RESUMO
Stryphnodendron spp., popularly known as "barbatimão", is the native Brazilian tree most often employed to treat wounds and infections. The aim of the present study was to highlight the importance of S. adstringens, as well as other Stryphnodendron species recognized as "barbatimão", to human health, depicting the relevance of ethnopharmacological knowledge to scientific evidence for uses, related chemical compounds, development of pharmaceutical formulations, and the establishment of toxicity parameters. For this purpose, the literature databases PubMed, Scielo, Lilacs, CAPES Thesis and Google Scholar were searched until 2017. It was observed that stem bark was the primary part of the plant used, mainly as a decoction, for wound healing and treatment of infectious and inflammatory disorders. Confirmed biological activities, including wound healing, anti-inflammatory, antioxidant, and antimicrobial activities, were related to the presence of compounds from tannin class, mostly proanthocyanidins. Toxicity parameters for stem bark were inconclusive, but toxicity was observed to a significant extent when seeds were ingested by cattle or other animals. Due to these important and confirmed biological activities, government policy encourages the phytotherapic use of S. adstringens, and some formulations with stem bark extracts were developed and patented. Furthermore, antiprotozoal, hypoglycemic and antiviral activities were identified as promising.
Assuntos
Fabaceae/química , Bases de Dados como Assunto , Etnofarmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Publicações , Cicatrização/efeitos dos fármacosRESUMO
Tagetes patula L. shows a complex chemical composition, ranging from glycosylated flavonoids and thiophenes in extracts until terpenoids in the essential oil. In the present study, due to this rich flavonoidic constitution, its antioxidant potential was determined, having shown values of antiradical percentage superior to reference compounds, mainly the extracts prepared with flowers. Previous studies performed emphasized the acaricide potential of T. patula and thus, the present study aimed to verify the action of extractives obtained from aerial parts on growth of entomopathogenic fungi related to biological control of brown dog tick Rhipicephalus sanguineus and the action against pathogenic fungi closely associated with pets. None of the samples inhibited the growth of strains of Beauveria bassiana or Metarhizium anisopliae, enabling feasible future studies of synergism on acaricide activity of formulations containing fungi and extracts. The antimicrobial activity of ethanolic extract of flowers (FlEtOH70%) against Microsporum canis and Trichophyton rubrum was significant (193.3 µg/mL and 253.9 µg/mL, respectively), as well as ethanolic extract from aerial parts (APEtOH70%) against T. rubrum (312.5 µg/mL). In order to ensure the safety of a topical formulation containing the extractives of T. patula, the cytotoxic potential of these samples were tested in murine macrophages cells. At higher concentrations all extracts were quite lethal, with IC50 ranging from 210.96 µg/mL to 468.75 µg/mL for APEtOH70% and FlEtOH70%, respectively. These results suggest that the application of a product containing T. patula extractives in the control of ticks could be used, at principle, only on the environment.
Assuntos
Antifúngicos/farmacologia , Antifúngicos/toxicidade , Antioxidantes/farmacologia , Antioxidantes/toxicidade , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Tagetes/química , Animais , Antifúngicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Concentração Inibidora 50 , Macrófagos/efeitos dos fármacos , Camundongos , Extratos Vegetais/isolamento & purificaçãoRESUMO
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.
Assuntos
Extratos Vegetais/farmacologia , Alcaloides de Solanáceas/farmacologia , Solanum/química , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Concentração Inibidora 50 , Testes de Sensibilidade Parasitária , Solanum/classificação , Tripanossomicidas/isolamento & purificaçãoRESUMO
In addition to the bio-guided investigation of the antifungal activity of Plinia cauliflora leaves against different Candida species, the major aim of the present study was the search for targets on the fungal cell. The most active antifungal fraction was purified by chromatography and characterized by NMR and mass spectrometry. The antifungal activity was evaluated against five Candida strains according to referenced guidelines. Cytotoxicity against fibroblast cells was determined. The likely targets of Candida albicans cells were assessed through interactions with ergosterol and cell wall composition, porosity and architecture. The chemical major component within the most active antifungal fraction of P. cauliflora leaves identified was the hydrolysable tannin casuarinin. The cytotoxic concentration was higher than the antifungal one. The first indication of plant target on cellular integrity was suggested by the antifungal activity ameliorated when using an osmotic support. The most important target for the tannin fraction studied was suggested by ultrastructural analysis of yeast cell walls revealing a denser mannan outer layer and wall porosity reduced. It is possible to imply that P. cauliflora targeted the C. albicans cell wall inducing some changes in the architecture, notably the outer glycoprotein layer, affecting the cell wall porosity without alteration of the polysaccharide or protein level.
Assuntos
Antifúngicos/farmacologia , Candida/efeitos dos fármacos , Parede Celular/efeitos dos fármacos , Taninos Hidrolisáveis/farmacologia , Myrtaceae/metabolismo , Candida/classificação , Candidíase/tratamento farmacológico , Glicoproteínas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Folhas de Planta/metabolismo , Porosidade/efeitos dos fármacosRESUMO
Introduction. Plants have been used as medicines for centuries to treat human diseases. Studies with plants are extremely important for the development of future drugs that can benefit the human population.Hypothesis/Gap Statement. With the emergence of pathogens resistant to antimicrobial agents, there is an urgent need to direct research towards the discovery of new antimicrobials.Aim. In this study, Spondias purpurea L. (Anacardiaceae) was evaluated for its antimicrobial activity, antioxidant activity and cytotoxicity.Methodology. Antimicrobial activity was evaluated by the MIC using the 96-well plate microdilution technique of ethanolic, hexanic and dicloromethanic extracts of dried S. purpurea leaves against bacteria, yeast and filamentous fungi. The antioxidant activity of extracts was evaluated by the 2,2-diphenyl-1-picrylhydrazine (DPPH) method. To evaluate the safety of extracts, a cytotoxicity study against HaCat, J774 and HepG2 cells was performed.Results. The extracts had no activity against the bacteria at the maximum concentration of 5.0 mg ml-1, but showed fungistatic action against Candida species and dermatophytes. The ethanolic extract showed 88â% antioxidant activity and showed no significant cytotoxicity against the previously mentioned cells.Conclusion. This study showed that the 100â% ethanolic (EtOH) extract was favourable for antifungal and antioxidant activities and did not present significant cytotoxicity against the three studied cell lines, indicating that S. purpurea leaves are promising for the development of new antimicrobials.
Assuntos
Anacardiaceae , Anti-Infecciosos , Antibacterianos , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Bactérias , Humanos , Extratos Vegetais/farmacologiaRESUMO
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.
Assuntos
Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Magnoliopsida/química , Casca de Planta/química , Extratos Vegetais/farmacologia , Taninos/farmacologia , Animais , Anti-Infecciosos/química , Antioxidantes/química , Antioxidantes/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Magnoliopsida/metabolismo , Testes de Sensibilidade Microbiana , Casca de Planta/metabolismo , Extratos Vegetais/química , Coelhos , Taninos/químicaRESUMO
Antimicrobial Photodynamic Therapy (A-PDT) is a modern and non-invasive therapeutic modality. Nanostructures like the polymeric nanocapsules (NC) has proved to be a system that has enormous potential to improve current antimicrobial therapeutic practice. NC of Zinc phenyl-thio-phthalocyanine and Amphotericin B association (NC/ZnS4Pcâ¯+â¯AMB) built with poly(lactide-co-glycolide) (PLGA) 50:50 using the preformed polymer interfacial deposition method were developed at a 0.05â¯mgâ¯mL- 1 theoretical concentration to improve antifungal activity with two actives association and assistance from PDTa. It showed an average particle diameter of 253.8⯱â¯17.3, an average polydispersity index of 0.36⯱â¯0.01, and a negative Zeta potential average of -31.03⯱â¯5.54 for 158 days. UV-vis absorption and emission spectroscopy analyses did not show changes in photophysical properties in the steady-state of NC/ZnS4Pcâ¯+â¯AMB counterparts free ZnS4Pc. The encapsulation percentage of actives was 89.24 % and 7.40 % for ZnS4Pc and AMB, respectively. Cell viability assay using NIH/3T3 ATCC® CRL-1658 ™ cells line showed no cytotoxicity for the concentrations tested. The photodynamic activity assay using NC/ZnS4Pcâ¯+â¯AMB diluted showed fungal toxicity against Candida albicans yeast with energetic fluences of 12â¯J.cm-2 and 25â¯J.cm-2 by a decrease in cell viability. The MFC assay demonstrated a fungistatic activity for the conditions employed in the PDTa assay. The results show that NC/ZnS4Pcâ¯+â¯AMB is a promising nanomaterial for antimicrobial inactivation using PDT.
Assuntos
Nanocápsulas , Fotoquimioterapia , Anfotericina B , Antifúngicos/farmacologia , Candida albicans , Indóis , Isoindóis , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes/farmacologia , Polímeros , ZincoRESUMO
Fractionation of extracts from the culture broth of the marine-derived fungus, Paecilomyces sp. 7A22, resulted in the isolation of the harzialactone A (HA), a known compound previously isolated from fungi of marine environments. The chemical structure of HA was determined by spectroscopic analyses. Upon evaluation of HA on antileishmanial assays against Leishmania amazonensis, HA exhibited significant activity against promastigotes forms with IC50 of 5.25 µg mL-1 and moderate activity against intracellular amastigotes with IC50 of 18.18 µg mL-1. This is the first report on the antileishmanial activity of HA, and the effects of HA presented in this work suggest that this class of compounds are suitable for future biological in vitro and in vivo studies for the search of natural products with activity against Leishmania spp. Furthermore, the present results corroborate marine-derived fungi as a promising source of natural products with antiparasitic activity.
Assuntos
Antiprotozoários/farmacologia , Lactonas/farmacologia , Leishmania mexicana/efeitos dos fármacos , Paecilomyces/química , Animais , Organismos Aquáticos , Avaliação Pré-Clínica de Medicamentos/métodos , Lactonas/química , Lactonas/isolamento & purificação , Leishmaniose Cutânea/tratamento farmacológico , Macrófagos Peritoneais/parasitologia , Camundongos Endogâmicos BALB C , Estrutura Molecular , Paecilomyces/isolamento & purificaçãoRESUMO
Dermatophytosis is a dermic disease caused by fungi. The aim of this study was to search anti-dermatophyte bioactive compounds in Piper umbellatum leaves. Cytotoxicity evaluation was performed against MRC-5 and HepG2 as a selectivity parameter. Crude ethanol extract presented MIC value of 39.1 µg/mL against M. canis and no cytotoxicity to Hep G2 (human liver cancer) and MRC-5 (normal lung fibroblast). 4-nerolydilcatechol was isolated from P. umbellatum ethanolic extract. MIC values for 4-NC were 7.6µM to M. canisand 15.6µM to Trichophyton rubrum. 4-NC presented activity against M. canis14 times lower than to MRC-5 (non-tumoral human cell line), which suggest selective activity for this fungus. Molecular modeling suggests 4-NC could bind to CYP51, present in lanosterol synthesis, blocking fungi development. In conclusion, P. umbellatum crude ethanol extract and 4-NC demonstrated high and selective in vitro antifungal activity.[Formula: see text].
Assuntos
Antifúngicos/farmacologia , Arthrodermataceae/efeitos dos fármacos , Catecóis/farmacologia , Microsporum/efeitos dos fármacos , Piper/química , Antifúngicos/química , Antifúngicos/isolamento & purificação , Bioensaio , Domínio Catalítico , Catecóis/química , Catecóis/metabolismo , Dermatomicoses/microbiologia , Avaliação Pré-Clínica de Medicamentos/métodos , Etanol/química , Proteínas Fúngicas/química , Proteínas Fúngicas/metabolismo , Células Hep G2 , Humanos , Testes de Sensibilidade Microbiana , Modelos Moleculares , Extratos Vegetais/química , Folhas de Planta/química , Esterol 14-Desmetilase/química , Esterol 14-Desmetilase/metabolismoRESUMO
Plinia cauliflora is a plant species with edible fruits but its chemical composition is not totally known yet although former studies showed its potential as antifungal agent. This work aimed the chemical analysis of the leaves, the activity against fungi species and evaluated cytotoxicity. Extract was obtained with 70% ethanol. An ethyl acetate fraction was obtained and glycosylated quercetin and myricetin were isolated. Samples were tested against Candida species, dermatophytes and entomopathogenic fungi. Cytotoxicity was evaluated against fibroblast cells. Extract showed good activity against C. albicans (minimum inhibitory concentration at 156 µg/mL), C. parapsilosis (78 µg/mL), C. krusei (19 µg/mL), Trichophyton rubrum (78 µg/mL) and Microsporum canis (156 µg/mL). Isolated compounds were more active against C. krusei and T. rubrum. The extract, which was the more active sample, demonstrated low cytotoxic effect and encourage more studies against rising non-albicans species and dermatophyte T. rubrum.
Assuntos
Antifúngicos/isolamento & purificação , Flavonoides/isolamento & purificação , Myrtaceae/química , Folhas de Planta/química , Animais , Antifúngicos/farmacologia , Arthrodermataceae/efeitos dos fármacos , Candida/efeitos dos fármacos , Citotoxinas/isolamento & purificação , Citotoxinas/farmacologia , Fibroblastos/efeitos dos fármacos , Flavonoides/farmacologia , Humanos , Testes de Sensibilidade Microbiana , Microsporum/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Quercetina/isolamento & purificação , Quercetina/farmacologia , Trichophyton/efeitos dos fármacosRESUMO
Following the information obtained by a rational design study, a cyclic and helical-stabilized analogue of the peptide Cm-p5 was synthetized. The cyclic monomer showed an increased activity in vitro against Candida albicans and Candida parapsilosis, compared to Cm-p5. Initially, 14 mutants of Cm-p5 were synthesized following a rational design to improve the antifungal activity and pharmacological properties. Antimicrobial testing showed that the activity was lost in each of these 14 analogues, suggesting, as a main conclusion, that a Glu-His salt bridge could stabilize Cm-p5 helical conformation during the interaction with the plasma membrane. A derivative, obtained by substitution of Glu and His for Cys, was synthesized and oxidized with the generation of a cyclic monomer with improved antifungal activity. In addition, two dimers were generated during the oxidation procedure, a parallel and antiparallel one. The dimers showed a helical secondary structure in water, whereas the cyclic monomer only showed this conformation in SDS. Molecular dynamic simulations confirmed the helical stabilizations for all of them, therefore indicating the possible essential role of the Glu-His salt bridge. In addition, the antiparallel dimer showed a moderate activity against Pseudomonas aeruginosa and a significant activity against Listeria monocytogenes. Neither the cyclic monomer nor the dimers were toxic against macrophages or THP-1 human cells. Due to its increased capacity for fungal control compared to fluconazole, its low cytotoxicity, together with a stabilized α-helix and disulfide bridges, that may advance its metabolic stability, and in vivo activity, the new cyclic Cm-p5 monomer represents a potential systemic antifungal therapeutic candidate.
RESUMO
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.
Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Equisetum/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Antifúngicos/farmacologia , Arthrodermataceae/efeitos dos fármacos , Bactérias/efeitos dos fármacos , Flavonoides/análise , Sequestradores de Radicais Livres/farmacologia , Fenóis/análise , Fitoterapia , Plantas MedicinaisRESUMO
CR-LAAO is an L-amino acid oxidase from Calloselasma rhodostoma snake venom that has been broadly studied regarding its structural and biochemical characteristics, however, few studies have investigated its pharmacological effects. The present study aimed at the evaluation of the biotechnological potential of CR-LAAO by determining its bactericidal, antifungal, leishmanicidal and trypanocidal activity, as well as its cytotoxicity on human tumor and non-tumor cell lines. After 24 h of preincubation, CR-LAAO showed bactericidal effects against both Staphylococcus aureus (MIC 0.78 µg/mL) and Escherichia coli (MIC 31.25 µg/mL) strains, inducing dismantle of bacterial cell walls. After 6 h of preincubation with Candida albicans, CR-LAAO was able to inhibit 80% of the yeast growth, and it also showed cytotoxic activity on Leishmania species and Trypanosoma cruzi. Additionally, CR-LAAO showed high cytotoxicity on HepG2 and HL-60 tumor cells (IC50 10.78 and 1.7 µg/mL), with lower effects on human mononuclear cells (PBMC). The cytotoxic effects of CR-LAAO were significantly inhibited in the presence of catalase, which suggests the involvement of hydrogen peroxide in its mechanisms of toxicity. Therefore, CR-LAAO showed promising pharmacological effects, and these results provide important information for the development of therapeutic strategies with directed action, such as more effective antimicrobial agents.
Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Antiparasitários/farmacologia , L-Aminoácido Oxidase/farmacologia , Venenos de Víboras/farmacologia , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Parede Celular , Ensaios de Seleção de Medicamentos Antitumorais , Escherichia coli/efeitos dos fármacos , Células HL-60 , Células Hep G2 , Humanos , Concentração Inibidora 50 , Leishmania/efeitos dos fármacos , Leucócitos Mononucleares , Testes de Sensibilidade Microbiana , Proteínas de Répteis/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Trypanosoma cruzi/efeitos dos fármacosRESUMO
Many plants are used in traditional medicine as active agents against various effects induced by snakebite. Few attempts have been made however to identify the nature of plant natural products with anti-ophidian properties. Baccharis trimera (Less) DC (Asteraceae), known in Brazil as carqueja, has been popularly used to treat liver diseases, rheumatism, diabetes, as well as digestive, hepatic and renal disorders. The active component was identified as 7alpha-hydroxy-3,13-clerodadiene-16,15:18,19-diolide, C20H28O5, (clerodane diterpenoid, Bt-CD). We report now the anti-proteolytic and anti-hemorrhagic properties against snake venoms of a Bt-CD inhibitor from B. trimera. Bt-CD exhibited full inhibition of hemorrhage and proteolytic activity caused by Bothrops snake venoms. The inhibitor was able to neutralize the hemorrhagic, fibrinogenolytic and caseinolytic activities of class P-I and III metalloproteases isolated from B. neuwiedi and B. jararacussu venoms. No inhibition of the coagulant activity was observed. Bt-CD also partially inhibited the edema induced by other crude venoms, metalloproteases, basic and acidic phospholipases A2. To further elucidate the inhibitory specificity of Bt-CD against metalloproteases isolated from snake venoms, a deeper understanding of its structure and function is necessary. Furthermore, the potential use of these inhibitors to complement anti-venom as an alternative treatment of snakebite envenomations needs to be evaluated in future studies.
Assuntos
Baccharis/química , Venenos de Crotalídeos/antagonistas & inibidores , Diterpenos/farmacologia , Hemorragia/prevenção & controle , Metaloproteases/antagonistas & inibidores , Animais , Coagulação Sanguínea/efeitos dos fármacos , Bothrops , Brasil , Caseínas/metabolismo , Venenos de Crotalídeos/toxicidade , Diterpenos/isolamento & purificação , Edema/induzido quimicamente , Edema/prevenção & controle , Hemorragia/induzido quimicamente , Masculino , Medicina Tradicional , Camundongos , Conformação Molecular , Estrutura Molecular , Músculo Esquelético/efeitos dos fármacos , Extratos Vegetais/químicaRESUMO
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.
Assuntos
Anti-Infecciosos/farmacologia , Antidiarreicos/farmacologia , Frutas/química , Motilidade Gastrointestinal/efeitos dos fármacos , Myrtaceae/química , Extratos Vegetais/farmacologia , Animais , Bactérias/efeitos dos fármacos , Cromatografia em Camada Fina , Feminino , Flavonoides/análise , Camundongos , Testes de Sensibilidade Microbiana , Modelos Animais , Saponinas/análise , Taninos/análiseRESUMO
Plinia cauliflora (Mart.) Kausel, widespread in South America, has edible fruits, and its bark is commonly used against diarrhea and other disorders, on account of its astringency. Because diarrhea is still one of the most important causes of illness and death among children in developing countries, where the population turns to traditional medicine for its treatment, the present study determined the composition of fruit and leaf extracts of P. cauliflora, analyzed the activity against diarrhea by antimicrobial and gastrointestinal motility, and evaluated the cytotoxicity of the extracts. Chemical composition was determined by high-performance liquid chromatograpy-ultraviolet/photodiode array detection. Antimicrobial activity was analyzed by agar diffusion and the microdilution method against etiological agents of diarrhea. The effect on gastrointestinal motility was analyzed using an experimental model in mice. Cytotoxicity was evaluated in vitro with the fibroblast cell line SIRC CCL 60, and leaf extract showed a 50% inhibitory concentration of 0.48 µg/mL. Gallic acid, ellagic acid, and flavonoid derivatives were detected in the extracts. It was observed that fruit and leaf extracts showed some activity against Enterococcus faecalis, Escherichia coli, Salmonella sp., and Shigella sp. However, neither extract had any effect on gastrointestinal motility.
Assuntos
Antidiarreicos/farmacologia , Diarreia/tratamento farmacológico , Motilidade Gastrointestinal/efeitos dos fármacos , Myrtaceae/química , Extratos Vegetais/farmacologia , Animais , Anti-Infecciosos/farmacologia , Linhagem Celular , Ácido Elágico/farmacologia , Enterococcus faecalis/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Feminino , Flavonoides/farmacologia , Frutas/química , Ácido Gálico/farmacologia , Camundongos , Testes de Sensibilidade Microbiana , Folhas de Planta/química , Salmonella/efeitos dos fármacos , Shigella sonnei/efeitos dos fármacos , América do SulRESUMO
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.
RESUMO
Atualmente, as plantas medicinais movem altos valores financeiros em todo o mundo e representam o tipo de tratamento mais acessível para cerca de 80 por cento da população, principalmente entre os países em desenvolvimento. Entretanto, existe ainda uma falta de conhecimento sobre propriedades químicas, farmacológicas e toxicológicas a fim de assegurar a eficácia e segurança das plantas medicinais. Os critérios de eficácia e segurança de plantas medicinais estão relacionados a qualidade, isto é, as plantas necessitam ser corretamente identificadas, cultivadas e coletadas, devem estar livres de material estranho, partes de outras plantas e contaminações inorgânicas e/ou microbianas. O objetivo deste estudo foi o de elucidar os diferentes processos e padronizações sobre o controle de drogas vegetais, principalmente no Brasil.
Nowadays medicinal plants move high financial values at the world and represent a type of treatment more accessible for about 80 percent of people, mainly among developing countries. However, there is a lack of knowledge about chemical, pharmacological and toxicological properties towards ensure their efficacy and safety. Efficacy and safety criteria of medicinal plants are related to quality, that is, the plants need to be correctly identified, cultivated and harvested, they must be free of strange material, part of other plants and inorganic and/or microorganisms contamination. The aim of this study was to elucidate different process and standardizations about quality control of vegetal drugs mainly in Brazil.
RESUMO
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.
RESUMO
The isolation and biochemical/enzymatic characterization of an L-amino acid oxidase, Balt-LAAO-I, from Bothrops alternatus snake venom, is described. Balt-LAAO-I is an acidic glycoprotein, pI approximately 5.37, homodimeric, Mr approximately 123,000, whose N-terminal sequence is ADVRNPLE EFRETDYEVL. It displays a high specificity toward hydrophobic and basic amino acids, while deglycosylation does not alter its enzymatic activity. Balt-LAAO-I induces platelet aggregation and shows bactericidal activity against Escherichia coli and Staphylococcus aureus. In addition, this enzyme is slightly hemorrhagic and induces edema in the mouse paw. Balt-LAAO-I is a multifunctional enzyme with promising relevant biotechnological and medical applications.