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LECTINAS ISOLADAS DE PLANTAS COM ATIVIDADE ANTIFÚNGICA

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Lectins are a special class of proteins widely distributed in nature, which selectively recognize and reversibly bind to carbohydrates and glycoconjugates through their binding sites. These proteins, which can be detected through haemagglutination assays, interact with different carbohydrates present in cell surfaces. Lectins are generally classified according to their structure, specificity for carbohydrates and species location. Depending on their properties and distribution in tissues, lectins can play important physiological roles. The characteristic property of lectins to recognize other molecules in a distinct way makes it relevant in research involving purification, structural analysis, in vitro/in vivo applications of these macromolecules and biotechnological uses in different areas such as molecular and cell biology, immunology, pharmacology, medicine, clinical analysis, nanotechnology as well as in systems for drug release. Lectins can be used for analysis of structure and physiology of cells, tissues and pathogenic microorganisms. In agriculture, these proteins are used as insecticidal agents. Lectins have already been shown to exhibit different biological activities and effects, such as mitogenic and antiproliferative activities on cell lines of human cancer, inhibition of bacterial and fungal growth, action as promoting agents in cell aggregation, immunomodulatory activities and toxic effects. These proteins are promising as drugs for treatment and in diagnosis of human diseases; they are important tools in cytochemistry, histochemistry and immunohisto-chemistry and are also useful in forensic medicine. In summary, this review provides an overview of lectin research, with focus on physiological functions, structural performance, classification, potential biotechnological properties and applications.
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This study aimed to evaluate the in vitro effect of neem extract (Azadirachta indica) and clove essential oil (Syzygium aromaticum) on the tick Rhipicephalus (Boophilus) microplus. Extracts from the fresh leaves of the neem plant were obtained using water and ethanol solvents, while clove essential oil was obtained from the fruits of the Clove tree by hydrodistillation. The concentrations of aqueous and ethanoic neem extracts used were 10% and 50%, while of clove essential oil was used as 2.5% and 5%.These experiments were carried out on engorged females tick with in vitro immersion test. The average effectiveness of the extracts of neem was 15.04% until 74,39% depending de concentration and the solvent The average effectiveness of the 2.5% and 5% clove essential oil was 97.15 and 99.4%, respectively.
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The aim of this study is to provide concise information about recent developments in understanding of fungal lectins. Lectins, a well-known class of multivalent carbohydrate binding proteins of non-immune origin that recognize diverse sugar structures with a high degree of stereo-specificity in a non-catalytic manner are wide spread in distribution. Plant and animal lectins are subjected to extensive studies and only limited information was available on fungal lectins. In last few years mushroom and other fungal lectins have attracted wide attention due to their antitumor, antiproliferative and immunomodulatory activities. Earlier fungal lectin reports deal only with their purification, carbohydrate specificity, basic characterization and possible roles. In last ten years, several fungal lectins have been cloned, sequenced and crystallized. More subtle information about their structure and binding properties is available, obtained by employing more advanced techniques such as X-ray crystallography, surface plasmon resonance and enzyme linked lectinsorbent assay etc. Several fungal lectins have been discovered in the recent years and their structural and biochemical properties have been explored. However, some of them show resemblance with plant and bacterial lectins, but still there are enough evidence to place them in a diverse lectin group. This article will provide concise information about recent advancement in understanding of fungal lectins regarding their biochemical and molecular properties.
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Introduction: Parkinson's disease (PD) has a progressive course and is characterized by the degeneration of dopaminergic neurons. Although no neuroprotective treatments for PD have been found to date, the endocannabinoid system has emerged as a promising target. Methods: From a sample of 119 patients consecutively evaluated in a specialized movement disorders outpatient clinic, we selected 21 PD patients without dementia or comorbid psychiatric conditions. Participants were assigned to three groups of seven subjects each who were treated with placebo, cannabidiol (CBD) 75 mg/day or CBD 300 mg/day. One week before the trial and in the last week of treatment participants were assessed in respect to (i) motor and general symptoms score (UPDRS); (ii) well-being and quality of life (PDQ-39); and (iii) possible neuroprotective effects (BDNF and H(1)-MRS). Results: We found no statistically significant differences in UPDRS scores, plasma BDNF levels or H(1)-MRS measures. However, the groups treated with placebo and CBD 300 mg/day had significantly different mean total scores in the PDQ-39 (p = 0.05). Conclusions: Our findings point to a possible effect of CBD in improving quality of life measures in PD patients with no psychiatric comorbidities; however, studies with larger samples and specific objectives are required before definitive conclusions can be drawn.
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Several recent findings suggest that targeting the endogenous cannabinoid system can be considered as a potential therapeutic approach to treat Alzheimer's disease (AD). The present study supports this hypothesis demonstrating that delta-9-tetrahydrocannabinol (THC) or cannabidiol (CBD) botanical extracts, as well as the combination of both natural cannabinoids, which are the components of an already approved cannabis-based medicine, preserved memory in AβPP/PS1 transgenic mice when chronically administered during the early symptomatic stage. Moreover, THC + CBD reduced learning impairment in AβPP/PS1 mice. A significant decrease in soluble Aβ42 peptide levels and a change in plaques composition were also observed in THC + CBD-treated AβPP/PS1 mice, suggesting a cannabinoid-induced reduction in the harmful effect of the most toxic form of the Aβ peptide. Among the mechanisms related with these positive cognitive effects, the anti-inflammatory properties of cannabinoids may also play a relevant role. Here we observed reduced astrogliosis, microgliosis, and inflammatory-related molecules in treated AβPP/PS1 mice, which were more marked after treatment with THC + CBD than with either THC or CBD. Moreover, other cannabinoid-induced effects were uncovered by a genome-wide gene expression study. Thus, we have identified the redox protein thioredoxin 2 and the signaling protein Wnt16 as significant substrates for the THC + CBD-induced effects in our AD model. In summary, the present findings show that the combination of THC and CBD exhibits a better therapeutic profile than each cannabis component alone and support the consideration of a cannabis-based medicine as potential therapy against AD.
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The purpose of this study was to investigate the potential therapeutic qualities of Δ9-tetrahydrocannabinol (THC) with respect to slowing or halting the hallmark characteristics of Alzheimer's disease. N2a-variant amyloid-β protein precursor (AβPP) cells were incubated with THC and assayed for amyloid-β (Aβ) levels at the 6-, 24-, and 48-hour time marks. THC was also tested for synergy with caffeine, in respect to the reduction of the Aβ level in N2a/AβPPswe cells. THC was also tested to determine if multiple treatments were beneficial. The MTT assay was performed to test the toxicity of THC. Thioflavin T assays and western blots were performed to test the direct anti-Aβ aggregation significance of THC. Lastly, THC was tested to determine its effects on glycogen synthase kinase-3β (GSK-3β) and related signaling pathways. From the results, we have discovered THC to be effective at lowering Aβ levels in N2a/AβPPswe cells at extremely low concentrations in a dose-dependent manner. However, no additive effect was found by combining caffeine and THC together. We did discover that THC directly interacts with Aβ peptide, thereby inhibiting aggregation. Furthermore, THC was effective at lowering both total GSK-3β levels and phosphorylated GSK-3β in a dose-dependent manner at low concentrations. At the treatment concentrations, no toxicity was observed and the CB1 receptor was not significantly upregulated. Additionally, low doses of THC can enhance mitochondria function and does not inhibit melatonin's enhancement of mitochondria function. These sets of data strongly suggest that THC could be a potential therapeutic treatment option for Alzheimer's disease through multiple functions and pathways.
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Aim: Proteins with legume lectin domains are known to possess a wide range of biological functions. Here, the antitumor effects of two representative legume lectins, concanavalin A (ConA) and Sophora flavescens lectin (SFL), on human breast carcinoma cells were investigated in vitro and in vivo. Methods: Human breast carcinoma MCF-7 cells and human normal mammary epithelial MCF-10A cells were examined. Cell viability was detected using WST-1 and CCK-8 assays. Cell apoptosis was analyzed with Hoechst 33258 staining. Cell cycle was investigated using flow cytometry. The expression of relevant proteins was measured using Western blotting. Breast carcinoma MCF-7 bearing nude mice were used to study the antitumor effects in vivo. The mice were injected with ConA (40 mg/kg, ip) and SFL (55 mg/kg, ip) daily for 14 d. Results: ConA and SFL inhibited the growth of MCF-7 cells in dose- and time-dependent manners (IC50 values were 15 and 20 μg/mL, respectively). Both ConA and SFL induced apoptotic morphology in MCF-7 cells without affecting MCF-10A cells. ConA and SFL dose-dependently increased the sub-G1 proportion in MCF-7 cells, while SFL also triggered the G2/M phase cell cycle arrest. Both ConA and SFL dose-dependently increased the activities of caspase-3 and caspase-9 and release of cytochrome C from mitochondria into cytoplasm, up-regulated Bax and Bid, and down-regulated Bcl-2 and Bcl-XL in MCF-7 cells. ConA reduced NF-κB, ERK, and JNK levels, and increased p53 and p21 levels, while SFL caused similar changes in NF-κB, ERK, p53, and p21 levels, but did not affect JNK expression. Administration of ConA and SFL significantly decreased the subcutaneous tumor mass volume and weight in MCF-7 bearing nude mice. Conclusion: ConA and SFL exert anti-tumor actions against human breast carcinoma MCF-7 cells both in vitro and in vivo.
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A prosopis juliflora (algaroba) é uma espécie que foiintroduzida no Brasil por volta da década de 1940. A planta apresenta uma aplicabilidade bastante elevada resultando em produtos diversificados como biocombustíveis e alimentos. Este artigo trata de um estudo de prospecção tecnológica sobre a algaroba, usando patentes como fontes de informações. Para levantamento das informações foram utilizados termos-chave na plataforma PatentInsparation®. Foram realizadas análises “macro”, “meso” e “micro”, com o objetivo de levantar as principais características tecnológicas. A busca resultou em 43 patentes que foram analisadas sobre os aspectos, quantitativos, cronológicos, países depositantes e instituições detentoras. Depois de realizar uma filtragem, duas patentes de interesse foram selecionadas, abordando tecnologias sobre a produção de etanol e a aguardente. O monitoramento apontou que poucas são as tecnologias protegidas nos últimos 20 anos sobre o tema e quando se trata das tecnologias de interesse apenas duas patentes foram encontradas.
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Background: Little is known about the patients' view on treatment with medical cannabis (MC) for Parkinson's disease (PD). Objective: To assess the PD community's perception of MC and patients' experience with MC. Methods: Applying a questionnaire-based survey, we evaluated general knowledge and interest in MC as well as the frequency, modalities, efficacy, and tolerability of application. Questionnaires were distributed nationwide via the membership journal of the German Parkinson Association and locally in our clinic to control for report bias. Results: Overall, 1.348 questionnaires (1.123 nationwide, 225 local) were analysed. 51% of participants were aware of the legality of MC application, 28% of various routes of administration (ROA) and 9% of the difference between delta9-tetrahydrocannabinol (Δ9-THC) and cannabidiol (CBD). PD-related cannabis use was reported by 8.4% of patients and associated with younger age, living in large cities and better knowledge about the legal and clinical aspects of MC. Reduction of pain and muscle cramps was reported by more than 40% of cannabis users. Stiffness/akinesia, freezing, tremor, depression, anxiety and restless legs syndrome subjectively improved for more than 20% and overall tolerability was good. Improvement of symptoms was reported by 54% of users applying oral CBD and 68% inhaling THC-containing cannabis. Compared to CBD intake, inhalation of THC was more frequently reported to reduce akinesia and stiffness (50.0% vs. 35.4%; p < 0.05). Interest in using MC was reported by 65% of non-users. Conclusion: MC is considered as a therapeutic option by many PD patients. Nevertheless, efficacy and different ROA should further be investigated.
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Cannabis has been used as a medicine for millennia. Crude extracts of cannabis inflorescence contain numerous phytomolecules, including phytocannabinoids, terpenes, and flavonoids. Combinations of phytomolecules have been recently established as superior to the use of single molecules in medical treatment owing to the ‘entourage effect’. Two types of entourage effects are defined: ‘intra-entourage', resulting from interactions among phytocannabinoids or terpenes, and ‘inter-entourage', attributed to interactions between phytocannabinoids and terpenes. It is suggested that the phytomolecule assemblages found in cannabis chemovars today derive from selective breeding during ancient cultivation. We propose that the current cannabis chemotaxonomy should be redefined according to chemical content and medicinal activity. In parallel, combinations of phytomolecules that exhibit entourage activity should be explored further for future drug development.
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Anecdotal evidence of successful cannabis treatment in autism spectrum disorder (ASD) are accumulating but clinical studies are lacking. This retrospective study assessed tolerability and efficacy of cannabidiol-rich cannabis, in 60 children with ASD and severe behavioral problems (age = 11.8 ± 3.5, range 5.0–17.5; 77% low functioning; 83% boys). Efficacy was assessed using the Caregiver Global Impression of Change scale. Adverse events included sleep disturbances (14%) irritability (9%) and loss of appetite (9%). One girl who used higher tetrahydrocannabinol had a transient serious psychotic event which required treatment with an antipsychotic. Following the cannabis treatment, behavioral outbreaks were much improved or very much improved in 61% of patients. This preliminary study supports feasibility of CBD-based cannabis trials in children with ASD.
Chapter
Almost three decades have passed since the identification of the two specific metabotropic receptors mediating cannabinoid pharmacology. Thereafter, many cannabinoid effects, both at central and peripheral levels, have been well documented and characterized. However, numerous evidences demonstrated that these pharmacological actions could not be attributable solely to the activation of CB1 and CB2 receptors since several important cannabimimetic actions have been found in biological systems lacking CB1 or CB2 gene such as in specific cell lines or transgenic mice. It is now well accepted that, beyond their receptor-mediated effects, these molecules can act also via CB1/CB2-receptor-independent mechanism. Cannabinoids have been demonstrated to modulate several voltage-gated channels (including Ca²⁺, Na⁺, and various type of K⁺ channels), ligand-gated ion channels (i.e., GABA, glycine), and ion-transporting membranes proteins such as transient potential receptor class (TRP) channels. The first direct, cannabinoid receptor-independent interaction was reported on the function of serotonin 5-HT3 receptor-ion channel complex. Similar effects were reported also on the other above mentioned ion channels. In the early ninety, studies searching for endogenous modulators of L-type Ca²⁺ channels identified anandamide as ligand for L-type Ca²⁺ channel. Later investigations indicated that other types of Ca²⁺ currents are also affected by endocannabinoids, and, in the late ninety, it was discovered that endocannabinoids activate the vanilloid receptor subtype 1 (TRPV1), and nowadays, it is known that (endo)cannabinoids gate at least five distinct TRP channels. This chapter focuses on cannabinoid regulation of ion channels and lays special emphasis on their action at transient receptor channels.
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The endocannabinoid system is currently defined as the ensemble of the two 7-transmembrane-domain and G protein-coupled receptors for Δ(9)-tetrahydrocannabinol (but not for most other plant cannabinoids or phytocannabinoids)-cannabinoid receptor type-1 (CB1R) and cannabinoid receptor type-2 (CB2R); their two most studied endogenous ligands, the "endocannabinoids" N-arachidonoylethanolamine (anandamide) and 2-arachidonoylglycerol (2-AG); and the enzymes responsible for endocannabinoid metabolism. However, anandamide and 2-AG, and also the phytocannabinoids, have more molecular targets than just CB1R and CB2R. Furthermore, the endocannabinoids, like most other lipid mediators, have more than just one set of biosynthetic and degrading pathways and enzymes, which they often share with "endocannabinoid-like" mediators that may or may not interact with the same proteins as Δ(9)-tetrahydrocannabinol and other phytocannabinoids. In some cases, these degrading pathways and enzymes lead to molecules that are not inactive and instead interact with other receptors. Finally, some of the metabolic enzymes may also participate in the chemical modification of molecules that have very little to do with endocannabinoid and cannabinoid targets. Here, we review the whole world of ligands, receptors, and enzymes, a true "endocannabinoidome", discovered after the cloning of CB1R and CB2R and the identification of anandamide and 2-AG, and its interactions with phytocannabinoids.