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Plant extracts are increasingly recognized as potential prophylactic agents in poultry production due to their diverse bioactive properties. This study investigated the phytochemical and biological properties of Libidibia ferrea (L. ferrea), a plant species native to the Caatinga region of northeastern Brazil. The aim of this study was to identify secondary metabolites and to demonstrate the antimicrobial, antioxidant and protective effects of the plant extract. Three extracts were produced: EHMV, a hydroalcoholic extract from the maceration of pods, and EEMC and EEMV ethanolic extracts from the maceration of peels and pods, respectively, from L. ferrea. High-performance liquid chromatography (HPLC-MS/MS) and atomic absorption spectroscopy (AAS) were used to characterize the metabolites and metals. The antimicrobial activity against Salmonella Galinarum (SG), Salmonella pullorum (SP), Salmonella Heidelberg (SH) and Avian pathogenic Escherichia coli (APEC) was evaluated alone and in combination with probiotic bacteria (Bacillus velenzensis) using agar diffusion and the bactericidal minimum concentration (CBM). The antioxidant potential of the extracts was evaluated in 5 in vitro assays and 6 assays in 3t3 cells. The toxicity of EHMV was tested, and its ability to combat SP infection was demonstrated using a chicken embryo model. The results showed that EHMV exhibited significant antimicrobial activity. The combination of EHMV with BV had synergistic effects, increased antimicrobial activity and induced bacterial sporulation. Composition analysis revealed the presence of 8 compounds, including tannins and phenolic compounds. In vitro antioxidant tests demonstrated that total antioxidant capacity(TAC) activity was increased, and the extract had strong reducing power and notable metal chelating effects. Analysis of 3T3 cells confirmed the protective effect of EHMV against oxidative stress. Toxicity assessments in chicken embryos confirmed the safety of EHMV and its protective effect against SP-induced mortality. EHMV from L. ferrea is rich in proteins and contains essential metabolites that contribute to its antimicrobial and antioxidant properties. When associated with probiotic bacteria such as B. velezensis, this extract increases the inhibition of SH, SG, SP, and APE. The nontoxic nature of EHMV and its protective effects on chicken embryos make it a potential supplement for poultry.
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Antioxidantes , Extractos Vegetales , Animales , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/química , Antibacterianos/farmacología , Antibacterianos/química , Enfermedades de las Aves de Corral/prevención & control , Enfermedades de las Aves de Corral/microbiología , Pollos , Embrión de Pollo , Brasil , Salmonella/efectos de los fármacos , Salmonella/fisiología , Ratones , Escherichia coli/efectos de los fármacosRESUMEN
Maize ranks as the second most widely produced crop globally, yielding approximately 1.2 billion tons, with corn cob being its primary byproduct, constituting 18 kg per 100 kg of corn. Agricultural corn production generates bioactive polysaccharide-rich byproducts, including xylan (Xyl). In this study, we used the redox method to modify corn cob xylan with gallic acid, aiming to enhance its antioxidant and protective capacity against oxidative stress. The conjugation process resulted in a new molecule termed conjugated xylan-gallic acid (Xyl-GA), exhibiting notable improvements in various antioxidant parameters, including total antioxidant capacity (1.4-fold increase), reducing power (1.2-fold increase), hydroxyl radical scavenging (1.6-fold increase), and cupric chelation (27.5-fold increase) when compared with unmodified Xyl. At a concentration of 1 mg/mL, Xyl-GA demonstrated no cytotoxicity, significantly increased fibroblast cell viability (approximately 80%), and effectively mitigated intracellular ROS levels (reduced by 100%) following oxidative damage induced by H2O2. Furthermore, Xyl-GA exhibited non-toxicity toward zebrafish embryos, offered protection against H2O2-induced stress, and reduced the rate of cells undergoing apoptosis resulting from H2O2 exposure. In conclusion, our findings suggest that Xyl-GA possesses potential therapeutic value in addressing oxidative stress-related disturbances. Further investigations are warranted to elucidate the molecular structure of this novel compound and establish correlations with its pharmacological activities.
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Antioxidantes , Ácido Gálico , Animales , Antioxidantes/farmacología , Ácido Gálico/farmacología , Xilanos/farmacología , Zea mays/metabolismo , Peróxido de Hidrógeno/farmacología , Pez Cebra/metabolismo , Estrés OxidativoRESUMEN
Natural substances are strategic candidates for drug development in cancer research. Marine-derived molecules are of special interest due to their wide range of biological activities and sustainable large-scale production. Melanoma is a type of skin cancer that originates from genetic mutations in melanocytes. BRAF, RAS, and NF1 mutations are described as the major melanoma drivers, but approximately 20% of patients lack these mutations and are included in the triple wild-type (tripleWT) classification. Recent advances in targeted therapy directed at driver mutations along with immunotherapy have only partially improved patients' overall survival, and consequently, melanoma remains deadly when in advanced stages. Fucose-containing sulfated polysaccharides (FCSP) are potential candidates to treat melanoma; therefore, we investigated Fucan A, a FCSP from Spatoglossum schröederi brown seaweed, in vitro in human melanoma cell lines presenting different mutations. Up to 72 h Fucan A treatment was not cytotoxic either to normal melanocytes or melanoma cell lines. Interestingly, it was able to impair the tripleWT CHL-1 cell proliferation (57%), comparable to the chemotherapeutic cytotoxic drug cisplatin results, with the advantage of not causing cytotoxicity. Fucan A increased CHL-1 doubling time, an effect attributed to cell cycle arrest. Vascular mimicry, a close related angiogenesis process, was also impaired (73%). Fucan A mode of action could be related to gene expression modulation, in special ß-catenin downregulation, a molecule with protagonist roles in important signaling pathways. Taken together, results indicate that Fucan A is a potential anticancer molecule and, therefore, deserves further investigation.
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Antineoplásicos , Melanoma , Phaeophyceae , Humanos , Fucosa , Sulfatos/farmacología , Melanoma/tratamiento farmacológico , Línea Celular , Polisacáridos/farmacología , Polisacáridos/metabolismo , Antineoplásicos/farmacologíaRESUMEN
Lippia origanoides essential oil (LOEO) is extensively utilised as food preservative due to its antioxidant and antibacterial activities. In this study, the antioxidant and anti-ageing effects of LOEO was investigated in vivo using the nematode Caenorhabditis elegans. The gas chromatography-mass spectrometry analysis indicated that the main components of LOEO are carvacrol and thymol. LOEO treatment improved physiological parameters such as pharyngeal pumping, locomotion and body size indicating that is not toxic to C. elegans. LOEO treatment showed antioxidant effect in C. elegans by reducing endogenous ROS (Reactive Oxygen Species) production and increasing their survival under oxidative stress. Finally, LOEO treatment significantly extended C. elegans lifespan and alleviated the paralysis induced by ß-amyloid peptide overexpression in the muscle. This work demonstrates for the first time LOEO antioxidant and anti-ageing properties on an organism level providing a valuable proof of principle to support further studies in the development of nutraceuticals or antioxidant phytotherapy.
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Oxidative stress has been associated with different diseases, and different medicinal plants have been used to treat or prevent this condition. The leaf ethanolic extract (EE) and aqueous extract (AE) from Coccoloba alnifolia have previously been characterized to have antioxidant potential in vitro and in vivo. In this study, we worked with EE and AE and two partition phases, AF (ethyl acetate) and BF (butanol), from AE extract. These extracts and partition phases did not display cytotoxicity. The EE and AE reduced NO production and ROS in all three concentrations tested. Furthermore, it was observed that EE and AE at 500 µg/mL concentration were able to reduce phagocytic activity by 30 and 50%, respectively. A scratch assay using a fibroblast cell line (NHI/3T3) showed that extracts and fractions induced cell migration with 60% wound recovery within 24 h, especially for BF. It was also observed that AF and BF had antioxidant potential in all the assays evaluated. In addition, copper chelation was observed. This activity was previously not detected in AE. The HPLC-DAD analysis showed the presence of phenolic compounds such as p-cumaric acid and vitexin for extracts, while the GNPS annotated the presence of isoorientin, vitexin, kanakugiol, and tryptamine in the BF partition phase. The data presented here demonstrated that the EE, AE, AF, and BF of C. alnifolia have potential immunomodulatory effects, antioxidant effects, as well as in vitro wound healing characteristics, which are important for dynamic inflammation process control.
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Antioxidantes , Cicatrización de Heridas , Antioxidantes/farmacología , Estrés Oxidativo , Fenoles/farmacología , Línea Celular , Extractos Vegetales/farmacología , Extractos Vegetales/análisis , Etanol/farmacología , Hojas de la PlantaRESUMEN
Fucans from marine algae have been the object of many studies that demonstrated a broad spectrum of biological activities, including anti-inflammatory effects. The aim of this study was to verify the protective effects of a fucan extracted from the brown algae Spatoglossum schröederi in animals submitted to a generalized inflammation model induced by zymosan (ZIGI). BALB/c mice were first submitted to zymosan-induced peritonitis to evaluate the treatment dose capable of inhibiting the induced cellular migration in a simple model of inflammation. Mice were treated by the intravenous route with three doses (20, 10, and 5 mg/kg) of our fucan and, 1 h later, were inoculated with an intraperitoneal dose of zymosan (40 mg/kg). Peritoneal exudate was collected 24 h later for the evaluation of leukocyte migration. Doses of the fucan of Spatoglossum schröederi at 20 and 10 mg/kg reduced peritoneal cellular migration and were selected to perform ZIGI experiments. In the ZIGI model, treatment was administered 1 h before and 6 h after the zymosan inoculation (500 mg/kg). Treatments and challenges were administered via intravenous and intraperitoneal routes, respectively. Systemic toxicity was assessed 6 h after inoculation, based on three clinical signs (bristly hair, prostration, and diarrhea). The peritoneal exudate was collected to assess cellular migration and IL-6 levels, while blood samples were collected to determine IL-6, ALT, and AST levels. Liver tissue was collected for histopathological analysis. In another experimental series, weight loss was evaluated for 15 days after zymosan inoculation and fucan treatment. The fucan treatment did not present any effect on ZIGI systemic toxicity; however, a fucan dose of 20 mg/kg was capable of reducing the weight loss in treated mice. The treatment with both doses also reduced the cellular migration and reduced IL-6 levels in peritoneal exudate and serum in doses of 20 and 10 mg/kg, respectively. They also presented a protective effect in the liver, with a reduction in hepatic transaminase levels in both doses of treatment and attenuated histological damage in the liver at a dose of 10 mg/kg. Fucan from S. schröederi presented a promising pharmacological activity upon the murine model of ZIGI, with potential anti-inflammatory and hepatic protective effects, and should be the target of profound and elucidative studies.
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Peritonitis , Phaeophyceae , Ratones , Animales , Zimosan/toxicidad , Interleucina-6 , Modelos Animales de Enfermedad , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Peritonitis/inducido químicamente , Peritonitis/tratamiento farmacológico , Antiinflamatorios/efectos adversos , Ascitis , Pérdida de PesoRESUMEN
Medicinal plants, such as Talisia esculenta, are rich in antioxidant biomolecules, which are used in the treatment and prevention of many diseases. The antioxidant potential of T. esculenta extracts obtained from leaves and fruit peels was investigated using biochemical and 3T3 cell line assays as well as in vivo assays using an organism model Tenebrio molitor. Four extracts were tested: hydroethanolic extracts from leaves (HF) and from fruit peels (HC), and infusion extracts from leaves (IF) and from fruit peels (IC). The biochemical assays demonstrated an antioxidant capacity verified by TAC, reducing power, DPPH, and copper chelating assays. None of the extracts exhibited cytotoxicity against 3T3 cells, instead offering a protection against CuSO4-induced oxidative stress. The antioxidant activity observed in the extracts, including their role as free radical scavengers, copper chelators, and stress protectors, was further confirmed by T. molitor assays. The CLAE-DAD analysis detected phenolic compounds, including gallic acid, rutin, and quercitrin, as the main constituents of the samples. This study highlights that leaf and fruit peels extracts of T. esculenta could be effective protectors against ROS and copper-induced stress in cellular and invertebrate models, and they should be considered as coadjutants in the treatment and prevention of diseases related to oxidative stress and for the development of natural nutraceutical products.
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Productos Biológicos , Sapindaceae , Animales , Ratones , Antioxidantes/farmacología , Cobre , Extractos Vegetales/farmacologíaRESUMEN
A blend refers to the combination of two or more components to achieve properties that are superior to those found in the individual products used for their production. Gracilaria birdiae agaran (SPGb) and chromium picolinate (ChrPic) are both antioxidant agents. However, there is no documentation of blends that incorporate agarans and ChrPic. Hence, the objective of this study was to generate blends containing SPGb and ChrPic that exhibit enhanced antioxidant activity compared to SPGb or ChrPic alone. ChrPic was commercially acquired, while SPGb was extracted from the seaweed. Five blends (B1; B2; B3; B4; B5) were produced, and tests indicated B5 as the best antioxidant blend. B5 was not cytotoxic or genotoxic. H2O2 (0.6 mM) induced toxicity in fibroblasts (3T3), and this effect was abolished by B5 (0.05 mg·mL-1); neither ChrPic nor SPGb showed this effect. The cells also showed no signs of toxicity when exposed to H2O2 after being incubated with B5 and ChrPic for 24 h. In another experiment, cells were incubated with H2O2 and later exposed to SPGb, ChrPic, or B5. Again, SPGb was not effective, while cells exposed to ChrPic and B5 reduced MTT by 100%. The data demonstrated that B5 has activity superior to SPGb and ChrPic and points to B5 as a product to be used in future in vivo tests to confirm its antioxidant action. It may also be indicated as a possible nutraceutical agent.
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Gracilaria , Rhodophyta , Algas Marinas , Antioxidantes/farmacología , Peróxido de Hidrógeno/farmacología , VerdurasRESUMEN
Oxybenzone (BP-3) is an ultraviolet (UV) filter widely used in industries that is directly or indirectly released into the aquatic environment. However, little is known about its effects on brain performance. Here, we investigated whether BP-3 exposure affects the redox imbalance in zebrafish and how they respond to a task that requires memory of an aversive situation. Fish were exposed to BP-3 10 and 50 µg L-1 for 15 days and then tested using an associative learning protocol with electric shock as a stimulus. Brains were extracted for reactive oxygen species (ROS) measurement and qPCR analysis of antioxidant enzyme genes. ROS production increased for exposed animals, and catalase (cat) and superoxide dismutase 2 (sod 2) were upregulated. Furthermore, learning and memory were reduced in zebrafish exposed to BP-3. These results suggested that BP-3 may lead to a redox status imbalance, causing impaired cognition and reinforcing the need to replace the toxic UV filters with filters that minimize environmental effects.
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Benzofenonas , Contaminantes Químicos del Agua , Pez Cebra , Animales , Encéfalo/metabolismo , Catalasa/metabolismo , Estrés Oxidativo , Especies Reactivas de Oxígeno , Superóxido Dismutasa/metabolismo , Contaminantes Químicos del Agua/toxicidad , Contaminantes Químicos del Agua/análisis , Pez Cebra/metabolismo , Benzofenonas/toxicidadRESUMEN
Oreochromis niloticus (tilapia) is one of the most cultivated fish species worldwide. Tilapia farming generates organic waste from fish removal processes in nurseries. Visceral waste can damage natural ecosystems. Therefore, the use of this material as a source of biomolecules helps reduce environmental impacts and improve pharmacological studies. Tilapia viscera were subjected to proteolysis and complexation with an ion-exchange resin. The obtained glycosaminoglycans were purified using ion exchange chromatography (DEAE-Sephacel). The electrophoretic profile and analysis of 1H/13C nuclear magnetic resonance (NMR) spectra allowed for the characterization of the compound as chondroitin sulfate and its sulfation position. This chondroitin was named CST. We tested the ability of CST to reduce leukocyte influx in acute peritonitis models induced by sodium thioglycolate and found a significant reduction in leukocyte migration to the peritoneal cavity, similar to the polymorphonuclear population of the three tested doses of CST. This study shows, for the first time, the potential of CST obtained from O. niloticus waste as an anti-inflammatory drug, thereby contributing to the expansion of the study of molecules with pharmacological functions.
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Cíclidos , Peritonitis , Tilapia , Animales , Sulfatos de Condroitina , Ecosistema , Peritonitis/inducido químicamente , Peritonitis/tratamiento farmacológicoRESUMEN
Depression is a psychiatric disorder affecting the lives of patients and their families worldwide. It is an important pathophysiology; however, the molecular pathways involved are not well understood. Pharmacological treatment may promote side effects or be ineffective. Consequently, efforts have been made to understand the molecular pathways in depressive patients and prevent their symptoms. In this context, animal models have suggested phytochemicals from medicinal plants, especially phenolic acids, as alternative treatments. These bioactive molecules are known for their antioxidant and antiinflammatory activities. They occur in some fruits, vegetables, and herbal plants. This review focused on phenolic acids and extracts from medicinal plants and their effects on depressive symptoms, as well as the molecular interactions and pathways implicated in these effects. Results from preclinical trials indicate the potential of phenolic acids to reduce depressive-like behaviour by regulating factors associated with oxidative stress, neuroinflammation, autophagy, and deregulation of the hypothalamic-pituitary-adrenal axis, stimulating monoaminergic neurotransmission and neurogenesis, and modulating intestinal microbiota.
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Antioxidantes , Plantas Medicinales , Animales , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Antioxidantes/química , Sistema Hipotálamo-Hipofisario , Sistema Hipófiso-Suprarrenal , Antidepresivos/farmacología , Antidepresivos/uso terapéutico , Plantas Medicinales/química , Extractos Vegetales/farmacologíaRESUMEN
Obesity is a global public health problem that is associated with oxidative stress. One of the strategies for the treatment of obesity is the use of drugs; however, these are expensive and have numerous side effects. Therefore, the search for new alternatives is necessary. Baccharis trimera is used in Brazilian folk medicine for the treatment of obesity. Here, B. trimera leaf extract (BT) showed antioxidant activity in seven in vitro tests, and it was not toxic to 3T3 murine fibroblasts or Caenorhabditis elegans. Furthermore, BT reduces the intracellular amount of reactive oxygen species and increases C. elegans survival. Moreover, these effects were not dependent on transcription factors. The inhibition of fat accumulation by BT in the C. elegans model was also investigated. BT reduced lipid accumulation in animals fed diets without or with high amount of glucose. Furthermore, it was observed using RNA interference (iRNA) that BT depends on the transcription factor NHR-49 to exert its effect. Phytochemical analysis of BT revealed rutin, hyperoside, and 5-caffeoylquinic acid as the main BT components. Thus, these data demonstrate that BT has antioxidant and anti-obesity effects. However, further studies should be conducted to understand the mechanisms involved in its action.
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Leishmanolysin, also known as major promastigote protease (PSP) or gp63, is the most abundant surface glycoprotein of Leishmania spp., and has been extensively studied and recognized as the main parasite virulence factor. Characterized as a metalloprotease, gp63 can be powerfully inactivated in the presence of a metal chelator. In this study, we first used the structural parameters of a 7-hydroxycoumarin derivative, L1 compound, to evaluate the theoretical-computational experiments against gp63, comparing it with an available metal chelator already described. The methodology followed was (i) analysis of the three-dimensional structure of gp63 as well as its active site, and searching the literature and molecular databases for possible inhibitors; (ii) molecular docking simulations and investigation of the interactions in the generated protein-ligand complexes; and (iii) the individual energy of the gp63 amino acids that interacted most with the ligands of interest was quantified by ab initio calculations using Molecular Fraction with Conjugated Caps (MFCC). MFCC still allowed the final quantum balance calculations of the protein interaction to be obtained with each inhibitor candidate binder. L1 obtained the best energy quantum balance result with -2 eV, followed by DETC (-1.4 eV), doxycycline (-1.3 eV), and 4-terpineol (-0.6 eV), and showed evidence of covalent binding in the enzyme active site. In vitro experiments confirmed L1 as highly effective against L. amazonensis parasites. The compound also exhibited a low cytotoxicity profile against mammalian RAW and 3T3 cells lines, presenting a selective index of 149.19 and 380.64 µM, respectively. L1 induced promastigote forms' death by necrosis and the ultrastructural analysis revealed disruption in membrane integrity. Furthermore, leakage of the contents and destruction of the parasite were confirmed by Spectroscopy Dispersion analysis. These results together suggested L1 has a potential effect against L. amazonensis, the etiologic agent of diffuse leishmaniasis, and the only one that currently does not have a satisfactory treatment.
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Leishmania , Animales , Quelantes , Leishmania/metabolismo , Mamíferos/metabolismo , Metaloendopeptidasas/metabolismo , Metaloproteasas , Ratones , Simulación del Acoplamiento Molecular , FagocitosisRESUMEN
Antioxidant compounds decrease the amount of intracellular reactive oxygen species (ROS) and, consequently, reduce the deleterious effects of ROS in osteoblasts. Here, we modified a 21 kDa fucoidan (FucA) with gallic acid (GA) using the redox method, to potentiate its antioxidant/protective capacity on pre-osteoblast-like cells (MC3T3) against oxidative stress. The 20 kDa FucA-GA contains 37 ± 3.0 mg GA per gram of FucA. FucA-GA was the most efficient antioxidant agent in terms of total antioxidant capacity (2.5 times), reducing power (five times), copper chelation (three times), and superoxide radical scavenging (2 times). Exposure of MC3T3 cells to H2O2 increased ROS levels and activated caspase-3 along with caspase-9. In addition, the cell viability decreased approximately 80%. FucA-GA also provided the most effective protection against oxidative damage caused by H2O2. Treatment with FucA-GA (1.0 mg/mL) increased cell viability (~80%) and decreased intracellular ROS (100%) and caspase activation (~80%). In addition, Fuc-GA (0.1 mg/mL) abolished H2O2-induced oxidative stress in zebra fish embryos. Overall, FucA-GA protected MC3T3 cells from oxidative stress and could represent a possible adjuvant for the treatment of bone fragility by counteracting oxidative phenomena.
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Antioxidantes , Ácido Gálico , Animales , Antioxidantes/farmacología , Ácido Gálico/farmacología , Peróxido de Hidrógeno/farmacología , Oxidación-Reducción , Estrés Oxidativo , Polisacáridos , Especies Reactivas de OxígenoRESUMEN
Sulfated polysaccharides (SPS) from seaweeds have great biochemical and biotechnological potential. This study aimed to investigate the effect of SPS isolated from the seaweed Caulerpa sertularioides on adipogenic differentiation as a possible alternative treatment for obesity. The SPS-rich extract from the seaweed C. sertularioides was fractioned into three SPS-rich fractions (F0.5; F0.9; and F1.8) chemically characterized. Among these four samples, only F0.9 showed a significant inhibitory effect on adipogenesis of 3T3-L1 preadipocytes. Ten SPS-rich fractions were isolated from F0.9 through ion-exchange chromatography. However, only the fraction (CS0.2) containing a sulfated glucan was able to inhibit adipogenesis. CS0.2 reduces lipid accumulation and inhibits the expression of key adipogenic (PPARγ, C/EBPß, and C/EBPα) and lipogenic markers (SREBP-1c, Fabp4, and CD36). The data points to the potential of sulfated glucan from C. sertularioides for the development of functional approaches in obesity management.
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Caulerpa , Algas Marinas , Células 3T3-L1 , Adipocitos , Adipogénesis , Animales , Caulerpa/metabolismo , Glucanos/farmacología , Ratones , PPAR gamma/metabolismo , Polisacáridos/metabolismo , Polisacáridos/farmacología , Algas Marinas/química , Sulfatos/farmacologíaRESUMEN
Antioxidants fucoidans from three seaweeds, Undaria pinnatifida (FUP), Macrocystis pyrifera (FMP) and Fucus vesiculosus (FFV) are sold commercially. However, it is unclear which fucoidan is the most potent antioxidant. Therefore, our objective was to compare the antioxidant activities of these fucoidans. For this purpose, six in vitro antioxidant tests were used, total antioxidant capacity, hydroxyl radical scavenging assay, ferrous and cupric chelating assay, reducing power and H2O2 scavenging assay. The data showed that the fucoidans had a low capacity to donate electrons, and a low capacity to chelate metals. The best activity obtained was in the scavenging of hydroxyl radical. When macrophages were exposed to H2O2 and fucoidans, MTT and live/dead assays showed that all fucoidans protected cells from oxidative damage. The survival rate of zebrafish embryos was significantly higher when exposed to H2O2 and fucoidans than H2O2 alone. In summary, the fucoidans evaluated were ranked according to their antioxidant activity as follows: FMP > FFV > FUP, and the results suggest that these fucoidans, mainly FMP, can be used in the formulation of medicines/foods.
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Fucus , Macrocystis , Undaria , Animales , Antioxidantes/farmacología , Peróxido de Hidrógeno , Radical Hidroxilo , Polisacáridos/farmacología , Pez CebraRESUMEN
The brown seaweed Spatoglossum schröederi synthesizes three bioactive fucoidans, the most abundant of which is fucan A. This fucoidan was extracted and its identity was confirmed by chemical analysis, Fourier-transform infrared spectroscopy (FTIR), and agarose gel electrophoresis. Thereafter, silver nanoparticles containing fucan A (AgFuc) were produced using an environmentally friendly synthesis method. AgFuc synthesis was analyzed via UV-vis spectroscopy and FTIR, which confirmed the presence of both silver and fucan A in the AgFuc product. Dynamic light scattering (DLS), X-ray diffraction, scanning electron microscopy, and atomic force microscopy revealed that the AgFuc particles were ~180.0 nm in size and spherical in shape. DLS further demonstrated that AgFuc was stable for five months. Coupled plasma optical emission spectrometry showed that the AgFuc particles contained 5% silver and 95% sugar. AgFuc was shown to be more effective in inhibiting the ability of parasites to reduce MTT than fucan A or silver, regardless of treatment time. In addition, AgFuc induced the death of ~60% of parasites by necrosis and ~17% by apoptosis. Therefore, AgFuc induces damage to the parasites' mitochondria, which suggests that it is an anti-Trypanosoma cruzi agent. This is the first study to analyze silver nanoparticles containing fucan as an anti-Trypanosoma cruzi agent. Our data indicate that AgFuc nanoparticles have potential therapeutic applications, which should be determined via preclinical in vitro and in vivo studies.
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Sulfated polysaccharides (SPs) from seaweeds are potential bioactive natural compounds, but their DNA protective activity is poorly explored. This article aimed to evaluate the genotoxic/antigenotoxic potentials of a sulfated heterofucan from brown seaweed Spatoglossum schröederi (Fucan A - FA) and a sulfated galactan from green seaweed Codium isthomocladum (3G4S) using in vitro Comet assay (alkaline and oxidative versions) with HepG2 cells. The antioxidant activity of these SPs was evaluated by total antioxidant capacity, radical scavenging, metal chelating, and antioxidant enzyme activity assays. Both SPs were not genotoxic. FA and 3G4S displayed strong antigenotoxic activity against oxidizing chemical (H2O2) but not against alkylating chemical (MMS). The DNA damage reduction after a pre-treatment of 72 h with these SPs was 81.42% to FA and 81.38% to 3G4S. In simultaneous exposure to FA or 3G4S with H2O2, HepG2 cells presented 48.04% and 55.41% of DNA damage reduction compared with the control, respectively. The antigenotoxicity of these SPs relates to direct antioxidant activity by blockage of the initiation step of the oxidative chain reaction. Therefore, we conclude that FA and 3G4S could be explored as functional natural compounds with antigenotoxic activity due to their great protection against oxidative DNA damage.
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Algas Marinas , Sulfatos , Antioxidantes/química , Antioxidantes/farmacología , Daño del ADN , Peróxido de Hidrógeno , Oxidación-Reducción , Polisacáridos/química , Polisacáridos/farmacología , Algas Marinas/química , Sulfatos/químicaRESUMEN
Trypanosoma cruzi is a protozoan parasite responsible for Chagas disease, which affects millions around the world and is not treatable in its chronic stage. Sodium diethyldithiocarbamate is a compound belonging to the carbamate class and, in a previous study, demonstrated high efficacy against T. cruzi, showing itself to be a promising compound for the treatment of Chagas disease. This study investigates the encapsulation of sodium diethyldithiocarbamate by poly-lactic acid in nanoparticles, a system of biodegradable nanoparticles that is capable of reducing the toxicity caused by free DETC against cells and maintaining the antiparasitic activity. The nanosystem PLA-DETC was fabricated using nanoprecipitation, and its physical characterization was measured via DLS, SEM, and AFM, demonstrating a small size around 168 nm and a zeta potential of around -19 mv. Furthermore, the toxicity was determined by MTT reduction against three cell lines (VERO, 3T3, and RAW), and when compared to free DETC, we observed a reduction in cell mortality, demonstrating the importance of DETC nanoencapsulation. In addition, the nanoparticles were stained with FITC and put in contact with cells for 24 h, followed by confirmation of whether the nanosystem was inside the cells. Lastly, the antiparasitic activity against different strains of T. cruzi in trypomastigote forms was determined by resazurin reduction and ROS production, which demonstrated high efficacy towards T. cruzi equal to that of free DETC.
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Oxidative stress is the cause of numerous diseases in humans; therefore, there has been a continuous search for novel antioxidant molecules. Fungal chitosan is an attractive molecule that has several applications (antifungal, antibacterial, anticancer and antiparasitic action) owing to its unique characteristics; however, it exhibits low antioxidant activity. The aim of this study was to obtain fungal chitosan (Chit-F) from the fungus Rhizopus arrhizus and synthesize its derivative, fungal chitosan-gallic acid (Chit-FGal), as a novel antioxidant chitosan derivative for biomedical use. A low molecular weight Chi-F (~3.0 kDa) with a degree of deacetylation of 86% was obtained from this fungus. Chit-FGal (3.0 kDa) was synthesized by an efficient free radical-mediated method using hydrogen peroxide (H2O2) and ascorbic acid. Both Chit-F and Chit-FGal showed similar copper chelating activities; however, Chit-FGal was more efficient as an antioxidant, exhibiting twice the total antioxidant capacity than Chi-F (p < 0.05). Furthermore, H2O2 (0.06 M) promoted a 50% decrease in the viabilities of the 3T3 fibroblast cells. However, this effect was abolished in the presence of Chit-FGal (0.05-0.25 mg/mL), indicating that Chit-FGal protected the cells from oxidative damage. These results suggest that Chit-FGal may be a promising agent to combat oxidative stress.