RESUMO

Eugenia flavescens is a species cultivated in Brazil for food purposes. Given the potential application of essential oils from plants of the genus Eugenia, this study was carried out to investigate the chemical composition, acute toxicity, antioxidant, antinociceptive, gastroprotective activities, and possible mechanisms of action of the essential oil from the leaves of E. flavescens (EOEf). The EOEf was extracted by hydrodistillation, and the chemical composition was obtained using gas chromatography-mass spectrometry. The antioxidant activity was evaluated, as well as the acute toxicity and the antinociceptive and anti-inflammatory effects in mice. In addition, the gastroprotective effect was investigated using an acute gastric lesion model, considering possible mechanisms of action. The major components found in the EOEf were guaiol (19.97%), germacrene B (12.53%), bicyclogermacrene (11.11%), and E-caryophyllene (7.53%). The EOEf did not cause signs of toxicity in the acute oral toxicity test and showed in vitro antioxidant activity with IC50 ranging from 247.29 to 472.39 µg/mL in the tests ABTS and DPPH. In the nociceptive test, EOEf showed a 72.05% reduction in nociception at a dose of 100 mg/kg. In evaluating the anti-inflammatory effect, the essential oil inhibited paw edema by 95.50% and 97.69% at doses of 50 and 100 mg/kg. The results showed that EOEf has a gastroprotective effect, acting through the sulfhydryl compounds (-SH), nitric oxide (NO), and synthesis PGE2 pathways. The results suggested that EOEf is a promising source of constituents with antioxidant, antinociceptive, anti-inflammatory, and gastroprotective properties with application in the food and pharmaceutical industries.

Assuntos

Analgésicos , Anti-Inflamatórios , Antioxidantes , Etanol , Eugenia , Inflamação , Óleos Voláteis , Dor , Folhas de Planta , Úlcera Gástrica , Animais , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/induzido quimicamente , Óleos Voláteis/farmacologia , Camundongos , Folhas de Planta/química , Analgésicos/farmacologia , Analgésicos/isolamento & purificação , Antioxidantes/farmacologia , Masculino , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , Dor/tratamento farmacológico , Dor/induzido quimicamente , Eugenia/química , Inflamação/tratamento farmacológico , Brasil , Antiulcerosos/farmacologia , Antiulcerosos/isolamento & purificação , Feminino

RESUMO

This study aims to investigate the essential oil from leaves of Eugenia pohliana (EOEP) in regard to its chemical composition, antimicrobial and drug-enhancing activity, as well as the reduction of fungal virulence capacity. Chemical characterization using GC-MS showed as major components the sesquiterpenes δ-cadinene, Epi-α-Muurolol, and bicyclogermacrene. The results of antibacterial tests indicated that Staphylococcus aureus was more sensitive to EOEP, that also enhanced the efficacy of gentamicin, erythromycin, and norfloxacin. EOEP exhibited antifungal properties against Candida albicans, in addition to potentiating the effectiveness of fluconazole against Candida tropicalis. It showed anti-virulence effects in all fungal strains. These findings underscore E. pohliana as a potential candidate for the prospection of novel therapeutic agents to treat infectious diseases caused by resistant microbes.

RESUMO

Syagrus coronata, a native palm tree in the Caatinga domain, produces fixed oil (ScFO) used therapeutically and dietary by Northeast Brazilian communities. This study evaluated its anti-inflammatory potential of CFA-induced arthritis and its effect on behavioral parameters. In the acute model, ScFO at 25, 50, and 100 mg/kg showed edematogenic effects similar to indomethacin at 4 mg/kg (p > 0.05). In the arthritis model, 100 mg/kg ScFO treatment was comparable to indomethacin (4 mg/kg) (p > 0.05). TNF-α and IL-1ß levels were significantly reduced in ScFO-treated groups at 25, 50, and 100 mg/kg, and the indomethacin group (4 mg/kg) versus the positive control (p > 0.05). Radiographs showed severe soft-tissue swelling and bone deformities in the control group, while the 100 mg/kg ScFO group had few alterations, similar to the indomethacin group. Histopathological analysis revealed intense lymphocytic infiltration in the control group, mild diffuse lymphocytic infiltration in the indomethacin group, and mild lymphoplasmacytic infiltration with focal polymorphonuclear infiltrates in the 100 mg/kg ScFO group. Behavioral analysis showed improved exploratory stimuli in ScFO and indomethacin-treated mice compared to the positive control (p > 0.05). ScFO demonstrated anti-inflammatory effects in both acute and chronic arthritis models, reducing edema and pro-inflammatory cytokines, and improved exploratory behavior due to its analgesic properties.

Assuntos

Anti-Inflamatórios , Artrite Experimental , Adjuvante de Freund , Animais , Artrite Experimental/tratamento farmacológico , Artrite Experimental/patologia , Camundongos , Anti-Inflamatórios/farmacologia , Masculino , Óleos de Plantas/farmacologia , Arecaceae/química , Edema/tratamento farmacológico , Fator de Necrose Tumoral alfa/metabolismo , Interleucina-1beta/metabolismo , Óleo de Palmeira/farmacologia , Indometacina/farmacologia , Brasil , Relação Dose-Resposta a Droga

RESUMO

To assess the antibacterial effectiveness of Lippia macrophylla essential oil (LMEO) against multidrug-resistant Acinetobacter baumannii isolates, both as a standalone treatment and in combination with conventional antibiotics. LMEO demonstrated a significant inhibitory effect on the growth of A. baumannii, with a minimum inhibitory concentration (MIC) below 500 µg/mL. Notably, LMEO was capable of reversing the antibiotic resistance of clinical isolates or reducing their MIC values when used in combination with antibiotics, showing synergistic (FICI≤0.5) or additive effects. The combination of LMEO and imipenem was particularly effective, displaying synergistic interactions for most isolates. Ultrastructural analyses supported these findings, revealing that the combination of LMEO+ceftazidime compromised the membrane integrity of the Acb35 isolate, leading to cytoplasmic leakage and increased formation of Outer Membrane Vesicles (OMVs). Taken together our results point for the use of LMEO alone or in combination as an antibacterial agent against A. baumannii. These findings offer promising avenues for utilizing LMEO as a novel antibacterial strategy against drug-resistant infections in healthcare settings, underscoring the potential of essential oils in enhancing antibiotic efficacy.

Assuntos

Acinetobacter baumannii , Antibacterianos , Farmacorresistência Bacteriana Múltipla , Lippia , Testes de Sensibilidade Microbiana , Óleos Voláteis , Acinetobacter baumannii/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Lippia/química , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Humanos , Relação Dose-Resposta a Droga

RESUMO

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.

Assuntos

Analgésicos , Anti-Inflamatórios , Edema , Óleos de Plantas , Animais , Analgésicos/farmacologia , Analgésicos/isolamento & purificação , Analgésicos/toxicidade , Camundongos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , Óleos de Plantas/farmacologia , Masculino , Edema/tratamento farmacológico , Edema/induzido quimicamente , Dor/tratamento farmacológico , Peritonite/tratamento farmacológico , Antipiréticos/farmacologia , Arecaceae/química , Feminino , Inflamação/tratamento farmacológico , Inflamação/induzido quimicamente , Febre/tratamento farmacológico , Febre/induzido quimicamente , Administração Oral , Modelos Animais de Doenças

RESUMO

Pseudobombax marginatum, popularly known as "embiratanha," is widely used by traditional communities as anti-inflammatory and analgesic agent. This study aimed to determine the phytochemical profile as well as cytotoxicity, acute oral toxicity, genotoxicity, and mutagenicity attributed to exposure to aqueous (AqEx) and ethanolic (EtEx) extracts of embiratanha bark. Phytochemical screening was conducted using thin-layer chromatography (TLC). Cell viability was analyzed using MTT assay with human mammary gland adenocarcinoma (MDA-MB-231) and macrophage (J774A.1) cell lines, exposed to concentrations of 12.5, 25, 50, or 100 µg/ml of either extract. For acute oral toxicity, comet assay and micronucleus (MN) tests, a single dose of 2,000 mg/kg of either extract was administered orally to Wistar rats. TLC analysis identified classes of metabolites in the extracts, including cinnamic acid derivatives, flavonoids, hydrolyzable tannins, condensed tannins, coumarins, and terpenes/steroids. In the cytotoxicity assay, the varying concentrations of extracts derived from embiratanha induced no significant alterations in the viability of MDA-MB-231 cells. The lowest concentration of EtEx significantly increased macrophage J774A.1 viability. However, the higher concentrations of AqEx markedly lowered macrophage J774A.1 viability. Animals exhibited no toxicity in the parameters analyzed in acute oral toxicity, comet assay, and MN tests. Further, EtEx promoted a significant reduction in DNA damage index and DNA damage frequency utilizing the comet assay, while the group treated with AqEx exhibited no marked differences. Thus, data demonstrated that AqEx or EtEx of embiratanha may be considered safe at a dose of 2,000 mg/kg orgally under our experimental conditions tested.

Assuntos

Extratos Vegetais , Ratos Wistar , Extratos Vegetais/toxicidade , Extratos Vegetais/química , Animais , Humanos , Ratos , Linhagem Celular Tumoral , Masculino , Ensaio Cometa , Testes para Micronúcleos , Feminino , Sobrevivência Celular/efeitos dos fármacos , Compostos Fitoquímicos/toxicidade , Compostos Fitoquímicos/análise , Camundongos , Casca de Planta/química , Mutagênicos/toxicidade , Testes de Mutagenicidade , Etanol/química

RESUMO

Punica granatum, popularly known as pomegranate, is a fruit tree with wide worldwide distribution, containing numerous phytochemicals of great medicinal value. The aim of the present study was to determine the phytochemical profile and antioxidant potential of a protein fraction (PF) derived from P. granatum sarcotesta which is rich in lectin. In addition, the acute oral toxicity, genotoxicity and antigenotoxicity of this protein fraction (PF) from P. granatum sarcotesta was measured. The phytochemical profile of PF was determined using HPLC. The in vitro antioxidant effect was assessed using the methods of total antioxidant capacity (TAC) and DPPH and ABTS+ radical scavenging. Acute oral toxicity was determined in female Swiss mice administered a single dose of 2000 mg/kg. This PF was examined for genotoxicity and antigenotoxicity at doses of 500, 1000 and 2000 mg/kg, utilizing mouse peripheral blood cells. Phytochemical characterization detected a high content of ellagic acid and antioxidant capacity similar to that of ascorbic acid (positive control). PF was not toxic (LD50 >2000 mg/kg) and did not exert a genotoxic effect in mice. PF protected the DNA of peripheral blood cells against damage induced by cyclophosphamide. In conclusion, this PF fraction exhibited significant antioxidant activity without initiating toxic or genotoxic responses in mice.

Assuntos

Antioxidantes , Extratos Vegetais , Punica granatum , Animais , Camundongos , Antioxidantes/farmacologia , Feminino , Extratos Vegetais/toxicidade , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Punica granatum/química , Lectinas/toxicidade , Testes de Mutagenicidade , Dano ao DNA/efeitos dos fármacos , Testes de Toxicidade Aguda

RESUMO

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.

RESUMO

Wounds encompass physical, chemical, biological, induced damages to the skin or mucous membranes. In wound treatment, combating infections is a critical challenge due to their potential to impede recovery and inflict systemic harm on patients. Previously, the essential oil extracted from Psidium glaziovianum (PgEO) demonstrated antinociceptive and anti-inflammatory attributes, along with negligible oral toxicity. Hence, our study aimed to assess the effects of topically applying a gel formulation containing PgEO to excisional wounds in mice. Additionally, an in vitro antimicrobial assessment was conducted. The formulated gel underwent characterization and toxicological evaluation on erythrocytes, as well as a dermal irritation test. Its antimicrobial activity was tested against both gram-positive and gram-negative bacteria, as well as fungi. Subsequently, an assessment of its efficacy in excisional wound healing was conducted in mice. The findings of this investigation highlight the gel's efficacy against both gram-positive and gram-negative bacteria, as well as fungi. Moreover, this study underscores that the PgEO-gel treatment enhances skin wound healing, potentially due to its capacity to trigger antioxidant enzymes and suppress pro-inflammatory cytokines. Furthermore, the gel exhibited minimal toxicity to erythrocytes and skin irritation. These findings hold promise for prospective preclinical and clinical trials across diverse wound types. In conclusion, this study sheds light on the potential therapeutic applications of the gel formulation containing essential oil from P. glaziovianum in the context of wound healing.

Assuntos

Óleos Voláteis , Psidium , Humanos , Animais , Camundongos , Antibacterianos , Estudos Prospectivos , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Cicatrização , Óleos Voláteis/farmacologia

RESUMO

Myrciaria floribunda is a plant that is distributed across different Brazilian biomes such as the Amazon, Caatinga, Cerrado, and Atlantic Forest, and it possesses antioxidant, antimicrobial, and anticancer properties. The antinociceptive and anti-inflammatory properties of the essential oil from M. floribunda leaves (MfEO) were examined in this study using mouse models. Gas chromatography-mass spectrometry was employed to describe the oil, and the results revealed that δ-cadinene, bicyclogermacrene, α-cadinol, and epi-α-muurolol predominated in the chemical profile. The oil stimulated a decrease in nociception in the chemical and thermal models used to evaluate acute antinociceptive activity. Findings from the use of pain pathway blockers to study the presumed underlying mechanism indicated opioid pathway activity. The anti-edematogenic effect, decreased cell migration, and generation of pro-inflammatory cytokines provided evidence of the anti-inflammatory potential of the essential oil from M. floribunda. According to this research, the essential oil from M. floribunda can effectively alleviate acute pain and inflammation.

Assuntos

Anti-Infecciosos , Óleos Voláteis , Camundongos , Animais , Óleos Voláteis/farmacologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Antioxidantes/farmacologia , Anti-Infecciosos/farmacologia , Extratos Vegetais/química , Analgésicos/farmacologia , Analgésicos/química , Folhas de Planta/química

RESUMO

This study aimed to characterize the phytochemical profile of bark and leaves aqueous extract Commiphora leptophloeos, and conduct in vivo and in vitro assays to determine the presence of any toxicological consequences due to exposure. The phytochemical analysis was carried out using high-performance liquid chromatography (HPLC). The antioxidant activity was estimated utilizing DPPH free radical scavenging and phosphomolybdenum assays. Cell viability was measured by the MTT method on J774 and human adenocarcinoma cells, which were treated with concentrations of 12,5, 25, 50, 100 or 200 µg/ml of both extracts. Acute oral toxicity, genotoxicity, and mutagenicity assays were determined using a single oral dose of 2000 g/kg in male Swiss albino mice (Mus musculus). Biochemical analysis of the blood and histological analyses of the kidneys, liver, spleen, pylorus, duodenum and jejunum were undertaken. Genotoxicity and mutagenicity were determined utilizing blood samples. Gallic acid, catechin, and epicatechin were identified in the bark and chlorogenic acid in leaves. Data demonstrated a high content of phenolic compounds and flavonoids associated with significant antioxidant potential. No significant signs in damage or symptoms of toxicity were detected. No marked reduction in cell viability was found at lower concentrations tested. On histomorphometry, only the gastrointestinal organs exhibited significant difference. Renal hepatic and blood parameters were within the normal range. No apparent signs of toxicity, genotoxicity, mutagenicity or cytotoxicity were found in vivo and in vitro experiments.

Assuntos

Antioxidantes , Catequina , Camundongos , Animais , Masculino , Humanos , Antioxidantes/química , Extratos Vegetais/toxicidade , Extratos Vegetais/química , Commiphora , Casca de Planta/química , Compostos Fitoquímicos/toxicidade , Folhas de Planta/química

RESUMO

Candida albicans is associated with serious infections in immunocompromised patients. Terpenes are natural-product derivatives, widely studied as antifungal alternatives. In a previous study reported by our group, the antifungal activity of α-pinene against C. albicans was verified; α-pinene presented an MIC between 128-512 µg/mL. In this study, we evaluate time-kill, a mechanism of action using in silico and in vitro tests, anti-biofilm activity against the Candida albicans, and toxicity against human cells (HaCaT). Results from the molecular-docking simulation demonstrated that thymidylate synthase (-52 kcal mol-1), and δ-14-sterol reductase (-44 kcal mol-1) presented the best interactions. Our in vitro results suggest that α-pinene's antifungal activity involves binding to ergosterol in the cellular membrane. In the time-kill assay, the antifungal activity was not time-dependent, and also inhibited biofilm formation, while rupturing up to 88% of existing biofilm. It was non-cytotoxic to human keratinocytes. Our study supports α-pinene as a candidate to treat fungal infections caused by C. albicans.

RESUMO

The current trichomoniasis treatment is restrict to 5-nitroimidazole drugs and the emergence of resistant isolates points the need for new therapeutical alternatives. In this study the anti-Trichomonas vaginalis activity of essential oils obtained from Myrtaceae occurring in Caatinga, a plant family with potential antiparasitic activity, was showed. The essential oils varied in their capacity to kill ATCC and fresh clinical T. vaginalis isolates, which was associated with heterogeneity and different patterns of endosymbiosis. Essential oils caused moderate to strong cytotoxicity against mammalian cells, but essential oil of Eugenia pohliana (EOEp) exhibited promising selectivity index towards vaginal epithelial cells. A checkerboard assay revealed a synergistic effect when EOEp and metronidazole were associated, indicating different mechanisms of action. The GC/MS analysis demonstrated the volatile composition of EOEp, with δ-cadinene as majoritary component. This molecule seems to contribute to the trichomonacidal effect and shows potential for the prospection of new antiparasitic compounds.

Assuntos

Eugenia , Myrtaceae , Óleos Voláteis , Trichomonas vaginalis , Animais , Feminino , Óleos Voláteis/química , Antiparasitários/farmacologia , Metronidazol/farmacologia , Mamíferos

RESUMO

Eugenia brejoensis Mazine (Myrtaceae) is source of an essential oil (EbEO) with anti-infective activities against Staphylococcus aureus. This study evaluated the antimicrobial and anti-inflammatory potentials of EbEO in S. aureus-infected skin wounds. The excisional lesions (64 mm2) were induced on Swiss mice back (6 to 8-week-old) that were allocated into 3 groups (n = 12): 1) non-infected wounds (CON); 2) wounds infected with S. aureus ATCC 6538 (Sa); 3) S. aureus-infected wounds and treated with EbEO (Sa + EbEO). The infected groups received approximately 104 CFU/wound. The animals were treated with EbEO (10 µg/wound/day) or vehicle from the 1-day post-infection (dpi) until the 10th dpi. The clinical parameters (wound area, presence of exudate, edema intensity, etc.) were daily analyzed. The levels of inflammatory mediators (cytokines, nitric oxide, VEGF) and bacterial load were measured at the cutaneous tissue at 4th dpi and 10th dpi. Topical application of EbEO accelerated wound contraction with an average contraction of 83.48 ± 11.27 % of the lesion area until 6th dpi. In this period, the rates of lesion contraction were 54.28 ± 5.57% and 34.5 ± 2.67% for CON and Sa groups, respectively. The positive effects of EbEO on wound contraction were associated with significantly (p < 0.05) reduction on bacterial load and the release of inflammatory mediators (IL-6, IL-17A, TNF-α, NO and VEGF). Taken together, these data confirm the antimicrobial potential of EbEO and provide insights into its anti-inflammatory effects, making this essential oil an interesting candidate for the development of new therapeutic alternatives for infected cutaneous wounds.

RESUMO

The Gram-positive bacterium Staphylococcus aureus is responsible for a number of infections and has been described to exhibit resistance to antibacterial drugs through different resistance mechanisms. Among these, active efflux has been shown to be one of the main mechanisms of bacterial resistance associated with S. aureus. In this sense, the aim of the present study was to evaluate the ability of ellagic acid and gallic acid to reverse resistance by inhibiting the efflux pumps present in S. aureus strains IS-58 and K2068, which express the TetK and MepA flux pumps, respectively. In addition, the toxicity of both compounds was verified in Drosophila melanogaster. Broth microdilution assays were performed to obtain the minimum inhibitory concentration (MIC) values of ellagic acid and gallic acid, whereas efflux pump inhibition was tested using a subinhibitory concentration of standard efflux pump inhibitors, gallic acid and ellagic acid (MIC/8), where the ability of these compounds to decrease the MIC of ethidium bromide (EtBr) and antibiotics was verified. Toxicity was evaluated by mortality and negative geotaxis assays in D. melanogaster. Ellagic acid and gallic acid showed no direct antibacterial activity on S. aureus strains carrying the efflux pumps TetK and MepA. However, when we looked at the results for the TetK pump, we saw that when the two acids were associated with the antibiotic tetracycline, a potentiation of the antibacterial effect occurred; this behavior was also observed for the antibiotic ciprofloxacin in the MepA strain. For the efflux pump inhibition results, only the compound gallic acid showed potentiating effect on antibacterial activity when associated with the substrate EtBr for the IS-58 strain carrying the TetK efflux pump. Ellagic acid and gallic acid showed no toxicity on the model arthropod D. melanogaster. These results indicate the possible use of gallic acid as an adjuvant in antibiotic therapy against multidrug-resistant bacteria.

Assuntos

Ácido Elágico , Staphylococcus aureus , Animais , Antibacterianos/farmacologia , Proteínas de Bactérias/química , Proteínas de Bactérias/farmacologia , Ciprofloxacina/farmacologia , Drosophila melanogaster , Ácido Elágico/farmacologia , Etídio/farmacologia , Ácido Gálico/farmacologia , Tetraciclina/farmacologia

RESUMO

Dental caries is a multifactorial, biofilm-dependent infectious disease that develops when detrimental changes occur in the oral cavity microenvironment. The antimicrobial and antivirulence properties of the essential oil obtained from the leaves of Eugenia brejoensis Mazine (EBEO) have been reported against Gram-positive and Gram-negative bacteria. Herein, the antimicrobial action of EBEO towards Streptococcus mutans is reported, along with the development and characterization of dental adhesives doped with. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of EBEO were determined against S. mutans, while its toxicity was analyze using Tenebrio molitor larvae. EBEO (MIC and 10×MIC) was incorporated into the Ambar Advanced Polymerization System® (Ambar APS), a two-step total-etch adhesive system (FGM Dental Group), and the antibiofilm action was evaluated. The reflective strength, modulus of elasticity, degree of conversion, and maximum rate of polymerization of each adhesive were also determined. The MIC and MBC values of EBEO against S. mutans were 62.5 µg/mL. The tested concentrations of EBEO were non-toxic to T. molitor larvae. The formation of S. mutans biofilms was significantly inhibited by EBEO and EBEO-coated resin discs (p < 0.05). Importantly, EBEO incorporation did not affect the mechanical and physicochemical properties in relation to oil-free adhesive version. EBEO showed strong antibacterial and antibiofilm activity against S. mutans, no toxicity effect against T. molitor larvae, and did not jeopardize the physical-chemical properties tested.

RESUMO

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 74.93‒81.41% was observed in the paw edema test and inhibition of the influx of leukocytes by 51.86‒70.38% and neutrophils by 37.74‒54.72% 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.

Assuntos

Eugenia , Myrtaceae , Óleos Voláteis , Peritonite , Camundongos , Animais , Eugenia/química , Óleos Voláteis/farmacologia , Óleos Voláteis/uso terapêutico , Nociceptividade , Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Edema/induzido quimicamente , Edema/tratamento farmacológico , Dor/tratamento farmacológico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Inflamação/tratamento farmacológico , Peritonite/tratamento farmacológico , Naloxona/uso terapêutico

RESUMO

Background: Efflux pumps are transmembrane proteins that expel drugs out of a bacterial cell contributing to microorganism drug resistance. Several studies addressing the use of natural products with medicinal properties have intensified given the above. Thus, the aim of the present study was to investigate the antibacterial activity and the O-eugenol potential in Staphylococcus aureus resistance reversal by efflux pump inhibition, as well as to evaluate its toxicity in the Drosophila melanogaster arthropod model. The broth microdilution method was used to determine the minimum inhibitory concentration (MIC) and the O-eugenol efflux pump inhibition. For the D. melanogaster toxicity assays, mortality and locomotor system damage were performed using the fumigation method. Results: O-eugenol presented a MIC of 1024 µg/mL against S. aureus. The association of this compound with the antibiotic tetracycline demonstrated a synergistic effect (p < 0.0001), this also being observed when the antibiotic was associated with ethidium bromide (p < 0.0001); thus, these results may be attributable to an efflux pump inhibition. The D. melanogaster mortality and geotaxis assays revealed the compound is toxic, with an EC50 of 18 µg/mL within 48 hours of exposure. Conclusions: While we can conclude that the tested product has an efflux pump inhibitory effect, further studies are needed to elucidate its mechanisms of action, in addition to assays using other strains to verify whether the substance has the same inhibitory effect.

Assuntos

Infecções Estafilocócicas , Staphylococcus aureus , Animais , Antibacterianos/metabolismo , Antibacterianos/farmacologia , Proteínas de Bactérias/metabolismo , Drosophila melanogaster/metabolismo , Eugenol/farmacologia , Testes de Sensibilidade Microbiana , Modelos Animais , Proteínas Associadas à Resistência a Múltiplos Medicamentos , Infecções Estafilocócicas/tratamento farmacológico

RESUMO

The purpose of this study was to analyses the influence of seasonal variation on the chemical composition and antimicrobial, antioxidant and cytotoxicity activities of the essential oil (EO) extracted from the leaves of Eugenia pohliana. Chemical characterization of the samples - by gas chromatography-mass spectrometry - found 35 and 38 components for summer and winter, respectively, of the EO from E. pohliana leaves, totaling 47 different compounds. Analysis of antioxidant capacity (DPPH, ABTS and TAC) revealed that the summer EO showed greater free radical scavenging capacity than the winter. Similarly, the summer EO exhibited superior antimicrobial potential (MIC=128-512 µg/mL and MMC=128-1024 µg/mL, compared to the winter EO (128-2048 µg/mL and 256-2048 µg/mL, respectively). Results showed that both oils had a low potential to cause hemolysis. This study provides new scientific evidence on the influence of seasonality on the pharmacological properties of E. pohliana leaves and its potential for the development of herbal medicines.

Assuntos

Anti-Infecciosos , Eugenia , Óleos Voláteis , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Antioxidantes/química , Radicais Livres , Testes de Sensibilidade Microbiana , Óleos Voláteis/química , Folhas de Planta/química , Estações do Ano

RESUMO

Plants of the genus Psidium have been employed in "in natura" consumption and agroindustry, and owing to the diversity of phytochemicals, the development of new pharmaceutical forms has received remarkable research interest. In this study, the essential oil obtained from Psidium glaziovianum (PgEO) leaves were evaluated antinociceptive and anti-inflammatory activities were evaluated in mouse models. Initially, PgEO was characterized by gas chromatography-mass spectrometry and gas chromatography with flame ionization detection, and the profile was dominated by sesquiterpene compounds. In the evaluation of acute antinociceptive activity (abdominal contortions induced by acetic acid, formalin, tail immersion, and hot plate tests), PgEO promoted a reduction in nociception in the chemical and thermal models. Additionally, the potential underlying mechanism was investigated using pain pathway blockers, and the results revealed a combined action of opioidergic and muscarinic pathways. The anti-inflammatory potential was confirmed by anti-edematogenic action, reduced cell migration, pro-inflammatory cytokine production, and granuloma formation in chronic processes. This study provides evidence that PgEO can be effective for the treatment of pain and acute and chronic inflammation.

Assuntos

Óleos Voláteis , Psidium , Administração Oral , Analgésicos , Animais , Edema/induzido quimicamente , Edema/tratamento farmacológico , Inflamação/tratamento farmacológico , Camundongos , Óleos Voláteis/farmacologia , Dor/tratamento farmacológico , Extratos Vegetais , Folhas de Planta/química , Psidium/química