to be more active (IC50 = 175.9 µg.ml-1) than S. lycocarpum (IC50 = 194.7 µg.ml-1). Solamargine presented a strong activity (IC50 = 15.3 µg.ml-1), which can explain the better activity of the both extracts. Benznidazol (IC50 = 9.0 µg.ml-1) is the only drug used to treat Chagas' disease. These findings demonstrate for the first time that ethanol extracts obtained from both fruits of S. palinacanthum and S. lycocarpum and also solamargine have a potential anti-trypanosomal activity.

Paepalanthus spp: antimycobacterial activity of extracts, methoxylated flavonoids and naphthopyranone fractions

Paepalanthus spp., Eriocaulaceae, are native plants from Brazil known as "sempre-vivas" (everlasting flowers). In this work, we evaluated the potential anti-mycobacterial activity of two methoxylated flavonoids (flavonoid 7-methylquercetagetin and 7-methylquercetagetin-4'-O-β-D-glucopyranoside) isolated and identified from P. latipes and the naphthopyranone fractions from P. bromeliodes ethanolic extracts. The MIC value of 500 µg/mL was verified for all compounds tested against M. tuberculosis H37Rv. For M. avium, the MIC value ranged from 1000-2000 µg/mL excepting to naphthopyranone fractions with MIC of 500 µg/mL. This is the first report of activity determination of Paepalanthus spp. flavonoids activity against Mycobacterium tuberculosis and M. avium.

Antimicrobial, cytotoxic and antioxidant activities and determination of the total tannin content of bark extracts Endopleura uchi.

Endopleura uchi is a typical Amazonian tree and its bark is popularly employed in the preparation of teas against myomas, arthritis, influenza, diarrhea and cancer. In this study, the antioxidant activity, cytotoxicity and antimicrobial activity of five different extracts of the bark, selected by their total tannin content, were assessed. The potential antioxidant activity of the extracts was determined by 2.2-diphenyl-1-picrylhydrazyl radical scavenging assay and the values found were very similar among the extracts and to the standards antioxidants used in the tests. Cytotoxicity analysis in mammalian cells indicated that all the tested extracts exhibited IC(50) values higher than the highest concentration used, showing that they do not present a risk when consumed under these conditions. Extract tested against five bacterial strains and one yeast strain did not show satisfactory growth inhibitory activity, and even the extracts that showed some antimicrobial activity were not effective at any dilution to determine the minimum inhibitory concentration. The results may serve as a reference for subsequent works, since such reference values described in the literature for the bark of E. uchi.

Antidiarrheal activity of Campomanesia xanthocarpa fruit.

The growing list of drug-resistant microorganisms and the persistence of deaths due to diarrhea are compelling reasons to study plants in search of new therapeutic agents. The chemical constitution and popular use of the edible fruits of Campomanesia xanthocarpa O. Berg motivated this study to assess the antimicrobial and antidiarrheal properties of the fruits. An extract in 70% ethanol was prepared, and its antimicrobial activity was tested against several strains of bacteria by the agar diffusion and microdilution methods. Antidiarrheal activity was analyzed by testing intestinal motility in an animal model. Preliminary phytochemical study indicated the presence of flavonoids, saponins, and tannins in the hydroalcoholic extract. Antimicrobial activity was significant, but the minimum inhibitory concentration proved to be higher than the maximum extract concentration tested. The extract did not show significant activity for intestinal motility. Although this fruit extract did not show great results as an antimicrobial or antidiarrheal agent, the study contributes to the search for new plant agents and could be referred to as a research protocol by investigators in this area.

Histochemical, phytochemical and biological screening of Plinia cauliflora (DC. ) Kausel, Myrtaceae, leaves / Rastreamento histoquímico, fitoquímico e biológico de folhas de Plinia cauliflora (DC. ) Kausel (Myrtaceae)

In this work, chemical and biological activities of crude extracts obtained with 50 percent ethanol, 70 percent ethanol, acetone:water (7:3; v/v) and chloroform of Plinia cauliflora (DC.) Kausel, Myrtaceae, leaves, a native tree from several regions of Brazil, was investigated. Histochemical and phytochemical screenings were done according to characterization reactions and thin layer chromatography. To assist in extracts standardization, total phenol and flavonoids content spectrophotometric was performed. Antioxidant activity was analyzed by percentage of radical scavenging using DPPH solution. Antimicrobial activity was evaluated against Gram-positive, Gram-negative pathogenic bacteria and species of Candida using agar diffusion and minimal inhibitory concentration (MIC) determination methods according to standard methods. The leaves presented lipids at secretory cavity and phenols, mainly tannins, in nervures and palisade parenchyma. Polar extracts showed flavonoids, tannins and high content of phenols and flavonoids. The extracts showed great antioxidant activity and antimicrobial activity was better against Candida species than against bacteria.

No presente trabalho, foram investigadas a composição química e atividades biológicas de extratos brutos obtidos com etanol 50 por cento, etanol 70 por cento, acetona:água (7:3; v/v) e clorofórmio das folhas de Plinia cauliflora (DC.) Kausel, Myrtaceae, uma árvore nativa de várias regiões do Brasil. Os rastreamentos histoquímico e fitoquímico foram feitos de acordo com reações de caracterização e cromatografia em camada delgada. Para auxiliar na padronização dos extratos foram realizadas determinações do teor de fenóis totais e de flavonoides totais, espectrofotometricamente. A atividade antioxidante foi analisada pela porcentagem de sequestro de radicais livres usando solução de DPPH. A atividade antimicrobiana foi avaliada frente a bactérias patogênicas Gram-positivas, Gram-negativas e espécies de Candida utilizando os métodos de difusão em ágar e determinação da concentração inibitória mínima (MIC) de acordo com métodos padronizados. As folhas apresentaram lipídeos nas cavidades secretoras e fenóis, principalmente taninos, nas nervuras e parênquima paliçádico. Os extratos polares apresentaram flavonoides, taninos, alto teor de fenóis totais e de flavonoides totais. Os extratos mostraram elevada atividade antioxidante e a atividade antimicrobiana foi melhor contra as espécies de Candida do que contra as bactérias.

Controles físico, físico-químico, químico e microbiológico dos frutos de Dimorphandra mollis Benth., Fabaceae / Physic, physic-chemical, chemical and microbiological control of fruits of Dimorphandra mollis Benth., Fabaceae

Considerando-se a qualidade dos fitoterápicos, é importante salientar que a preocupação com esta questão inclui rigoroso acompanhamento das diferentes etapas de desenvolvimento e produção, desde a coleta do vegetal até o produto final. O controle de qualidade de drogas vegetais e seus extratos é essencial quando utilizados como matéria-prima para o desenvolvimento de fitoterápicos. Neste trabalho foram utilizadas diversas técnicas (farmacopeicas e não farmacopeicas) visando estabelecer parâmetros de qualidade dos frutos de Dimorphandra mollis Benth. (Leguminosae), popularmente conhecida como faveiro. Os resultados obtidos determinaram as características físico-químicas da droga vegetal e mostraram que o pó dos frutos e o extrato etanólico 70 por cento de D. mollis apresentam um teor de flavonóides de 10,25 por cento e 17,21 por cento, respectivamente. A análise fitoquímica preliminar dos frutos caracterizou a presença de taninos, saponinas e flavonóides. Na análise microbiológica do extrato não houve crescimento de patógenos entre os testes realizados.

Considering the quality of phytotherapic agents, it is important to point out that the concern with this subject includes rigorous attendance the different steps of development and production of these products, from the collection of the vegetable to the availability of the final product. The quality control for the plants and their extracts is essential when they are used in the development of phytotherapics. In this work, methodologies (pharmacopoeic and no pharmacopoeic) were employed to establish norms for the quality control of Dimorphandra mollis Benth. (Leguminosae) fruit, popularly known as faveira. Pharmacopoeic and no pharmacopoeic methodologies were employed to physic, physic-chemical, chemical and microbiological quality control. The results obtained established the physic-chemical characters of the drug and showed that the fruits and the ethanol 70 percent extract present a content of flavonoids of 10.25 percent and 17.21 percent, respectively. The preliminary phytochemical analysis of the D. mollis fruits evidenced tannins, saponnins and flavonoids. The microbiological analysis did not present pathogenic growth among the accomplished tests.

Avaliação da atividade anti-séptica de extrato seco de Stryphnodendron adstringens (Mart. ) Coville e de preparação cosmética contendo este extrato / Antiseptic activity evaluation of the dry extract from Stryphnodendron adstringens (Mart. ) Coville and cosmetic preparation

As espécies pertencentes ao gênero Stryphnodendron são conhecidas como "barbatimão" e são nativas do cerrado brasileiro. Possuem taninos como metabólitos secundários primordiais de suas cascas apresentando, entre outras, atividade antimicrobiana e cicatrizante. A concentração bactericida mínima (CBM) do extrato seco das cascas de Stryphnodendron adstringens frente a duas bactérias Gram-positivas e uma bactéria Gram-negativa foi determinada pela técnica de diluição em tubos. A atividade antimicrobiana do extrato seco e a atividade anti-séptica de sabonete líquido contendo o extrato seco foram avaliadas pelo método de difusão em ágar. O extrato apresentou valores de concentração bactericida mínima de 50 mg/mL frente a Staphylococcus aureus e 75 mg/mL contra Staphylococcus epidermidis e Escherichia coli e no teste de difusão em ágar, S. aureus apresentou maior sensibilidade ao extrato seco que as outras bactérias. O sabonete líquido mostrou maior eficiência na atividade anti-séptica contra as bactérias testadas na concentração de 100 mg de extrato/mL de sabonete.

The species of the genus Stryphnodendron are known as "barbatimão" and are native from Brazilian "cerrado". They present tannins as main secondary metabolites of their barks and show antimicrobial and cicatrisation activity among others. The minimum bactericidal concentration (MBC) of the dry extract from the barks of Stryphnodendron adstringens against two Gram-positive and one Gram-negative bacteria was done using methodology of broth dilution in tubes. The antimicrobial activity of the dry extract and the antiseptic activity of the liquid soap containing that dry extract were evaluated by agar difusion method. For the extract were obtained the minimum bactericidal concentration values of 50 mg/mL against Staphylococcus aureus and 75 mg/mL against Staphylococcus epidermidis and Escherichia coli and by agar difusion, S. aureus showed more sensibility to the dry extract than the other bacteria. The liquid soap showed efficiency in the antiseptic activity against the bacteria studied at the concentration of 100 mg of extract/mL of soap.

Controle da qualidade do fruto de Syzygium cumini (L. ) Skeels / Quality control of Syzygium cumini (L. ) Skeels fruits

Considerando-se a qualidade dos fitoterápicos, é importante salientar que a preocupação com esta questão inclui rigoroso acompanhamento das diferentes etapas do desenvolvimento e produção destes produtos, desde a coleta do vegetal até a disponibilidade do produto final. Neste trabalho foi realizado o controle da qualidade do fruto de Syzygium cumini (L.) Skeels, popularmente conhecido como jambolão. Para o controle físico-químico e microbiológico utilizaram-se metodologias farmacopéicas e não farmacopeicas. Os resultados obtidos mostraram que o fruto apresenta um teor de taninos de 4,2 por cento e a análise fitoquímica preliminar dos frutos de S. cumini evidenciou taninos, flavonóides, antocianidinas, iridóides, alcalóides e heterosídeos fenólicos simples. A análise microbiológica não apresentou crescimento de patógenos entre os outros testes realizados. Destaca-se a importância do estabelecimento de normas para o controle da qualidade para as plantas, a fim de que sejam utilizadas com finalidade fitoterápica.

Considering the quality of the phytotherapic agents, it is important to point out that the concern with this subject includes rigorous attendance of the different steps of the development and production of these products, from the collection of the vegetable to the availability of the final product. In this work the quality control of the Syzygium cumini (L.) Skeels fruit, popularly known as jambolão, was carried out. Pharmacopoeic and no pharmacopoeic methodologies were employed to physico-chemical and microbiological quality control. The obtained results showed that the fruits presents a content of tannins of 4.2 percent, the preliminary phytochemical analysis of the S. cumini fruits evidenced tannins, flavonoids, antocianidin, iridoids, alkaloids and heterosides simple phenols. The microbiological analysis didnÆt present phatogenic growth among the other accomplished tests. The work stands out the importance of the establishment of norms for the quality control for the plants, so that they are used with phytotherapic purpose.

Antidiarrhoeal effects of Mikania glomerata Spreng. (Asteraceae) leaf extract in mice

Mikania glomerata Spreng. (Asteracae) is a plant widely used to treat gastrointestinal disorders in Brazilian traditional medicine. In the present work, an aqueous extract of the leaves of Mikania glomerata has shown a decrease in the propulsive movements of the intestinal contents in mice. Oral administration produced an inhibition of gastrointestinal transit as effective as that produced by loperamide. These findings suggested that the aqueous extract of the leaves of Mikania glomerata might elicit an antidiarrhoeal effect by inhibiting intestinal motility.

Sensitivity of mycobacteria to different species of Eucalyptus L'herit

Sensitivity profile of 10 mycobacteria of clinical interest to eigth different species of Eucalyptus L'herit was studied. A proportion Method Indirect test was performed to detect resistant bacilli utilizing 5 and 10 mg/ml of essential oils incorporated to Lowestein-Jensen medium. Mycobaterium tuberculosis and other slow growing mycobacteria were more sensitive to essential oils than faster growing ones. The most effective essential oils, in decreasing order, were Eucalyptus citriodora. Eucalyptus maculata and Eucalyptus tereticornis.