RESUMEN
Sixteen triterpenoids with various skeletal types, five phenylpropanoid derivatives, and two flavonoids were isolated from a propolis sample produced by Apis mellifera collected in the Atlantic Forest of Midwest Brazil. Among these compounds, six triterpenes, namely 3ß,20R-dihydroxylanost-24-en-3-yl-palmitate, (23E)-25-methoxycycloartan-23-en-3-one, 24-methylenecycloartenone, epi-lupeol, epi-α-amyrin, and epi-ß-amyrin are being reported for the first time in propolis, while cycloartenone, (E)-cinnamyl benzoate, and (E)-cinnamyl cinnamate are new findings in Brazilian propolis. The presence of cycloartane- and lanostane-type triterpenoids, the latter being a class of compounds of restricted distribution in propolis worldwide, has not been reported in propolis from Midwest Brazil until now. The ethyl acetate phase obtained from the ethanol extract was effective in preventing biofilm formation by Staphylococcus aureus, with an inhibition rate of about 96 % at 0.5â mg.mL-1 , and with quercetin isolated as one of its active constituents. In contrast, the hexane phase exhibited notable antibacterial activity against Pseudomonas aeruginosa, inhibiting bacterial growth by 92 % at 0.5â mg.mL-1 ; however, none of the triterpenoids isolated from this phase proved active against this pathogen. The ethanol extract was neither toxic nor mutagenic at the concentrations tested, as determined by the inâ vivo SMART assay on Drosophila melanogaster, even under conditions of high metabolic activation.
Asunto(s)
Ascomicetos , Própolis , Triterpenos , Animales , Própolis/farmacología , Própolis/química , Brasil , Mutágenos , Drosophila melanogaster , Antibacterianos/química , Etanol , Biopelículas , Extractos Vegetales , Pruebas de Sensibilidad MicrobianaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Baccharis trimera (Less.) DC known as "carqueja" in Brazil has been acknowledged as a medicinal plant in folk medicine for the treatment of stomach aches and gastrointestinal disorders. AIM OF THE STUDY: The present study aimed to evaluate the gastroprotective and healing effects of essential oil from B. trimera (EOBT) against gastric ulcer lesions caused by absolute ethanol and acetic acid, respectively, and to identify the mechanism of action of this essential oil in male Wistar rats. MATERIALS AND METHODS: The plant material used to obtain EOBT was collected in the southern region of Brazil and was analyzed by chromatography-mass spectrometry (GCMS) demonstrate its characteristic chemical composition, with carquejyl acetate as its main component. Different doses of EOBT (50, 100, and 200 mg/kg) were administered orally in male Wistar rats as an acute treatment against absolute ethanol-induced gastric lesions. The gastric healing effect of EOBT (100 mg/kg) was evaluated once a day after 7, 10, and 14 days of treatment. After treatment, the stomachs of rats from all groups were collected to measure the lesion area (mm2), the activity of myeloperoxidase (MPO), and the relative expression of caspases -3, -8, -9, cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), vascular endothelial growth factor (VEGF), and epidermal growth factor (EGF). The zymography method was used to elucidate the activity of matrix metalloproteinase-2 (MMP-2) and -9 (MMP-9) in the healing action of EOBT. We also analyzed toxicological parameters (body weight evolution and biochemical parameters) that could result after treatment with this essential oil for 14 days. RESULTS: Pretreatment with EOBT (100 and 200 mg/kg) significantly decreased the severity of gastric damage induced by absolute ethanol and decreased MPO activity in gastric tissue. After 10 and 14 days of treatment with EOBT (100 mg/kg) once a day, the lesion area was significantly reduced by 61% and 65.5%, respectively, compared to the negative control group. The gastric healing effect of EOBT was followed by a decrease in the expression of COX-1 compared to that in the negative control group. Notably, treatment with EOBT for 14 days increased the expression of VEGF compared to that using an anti-ulcer drug (lansoprazole). Additionally, analyses of MMP-2 and MMP-9 activities in the gastric mucosa confirmed the accelerated gastric healing effect of EOBT, with a significant decrease in the activity of pro-MMP-2. No sign of toxicity was observed after treatment with EOBT for 14 consecutive days. CONCLUSION: These findings indicated that EOBT was effective in preventing and accelerating ulcer healing by decreasing MPO activity, increasing VEGF expression, and decreasing MMP-2 activity. These actions collectively contribute to the rapid recovery of gastric mucosa following treatment with EOBT, without any observed toxicity.
Asunto(s)
Antiulcerosos/farmacología , Baccharis/química , Metaloproteinasa 2 de la Matriz/metabolismo , Aceites Volátiles/farmacología , Úlcera Gástrica/tratamiento farmacológico , Factor A de Crecimiento Endotelial Vascular/metabolismo , Ácido Acético/toxicidad , Animales , Antiulcerosos/uso terapéutico , Antiulcerosos/toxicidad , Brasil , Caspasas/metabolismo , Ciclooxigenasa 1/metabolismo , Ciclooxigenasa 2/metabolismo , Modelos Animales de Enfermedad , Etanol/toxicidad , Mucosa Gástrica/efectos de los fármacos , Lansoprazol/farmacología , Lansoprazol/uso terapéutico , Masculino , Metaloproteinasa 9 de la Matriz/metabolismo , Medicina Tradicional , Proteínas de la Membrana/metabolismo , Aceites Volátiles/uso terapéutico , Aceites Volátiles/toxicidad , Tamaño de los Órganos/efectos de los fármacos , Ratas Wistar , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patologíaRESUMEN
Citral is a mixture of monoterpenes present in the essential oil of several plants, such as Cymbopogon citratus and Zingiber officinale, possessing anti-inflammatory, anti-ulcerogenic, and antipyretic actions. We investigated the action of citral on body temperature (Tb) and inflammatory signaling in eutrophic and obese mice during Systemic Inflammation (SI) induced by Lipopolysaccharide (LPS). Thus, we assessed the effect of citral (25, 100, and 300 mg/kg) and ibuprofen in LPS-induced SI in Swiss male mice fed a standard diet (SD) or high-fat diet (HFD) for 12 weeks. Following SI induction, we measured Tb and collected the serum, hypothalamus, and gastric mucosa for biochemical measurements. Acute treatment with citral decreased the Tb of both SD and HFD-fed animals. Citral (300 mg/kg) treatment caused a significantly lower Tb variation in HFD-fed animals than in those fed the SD. Citral reduced peripheral levels of tumor necrosis factor (TNF)-α in SD and HFD mice and decreased serum leptin concentration in HFD mice 90 min after the LPS challenge. Furthermore, citral also reduced interleukin (IL)-6 levels in the hypothalamus of obese mice. In summary, citral effectively reduced Tb during SI by reducing inflammatory mediators with a distinct action profile in HFD mice when compared with SD.
Asunto(s)
Monoterpenos Acíclicos/farmacología , Inflamación/tratamiento farmacológico , Leptina/sangre , Factor de Necrosis Tumoral alfa/sangre , Monoterpenos Acíclicos/química , Animales , Antiinflamatorios/química , Antiinflamatorios/farmacología , Citocinas/sangre , Dieta Alta en Grasa/efectos adversos , Zingiber officinale/química , Humanos , Inflamación/sangre , Inflamación/inducido químicamente , Inflamación/patología , Interleucina-6/sangre , Leptina/genética , Lipopolisacáridos/toxicidad , Ratones , Ratones Obesos , Aceites Volátiles/química , Aceites Volátiles/farmacologíaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Terminalia catappa L. (Combretaceae), known as "amendoeira da praia" in Brazil, has been recognized as a medicinal plant in folk medicine for the treatment of gastrointestinal disorders and other inflammatory conditions. The present study aimed to investigate the preventive and healing effects of the infusion of leaves of T. catappa (ILTC) against gastric lesions caused by ischemia and reperfusion (I/R) injury and characterize its mechanism of action in the gastric mucosa of rats. MATERIALS AND METHODS: Different doses (30, 100, and 300 mg/kg) of ILTC were orally administered as acute and subacute treatments against I/R-induced gastric lesion in rats. After treatment, the stomach of rats was collected to measure the lesion area, redox parameters malondialdehyde (MDA), superoxide dismutase (SOD), catalase (CAT), and reduced glutathione (GSH) and inflammatory parameters myeloperoxidase activity (MPO), interleukin 1ß (IL-1ß) and tumor necrosis factor α (TNF-α). The activities of matrix metalloproteinases 2 and 9 (MMPs 2 and 9) were assessed by zymography method to clarify the mechanisms of the healing acceleration promoted by ILTC. RESULTS: Pretreatment with ILTC (100 mg/kg) was effective in preventing the aggravation of lesions in the acute model by reducing MPO activity by 38% relative to control group, despite the lack of clarity of this action at the macroscopical level at the lesion area (p < 0.05). After three days of treatment with ILTC (30 and 100 mg/kg), this infusion significantly reduced the lesion area by 95% and 89%, respectively, compared the control (p < 0.05). The gastric healing effect of all doses of ILTC was followed by a reduction in MPO activity (decrease by 70-78%). Compared to the negative control, an improvement in gastric healing owing to treatment with ILTC was observed and this was followed by an increase in MMP-2 (20-47%) (p < 0.05). CONCLUSION: Three days of treatment with ILTC could accelerate the healing process in I/R-induced lesions in rats. By decreasing MPO levels, ILTC enabled the action of MMP-2, which led to tissue recovery in the gastric mucosa.
Asunto(s)
Antiulcerosos/farmacología , Extractos Vegetales/farmacología , Daño por Reperfusión/tratamiento farmacológico , Úlcera Gástrica/tratamiento farmacológico , Estómago/efectos de los fármacos , Terminalia/química , Cicatrización de Heridas/efectos de los fármacos , Animales , Araquidonato 15-Lipooxigenasa/metabolismo , Catalasa/metabolismo , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/metabolismo , Masculino , Medicina Tradicional/métodos , Ratones , Ratones Endogámicos C57BL , Fitoterapia/métodos , Hojas de la Planta/química , Plantas Medicinales/química , Ratas , Ratas Sprague-Dawley , Daño por Reperfusión/metabolismo , Úlcera Gástrica/metabolismo , Superóxido Dismutasa/metabolismoRESUMEN
AIM: To evaluate the sex-specific effects of a hydroalcoholic extract from Eugenia punicifolia (HEEP) leaves on gastric ulcer healing. METHODS: In this rat study involving males, intact (cycling) females, and ovariectomized females, gastric ulcers were induced using acetic acid. A vehicle, lansoprazole, or HEEP was administered for 14 d after ulcer induction. Body weight was monitored throughout the treatment period. At the end of treatment, the rats were euthanized and the following in vivo and in vitro investigations were performed: macroscopic examination of the lesion area and organ weights, biochemical analysis, zymography, and evaluation of protein expression levels. Additionally, the concentration-dependent effect of HEEP was evaluated in terms of subacute toxicity and cytotoxicity. RESULTS: Compared to the vehicle, HEEP demonstrated a great healing capacity by substantially reducing the ulcerative lesion area in males (52.44%), intact females (85.22%), and ovariectomized females (65.47%), confirming that HEEP accelerates the healing of acetic acid-induced gastric lesions and suggesting that this effect is modulated by female sex hormones. The antiulcer effect of HEEP was mediated by prostaglandin E2 only in male rats. Overall, the beneficial effect of HEEP was the highest in intact females. Notably, HEEP promoted the expression of vascular endothelial growth factor (intact vs ovariectomized females) and decreased the expression of Caspase-8 and Bcl-2 (intact female vs male or ovariectomized female). Additionally, HEEP enhanced fibroblast proliferation and migration into a wounded area in vitro, confirming its healing effect. Finally, no sign of subacute toxicity or cytotoxicity of HEEP was observed. CONCLUSION: In gastric ulcers, HEEP-induced healing (modulated by female sex hormones; in males, mediated by prostaglandin) involves extracellular matrix remodeling, with gastric mucosa cell proliferation and migration.
Asunto(s)
Eugenia/química , Extractos Vegetales/farmacología , Repitelización/efectos de los fármacos , Úlcera Gástrica/tratamiento farmacológico , Ácido Acético/toxicidad , Animales , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Femenino , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/patología , Humanos , Masculino , Extractos Vegetales/uso terapéutico , Hojas de la Planta/química , Ratas , Ratas Wistar , Factores Sexuales , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/patología , Pruebas de Toxicidad Subaguda , Resultado del TratamientoRESUMEN
INTRODUÇÃO: Este trabalho apresenta a avaliação de uma experiência educacional inovadora que articula a construção do conhecimento às questões subjetivas do sujeito. A disciplina Desenvolvimento do Ciclo de Vida (DCV), ministrada no terceiro semestre, usa ludicidade e Narrativa Autobiográfica como método e busca compreender os processos psicológicos típicos da gestação ao envelhecimento e desenvolver competências interpessoais necessárias à prática médica. OBJETIVO: Descrever a avaliação de estudantes egressos da disciplina sobre seus efeitos educacionais. METODOLOGIA: Estudo descritivo qualitativo, realizado numa instituição privada de ensino superior em Salvador, na Bahia. Análise de conteúdo de sete entrevistas semiestruturadas com um estudante de cada semestre, desde que a disciplina começou a ser oferecida. Utilizou-se a análise de domínios, e o estudo foi aprovado pelo Comitê de Ética. RESULTADOS: Os entrevistados percebem o método utilizado como uma estratégia de aprendizagem positiva e referem um importante reflexo desta em seu processo formativo. DISCUSSÃO/CONSIDERAÇÕES: A aquisição do conhecimento se faz com processos reflexivos e possibilita a percepção dos limites e possibilidades do sujeito, qualificando suas competências interpessoais. A humanização emerge espontaneamente, evidenciando o impacto da disciplina na construção da identidade profissional desses estudantes.
INTRODUCTION: This article describes students' evaluations of an innovative educational experience that connects the construction of knowledge to individuals' subjective issues. The course entitled "Life Cycle Development" is administered during the third semester of medical school and uses playful activities and autobiographical narrative as the methodology, while seeking to understand the typical psychological processes over the course of life, from conception to senescence, and to describe the interpersonal skills required in medical practice. OBJECTIVE: To describe the evaluation by students who have taken the course in terms of its effects on their education. METHODOLOGY: A qualitative, descriptive study was conducted in a private university in Salvador, Bahia, Brazil, consisting of a domain content analysis of 7 semi-structured interviews with students from each semester since the subject was first introduced. The study was approved by the university's Institutional Review Board. RESULTS: The methodology was perceived by interviewees as a positive learning strategy, and students reported that the course was significant in defining their professional backgrounds. DISCUSSION/REMARKS: Knowledge is acquired through reflective processes that enable individuals to perceive their limits and possibilities, qualifying their interpersonal skills. Humanization emerges spontaneously, confirming the effect of this course on the construction of the students' professional identity.