ABSTRACT
Fridericia chica is widely distributed in Brazil, where it is commonly known as crajiru or pariri in several regions. Despite its popular use for treating inflammations and as an insect repellent, there has been limited assessment of its chemical and biological properties, including its bioinsecticide activities. In this study, we conducted phytochemical analyses and investigated the larvicidal and repellent effects of F. chica against the mosquito Aedes aegypti. The F. chica (HEFc) hydroalcoholic extract was partitioned using column chromatography, and subfractions were analyzed using chromatographic and spectroscopic analyses (ESI-IT-MSn and NMR). In addition, HEFc was evaluated for its larvicidal and repellent activities. Phytochemical analyses revealed the presence of 17 constituents, including 2,4-dihydroxybenzoic and p-coumaric acids, along with umbelliferone, acetovanilone, myricetin-3-O-glucuronide, and cis-isorhapontigenin, which are reported for the first time in this species. Although no larvicidal effect was observed at the doses tested, the HEFc exhibited promising repellent effects against A. aegypti, which aligns with its ethnopharmacological potential. In addition, molecular docking studies demonstrated that the compounds of HEFc interacted efficiently with insect odorant binding proteins (OBPs), providing repellent effects. Consistent with the chemical profile and in silico studies, preparations of F. chica have considerable repellent potential.
ABSTRACT
Propolis has been used for the treatment of gastric disturbances in folk medicine, nevertheless, the gastric healing effects of Brazilian red propolis have not been unveiled. This study aimed to assess the gastric healing effect of the hydroalcoholic extract of red propolis (HERP) in the acetic acid-induced ulcer model. Rats under acetic acid-induced-ulcer were treated with HERP (100â mg/kg, p.o.) twice a day for seven days. Histological changes, oxidative stress, and inflammatory parameters were analyzed in the gastric tissue. Moreover, the gastric wall thickness was measured by ultrasound. The inâ vitro cytotoxicity of HERP and cellular migration of fibroblasts were evaluated. The treatment with HERP promoted gastric healing, reducing gastric wall thickness, macroscopic lesion area, and histopathological damages compared to the vehicle. Moreover, HERP reduced oxidative stress and inflammation in the gastric tissue but did not change mucin or collagen levels. HERP did not show signs of toxicity either inâ vivo or inâ vitro. HERP displayed a healing effect inâ vivo by reducing oxidative stress and inflammation. These data contribute to validating the popular use of this product in the treatment of gastric disorders and advance scientific knowledge in the search for new drugs for the management of gastric ulcers.
Subject(s)
Propolis , Rats , Animals , Rats, Wistar , Propolis/pharmacology , Propolis/therapeutic use , Ulcer , Brazil , Inflammation/drug therapyABSTRACT
BACKGROUND: Considering the pharmacological potential of solidagenone from Solidago chilensis, the present investigation was carried out to evaluate its antidepressant-like effect in mice with bacterial lipopolysaccharide (LPS)-induced depressive like behavior and its mode of action through the measurement of neuroinflammatory and oxidative markers. MATERIALS AND METHODS: In the prophylactic test, the mice were pretreated with solidagenone (1, 10 or 100 mg/kg, p.o) and after one hour received LPS. In therapeutic test, the mice received LPS and after 5 h were treated with solidagenone (1, 10 or 100 mg/kg, p.o). In both experimental approaches, the animals were submitted to OFT and to the TST after 6 and 24 h of the LPS administration, respectively. One hour after the TST the animals were euthanized, the blood was collected, the cortex was removed and biochemical analyzes were performed for measurement of the inflammatory and oxidative stress markers. RESULTS: The LPS induced sickness- and depressive-like behaviors and increased the cortical activity of myeloperoxidase (MPO), as well as the IL-6 and TNF amount. Interestingly, the pretreatment with solidagenone at 100 mg/kg avoided the behavioral alterations in OFT. In the mice post treated with solidagenone, all tested doses of resulted in an antidepressant-like effect evidenced by the decrease in immobility time in the TST. This effect was accompanied by a decrease in the MPO activity and in the IL-6 and TNF levels in the cortex in parallel to the increase in catalase activity. CONCLUSIONS: The solidagenone has a promissor antidepressant-like potential, which can result of its beneficial action in the neuroinflammation process and due its antioxidant capability at the central nervous system.
Subject(s)
Depression/drug therapy , Furans/pharmacology , Naphthalenes/pharmacology , Animals , Antidepressive Agents/metabolism , Antidepressive Agents/pharmacology , Behavior, Animal/drug effects , Brain-Derived Neurotrophic Factor/metabolism , Depression/physiopathology , Disease Models, Animal , Furans/metabolism , Interleukin-1beta/metabolism , Lipopolysaccharides/pharmacology , Male , Mice , Naphthalenes/metabolism , Oxidative Stress/drug effects , Signal Transduction/drug effects , Tumor Necrosis Factor-alpha/metabolismABSTRACT
O mosquito Aedes albopictus possui ampla distribuição em regiões tropicais, bem como nos países de clima temperado e tem sido apontado pela literatura científica como importante para a saúde pública. Observa-se a carência de estudos acerca da infestação, dispersão e a associação da espécie com o grau de urbanização, criadouros, tipos de imóveis e sazonalidade. Este estudo teve como objetivos, dentre outros, analisar a evolução da infestação por A. albopictus ao longo de um gradiente de urbanização. O estudo teve como referência geográfica o município de Chapecó (SC). Para avaliar a dispersão e a flutuação populacional foi criado um gradiente de urbanização. Para avaliar a tendência da infestação em cada região no período, foram utilizadas análises de regressão linear. A infestação pelo mosquito foi maior nas regiões periurbanas e rurais e menor nas regiões mais urbanizadas. Os resultados encontrados são relevantes no planejamento e na implantação de ações de prevenção das arboviroses transmitidas.
Aedes albopictus mosquito is widely distributed in tropical regions, as well as in temperate countries, and has been identified by the scientific literature as important to public health. There is a lack of studies on infestation, dispersion and the species association with the level of urbanization, breeding sites, types of property and seasonality. This study aimed to analyze the evolution of A. albopictus infestation along an urbanization gradient. The geographical reference of this study was the municipality of Chapecó, State of Santa Catariana. To assess dispersion and population fluctuation an urbanization gradient was created. Linear regression analysis was applied to evaluate the trend of infestation in each region in the study period. Mosquito infestation was higher in peri-urban and rural regions, and lower in more urbanized regions. The results are relevant for planning and implementing prevention actions for transmitted arbovirus diseases.
Subject(s)
Arbovirus Infections , Urbanization , Public Health , CitiesABSTRACT
ETHNOPHARMACOLOGICAL IMPORTANCE: The species Urera baccifera (L.) Gaudich. ex Wedd. (Urticaceae) is native to the Americas and is distributed widely throughout Brazil, where it is known as urtiga-brava, urtiga-vermelha, or urtigão. The leaves are often used as anti-inflammatory and antirheumatic agents and for the treatment of gastric disorders. However, the pharmacological mode of action underlying the gastroprotection induced by this species has not been investigated. AIM OF THE STUDY: To contribute to the knowledge of the gastroprotective mode of action of the hydroalcoholic extract of U. baccifera (HEU) leaves. MATERIALS AND METHODS: Antiulcerogenic effect of HEU against ethanol-induced acute gastric ulcer was evaluated in rats and mice at doses of 3-300 mg/kg. NO-synthase inhibitor (L-NAME), SH blocker (NEM), cyclooxygenase inhibitor (indomethacin) and alpha 2-adrenergic receptor antagonist yohimbine were used to evaluate the participation of cytoprotective factors in HEU gastroprotection. Moreover, the levels of reduced gluthatione (GSH) and cytokines (TNF, IL-6, IL4 and IL-10), as well as the enzymatic activity of gluthatione S-transferase (GST), myeloperoxidase (MPO), superoxide dismutase (SOD) and catalase (CAT) were measure. Moreover, the samples were analyzed histologically and the antisecretory capability of HEU were quantified using pylorus ligated rats. RESULTS: The phytochemical analysis of HEU (UPLC/ESI-IT-MS) identified the flavonoids diosmetin and apigenin glucuronide. Furthermore, HEU decreased the occurrence of ethanol-induced ulcers at 30 and 300 mg/kg by 57% and 66%, respectively, compared with the vehicle. The gastroprotective effects were accompanied by increased GSH levels and GST and SOD activity as well as by reduced MPO activity in vivo and in vitro, revealing antioxidant effects and inhibition of neutrophil infiltration. The beneficial effects of 30 and 300 mg/kg HEU were also observed upon histological analyses. Regarding the mode of action, the gastroprotective effect of HEU was abolished by the pre-administration of L-NAME, NEM, indomethacin or yohimbine. Moreover, HEU was able to decrease the IL-6, IL-4 and IL-10 in ulcerated tissue, as well as the pepsin activity of the gastric juice in pylorus-ligated rats. CONCLUSION: Together, the results confirmed that the gastroprotection elicited by HEU was due reduction in oxidative damage, neutrophil migration, and peptic activity. This work validates the popular use of U. baccifera to treat gastric disorders and supports important future research for the identification of gastroprotective molecules from this species.
Subject(s)
Anti-Ulcer Agents/pharmacology , Plant Extracts/pharmacology , Stomach Ulcer/prevention & control , Urticaceae/chemistry , Animals , Anti-Ulcer Agents/administration & dosage , Anti-Ulcer Agents/isolation & purification , Antioxidants/metabolism , Cytokines/metabolism , Disease Models, Animal , Dose-Response Relationship, Drug , Male , Mice , Neutrophil Infiltration/drug effects , Plant Extracts/administration & dosage , Plant Leaves , Rats , Rats, WistarABSTRACT
Abstract To the moment, there is no ideal substance for home-based denture disinfection. This study assessed in vitro the antimicrobial effect of the hydroalcoholic extract of Eugenia uniflora and the effect on the physical properties of denture polymethylmethacrylate (PMMA). Candida albicans, Staphylococcus aureus, and Klebsiella oxytoca were isolated from samples of saliva collected from denture wearers. The extracts were produced in three concentrations, according to the Brazilian Pharmacopeia. One hundred eighty-eight disc-shaped specimens of thermopolymerizable PMMA were prepared and randomly allocated to five treatment groups: sterile saline solution (0.85%; control); chlorhexidine digluconate (0.2%); and hydroalcoholic extract of E. uniflora (0.2%, 0.8%, and 1.16%). The specimens were disinfected for 8 hours/day for 30 days. Adherence of microorganisms to the surface, PMMA surface roughness, and color stability were assessed. Inferential statistics were performed with one- and two-way ANOVA/Tukey test, and Kruskal Wallis, Mann-Whitney U, and paired t-tests, at α=0.05. The extract of E. uniflora at 0.2% and 1.16% reduced the microbial load of K. oxytoca, while chlorhexidine digluconate significantly reduced microbial load of all microrganisms. Microbial adherence at day 10 was reduced by all experimental substances (p<0.001). Surface roughness was not affected by the disinfecting substances (p>0.05). Nevertheless, all experimental groups produced unacceptable color change at the end of the disinfection protocol (p<0.001). The non-adherent potential against microorganisms isolated from the oral cavity confirm the potential of use of the hydroalcoholic extract of E. uniflora as a denture disinfectant. Yet, unacceptable color changes may occur, regardless of extract concentration.
Subject(s)
Humans , Staphylococcus aureus/drug effects , Candida albicans/drug effects , Plant Extracts/pharmacology , Dentures , Klebsiella oxytoca/drug effects , Eugenia/chemistry , Mouthwashes/pharmacology , Polymethyl MethacrylateABSTRACT
Abstract Natural products, especially phytochemicals, have been extensively studies and have exhibited important antiproliferative effects. The American native species Urera baccifera (L.) Gaudich. ex Wedd. (Urticaceae) is widely distributed in Brazil, where it is known as urtiga-vermelha or urtigão. The leaves are popularly used as anti-inflammatory, antirheumatic and in the treatment of gastric disorders. However, the antiproliferative potential of this plant against human tumor cells remain to be elucidated. In this study, we evaluated the antiproliferative effects of U. baccifera leaves extracts and fractions against a panel of human tumor cell lines in vitro besides a chemical evaluation of the most active sample by mass spectrometry (ESI-IT-MSn). The hydroalcoholic extract was inactive while dichloromethane extract showed moderate cytostatic activity against ovarian carcinoma cell line (OVCAR-3, GI50 = 1.5 μg/mL). More, the ethyl acetate and n-butanol fractions did not show important activity against tumour cell while the dichloromethane and hexane fractions showed moderate cytostatic activity against ovarian tumor cell line (OVCAR-3, GI50 = 12.7 and 9.4 μg/mL, respectively). Finally, the chemical profile evaluated by mass spectrometry (ESI-IT-MSn) allowed the detection of flavonoids in the HEU and hydroxylated fatty acid in DEU that can explain partially the biological effects observed. This is the first report of the antiproliferative effects of U. baccifera, and DEU has shown potential as a promising source of bioactive compounds.
Subject(s)
Ovarian Neoplasms/drug therapy , Plants, Medicinal/drug effects , Chemical Phenomena/drug effects , Antineoplastic Agents/pharmacology , Mass Spectrometry/instrumentationABSTRACT
Denture use may aggravate the occurrence of oral infections, considering it enhances microbial adherence. Aim: This study assessed the reduction of microbial loads of Candida albicans, Staphylococcus aureus, and Klebsiella oxytoca by disinfecting the polymethylmethacrylate (PMMA) of complete dentures with hydroalcoholic extract of Salvia officinalis. Additionally, the effect of such extract on the properties of PMMA was examined. Methods: Microorganisms were isolated from saliva samples collected from complete denture wearers. The hydroalcoholic extract of S. officinalis was produced according to the Brazilian Pharmacopoeia 5. The PMMA specimens (n=188) were immersed in microbial inoculum and incubated at 37°C for 16 hours per day. Then, they were subjected to a disinfection protocol for 30 days. The specimens were divided into five treatment groups: sterile saline solution (0.85%; control), 0.2% chlorhexidine digluconate, and hydroalcoholic extract of S. officinalis (0.2%, 0.8%, and 1.16%). Microorganism adherence to the PMMA surface was also assessed, as well as surface roughness (Ra in µm) and color stability of the PMMA (mean ΔE). Changes in microbial load and surface roughness after the disinfection protocol were verified with paired t-test. Substances at day 10, adherence, and color stability were compared by the Kruskall-Wallis and Mann-Whitney tests, and one-way ANOVA was used to compare substances at the beginning and end of the experiment (α=0.05). Results: The 1.16% S. officinalis extract significantly reduced the microbial load of all the microorganisms after 30 days of disinfection (p<0.05). The microbial load of K. oxytoca was also reduced at lower concentrations of the S. officinalis extract (0.2% and 0.8%) (p<0.02). Antimicrobial and anti-adherent effects against microorganisms isolated from the oral cavity were observed. There was no significant change in surface roughness (p>0.05) and color stability was significantly higher in the control group (p<0.0001). Conclusions: The hydroalcoholic extract of S. officinalis may be used as a disinfectant solution for dentures
Subject(s)
Plant Extracts , Colony Count, Microbial , Polymethyl Methacrylate , Denture Cleansers , Salvia officinalisABSTRACT
The jaboticaba tree, Plinia trunciflora (O. Berg) Kausel, is popularly named "jabuticabeira" in Brazil and is used in folk medicine to treat diabetes and chronic inflammation of the tonsils, but studies evaluating the central effects of this species are limited. This study evaluated the antidepressant-like and antioxidant effects of P. trunciflora (PT) aqueous extract, in which five different anthocyanins were identified. PT showed significant ferric-reduction power and DPPH radical scavenging activity in vitro and reduced lipid peroxidation both in vitro and ex vivo. At the behavioural level, PT (400 and 800 mg/kg, i.p.) dose-dependently reduced immobility time in the tail suspension test in Swiss male mice. The identification of bioactive compounds accompanied by the in vitro and ex vivo antioxidant activity of PT suggests that these activities might be related to the antidepressant-like activity of P. trunciflora.
ABSTRACT
Few data exists about the pharmacological properties of Heteropterys aphrodisiaca O. Mach. (Malpighiaceae), which is native to the scrubland regions of Brazil. The present study investigated the effects of oral treatment with H. aphrodisiaca extract (BST0298) on the learning and memory of young (3-6 months) and aged (21-23 months) rats, and compared the in vitro antioxidant activity of three lots collected in different years. An improvement in the number of sessions to learn the task was observed in the left/right discrimination test in aged rats treated for 45 days with 25 mg/kg (7.0 ± 0.5; p=0.005) or 50 mg/kg (7.6 ± 0.6; p=0.012) compared with control old rats (11.0 ± 1.6). On the other hand, pre-treatment did not improve the performance of scopolamine-treated mice in the passive avoidance test. The in vitro malondialdehyde test showed that all three different extracts presented similar antioxidant activity. The flavonoids astilbin, isoastilbin and neoastilbin were isolated from the extract and may contribute to the biological activity. These results suggest that repeated treatment with H. aphrodisiaca improves learning and memory, probably by a non-muscarinic mechanism.
Existem poucos dados disponíveis sobre as propriedades farmacológicas da Heteropterys aphrodisiaca O. Mach. (Malpighiaceae), nativa da região do pantanal brasileiro. O presente estudo investigou o efeito do tratamento oral com um extrato de H. aphrodisiaca (BST0298) sobre a memória e aprendizagem de ratos jovens (3-6 meses) e idosos (21-23 meses) e comparou a atividade antioxidante in vitro de três lotes, coletados em diferentes anos. Melhora quanto ao número de sessões necessárias para aprender a tarefa foi observada no teste de discriminação direita/esquerda em ratos idosos tratados por 45 dias com doses de 25 mg/kg (7,0 ± 0,5; p=0,005) e 50 mg/kg (7,6 ± 0,6; p=0,012) comparados com ratos idosos controle (11,0 ± 1,6). Por outro lado, o pré-tratamento com o extrato não melhorou o desempenho de camundongos tratados com escopolamina no teste da esquiva passiva. Em relação à avaliação da atividade antioxidante in vitro pelo teste do malonodialdeído, os três lotes analisados apresentaram atividade antioxidante semelhante. Os flavonóides astilbina, isoastilbina e neoastilbina foram isolados do extrato e podem contribuir para a atividade biológica. Estes resultados sugerem que a administração repetida de H. aphrodisiaca melhora a memória e aprendizagem provavelmente por um mecanismo não muscarínico.
Subject(s)
Rats , Rats/classification , Malpighiaceae , Memory/classification , Flavonoids/pharmacology , Plant Extracts/pharmacology , Antioxidants/analysisABSTRACT
O objetivo deste estudo foi avaliar a influência dos tratos culturais no desenvolvimento vegetal, morfologia e teor de flavonóides para Calendula officinalis L., Asteraceae. Os tratos culturais foram: calagem (CA), calagem + adubação orgânica (CAO) e calagem + adubação química NPK (CAQ). O experimento foi inteiramente casualizado com sessenta repetições e a comparação das médias realizada por ANOVA e teste de Duncan (significância de 95 por cento). Os resultados apontam que CAO e CAQ apresentaram maior desenvolvimento vegetal comparados com tratamento CA. O tratamento CAO produziu ainda, plantas com maior homogeneidade, massa fresca e número de capítulos florais por planta, mas menor biomassa de flores produzidas por cada indivíduo. Observou-se também, variações morfoanatômicas com flores tubulares com centro amarelado (TCA) e tubulares com centro acastanhado (TAC) que produziram maior teor de flavonóides (1,41 e 1,44 por cento respectivamente) comparadas com flores ligulares com centro amarelado (LCA) e ligulares com centro acastanhado (LAC) (0,89 e 0,95 por cento respectivamente). Os compostos químicos nas flores de calêndula, visualizados por cromatografia em camada delgada, demonstraram que os tratamentos não têm influencia sobre o perfil químico qualitativo do vegetal. Entretanto, cultivares de calêndula submetidas ao tratamento CAQ produziram maior quantidade de flavonóides totais (1,14 por cento) contra 1,04 por cento do CAO e 1,03 por cento de CA.
The objective of this study was to examine the influence of cultivation treatments on plant development, morphology and flavonoid content in Calendula officinalis L., Asteraceae. The cultivation treatments were liming (LIM), liming + organic fertilizer (LORG) and liming + NPK chemical fertilizer (LCHEM). The experiment was completely randomized with sixty repetitions and the means were compared by ANOVA and Duncan's test (significance of 95 percent). The results show that LORG and LCHEM produced greater plant development compared with LIM treatment. The LORG treatment also produced plants with greater homogeneity, fresh mass, and higher numbers of flowers per plant, but lower biomass of flower produced by each individual. Morphoanatomical variations were also observed with tubular flowers with yellow centres (TCA) and tubular flowers with brown centres (TAC) that produced a higher content of flavonoids (1.41 and 1.44 percent respectively), compared with ligulate flowers with yellow centres (LCA) and ligulate flowers with brown centres (LAC) (0.89 and 0.95 percent respectively). The chemical compounds in the flowers of calendula viewed by thin-layer chromatography showed that the treatments did not have any influence on the qualitative chemical profile of the plant. However, cultivars of calendula that underwent treatment LCHEM produced a greater quantity of total flavonoids (1.14 percent) against 1.04 percent for LORG and 1.03 percent for LIM.
ABSTRACT
O objetivo do presente estudo foi avaliar in vivo o potencial hipoglicemiante, de extratos obtidos da raiz e folha de bardana, Arctium minus (Asteraceae). Também realizaram-se ensaios farmacognósticos de controle de qualidade. Nos ensaios biológicos, 60 ratos foram induzidos ao diabetes experimental pela administração de aloxano por via endovenosa, na dose única de 42 mg/kg. No sétimo dia após a indução, dosou-se a glicemia de jejum. Os animais com glicemia superior a 190 mg/dL foram redistribuídos em quatro grupos para receberem, por 21 dias, algum tipo de tratamento. Grupo 1: Glibenclamida, na dose de 0,071 mg/kg; Grupo 2: extrato bruto liofilizado da raiz de bardana, 500 mg/kg; Grupo 3: extrato bruto liofilizado da folha de bardana, 200 mg/kg; e Grupo 4: soro fisiológico. Após o tratamento, o extrato bruto da raiz de bardana reduziu em 34,6 ± 5,8 por cento os níveis glicêmicos, o extrato bruto da folha reduziu 22,9 ± 6,2 por cento e a Glibenclamida 34,5 ± 6,2 por cento. O grupo placebo manteve a glicemia. Este estudo demonstrou que o extrato bruto de Arctium minus, principalmente a raiz, é capaz de diminuir os níveis plasmáticos de glicose, com potência semelhante ao medicamento sintético de referência Glibenclamida.
The objective of the present study was to analyze in vivo the hypoglycemiant potential of the extracts from the root and leaf of the medicinal plant bardana, Arctium minus (Asteraceae). It was also carried out through pharmacognostics analysis of quality control. In the biological assays, 60 rats were induced to the experimental diabetes through endovenous injection of alloxan administration, in an only dose of 42 mg/kg. On the seventh day after the induction, the fast glycemia was dosed. The animals with glycemia superior to 190 mg/dL were redistributed in four groups to receive, for 21 days, some kind of treatment. Group 1: Glibenclamide in the dose of 0.071 mg/kg; Group 2: pure lyophilized extract of bardana root, 500 mg/kg; Group 3: pure lyophilized extract of bardana leaf, 200 mg/kg; and Group 4: physiological serum. After treatment, the pure extract of bardana root reduced in 34.6 ± 5.8 percent the glycemic levels, the pure extract of the leaf reduced in 22.9 ± 6.2 percent and the Glibenclamide 34.5 ± 6.2 percent. The placebo group kept the glicemy. This study suggests that the pure extract of Arctium minus, mainly the root extract, is able to reduce the plasmatic levels of glucose, with similar power to the synthetic medicine of Glibenclamide reference.