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Melanoma is difficult to treat with chemotherapy, prompting the need for new treatments. Protease inhibitors have emerged as promising candidates as tumor cell proteases promote metastasis. Researchers have developed a chimeric form of the Bauhinia bauhinioides kallikrein inhibitor, rBbKIm, which has shown negative effects on prostate tumor cell lines DU145 and PC3. Crataeva tapia bark lectin, CrataBL, targets sulfated oligosaccharides in glycosylated proteins and has also demonstrated deleterious effects on prostate and glioblastoma tumor cells. However, neither rBbKIm nor its derived peptides affected the viability of SK-MEL-28, a melanoma cell line, while CrataBL decreased viability by over 60%. Two peptides, Pep. 26 (Ac-Q-N-S-S-L-K-V-V-P-L-NH2) and Pep. 27 (Ac-L-P-V-V-K-L-S-S-N-Q-NH2), were also tested. Pep. 27 suppressed cell migration and induced apoptosis when combined with vemurafenib, while Pep. 26 inhibited cell migration and reduced nitric oxide and the number of viable cells. Vemurafenib, a chemotherapy drug used to treat melanoma, was found to decrease the release of interleukin 8 and PDGF-AB/BB cytokines and potentiated the effects of proteins and peptides in reducing these cytokines. These findings suggest that protease inhibitors may be effective in blocking melanoma cells and highlight the potential of CrataBL and its derived peptides.
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Melanoma , Masculino , Humanos , Vemurafenib/farmacología , Melanoma/tratamiento farmacológico , Línea Celular Tumoral , Apoptosis , Citocinas/farmacología , Inhibidores de Proteasas/farmacologíaRESUMEN
Despite the fact that skin has a stronger potential to regenerate than other tissues, wounds have become a serious healthcare issue. Much effort has been focused on developing efficient therapeutical approaches, especially biological ones. This paper presents a comprehensive review on the wound healing process, the classification of wounds, and the particular characteristics of each phase of the repair process. We also highlight characteristics of the normal process and those involved in impaired wound healing, specifically in the case of infected wounds. The treatments discussed here include proteins, lipids, and carbohydrates. Proteins are important actors mediating interactions between cells and between them and the extracellular matrix, which are essential interactions for the healing process. Different strategies involving biopolymers, blends, nanotools, and immobilizing systems have been studied against infected wounds. Lipids of animal, mineral, and mainly vegetable origin have been used in the development of topical biocompatible formulations, since their healing, antimicrobial, and anti-inflammatory properties are interesting for wound healing. Vegetable oils, polymeric films, lipid nanoparticles, and lipid-based drug delivery systems have been reported as promising approaches in managing skin wounds. Carbohydrate-based formulations as blends, hydrogels, and nanocomposites, have also been reported as promising healing, antimicrobial, and modulatory agents for wound management.
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Antiinfecciosos , Cicatrización de Heridas , Animales , Piel , Lípidos , CarbohidratosRESUMEN
Eugenia pohliana DC.(Myrtaceae) is used in folk medicine by communities in Brazil. However, there are no reports on its biological activity. This is the first study to identify the components of E. pohliana essential oil (EpEO) and evaluate their antinociceptive and anti-inflammatory activities in an in vivo model at doses of 25, 50, and 100 mg/kg. The essential oil (EO) was obtained by hydrodistillation, and the analysis was performed by gas chromatography coupled with mass spectrometry. Antinociceptive activity was evaluated by writhing tests, tail movement, and formalin (neurogenic and inflammatory pain); naloxone was used to determine the nociception mechanism. Anti-inflammatory activity was assessed by oedema and peritonitis tests. We found that (E)-ß-caryophyllene (BCP) (15.56%), δ-cadinene (11.24%) and α-cadinol (10.89%) were the major components. In the writhing test, there was a decrease in writing by 42.95-70.70%, in the tail movement, an increase in latency time by 69.12-86.63%, and in the formalin test, there was a reduction in pain neurogenic by 29.54-61.74%, and inflammatory pain by 37.42-64.87%. The antinociceptive effect of EpEO occurs through the activation of opioid receptors. In addition, a reduction in inflammation by 74.93â81.41% was observed in the paw edema test and inhibition of the influx of leukocytes by 51.86â70.38% and neutrophils by 37.74â54.72% in the peritonitis test. It was concluded that EpEO has antinociceptive effect by the opioid pathway, as shown by the inhibitory effect of naloxone, and anti-inflammatory actions, and that its use does not cause hemolytic damage or behavioral change.
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Eugenia , Myrtaceae , Aceites Volátiles , Peritonitis , Ratones , Animales , Eugenia/química , Aceites Volátiles/farmacología , Aceites Volátiles/uso terapéutico , Nocicepción , Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Edema/inducido químicamente , Edema/tratamiento farmacológico , Dolor/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Inflamación/tratamiento farmacológico , Peritonitis/tratamiento farmacológico , Naloxona/uso terapéuticoRESUMEN
The objective of this study was to determine the cytotoxicity of organic extracts of P. moniliformis in vitro and identify the acute toxicity and genotoxicity in vivo. The leaves were extracted using three organic solvents (cyclohexane [EP1], ethyl acetate [EP2], and methanol [EP3]). Phytochemical qualitative analysis was performed by thin layer chromatography (TLC). Cytotoxicity tests were performed on human embryonic kidney (HEK) cells and J774 murine macrophages. Acute toxicity in mice was measured after intraperitoneal (ip) administration of 2000 mg/kg, while evaluation of genotoxicity and mutagenicity were assessed using the comet assay and the micronucleus (MN) test, respectively. The TLC analysis of the extracts revealed the presence of flavonoids, triterpenes, steroids, and saponins. In the cytotoxicity assay, extracts EP1 and EP3 altered proliferation of HEK cells, and all organic extracts increased the viability of J774 cells. In the toxicity tests, no deaths or behavioral alterations were observed in mice exposed to the acute dose of the extracts. Although some extracts led to changes in hematological and histological parameters, these results did not indicate physiological changes. In relation to the MN test and comet assay, no significant changes were detected in the DNA of the animals tested with the extracts EP1, EP2, and EP3. Thus, extracts of P. moniliformis were not considered to be toxic and did not induce formation of MN or damage to cellular DNA in the genotoxicity tests.
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Citotoxinas/toxicidad , Embrión de Mamíferos/efectos de los fármacos , Fabaceae/toxicidad , Mutagénesis/efectos de los fármacos , Mutágenos/toxicidad , Extractos Vegetales/toxicidad , Hojas de la Planta/toxicidad , Animales , Células Cultivadas/efectos de los fármacos , Fabaceae/química , Humanos , Riñón/efectos de los fármacos , Macrófagos/efectos de los fármacos , Ratones , Modelos Animales , Extractos Vegetales/química , Hojas de la Planta/química , Plantas Medicinales/química , Plantas Medicinales/toxicidadRESUMEN
Currently available drugs for treatment of glioblastoma, the most aggressive brain tumor, remain inefficient, thus a plethora of natural compounds have already been shown to have antimalignant effects. However, these have not been tested for their impact on tumor cells in their microenvironment-simulated cell models, e.g., mesenchymal stem cells in coculture with glioblastoma cell U87 (GB). Mesenchymal stem cells (MSC) chemotactically infiltrate the glioblastoma microenvironment. Our previous studies have shown that bone-marrow derived MSCs impair U87 growth and invasion via paracrine and cell-cell contact-mediated cross-talk. Here, we report on a plant-derived protein, obtained from Crataeva tapia tree Bark Lectin (CrataBL), having protease inhibitory/lectin activities, and demonstrate its effects on glioblastoma cells U87 alone and their cocultures with MSCs. CrataBL inhibited U87 cell invasion and adhesion. Using a simplified model of the stromal microenvironment, i.e., GB/MSC direct cocultures, we demonstrated that CrataBL, when added in increased concentrations, caused cell cycle arrest and decreased cocultured cells' viability and proliferation, but not invasion. The cocultured cells' phenotypes were affected by CrataBL via a variety of secreted immunomodulatory cytokines, i.e., G-CSF, GM-CSF, IL-6, IL-8, and VEGF. We hypothesize that CrataBL plays a role by boosting the modulatory effects of MSCs on these glioblastoma cell lines and thus the effects of this and other natural lectins and/or inhibitors would certainly be different in the tumor microenvironment compared to tumor cells alone. We have provided clear evidence that it makes much more sense testing these potential therapeutic adjuvants in cocultures, mimicking heterogeneous tumor-stroma interactions with cancer cells in vivo. As such, CrataBL is suggested as a new candidate to approach adjuvant treatment of this deadly tumor.
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Capparaceae/química , Células Madre Mesenquimatosas/efectos de los fármacos , Corteza de la Planta/química , Extractos Vegetales/farmacología , Lectinas de Plantas/farmacología , Inhibidores de Proteasas/farmacología , Adhesión Celular/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Técnicas de Cocultivo , Citocinas/biosíntesis , Glioblastoma/metabolismo , Humanos , Células Madre Mesenquimatosas/metabolismo , Metaloproteasas/antagonistas & inhibidores , Óxido Nítrico/biosíntesis , Extractos Vegetales/química , Lectinas de Plantas/química , Inhibidores de Proteasas/químicaRESUMEN
This study describes the first antibiofilm and antibacterial screening for plants from Caatinga against Ralstonia solanacearum, a causal agent of bacterial wilt that presents serious difficulties in control. There were prepared 22 aqueous extracts of plants collected in the Vale do Catimbau-PE, Brazil. The potential antibacterial activity was evaluated by absorbance in OD600 and the antibiofilm activity through the crystal violet method, both of them performed in microplate against isolates of R. solanacearum biofilm formers. The results of the screening showed that Jacaranda rugosa presented antimicrobial activity higher than 90%, while Harpochilus neesianus and Myroxylon peruiferum presented antibiofilm activity higher than 50% for all tested isolates. However, Croton heliotropiifolius showed both the activities, being thus very promising for application in the control of this phytopathogen. The search for viable alternatives to the development of new bioactive compounds safe for the environment, humans, and animals from an adverse and scarce environment such as the Caatinga and encouraged us to find plants that produce effective metabolites against phytopathogenic microorganisms. This in vitro screening is important to guide the development of new products in addition to guide research studies of bioactive compounds.
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Antibacterianos/farmacología , Biopelículas/efectos de los fármacos , Extractos Vegetales/farmacología , Ralstonia solanacearum/efectos de los fármacos , Tracheophyta/química , Biopelículas/crecimiento & desarrollo , Agentes de Control Biológico/farmacología , Brasil , Pruebas de Sensibilidad Microbiana , Enfermedades de las Plantas/microbiología , Enfermedades de las Plantas/prevención & control , Plantas Medicinales , Ralstonia solanacearum/fisiologíaRESUMEN
CONTEXT: Buchenavia tetraphylla (Aubl.) RA Howard (Combretaceae: Combretoideae) is an ethnomedicinal plant with reported antifungal action. OBJECTIVE: This study evaluates the antimicrobial activity of B. tetraphylla leaf extracts against clinical isolates of Candida albicans. The morphological alterations, combinatory effects with fluconazole and the cytotoxicity of the active extract were analyzed. MATERIALS AND METHODS: Extracts were obtained using different solvents (hexane: BTHE; chloroform: BTCE; ethyl acetate: BTEE; and methanol: BTME). Antimicrobial activity was determined by the broth microdilution method using nine strains of C. albicans isolated from vaginal secretions and one standard strain (UFPEDA 1007). RESULTS: All extracts showed anti-C. albicans activity, including against the azole-resistant strains. The MIC values ranged from 156 to 2500 µg/mL for the BTHE; 156 to 1250 µg/mL for the BTCE; 625 to 1250 µg/mL for the BTME and 625 µg/mL to 2500 µg/mL for the BTEE. BTME showed the best anti-C. albicans activity. This extract demonstrated additive/synergistic interactions with fluconazole. Scanning electron microscopy analysis suggested that the BTME interferes with the cell division and development of C. albicans. BTME showed IC50 values of 981 and 3935 µg/mL, against J774 macrophages and human erythrocytes, respectively. This extract also enhanced the production of nitric oxide by J774 macrophages. DISCUSSION AND CONCLUSION: Buchenavia tetraphylla methanolic extract (BTME) is a great source of antimicrobial compounds that are able to enhance the action of fluconazole against different C. albicans strains; this action seems related to inhibition of cell division.
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Antifúngicos/farmacología , Candida albicans/efectos de los fármacos , Combretaceae/química , Extractos Vegetales/farmacología , Vagina/microbiología , Animales , Antifúngicos/aislamiento & purificación , Antifúngicos/toxicidad , Candida albicans/crecimiento & desarrollo , Candida albicans/aislamiento & purificación , Candida albicans/ultraestructura , Línea Celular , Supervivencia Celular/efectos de los fármacos , Farmacorresistencia Fúngica , Quimioterapia Combinada , Femenino , Fluconazol/farmacología , Hemólisis/efectos de los fármacos , Humanos , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Macrófagos/patología , Ratones , Pruebas de Sensibilidad Microbiana , Óxido Nítrico/metabolismo , Fitoterapia , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/toxicidad , Plantas Medicinales , Solventes/química , Vagina/metabolismoRESUMEN
This work aimed to investigate the chemical composition, antioxidant capacity, antibacterial activity, and intestinal and gastric protective effects, in addition to the acute toxicity of the essential oil of E. stictopetala (EOEs). (E)-caryophyllene (18.01%), ß-pinene (8.84%), and (E)-nerolidol (8.24%), were the components found in higher content in the essential oil. The EOEs showed antioxidant capacity with IC50 values ranging from 220.28 to 283.67 µg/mL, in addition to presenting antibacterial activity against Escherichia coli, Enterobacter aerogenes, Vibrio cholerae, Salmonella enterica, and Listeria monocytogenes. The essential oil showed a gastroprotective effect, with a reduction in the levels of TNF-α, IL-1ß, and IL-6, having multiple pharmacological mechanisms of action. An antidiarrheal effect of EOEs was observed in the castor oil-induced diarrheal model, with reduced intestinal motility. Our findings demonstrate that essential oil can be beneficial in pharmaceutical and therapeutic applications for treating gastrointestinal diseases.
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Probiotic-containing foods are among the most appreciated functional foods; however, probiotic-based dairy products cannot be consumed by people who are lactose intolerant, allergic to milk, or vegetarian or vegan individuals. Thus, new non-dairy matrices have been tested for probiotics delivery. This study evaluated the growth and viability of Limosilactobacillus fermentum ATCC 23271 and Lacticaseibacillus rhamnosus ATCC 9595 in Pitanga juice (Eugenia uniflora L.). The effects of the fermentation on the antioxidant and anti-infective properties of the juice were also analyzed. The E. uniflora juice allowed lactobacilli growth without supplementation, reaching rates around 8.4 Log CFU/mL and producing organic acids (pH values < 4) after 72 h of fermentation. The strain remained viable after 35 days of refrigerated storage. Fermentation by these bacteria increases the antioxidant capacity of the juice. The central composite rotational design was employed to evaluate the effects of bacterial inoculum and pulp concentration on growth and organic acids production by L. fermentum ATCC 23271. The strain was viable and produced organic acids in all tested combinations. L. fermentum-fermented juice and its cell-free supernatant significantly increased the survival of Tenebrio molitor larvae infected by enteroaggregative Escherichia coli 042. The results obtained in this study provide more insights into the potential of Pitanga juice to develop a functional non-dairy probiotic beverage with antioxidant and anti-infective properties.
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Antioxidantes , Eugenia , Fermentación , Limosilactobacillus fermentum , Probióticos , Antioxidantes/farmacología , Antioxidantes/metabolismo , Limosilactobacillus fermentum/metabolismo , Limosilactobacillus fermentum/crecimiento & desarrollo , Limosilactobacillus fermentum/fisiología , Limosilactobacillus fermentum/efectos de los fármacos , Probióticos/farmacología , Eugenia/química , Antiinfecciosos/farmacología , Jugos de Frutas y Vegetales/microbiología , Jugos de Frutas y Vegetales/análisis , Lacticaseibacillus rhamnosus/metabolismo , Lacticaseibacillus rhamnosus/crecimiento & desarrollo , Lacticaseibacillus rhamnosus/efectos de los fármacos , Viabilidad Microbiana/efectos de los fármacosRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Syagrus coronata, a palm tree found in northeastern Brazil, popularly known as licuri, has socioeconomic importance for the production of vegetable oil rich in fatty acids with nutritional and pharmacological effects. Licuri oil is used in traditional medicine to treat inflammation, wound healing, mycosis, back discomfort, eye irritation, and other conditions. AIM OF THE STUDY: The study aimed to evaluate the antinociceptive, anti-inflammatory, and antipyretic effects of treatment with Syagrus coronata fixed oil (ScFO), as well as to determine the safety of use in mice. MATERIALS AND METHODS: Initially, the chemical characterization was performed by gas chromatography-mass spectrometry. Acute single-dose oral toxicity was evaluated in mice at a dose of 2000 mg/kg. Antinociceptive activity was evaluated through abdominal writhing, formalin, and tail dipping tests, and the anti-inflammatory potential was evaluated through the model of acute inflammation of ear edema, peritonitis, and fever at concentrations of 25, 50, and 100 mg/kg from ScFO. RESULTS: In the chemical analysis of ScFO, lauric (43.64%), caprylic (11.7%), and capric (7.2%) acids were detected as major. No mortality or behavioral abnormalities in the mice were evidenced over the 14 days of observation in the acute toxicity test. ScFO treatment decreased abdominal writhing by 27.07, 28.23, and 51.78% at 25, 50, and 100 mg/kg. ScFO demonstrated central and peripheral action in the formalin test, possibly via opioidergic and muscarinic systems. In the tail dipping test, ScFO showed action from the first hour after treatment at all concentrations. ScFO (100 mg/kg) reduced ear edema by 63.76% and leukocyte and neutrophil migration and IL-1ß and TNF-α production in the peritonitis test. CONCLUSION: Mice treated with ScFO had a reduction in fever after 60 min at all concentrations regardless of dose. Therefore, the fixed oil of S. coronata has the potential for the development of new pharmaceutical formulations for the treatment of pain, inflammation, and fever.
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Analgésicos , Antiinflamatorios , Edema , Aceites de Plantas , Animales , Analgésicos/farmacología , Analgésicos/aislamiento & purificación , Analgésicos/toxicidad , Ratones , Antiinflamatorios/farmacología , Antiinflamatorios/aislamiento & purificación , Aceites de Plantas/farmacología , Masculino , Edema/tratamiento farmacológico , Edema/inducido químicamente , Dolor/tratamiento farmacológico , Peritonitis/tratamiento farmacológico , Antipiréticos/farmacología , Arecaceae/química , Femenino , Inflamación/tratamiento farmacológico , Inflamación/inducido químicamente , Fiebre/tratamiento farmacológico , Fiebre/inducido químicamente , Administración Oral , Modelos Animales de EnfermedadRESUMEN
An increasing number of biological activities presented by medicinal plants has been investigated over the years, and they are used in the search for new substances with lower side effects. Eugenia uniflora L. and Eugenia malaccensis L. (Myrtaceae) have many folk uses in various countries. This current study was designed to quantify the polyphenols and flavonoids contents and evaluate the immunomodulatory, antioxidant, and cytotoxic potentials of fractions from E. uniflora L. and E. malaccensis L. It was observed that the polyphenol content was higher in ethyl acetate fractions. These fractions have high antioxidant potential. E. malaccensis L. seeds showed the largest DPPH radical scavenger capacity (EC50 = 22.62). The fractions of E. malaccensis L. leaves showed lower antioxidant capacity. The samples did not alter the profile of proinflammatory cytokines and nitric oxide release. The results indicate that species of the family Myrtaceae are rich in compounds with antioxidant capacity, which can help reduce the inflammatory response.
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Antioxidantes/química , Células/efectos de los fármacos , Flavonoides/análisis , Extractos Vegetales/farmacología , Polifenoles/análisis , Syzygium/química , Animales , Compuestos de Bifenilo/química , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Citocinas/análisis , Ratones , Ratones Endogámicos BALB C , Óxido Nítrico/química , Picratos/química , Extractos Vegetales/análisis , Hojas de la Planta/química , Semillas/químicaRESUMEN
The association of quantum dots (QDs) to carbohydrate-binding proteins - lectins - has revealed novel biotechnological strategies for glycobiology studies. Herein, carboxyl-coated QDs were conjugated by adsorption to Cramoll, a glucose/mannose lectin obtained from Cratylia mollis seeds. Then, the conjugates were optically characterized and used to evaluate the surface carbohydrate profiles of four Aeromonas species isolated from the tambaqui fish (Colossoma macropomum). All the Aeromonas cells were labeled by the conjugate. Inhibition assays with methyl-α-D-mannopyranoside and mannan were performed to confirm the labeling specificity. Cramoll-QDs conjugates presented high brightness and showed similar absorption and emission profiles compared to bare QDs. According to the labeling pattern of Aeromonas spp. by the conjugate, results suggested that A. jandaei and A. dhakensis strains may harbor a higher content of more complex glucose/mannose surface glycans, with more available sites for Cramoll-QDs interaction, than A. hydrophila and A. caviae. Noteworthy, the Cramoll-QDs conjugates demonstrated to be potential tools for bacterial characterization based on superficial carbohydrate detection.
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Aeromonas , Puntos Cuánticos , Animales , Puntos Cuánticos/química , Manosa , Lectinas/química , Carbohidratos , GlucosaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Eugenia gracillima is widely used by the population in the manufacture of pulps and jellies, with popular reports of its use in the treatment of infections in the urinary system, respiratory and dermatological problems. A previous study reports that EO from E. gracillima leaves proved to be a promising antioxidant agent in combating the promastigote forms of protozoa. Despite this, this species has been little studied due to its pharmacological properties. STUDY OBJECTIVE: In this study, an essential oil extracted (EO) from Eugenia gracillima leaves was evaluated for its acute toxicity and anti-inflammatory, antinociceptive and behavioral effects in mice. METHODS: The EO was obtained by hydrodistillation, and the composition analysis was performed by gas chromatography coupled to mass spectrometry. Acute toxicity assessment was performed with observation of hematological parameters and histopathological evaluation, as well as tests to investigate antinociceptive, anti-inflammatory activities and behavioral effects. RESULTS: Chromatographic analysis showed D-germacrene (16.10%), γ-muurolene-g (15.60%) and bicyclogermacrene (8.53%) as the majority of compounds. In the toxicity evaluation, no death or physiological changes were observed in mice treated with a single oral dose of up to 5000 mg/kg, and it did not lyse erythrocytes in vitro. The hematological parameters evaluated were not changed after treatment; however, 5,000 mg/kg promoted an increase in transaminase levels. In the histopathological evaluation, only the animals that received the dose of 5000 mg/kg showed discrete leukocyte infiltration around the centrilobular vein in the liver. Antinociceptive activity was detected through tests of acetic acid-induced writhing, formalin, and tail flick, promoted in part by the opioid receptor pathway. In the evaluation of anti-inflammatory activity, a reduction in inflammation was observed in the paw edema test and a decrease in the migration of leukocytes and neutrophils in the peritonitis test. The open field and elevated plus maze tests showed that EO did not affect the animals' motor functions or exploratory activity. CONCLUSION: It was concluded that the essential oil of E. gracillima has potential for the development of pharmaceutical formulations with analgesic and anti-inflammatory actions in non-toxic concentrations.
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Eugenia , Aceites Volátiles , Ratones , Animales , Aceites Volátiles/uso terapéutico , Aceites Volátiles/toxicidad , Eugenia/química , Cromatografía de Gases y Espectrometría de Masas , Dolor/inducido químicamente , Dolor/tratamiento farmacológico , Analgésicos/uso terapéutico , Analgésicos/toxicidad , Antiinflamatorios/uso terapéutico , Antiinflamatorios/toxicidad , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Extractos Vegetales/farmacología , Hojas de la Planta , Edema/inducido químicamente , Edema/tratamiento farmacológicoRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Preparations from the bark and leaves of Schinus terebinthifolia Raddi are commonly used to treat toothaches and sore throats. The use of medications based on leaves of this plant has also been reported for pain of arthritis, toothache, and sore throat. Some evidence indicated that the lectin SteLL is an antinociceptive agent from leaves. AIM OF THE STUDY: This study evaluated the antinociceptive activity of S. terebinthifolia leaf lectin (SteLL) using mouse models of peripheral and central nociception. MATERIALS AND METHODS: Animals were treated intraperitoneally with SteLL at 1, 5, and 10 mg/kg. An acetic acid-induced abdominal writhing test was performed to screen for the antinociceptive effect of the lectin. Next, the formalin test was used to assess the effects of SteLL on neurogenic (first phase) and inflammatory (second phase) pain, as well as to investigate the involvement of the carbohydrate-recognition domain (CRD) of SteLL and opioid receptors in the antinociceptive effect. The tail immersion test was performed to assess the central antinociception. Additionally, a rotarod test was performed to evaluate the effects of lectin on motor coordination in mice. RESULTS: SteLL reduced the number of acetic acid-induced writhes by 83.5-100.0%. In the first phase of the formalin test, SteLL reduced paw licking time by 49.4-50.5%, while in the second phase, SteLL reduced paw licking time by 80.5-82.6%. This antinociceptive effect was reversed by the previous incubation of the lectin with ovalbumin (indicating the possible involvement of the CRD) and by the administration of naloxone, a nonselective opioid receptor antagonist. When testing selective antagonists of opioid receptors (µ, δ, and κ), only naltrindole, a selective δ receptor antagonist, blocked the antinociceptive action of SteLL during the second phase of the formalin test. In the tail immersion test, SteLL (1, 5, and 10 mg/kg) administration reduced sensitivity to thermal stimulus, which was observed even after 2 h. SteLL (10 mg/kg) did not affect animal motor coordination in rotarod test when compared to the control group. CONCLUSION: SteLL has peripheral and central analgesic action involving opioid receptor modulation without affecting the motor coordination of animals. These results provide new perspectives for developing analgesic agents using lectins.
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Anacardiaceae , Lectinas , Animales , Ratones , Analgésicos , Carbohidratos , Dolor/inducido químicamente , Dolor/tratamiento farmacológico , Hojas de la Planta , Receptores OpioidesRESUMEN
Thermal lesions were produced in 12 male Wistar rats, positioning a massive aluminum bar 10 mm in diameter (51 g), preheated to 99°C ± 2°C/10 min. on the back of each animal for 15 sec. After 7, 14, 21, and 28 days, animals were euthanized. The edema intensity was mild, with no bubble and formation of a thick and dry crust from the 3rd day. The percentage of tissue shrinkage at 28 days was 66.67 ± 1.66%. There was no sign of infection, bleeding, or secretion. Within 28 days reepithelialization was incomplete, with fibroblastic proliferation and moderate fibrosis and presence of modeled dense collagen fibers. It is concluded that the model established is applicable in obtaining deep second-degree thermal burns in order to evaluate the healing action of therapeutic agents of topical use.
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Quemaduras/patología , Quemaduras/fisiopatología , Modelos Animales de Enfermedad , Cicatrización de Heridas/fisiología , Animales , Histocitoquímica , Masculino , Ratas , Ratas Wistar , Reproducibilidad de los Resultados , Piel/patología , Piel/fisiopatologíaRESUMEN
This study aimed at evaluating the use of hydrogel isolectin in the treatment of second-degree burns. Twenty male rats were randomly divided into two groups (G1 = treatment with hydrogel containing 100 µg/mL Cramoll 1,4 and G2 = Control, hydrogel). After 7, 14, 21, 28, and 35 days, animals were euthanized. On the 7th day, G1 showed intense exudates, necrosis and edema. On the 14th day, G1 showed tissue reepithelialization and moderate autolysis. On the 21st day, G1 showed intense fibroblastic proliferation, presence of dense collagen, and moderate fibrosis. On the 28th day, G1 showed complete tissue epithelialization. On the 35th day, G1 showed modeled dense collagen. The significant wound contraction was initiated from day, 14 in the G1. There were no significant differences in biochemical and hematological parameters analyzed. These results extend the potential of therapeutic applications for Cramoll 1,4 in the treatment of thermal burns.
Asunto(s)
Quemaduras/tratamiento farmacológico , Hidrogel de Polietilenoglicol-Dimetacrilato/farmacología , Lectinas de Plantas/farmacología , Cicatrización de Heridas/efectos de los fármacos , Administración Tópica , Animales , Análisis Químico de la Sangre , Quemaduras/sangre , Quemaduras/patología , Modelos Animales de Enfermedad , Epitelio/patología , Fabaceae/química , Pruebas de Hemaglutinación , Pruebas Hematológicas , Masculino , Ratas , Ratas Wistar , Estadísticas no ParamétricasRESUMEN
This study evaluated the antimicrobial and hemolytic activities and phytochemical constituents of hydroalcoholic extract and its fractions from Buchenavia tetraphylla leaves. Cyclohexane (BTCF), ethyl acetate (BTEF), and n-butanol-soluble (BTSBF) and non-soluble (BTNBF) fractions were obtained from a liquid-liquid partition of hydroalcoholic extract (BTHE) from B. tetraphylla leaves. The hemolytic activity of active fractions was checked. The BTHE inhibited the growth of Micrococcus luteus (MIC: 0.10 mg/mL), Pseudomonas aeruginosa (MIC: 0.20 mg/mL), Mycobacterium smegmatis (MIC: 0.39 mg/mL), Proteus vulgaris, and Staphylococcus aureus (MIC: 0.78 mg/mL for both). The more active fractions were BTCF and BTBSF. BTCF showed better potential to inhibit M. luteus (0.10 mg/mL), P. aeruginosa (0.20 mg/mL), S. enteritidis (0.39 mg/mL), and S. aureus (1.56 mg/mL). BTBSF showed the best results for M. luteus (0.10 mg/mL), M. smegmatis, B. subtilis (0.39 mg/mL for both), and P. vulgaris (0.10 mg/mL). The HC50 were greater than observed MIC: 20.30, 4.70 and 2.53 mg/mL, respectively, to BTBF, BTHE and BTCF, which. The phytochemical analysis detected the presence of flavanoids, triterpene, carbohydrate, and tannin. Our work showed for the first time the broad-spread antimicrobial activity of B. tetraphylla, which has nonhemolytic action, creating a new perspective on the interesting association of traditional and scientific knowledge.
Asunto(s)
Antibacterianos/farmacología , Combretaceae/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , 1-Butanol/química , Acetatos/química , Antibacterianos/aislamiento & purificación , Carbohidratos/análisis , Ciclohexanos/química , Relación Dosis-Respuesta a Droga , Flavonoides/análisis , Hemólisis/efectos de los fármacos , Humanos , Pruebas de Sensibilidad Microbiana , Micrococcus luteus/efectos de los fármacos , Micrococcus luteus/crecimiento & desarrollo , Mycobacterium smegmatis/efectos de los fármacos , Mycobacterium smegmatis/crecimiento & desarrollo , Proteus vulgaris/efectos de los fármacos , Proteus vulgaris/crecimiento & desarrollo , Pseudomonas aeruginosa/efectos de los fármacos , Pseudomonas aeruginosa/crecimiento & desarrollo , Solubilidad , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/crecimiento & desarrollo , Taninos/análisis , Triterpenos/análisisRESUMEN
The genus Aeromonas comprises more than 30 Gram-negative bacterial species and naturally inhabitants from aquatic environments. These microorganisms, commonly regarded as pathogens of fish and several other animals, have been gaining prominence on medical trial due to its ability to colonize and infect human beings. Besides water, Aeromonas are widely spreaded on most varied sources like soil, vegetables, and food; Although its opportunistic nature, they are able to cause infections on immunocompromised or immunocompetent patients. Aeromonas species regarded as potential human pathogens are usually A. hydrophila, A. caviae, and A. veronii biovar sobria. The main clinical manifestations are gastrointestinal tract disorders, wound, and soft tissue infections, as well as septicemia. Regarding to antibiotic responses, the bacteria present a diversified susceptibility profile and show inherence resistance to ampicillin. Aeromonas, as an ascending genus in microbiology, has been carefully studied aiming comprehension and development of methods for detection and medical intervention of infectious processes, not fully elucidated in medicine. This review focuses on current clinical knowledge related to human health disorders caused by Aeromonas to contribute on development of efficient approaches able to recognize and impair the pathological processes.
RESUMEN
The ability to reversibly bind carbohydrates is an incredible property from lectins. Such characteristic has led these molecules to be employed in several applications involving medical research and biotechnology. Generally, these proteins follow several steps towards purification. Here, the synthesis, physical characterization, and use of levan-coated magnetite nanoparticles (MNPs-levan) for lectin isolation is described. Canavalia ensiformis and Cratylia mollis were used as sources of Concanavalin A and Cramoll, respectively, that were purified by using MNPs-levan. Mass spectrometry, SDS-PAGE, and hemagglutinating activity were employed to assess the efficiency of the process. Moreover, by using mass spectrometry approaches, a novel lectin, similar to Canavalin, was also identified for C. mollis, corroborating the advantages of using nanoparticles over microparticles. MNPs-levan could also be recycled, making this a low-cost, scalable process that can be efficiently employed over crude samples.
Asunto(s)
Fabaceae , Nanopartículas de Magnetita , Fabaceae/química , Óxido Ferrosoférrico , Fructanos , Lectinas/análisis , Lectinas/química , Extractos Vegetales/análisis , Lectinas de Plantas/química , Plantas/metabolismo , Semillas/químicaRESUMEN
Myrciaria pilosa is a tree species of the Brazilian Caatinga biome. This paper is the first report on the chemical composition and the antimicrobial and antivirulence activities of essential oil extracted from its leaves. The oil was extracted by hydrodistillation. Chemical composition determined by GC-MS and CG-FID revealed 63 compounds; the sesquiterpenes guaiol (13.17%) and (E)-ß-caryophyllene (11.26%) dominated. Antimicrobial activity against strains of Staphylococcus aureus was evaluated by the broth microdilution method. It showed minimum inhibitory concentrations (MIC) of 5 µg/mL against evaluated strains and minimum bactericidal concentrations (MBC) ranging from 10 to 20 µg/mL. Evaluation of antivirulence activity showed reductions of 92.0% and 47.2%, respectively, in haemolytic action and production of staphyloxanthin. These findings show that the essential oil of M. pilosa has potential as an antimicrobial drug to control infection by multi-resistant strains of S. aureus.