RESUMO
Dual-species biofilms formed by Candida albicans and Staphylococcus aureus have high virulence and drug resistance. In this context, biosurfactants produced by Pseudomonas aeruginosa have been widely studied, of which a new derivative (RLmix_Arg) stands out for possible application in formulations. The objective of this study was to evaluate the antibiofilm activity of RLmix_Arg, both alone and incorporated in a gel prepared with Pluronic F-127, against dual-species biofilms of fluconazole-resistant C. albicans (FRCA) and methicillin-resistant S. aureus (MRSA) in impregnated catheters. Broth microdilution tests, MTT reduction assays of mature biofilms, impregnation of RLmix_Arg and its gel in peripheral venous catheters, durability tests and scanning electron microscopy (SEM) were performed. RLmix_Arg showed antimicrobial activity against Candida spp. and S. aureus, by reducing the cell viability of mixed biofilms of FRCA and MRSA, and preventing their formation in a peripheral venous catheter. The incorporation of this biosurfactant in the Pluronic F-127 gel considerably enhanced its antibiofilm activity. Thus, RLmix_Arg has potential application in gels for impregnation in peripheral venous catheters, helping to prevent development of dual-species biofilms of FRCA and MRSA.
Assuntos
Anti-Infecciosos , Staphylococcus aureus Resistente à Meticilina , Fluconazol/farmacologia , Candida albicans , Staphylococcus aureus , Resistência a Meticilina , Biofilmes , Poloxâmero/farmacologia , Testes de Sensibilidade Microbiana , Anti-Infecciosos/farmacologia , Catéteres , Antibacterianos/farmacologiaRESUMO
This work aimed to evaluate the in vitro anthelmintic effect of carvone nanoemulsions on Haemonchus contortus. Three R-carvone nanoemulsions were prepared: uncoated R-carvone nanoemulsions homogenized in a sonicator (UNAlg-son) and homogenized in an ultrahomogenizer (UNAlg-ultra) and sodium alginate-coated R-carvone (CNAlg-ultra). The physicochemical characterizations of the nanoemulsions were carried out. The anthelmintic activity was evaluated using egg hatch test (EHT), larval development test (LDT) and adult worm motility test (AWMT). Changes in cuticle induced in adult H. contortus were evaluated by scanning electron microscopy (SEM). The results were subjected to analysis of variance and compared using the Tukey test (P < 0.05). The effective concentration to inhibit 50% (EC50) of egg hatching and larval development was calculated. The particle sizes were 281.1 nm (UNAlg-son), 152.7 nm (UNAlg-ultra) and 557.8 nm (CNAlg-ultra), and the zeta potentials were −15 mV (UNAlg-son), −10.8 mV (UNAlg-ultra) and −24.2 mV (CNAlg-ultra). The encapsulation efficiency was 99.84 ± 0.01%. SEM of the nanoemulsions showed an increase in size. In EHT, the EC50 values of UNAlg-son, UNAlg-ultra and CNAlg-ultra were 0.19, 0.02 and 0.17 mg mL−1, respectively. In LDT, they were 0.29, 0.31 and 0.95 mg mL−1 for UNAlg-son, UNAlg-ultra and CNAlg-ultra, respectively. The adult motility inhibition was 100% after 12 h of exposure to UNAlg-ultra and CNAlg-ultra, while for UNAlg-son, it was 79.16%. SEM showed changes in the buccal capsule and cuticular damage. It was concluded that R-carvone nanoemulsions showed antiparasitic action demonstrating promise for the control of infections caused by gastrointestinal nematodes in small ruminants.
Assuntos
Anti-Helmínticos , Hemoncose , Haemonchus , Animais , Hemoncose/tratamento farmacológico , Hemoncose/veterinária , Hemoncose/parasitologia , Anti-Helmínticos/farmacologia , Anti-Helmínticos/uso terapêutico , Monoterpenos Cicloexânicos , Larva , Extratos Vegetais/farmacologiaRESUMO
Troxerutin is a natural flavonoid present abundantly in tea, coffee, olives, wheat, and a variety of fruits and vegetables. Due to its diverse pharmacological properties, this flavonoid has aroused interest for treatment of various diseases, and consequently prompted investigation into its toxicological characteristics. The aim of this study was to evaluate the genotoxic and mutagenic effects and chemoprotective activity attributed to troxerutin using human peripheral blood leukocytes (PBLs) through several well-established experimental protocols based upon different parameters. Data demonstrated that troxerutin (100 to 1000 µM) induced no marked cytotoxic effect on PBLs after 24 hr, and did not produce strand breaks and mutagenicity. Regarding chemoprevention, this flavonoid attenuated cytotoxicity, genotoxicity, and mutagenicity initiated by hydrogen peroxide (H2O2) in human PBLs. Further, troxerutin demonstrated no marked cytotoxic effect on PBLs and exerted a protective effect against oxidative stress induced by H2O2 through modulation of GSH-dependent enzymes.
Assuntos
Glutationa/metabolismo , Peróxido de Hidrogênio/farmacologia , Hidroxietilrutosídeo/análogos & derivados , Leucócitos/fisiologia , Oxidantes/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Substâncias Protetoras/farmacologia , Anticoagulantes/farmacologia , Humanos , Hidroxietilrutosídeo/farmacologia , Leucócitos/efeitos dos fármacos , Leucócitos/enzimologiaRESUMO
Mangiferin is found in many plant species as the mango tree (Mangifera indica) with ethnopharmacological applications and scientific evidence. The emergence of resistant herpes simplex virus (HSV) strains to Acyclovir (ACV) has encouraged the search for new drugs. We investigated the in vitro and in vivo activity of mangiferin obtained from M. indica against ACV-resistant HSV-1 (AR-29) and sensitive (KOS) strains. The in vitro activity was performed under varying treatment protocols. The substance showed a CC50 > 500 µg/mL and IC50 of 2.9 µg/mL and 3.5 µg/mL, respectively, for the AR-29 and KOS strains. The in vivo activity was performed in Balb/c mice treated with 0.7% topical mangiferin formulation. This formulation inhibited most effectively the AR-29 strain, attenuated the lesions, postponed their appearance or enhanced healing, in comparison to control group. We demonstrated the potentiality of mangiferin from M. indica to control HSV replication with emphasis to ACV-resistant infection.
Assuntos
Aciclovir/farmacologia , Antivirais/farmacologia , Herpes Simples/tratamento farmacológico , Herpesvirus Humano 1/efeitos dos fármacos , Mangifera/química , Xantonas/farmacologia , Aciclovir/química , Animais , Antivirais/química , Antivirais/isolamento & purificação , Células Cultivadas , Chlorocebus aethiops , Relação Dose-Resposta a Droga , Farmacorresistência Viral/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Células Vero , Xantonas/química , Xantonas/isolamento & purificaçãoRESUMO
Intestinal mucositis, characterized by inflammatory and/or ulcerative processes in the gastrointestinal tract, occurs due to cellular and tissue damage following treatment with 5-fluorouracil (5-FU). Rutin (RUT), a natural flavonoid extracted from Dimorphandra gardneriana, exhibits antioxidant, anti-inflammatory, cytoprotective, and gastroprotective properties. However, the effect of RUT on inflammatory processes in the intestine, especially on mucositis promoted by antineoplastic agents, has not yet been reported. In this study, we investigated the role of RUT on 5-FU-induced experimental intestinal mucositis. Swiss mice were randomly divided into seven groups: Saline, 5-FU, RUT-50, RUT-100, RUT-200, Celecoxib (CLX), and CLX + RUT-200 groups. The mice were weighed daily. After treatment, the animals were euthanized and segments of the small intestine were collected to evaluate histopathological alterations (morphometric analysis); malondialdehyde (MDA), myeloperoxidase (MPO), and glutathione (GSH) concentrations; mast and goblet cell counts; and cyclooxygenase-2 (COX-2) activity, as well as to perform immunohistochemical analyses. RUT treatment (200 mg/kg) prevented 5-FU-induced histopathological changes and reduced oxidative stress by decreasing MDA concentrations and increasing GSH concentrations. RUT attenuated the inflammatory response by decreasing MPO activity, intestinal mastocytosis, and COX-2 expression. These results suggest that the COX-2 pathway is one of the underlying protective mechanisms of RUT against 5-FU-induced intestinal mucositis.
Assuntos
Fluoruracila/efeitos adversos , Enteropatias , Mucosite , Estresse Oxidativo/efeitos dos fármacos , Rutina/farmacologia , Animais , Fluoruracila/farmacologia , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Inflamação/patologia , Enteropatias/induzido quimicamente , Enteropatias/tratamento farmacológico , Enteropatias/metabolismo , Enteropatias/patologia , Masculino , Camundongos , Mucosite/induzido quimicamente , Mucosite/tratamento farmacológico , Mucosite/metabolismo , Mucosite/patologiaRESUMO
Adenanthera pavonina is a native tree of Africa and Asia, introduced in Brazil for reforestation and wood industry. Several pharmacological activities have described scientifically, including antiviral activity. This study evaluated the antiviral effect of sulfated polysaccharide of Adenanthera pavonina (SPAp) against acyclovir (ACV)-resistant (AR-29) and sensitive (KOS) herpes simplex virus strains. The 50% cytotoxic concentration (CC50) was determined by MTT method and the 50% inhibitory concentration (IC50) was evaluated by plaque reduction assay. The in vivo SPAp antiviral activity was performed in Balb/c mice infected by skin scarification and treated with topical 0.5% (w/w) SPAp formulations. SPAp showed a CC50 of 47.81 µg/mL and the IC50 were 0.49 µg/mL (SI = 97.5) and 0.54 µg/mL (SI = 88.5) for the strains KOS and AR-29, respectively. Our results demonstrated that mice treated with SPAp presented a delay in the development and progression of skin lesions compared with the control group.
RESUMO
This study assessed new insecticidal activities of essential oils from Lippia sidoides and Croton species (Croton zehntneri, Croton nepetaefolius, Croton argyrophylloides, and Croton sonderianus) against Aedes aegypti mosquito. In addition, the acute toxicity upon mice was determined. All essential oils showed inhibition of egg hatching, with IC50 values ranging from 66.4 to 143.2 µg mL(-1), larvicidal activity with LC50 ranging from 25.5 to 94.6 µg mL(-1), and pupicidal action with PC50 ranging from 276.8 to over 500 µg mL(-1). Only L. sidoides, C. zehntneri, and C. argyrophylloides essential oils were able to inhibit the oviposition of female gravid mosquitoes with OD50 values of 35.3, 45.3, and 45.8 µg mL(-1), respectively. Oral acute toxicity in mice showed that C. sonderianus and C. argyrophylloides oils are nontoxic (LD50 > 6,000 mg.kg(-1)) while C. nepetaefolius, C. zehntneri, and L. sidoides oils are moderately toxic (LD50 3,840; 3,464, and 2,624 mg.kg(-1), respectively). The results indicate that these oils are promising sources of bioactive compounds, showing low or no toxicity to mammals.
Assuntos
Aedes/efeitos dos fármacos , Croton/química , Inseticidas/farmacologia , Lippia/química , Óleos Voláteis/farmacologia , Aedes/anatomia & histologia , Aedes/classificação , Aedes/fisiologia , Animais , Feminino , Inseticidas/toxicidade , Larva/efeitos dos fármacos , Dose Letal Mediana , Camundongos , Óleos Voláteis/toxicidade , Oviposição/efeitos dos fármacos , Óvulo/efeitos dos fármacos , Óvulo/crescimento & desenvolvimento , Óleos de Plantas/farmacologia , Óleos de Plantas/toxicidade , Especificidade da EspécieRESUMO
Gels containing juca seed galactomannan (JSG) were evaluated for their potential to prevent the progression of dentin erosive wear in an in vitro study with four experimental groups (n = 9). The treatments included distilled water (DW), 0.05% stannous fluoride (121 ppm F), and 0.5% or 1% JSG. The specimens underwent a cycle (3 times/day) consisting of immersion in 1% citric acid (5 minutes), treatment (5 minutes), and artificial saliva exposure (2 hours/overnight) for 5 days. Surface changes were assessed using mechanical profilometry (wear), scanning electron microscopy (SEM), and energy-dispersive X-ray spectroscopy (EDS). The data were analyzed using ANOVA followed by Tukey's post-test (p < 0.05). The negative control group exhibited the highest wear (6.0 µm ± 3.5), significantly differing from the group treated with 0.05% stannous fluoride gel (p = 0.007), which showed less dentin loss. The groups treated with 0.5% and 1% JSG showed results similar to the negative control (p = 0.661; p = 0.212, respectively) and the stannous fluoride group (p = 0.103; p = 0.379, respectively). In the SEM images, the specimen treated with stannous fluoride showed obliterated tubules, while the JSG gels formed crystals on the dentin surface, as confirmed by the presence of oxygen and calcium in the EDS analysis. Although the JSG gels showed similar results to the stannous fluoride, did not exhibit superior efficacy at the tested concentrations.
Assuntos
Caesalpinia , Erosão Dentária , Fluoretos de Estanho , Erosão Dentária/prevenção & controle , Dentina , Géis , Fluoretos , Fluoreto de SódioRESUMO
This work aimed the development and evaluation of the wound healing activity of films based on sodium alginate, polyvinyl alcohol (PVA) and Ca2+ loaded with Agaricus blazei Murill hydroalcoholic extract (AbE). Firstly, AbE was prepared using a previously standardized methodology. The films were prepared by casting technique and cross-linked with Ca2+ using CaCl2 as cross-linking agent. The physicochemical, morphological and water vapor barrier properties of the films were analyzed and the pre-clinical efficacy was investigated against the cutaneous wound model in mice. The films showed barrier properties to water vapor promising for wound healing. AbE showed physical and chemical interactions between both polymers, noticed by Fourier transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy, and thermal analysis. The delivery of AbE in alginate/PVA films enhanced the antioxidant and wound healing properties of these polymers. Consequently, a reduction of malondialdehyde levels was observed, as well as an increase of the epidermis/dermis thickness and enhancement in collagen I deposition. Thus, these formulations are promising biomaterials for wound care and tissue repairing.
Assuntos
Alginatos , Álcool de Polivinil , Camundongos , Animais , Alginatos/farmacologia , Alginatos/química , Álcool de Polivinil/farmacologia , Álcool de Polivinil/química , Vapor , CicatrizaçãoRESUMO
The skin is the largest organ in the human body and its physical integrity must be maintained for body homeostasis and to prevent the entry of pathogenic microorganisms. Sodium alginate (SA) and polyvinyl alcohol (PVA) are two polymers widely used in films for wound dressing applications. Furthermore, blends between SA and PVA improve physical, mechanical and biological properties of the final wound healing material when compared to the individual polymers. Different drugs have been incorporated into SA/PVA-based films to improve wound healing activity. It is noteworthy that SA/PVA films can be crosslinked with Ca2+ or other agents, which improves physicochemical and biological properties. Thus, SA/PVA associations are promising for the biomedical field, as a potential alternative for wound treatment. This review focuses on the main techniques for obtaining SA/PVA films, their physical-chemical characterization, drug incorporation, and the advantages and challenges of these films for wound healing.
Assuntos
Alginatos , Álcool de Polivinil , Humanos , Álcool de Polivinil/química , Alginatos/química , Cicatrização , Bandagens , PolímerosRESUMO
Macromolecules with antioxidant properties such as polysaccharides from Agaricus blazei Murill mushroom (PAbs) are an excellent option for manufacturing wound dressings. Based on this, this study aimed to analyze preparation, physicochemical characterization, and assessment of the potential wound-healing activity of films based on sodium alginate and polyvinyl alcohol loaded with PAbs. PAbs did not significantly alter the cell viability of human neutrophils in a concentration range of 1-100 µg mL-1. The Infrared Spectroscopy (FTIR) indicates that the components present in the films (PAbs/Sodium Alginate (SA)/Polyvinyl Alcohol (PVA)) present an increase in hydrogen bonds due to the increase of hydroxyls present in the components. Thermogravimetry (TGA), Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD) characterizations indicate a good miscibility between the components where PAbs increasing the amorphous characteristics of the films and that the addition of SA increased the mobility of the chains PVA polymers. The addition of PAbs to films significantly improves properties such as mechanical, thickness, and water vapor permeation. The morphological study evidenced good miscibility between the polymers. The wound healing evaluation indicated that F100 film presented better results from the fourth day onward compared to the other groups. It favored the formation of a thicker dermis (476.8 ± 18.99 µm), with greater collagen deposition and a significant reduction in malondialdehyde and nitrite/nitrate, markers of oxidative stress. These results indicate that PAbs is a candidate for wound dressing.
Assuntos
Alginatos , Álcool de Polivinil , Humanos , Álcool de Polivinil/química , Alginatos/química , Polissacarídeos/farmacologia , Cicatrização , Bandagens , PolímerosRESUMO
BACKGROUND: Clove volatile oil (CVO) and its major compound, eugenol (EUG), have anxiolytic effects, but their clinical use has been impaired due to their low bioavailability. Thus, their encapsulation in nanosystems can be an alternative to overcome these limitations. OBJECTIVES: This work aims to prepare, characterize and study the anxiolytic potential of CVO loaded-nanoemulsions (CVO-NE) against anxious-like behavior in adult zebrafish (Danio rerio). METHODS: The CVO-NE was prepared using Agaricus blazei Murill polysaccharides as stabilizing agent. The drug-excipient interactions were performed, as well as colloidal characterization of CVO-NE and empty nanoemulsion (B-NE). The acute toxicity and potential anxiolytic activity of CVO, EUG, CVO-NE and B-NE against adult zebrafish models were determined. RESULTS: CVO, EUG, CVO-NE and B-NE presented low acute toxicity, reduced the locomotor activity and anxious-like behavior of the zebrafish at 4 - 20 mg kg-1. CVO-NE reduced the anxious-like behavior of adult zebrafish without affecting their locomotor activity. In addition, it was demonstrated that anxiolytic activity of CVO, EUG and CVO-NE is linked to the involvement of GABAergic pathway. CONCLUSION: Therefore, this study demonstrates the anxiolytic effect of CVO, in addition to providing a new nanoformulation for its administration.
Assuntos
Ansiolíticos , Óleos Voláteis , Syzygium , Animais , Óleo de Cravo/farmacologia , Óleo de Cravo/metabolismo , Óleos Voláteis/farmacologia , Peixe-Zebra , Syzygium/metabolismo , Ansiolíticos/farmacologia , Ansiolíticos/metabolismo , Eugenol/farmacologia , Eugenol/metabolismoRESUMO
In this study, pentacyclic triterpene-loaded emulsions were stabilized by polysaccharides from Agaricus blazei Murill mushroom (PAb). The drug-excipient compatibility results by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) showed the absence of physicochemical incompatibilities. The use of these biopolymers at 0.75 % led to obtaining emulsions with droplets smaller than 300 nm, moderate polydispersity, and ζ-potential >30 mV in modulus. The emulsions presented high encapsulation efficiency, suitable pH for topical application, and absence of macroscopic signs of instability during 45 days. Morphological analysis suggested the deposition of thin layers of PAb around the droplets. The encapsulation of pentacyclic triterpene in emulsions, stabilized by PAb, improved the cytocompatibility of this drug against PC12 and murine astrocyte cells. There was a reduction in cytotoxicity, which resulted in a lower accumulation of intracellular reactive oxygen species and maintenance of the mitochondrial transmembrane potential. Based on these results, it is estimated that PAb are promising biopolymers for the emulsions' stabilization by improving their physicochemical and biological properties.
Assuntos
Agaricus , Citoproteção , Camundongos , Animais , Emulsões , Polissacarídeos/farmacologia , Polissacarídeos/química , Agaricus/química , Triterpenos PentacíclicosRESUMO
BACKGROUND: Lentinula edodes, known as shiitake, has been utilized as food, as well as, in popular medicine, moreover, compounds isolated from its mycelium and fruiting body have shown several therapeutic properties. The aim of this study was to determine the antiviral activity of aqueous (AqE) and ethanol (EtOHE) extracts and polysaccharide (LeP) from Lentinula edodes in the replication of poliovirus type 1 (PV-1) and bovine herpes virus type 1 (BoHV-1). METHODS: The time-of-addition assay was performed at the times -2, -1, 0, 1 and 2 h of the infection. The virucidal activity and the inhibition of viral adsorption were also evaluated. Plaque assay was used to monitor antiviral activity throughout. RESULTS: The AqE and LeP were more effective when added at 0 h of infection, however, EtOHE was more effective at the times 1 h and 2 h of the infection. AqE, EtOHE and LeP showed low virucidal activity, and the inhibition of viral adsorption was not significant. CONCLUSIONS: The results allowed us to conclude that AqE, EtOHE and LeP act on the initial processes of the replication of both strains of virus.
Assuntos
Antivirais/química , Polissacarídeos/química , Cogumelos Shiitake/química , Replicação Viral/efeitos dos fármacos , Antivirais/isolamento & purificação , Antivirais/farmacologia , Herpesvirus Bovino 1/efeitos dos fármacos , Viabilidade Microbiana/efeitos dos fármacos , Poliovirus/efeitos dos fármacos , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Ligação Viral/efeitos dos fármacosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The use of mushrooms in medicine is quite old and the first report about the use of genus Agaricus in treatment of ulcers occurred in Byzantine period. This mushroom is widely consumed as food, tea, food supplements, as well as nutraceutical and cosmeceutical applications, being cultivated and appreciated in several countries such as Brazil, Korea, Japan and China. AIM OF THE STUDY: This study aimed to characterize the chemical profile and the potential gastroprotective effect of hydroalcoholic extract from Agaricus blazei Murill (HEAb). MATERIALS AND METHODS: The extract was chemically characterized by elemental analysis, UPLC-QTOF-MSE, Nuclear Magnetic Resonance (NMR) and high-performance liquid chromatography (HPLC) techniques to elucidate the metabolites present in the extract. The quantification of phenolic compounds and the in vitro antioxidant activities were performed and the gastroprotective effect of this extract was evaluated against ethanol-induced gastric ulcer model. HEAb was administered by gavage at 5, 25 and 50 mg kg-1 and N-acetylcysteine at 300 mg kg-1 (positive control). Furthermore, the pathways of nitric oxide (NO), Cyclic Guanylate Monophosphate (cGMP), prostaglandins (PGs) and the involvement of ATP-sensitive K+ Channels were modulated. RESULTS: Mannitol, malic acid, pyroglutamic acid, L-agaritine and L-valine were putatively identified by UPLC-QTOF-MSE in HEAb. In addition, it was possible to identify mannitol by the intense signals in the NMR spectra, being still quantified as the main compound in the extract by HPLC. The contents of total phenols and flavonoids corroborated with the good antioxidant activity of HEAb. This study observed that HEAb at 25 and 50 mg kg-1 had gastroprotection effect demonstrated by the reduction of histopathological parameters and the reduction of mastocytosis in the stomach of mice. CONCLUSIONS: In this study was possible to conclude that HEAb has gastroprotective effect related to the involvement of NO and PG pathways in the ethanol-induced gastric ulcer model in mice.
Assuntos
Agaricus , Antiulcerosos , Úlcera Gástrica , Agaricus/metabolismo , Animais , Antiulcerosos/química , Antiulcerosos/farmacologia , Antiulcerosos/uso terapêutico , Etanol/química , Mucosa Gástrica , Manitol/metabolismo , Manitol/farmacologia , Manitol/uso terapêutico , Camundongos , Óxido Nítrico/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/prevenção & controleRESUMO
This study aimed to isolate, characterize chemical-structurally and evaluate the effects of polysaccharides from Caesalpinia (Libidibia) ferrea stem barks in the haemostatic system. The deproteinated-polysaccharide extract (PE-Cf) after being fractionated by ion exchange chromatography-DEAE-cellulose resulted in three fractions (FI, FII, FIII) containing total carbohydrates (14.3-38%), including uronic acid (5-16%), and polyphenols (0.94-1.7 mg/g GAE). The polysaccharide fractions presented polydisperse profile in polyacrylamide gel electrophoresis (detected by Stains-All) and molecular masses (9.5 × 104 Da-1.5 × 105 Da) identified by gel permeation chromatography. FT-IR showed absorption bands (1630 cm-1, 1396-1331 cm-1), indicative of uronic acid, and a band at 1071 cm-1, typical of COO- groups of galacturonic acid. The NMR spectra of C. ferrea polysaccharides revealed a central core composed mainly by 5-linked α-Araf and minority components as α-Rhap and α-GalAp. UV spectra of fractions revealed discrete shoulders at 269-275 nm, characteristic of polyphenolic compounds. In vitro, polysaccharides inhibited the intrinsic and/or common coagulation pathway (aPTT test) (2.0-3.7 fold) and the platelet aggregation induced by 3 µM adenosine diphosphate (25-48%) and 5 µg/mL collagen (24%), but not that induced by arachidonic acid. In vivo, the polysaccharides inhibited (36-69%) venous thrombosis induced by hypercoagulability and stasis, showing discrete hemorrhagic effect. In conclusion, the polysaccharides of C. ferrea barks, containing arabinose, galactose, rhamnose and uronic acid, possess anticoagulant, antiplatelet and antithrombotic properties of low hemorrhagic risk, suggesting potential applicability in thromboembolic disorders.
Assuntos
Caesalpinia/metabolismo , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Animais , Anticoagulantes/química , Coagulação Sanguínea/efeitos dos fármacos , Fibrinolíticos/química , Humanos , Tempo de Tromboplastina Parcial , Casca de Planta/química , Extratos Vegetais/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Polifenóis/farmacologia , Ratos , Ratos Wistar , Trombose VenosaRESUMO
The herpes simplex virus, also known as HSV, is an important human pathogen. Acyclovir (ACV) is the first-line antiviral for the treatment of HSV infections; nevertheless HSV resistance to ACV has been increasingly reported and, therefore, search for alternative drugs have been encouraged. Herein, the effect of Cucumis melo sulfated pectin (SPCm) was evaluated in the HSV-1 infection. Pectin cytotoxicity and its antiherpetic action were determined by assays of MTT and plaque reduction, respectively. The SPCm concentration that reduced the cell viability by 50% (CC50) was 1440 µg/mL, while the concentration that reduced PFU in 50% (IC50) was 6 µg/mL against ACV-sensitive (KOS) strain and 12 µg/mL for ACV-resistant (AR-29) strain. The pectin showed high selectivity index (SI) for both viral strains. Therefore, we suggest that SPCm has been effective for HSV-1, strenghten by viral protein and DNA syntheses inhibition. In conclusion, we have found that SPCm is a promising alternative compound to control HSV infection.
Assuntos
Antivirais/farmacologia , Cucumis melo/química , Herpesvirus Humano 1/efeitos dos fármacos , Pectinas/farmacologia , Aciclovir/farmacologia , Animais , Antivirais/isolamento & purificação , Chlorocebus aethiops , Farmacorresistência Viral/efeitos dos fármacos , Herpes Simples/virologia , Concentração Inibidora 50 , Pectinas/isolamento & purificação , Células Vero , Replicação Viral/efeitos dos fármacosRESUMO
Natural polymer-based hybrid nanocomposites have been proposed as one of the most promising tools for biomedical applications, including disease treatment and diagnosis procedures. Xyloglucan nanocapsules can simultaneously load magnetic iron oxide nanoparticles and bioactive for a specific tissue, reducing the processes of degradation and metabolic inactivation of molecules with biological activity. In this work, magnetic nanocapsules of xyloglucan loaded with hydrophilic sulfated quercetin (MNXQ_SO3) were successfully synthesized by inverse miniemulsion process through interfacial polymerization. The polymeric shell formation of nanocapsules was evidenced by Fourier Transform Infrared spectroscopy and Transmission Electron Microscopy. The ferrofluid (Fe3O4@PAAS) incorporated into the xyloglucan nanocapsules was synthesized by hydrothermal method, using polyacrylic acid sodium salt as coating. Dynamic Light Scattering technique confirmed the nanomeric dimensions (202.3 nm) and the good colloidal stability (-40.2 mV) of MNXQ_SO3. The saturation magnetization analyses pointed out the superparamagnetic behavior of Fe3O4@PAAS (48 emu/g) and MNXQ_SO3 (4.2 emu/g). MNXQ_SO3 was able to modify the release profile of sulfated quercetin (67%) when compared to the free bioactive (100%), exhibiting a release profile compatible with the zero-order kinetic model. The results showed that the development of MNXQ_SO3 presents a new perspective for biomedical applications, including studies of targeted drug delivery.
Assuntos
Glucanos/química , Quercetina/síntese química , Sulfetos/química , Xilanos/química , Sistemas de Liberação de Medicamentos , Difusão Dinâmica da Luz , Cinética , Nanopartículas de Magnetita , Microscopia Eletrônica de Transmissão , Tamanho da Partícula , Quercetina/química , Quercetina/farmacologia , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Edible mushrooms have been increasingly introduced into the human diet, which has driven research into their functional properties. Thus, Agaricus brasiliensis Murill or Agaricus blazei Murill (ABM) is a species native to the Brazilian biome, whose fruiting body has been used not only for dietary purposes, but also in the development of functional foods or as source of molecules of pharmacological interest. The bioactivity of ABM has been related to the presence of polysaccharides, although the contribution of other metabolites cannot be discharged. This work describes the polysaccharides isolation methodology and preparation of the extracts of ABM and their biological activities. Furthermore, it presents a general outline of its characterizations regarding composition, chemical structure and properties in solution. The ABM and its chemical constituents exhibit several biological activities that support their potential use for prevention or treatment of diseases with inflammatory background, such as cancer, diabetes and atherosclerosis. The mechanism of action of the extracts and polysaccharides from ABM is mainly related to a modulation of immune system response or reduction of inflammatory response. This review shows that the ABM has great potential in the pharmaceutical, biotechnological and food sectors that deserves additional research using standardized products.
Assuntos
Agaricus/metabolismo , Anti-Inflamatórios/farmacologia , Polissacarídeos Fúngicos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Brasil , Alimento Funcional , Polissacarídeos Fúngicos/química , Polissacarídeos Fúngicos/isolamento & purificação , HumanosRESUMO
The objective of the study was to prepare active films based on pectin and polyphenol-rich extracts from Tommy Atkins mango peels. Aqueous and methanolic extracts showed a variety of phenolic compounds that were identified by UPLC-MS analysis, and a high content of total phenolics that were quantified by the Folin-Ciocalteau method. The methanolic extract showed better results in antioxidant tests and was more effective in inhibiting the growth of Gram-positive and Gram-negative bacteria. The pectin extracted from mango peels showed good thermal stability and a degree of methoxylation of 58.3% by 1H NMR. The films containing the phenolic extracts showed lower water vapor permeability when compared to the control film (without any phenolic extracts). The incorporation of the extracts led to an increase in elongation (ε) and a decrease in tensile strength (σ) and modulus of elasticity (Y). The films with aqueous or methanolic extracts showed higher antioxidant activity in terms of inhibition of the DPPH radical. Therefore, the films developed in this work are presented as a promising alternative for food packaging and/or coating applications.