RESUMO
Terpenoids, also named terpenes or isoprenoids, are a family of natural products found in all living organisms. Many plants produce terpenoids as secondary metabolites, and these make up a large part of essential oils. One of most important characteristic is that the compounds are volatile, have odor and can be used in a variety of applications in different industrial segments and traditional medicine. Brazil has a rich and diverse flora that can be used as a source of research for obtaining new molecules. Within the Brazilian flora, it is worth mentioning the Caatinga as an exclusively Brazilian biome where plants adapt to a specific series of weather conditions and therefore become a great storehouse of the terpenoid compounds to be described herein. Fungal infections have become increasingly common, and a great demand for new agents with low toxicity and side effects has thus emerged. Scientists must search for new molecules exhibiting antifungal activity to develop new drugs. This review aims to analyze scientific data from the principal published studies describing the use of terpenes and their biological applications as antifungals.
Assuntos
Óleos Voláteis , Terpenos , Terpenos/farmacologia , Terpenos/metabolismo , Antifúngicos/farmacologia , Brasil , Óleos Voláteis/farmacologia , PlantasRESUMO
Terpenoids, also named terpenes or isoprenoids, are a family of natural products found in all living organisms. Many plants produce terpenoids as secondary metabolites, and these make up a large part of essential oils. One of most important characteristic is that the compounds are volatile, have odor and can be used in a variety of applications in different industrial segments and traditional medicine. Brazil has a rich and diverse flora that can be used as a source of research for obtaining new molecules. Within the Brazilian flora, it is worth mentioning the Caatinga as an exclusively Brazilian biome where plants adapt to a specific series of weather conditions and therefore become a great storehouse of the terpenoid compounds to be described herein. Fungal infections have become increasingly common, and a great demand for new agents with low toxicity and side effects has thus emerged. Scientists must search for new molecules exhibiting antifungal activity to develop new drugs. This review aims to analyze scientific data from the principal published studies describing the use of terpenes and their biological applications as antifungals.
Os terpenóides, também chamados terpenos ou isoprenóides, são uma família de produtos naturais encontrados em todos os organismos vivos. Muitas plantas são produtoras destes metabolitos secundários, que constituem uma grande parte dos óleos essenciais. Uma das características mais importantes é que os compostos são voláteis, têm odor e podem ser utilizados numa variedade de aplicações em diferentes segmentos industriais ou na medicina tradicional. O Brasil tem uma flora rica e diversificada que pode ser utilizada como fonte de pesquisa para a obtenção de novas moléculas. Dentro desta flora, vale a pena mencionar a Caatinga como um bioma exclusivamente brasileiro que possui plantas adaptadas a uma série de condições climáticas e, portanto, um armazém de compostos a serem descritos. As infecções fúngicas são doenças cada vez mais comuns, devido a isso existe uma grande procura de novos agentes com baixa toxicidade e efeitos secundários. Os cientistas devem procurar novas moléculas que exibam atividade antifúngica para o desenvolvimento de novos medicamentos contra as infecções fúngicas. Esta revisão visa analisar dados científicos dos principais estudos publicados que descrevem o uso de terpenóides e as suas aplicações biológicas como antifúngicos.
Assuntos
Terpenos , Óleos Voláteis , AntifúngicosRESUMO
Cryptococcosis is an opportunistic systemic mycosis whose treatment is limited to three drugs. In this work, we evaluated the antifungal activity of a hexane extract (HE) from Spondias tuberosa leaves against Cryptococcus neoformans and Cryptococcus gattii. Minimal inhibitory concentrations (MIC) were determined, and putative mechanisms were evaluated by flow cytometry. In addition, an in vivo infection assay was performed using Tenebrio molitor larvae. Treatment with HE inhibited the growth of standard and clinical isolates of C. neoformans and C. gattii (MICs ranging from 0.78 to 3.12mg/mL), significantly (P<0.05) increased mitochondrial superoxide anion levels, and induced mitochondrial membrane depolarization, loss of lysosomal membrane integrity, and phosphatidylserine externalization. The mean survival time of C. gattii-infected T. molitor larvae significantly (P<0.05) increased from 1.225 days in control to 3.067 and 3.882 days in HE-treated groups (78 and 156mg/kg, respectively). In conclusion, HE showed anticryptococcal activity, induced mitochondrial and lysosomal damage in yeast cells, and exhibited anti-infective action against C. gattii in T. molitor larvae.
Assuntos
Anacardiaceae/química , Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Criptococose/tratamento farmacológico , Hexanos/química , Animais , Antifúngicos/efeitos adversos , Antifúngicos/uso terapêutico , Criptococose/patologia , Cryptococcus gattii/citologia , Cryptococcus gattii/efeitos dos fármacos , Cryptococcus gattii/ultraestrutura , Cryptococcus neoformans/citologia , Cryptococcus neoformans/efeitos dos fármacos , Cryptococcus neoformans/ultraestrutura , Hexanos/farmacologia , Humanos , Larva/efeitos dos fármacos , Lisossomos/efeitos dos fármacos , Lisossomos/fisiologia , Testes de Sensibilidade Microbiana , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/fisiologia , Fitoterapia , Extratos Vegetais/química , Tenebrio/efeitos dos fármacos , Tenebrio/crescimento & desenvolvimento , Testes de ToxicidadeRESUMO
Infections are one of the main reasons for removal of implants from patients, and usually need difficult and expensive treatments. Staphylococcus aureus and Staphylococcus epidermidis are the most frequently detected pathogens. We reviewed the epidemiology and pathogenesis of implant-related infections. Relevant studies were identified by electronic searching of the following databases: PubMed, ScienceDirect, Academic Google, and CAPES Journal Portal. This review reports epidemiological studies of implant infections caused by S. aureus and S. epidermidis. We discuss some methodologies used in the search for new compounds with antibiofilm activity and the main strategies for biomaterial surface modifications to avoid bacterial plaque formation and consequent infection. S. aureus and S. epidermidis are frequently involved in infections in catheters and orthopaedic/breast implants. Different methodologies have been used to test the potential antibiofilm properties of compounds; for example, crystal violet dye is widely used for in-vitro biofilm quantification due to its low cost and good reproducibility. Changes in the surface biomaterials are necessary to prevent biofilm formation. Some studies have investigated the immobilization of antibiotics on the surfaces of materials used in implants. Other approaches have been used as a way to avoid the spread of bacterial resistance to antimicrobials, such as the functionalization of these surfaces with silver and natural compounds, as well as the electrical treatment of these substrates.
Assuntos
Infecções Relacionadas à Prótese/epidemiologia , Infecções Relacionadas à Prótese/microbiologia , Infecções Estafilocócicas/epidemiologia , Infecções Estafilocócicas/microbiologia , Staphylococcus aureus/isolamento & purificação , Staphylococcus epidermidis/isolamento & purificação , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Biofilmes/crescimento & desenvolvimento , Infecções Relacionadas a Cateter/epidemiologia , Infecções Relacionadas a Cateter/microbiologia , Materiais Revestidos Biocompatíveis , Humanos , Staphylococcus aureus/fisiologia , Staphylococcus epidermidis/fisiologia , Propriedades de SuperfícieRESUMO
BACKGROUND: Quantum dots (QDs) are outstanding nanomaterials of great interest to life sciences. Their conjugation versatility added to unique optical properties, highlight these nanocrystals as very promising fluorescent probes. Among uncountable new nanosystems, in the last years, QDs conjugated to glycans or lectins have aroused a growing attention and their application as a tool to study biological and functional properties has increased. SCOPE OF REVIEW: This review describes the strategies, reported in the literature, to conjugate QDs to lectins or carbohydrates, providing valuable information for the elaboration, improvement, and application of these nanoconjugates. It also presents the main applications of these nanosystems in glycobiology, such as their potential to study microorganisms, the development of diseases such as cancer, as well as to develop biosensors. MAJOR CONCLUSIONS: The development of glyconanoparticles based on QDs emerged in the last decade. Many works reporting the conjugation of QDs with carbohydrates and lectins have been published, using different strategies and reagents. These bioconjugates enabled studies that are very sensitive and specific, with potential to detect and elucidate the glycocode expressed in various normal or pathologic conditions. GENERAL SIGNIFICANCE: Produce a quick reference source over the main advances reached in the glyconanotechnology using QDs as fluorescent probes.
Assuntos
Glicoconjugados , Nanotecnologia/métodos , Pontos Quânticos , Técnicas Bacteriológicas , Técnicas Biossensoriais , Metabolismo dos Carboidratos , Carboidratos/análise , Linhagem Celular Tumoral , Técnicas de Química Analítica/métodos , Fluorescência , Glicoconjugados/administração & dosagem , Glicoconjugados/química , Glicoconjugados/uso terapêutico , Humanos , Lectinas/administração & dosagem , Lectinas/química , Nanopartículas Metálicas , Modelos Moleculares , Micologia/métodos , Nanotecnologia/tendências , Neoplasias/química , Neoplasias/diagnóstico , Imagem Óptica/métodos , Parasitologia/métodos , Pontos Quânticos/administração & dosagem , Pontos Quânticos/química , Pontos Quânticos/uso terapêuticoRESUMO
Fusarium wilt caused by Fusarium oxysporum f. sp lycopersici (Fol) is one of the main diseases affecting tomatoes. The BHRS 2,3 genotype of tomato is, however, resistant to this disease. A proteomic approach was used to understand the defense mechanisms of this genotype using the tomato root, the first tissue that interacts with the fungus, as a target. Protein was extracted and separated by two-dimensional electrophoresis followed by staining with Coomassie brilliant blue. The proteins were identified by MALDI-TOF/TOF mass spectrometry. A total of 22 proteins were identified, 21 of which showed differential expression with 12 proteins being upregulated and nine being downregulated. Plants responded to the pathogen with increased expression of pathogenesis-related proteins. We noted the induction of proteins involved in hypersensitivity reaction and other defense mechanisms. The expression of proteins of primary metabolism related to energy production, however, decreased, as did the expression of two proteins related to defense against abiotic stress. These results demonstrate the presence of important mechanisms for defense against Fol in the tomato genotype BHRS 2,3.
Assuntos
Resistência à Doença/genética , Fusarium/patogenicidade , Raízes de Plantas/metabolismo , Proteoma/genética , Solanum lycopersicum/genética , Regulação da Expressão Gênica de Plantas , Solanum lycopersicum/imunologia , Solanum lycopersicum/microbiologia , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Raízes de Plantas/genética , Raízes de Plantas/microbiologia , Proteoma/metabolismo , Estresse FisiológicoRESUMO
In the present study, we compared the performance of a ThinPrep cytological method with the conventional Papanicolaou test for diagnosis of cytopathological changes, with regard to unsatisfactory results achieved at the Central Public Health Laboratory of the State of Pernambuco. A population-based, cross-sectional study was performed with women aged 18 to 65 years, who spontaneously sought gynecological services in Public Health Units in the State of Pernambuco, Northeast Brazil, between April and November 2011. All patients in the study were given a standardized questionnaire on sociodemographics, sexual characteristics, reproductive practices, and habits. A total of 525 patients were assessed by the two methods (11.05% were under the age of 25 years, 30.86% were single, 4.4% had had more than 5 sexual partners, 44% were not using contraception, 38.85% were users of alcohol, 24.38% were smokers, 3.24% had consumed drugs previously, 42.01% had gynecological complaints, and 12.19% had an early history of sexually transmitted diseases). The two methods showed poor correlation (k=0.19; 95%CI=0.11-0.26; P<0.001). The ThinPrep method reduced the rate of unsatisfactory results from 4.38% to 1.71% (χ2=5.28; P=0.02), and the number of cytopathological changes diagnosed increased from 2.47% to 3.04%. This study confirmed that adopting the ThinPrep method for diagnosis of cervical cytological samples was an improvement over the conventional method. Furthermore, this method may reduce possible losses from cytological resampling and reduce obstacles to patient follow-up, improving the quality of the public health system in the State of Pernambuco, Northeast Brazil.
Assuntos
Teste de Papanicolaou/métodos , Doenças do Colo do Útero/diagnóstico , Adulto , Idoso , Brasil , Estudos Transversais , Método Duplo-Cego , Feminino , Humanos , Pessoa de Meia-Idade , Sensibilidade e Especificidade , Fatores Socioeconômicos , Adulto JovemRESUMO
Previous results provided evidence that Cratylia mollis seed lectin (Cramoll 1,4) promotes Trypanosoma cruzi epimastigotes death by necrosis via a mechanism involving plasma membrane permeabilization to Ca(2+) and mitochondrial dysfunction due to matrix Ca(2+) overload. In order to investigate the mechanism of Ca(2+) -induced mitochondrial impairment, experiments were performed analyzing the effects of this lectin on T. cruzi mitochondrial fraction and in isolated rat liver mitochondria (RLM), as a control. Confocal microscopy of T. cruzi whole cell revealed that Cramoll 1,4 binding to the plasma membrane glycoconjugates is followed by its internalization and binding to the mitochondrion. Electrical membrane potential (∆Ψm ) of T. cruzi mitochondrial fraction suspended in a reaction medium containing 10 µM Ca(2+) was significantly decreased by 50 µg/ml Cramoll 1,4 via a mechanism insensitive to cyclosporine A (CsA, membrane permeability transition (MPT) inhibitor), but sensitive to catalase or 125 mM glucose. In RLM suspended in a medium containing 10 µM Ca(2+) this lectin, at 50 µg/ml, induced increase in the rate of hydrogen peroxide release, mitochondrial swelling, and ∆Ψm disruption. All these mitochondrial alterations were sensitive to CsA, catalase, and EGTA. These results indicate that Cramoll 1, 4 leads to inner mitochondrial membrane permeabilization through Ca(2+) dependent mechanisms in both mitochondria. The sensitivity to CsA in RLM characterizes this lectin as a MPT inducer and the lack of CsA effect identifies a CsA-insensitive MPT in T. cruzi mitochondria.
Assuntos
Ciclosporina/farmacologia , Fabaceae/química , Lectinas/farmacologia , Mitocôndrias Hepáticas/metabolismo , Mitocôndrias/metabolismo , Sementes/química , Animais , Transporte Biológico/efeitos dos fármacos , Cálcio/metabolismo , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias Hepáticas/efeitos dos fármacos , Ratos , Espécies Reativas de Oxigênio/metabolismo , Trypanosoma cruzi/efeitos dos fármacos , Trypanosoma cruzi/metabolismoRESUMO
Few chronic food protein models have described the relationship between allergenicity and the molecular structure of food protein after physical processing. The effect of γ-radiation on the structure of food protein was measured by fluorescence, circular dichroism and microcalorimetry. BALB/c mice were intraperitoneally sensitized and then given non-irradiated and irradiated Con-A by daily gavage for 28days. The tendency to form insoluble amorphous aggregates and partially unfolded species was observed after irradiation. The administration of non-irradiated and irradiated samples at low-dose significantly increased weight loss as well as plasma levels of eotaxin in animals repeatedly exposed to Con-A. Significant lymphocytic infiltrate filling completely the stroma of microvilli and tubular glands was observed in the small intestinal of the group given Con-A irradiated at a low dose. This phenotype was not observed in animals treated with Con-A irradiated at a high dose.
Assuntos
Concanavalina A/química , Concanavalina A/imunologia , Concanavalina A/efeitos da radiação , Hipersensibilidade Alimentar/etiologia , Administração Oral , Animais , Varredura Diferencial de Calorimetria , Dicroísmo Circular , Concanavalina A/administração & dosagem , Modelos Animais de Doenças , Relação Dose-Resposta à Radiação , Feminino , Hipersensibilidade Alimentar/patologia , Raios gama , Intestino Delgado/imunologia , Intestino Delgado/patologia , Linfócitos/imunologia , Camundongos , Camundongos Endogâmicos BALB C , Microvilosidades/imunologia , Microvilosidades/patologia , Conformação Proteica , Redução de PesoRESUMO
Libidibia ferrea has been used in folk medicine throughout Brazil, and this study evaluated the biological activities of crude extract (CE) as well as a partially purified fraction (F80) obtained from its pods. Results from the MTT assay revealed that only F80 inhibited NCI-H292 cell growth; however, neither CE nor F80 reduced HEp-2 cell growth or sarcoma 180 tumor weight with the in vivo assay. Acute oral toxicity of the extract and fraction was evaluated following the steps of Guideline 423, using female mice; LD(50) for both preparations was determined as 2,500 mg/kg body weight. CE and F80 promoted a reduction of the leukocyte number and nitrite level in inflammatory exudates when the anti-inflammatory assay (carrageenan-induced peritonitis) was performed. CE and F80 inhibited writhing regarding antinociceptive activity (acetic acid-induced writhing response in mice). In conclusion, CE and F80 have no significant cytotoxic or antitumor activities in cell lines showing low toxicity and no action against tumors in vivo. Both preparations revealed anti-inflammatory and antinociceptive activities, corroborating the pharmacological basis of L. ferrea for ethnomedical use.