Evaluation of the antiedematogenic and anti-inflammatory properties of Ximenia americana L. (Olacaceae) bark extract in experimental models of inflammation.

Edema is one of the obvious indicators of inflammation and a crucial factor to take into account when assessing a substance's capacity to reduce inflammation. We aimed to evaluate the antiedematogenic and anti-inflammatory profile of the hydroethanolic barks extract of Ximenia americana (HEXA). The possible antiedematogenic and anti-inflammatory effect of EHXA (50, 100 mg/kg and 250 mg/kg v.o) was evaluated using the paw edema induced by carrageenan, zymosan, dextran, CFA and by different agents inflammatory (serotonin, histamine, arachidonic acid and PGE2), and pleurisy model induced by carrageenan and its action on IL-1ß and TNF-α levels was also evaluated. HEXA demonstrated a significant antiedematogenic effect at concentrations of 50, 100 and 250 mg/kg on paw edema induced by carrageenan, zymosan and dextran. However, the concentration of 50 mg/kg as standard, demonstrating the effect in the subchronic model, induced CFA with inhibition of 59.06 %. In models of histamine-induced paw edema, HEXA showed inhibition of - 30 min: 40.49 %, 60 min: 44.70 % and 90 min: 48.98 %; serotonin inhibition - 30 min: 57.09 %, 60 min: 66.04 % and 90 min: 61.79 %; arachidonic acid inhibition - 15 min: 36.54 %, 30 min: 51.10 %, 45 min: 50.32 % and 60 min: 76.17 %; and PGE2 inhibition - 15 min: 67.78 %, 30 min: 62.30 %, 45 min: 54.25 % and 60 min: 47.92 %. HEXA significantly reduced (p < 0.01) leukocyte migration in the pleurisy model and reduced TNF-α and IL-1ß levels in pleural lavage (p < 0.0001). The results showed that HEXA has the potential to have an antiedematogenic impact in both acute and chronic inflammation processes, with a putative mode of action including the suppression or regulation of inflammatory mediators.

Mechanisms of Actions Involved in The Antinociceptive Effect of Estragole and its ß-Cyclodextrin Inclusion Complex in Animal Models.

(1) Background: estragole is a monoterpene found in the essential oils of several aromatic plants, which can be used for several pharmacological activities. The aim of this study was to evaluate the antinociceptive effect of estragole (Es) and its ß-cyclodextrins inclusion complex (Es/ß-CD). (2) Methods: the effects of Es and Es/ß-CD on the central nervous system (CNS) were evaluated through open field and rota-rod assays, and the antinociceptive effect in formalin models, abdominal writhing induced by acetic acid, hot plate, tail flick test and plantar mechanical hyperalgesia. (3) Results: Es and Es/ß-CD showed no alterations on the CNS evaluated parameters and the results suggested there was an antinociceptive action in the formalin, abdominal writhing, hot plate, tail flick tests and plantar mechanical hyperalgesia, proposing the involvement of the nitric oxide, glutamatergic signaling pathways, cyclic guanosine monophosphate and vanilloid pathways. (4) Conclusion: the results suggest that Es and Es/ß-CD have a promising antinociceptive potential as a possible alternative for the pharmacological treatment of pain, also showing that the encapsulation of Es in ß-cyclodextrins probably improves its pharmacological properties, since the complexation process involves much lower amounts of the compound, contributing to better bioavailability and a lower probability of adverse effect development.

Biological properties of terpinolene evidenced by in silico, in vitro and in vivo studies: A systematic review.

BACKGROUND: Terpinolene, a monoterpene that is naturally found in a variety of herbs, is widely used as a flavoring agent in the industry. Although it's well established in the literature that terpinolene is an important component of plant extracts, the biological properties and the potential therapeutic use of this compound remain poorly explored. PURPOSE: This work aimed to answer the following guiding question: "What are the biological activities of terpinolene demonstrated through in silico, in vitro, and in vivo assays?". STUDY DESIGN AND METHODOLOGY: A systematic review was carried out in four electronic databases (Embase, Web of Science, Scopus, and PubMed) according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines, using the following search terms: terpinolene "AND" activity "OR" properties "OR" therapeutic "OR" treatment. This search included manuscripts published between 1960 and June 2020. Study selection was conducted by two independent reviewers according to predefined criteria. RESULTS: The initial search found a total of 2449 articles. However, only 57 of them were selected as they met the inclusion criteria and answered the guiding question. The analysis of these studies indicated that terpinolene presents a series of biological effects, from which the antioxidant, larvicide, and insecticide activities stand out. Despite the evidence demonstrating that terpinolene has the potential to be used in a broad pharmacological context, the mechanisms underlying its cellular and molecular effects remain to be better elucidated. In addition, the in vivo efficacy and safety of the administration of this compound have been poorly evaluated through either preclinical and clinical trials. Therefore, this study highlights the importance of characterizing the biological aspects and mechanisms of action of this natural compound. CONCLUSION: The data summarized in the present systematic review demonstrates the pharmacological potential of terpinolene. Nevertheless, most studies included in this review provide a superficial characterization of terpinolene biological effects and therefore, further research elucidating its mechanism of action and potential therapeutic benefits through preclinical and clinical trials are required. Nevertheless, due to its wide range of different biological activities, terpinolene will certainly attract the interest of scientific research, which could significantly contribute to the development of new products with both therapeutic and environmental applications.

Evaluation of Benzaldehyde as an Antibiotic Modulator and Its Toxic Effect against Drosophila melanogaster.

Products of natural origin remain important in the discovery of new bioactive molecules and are less damaging to the environment. Benzaldehyde is a product of the metabolism of plants, and similarly to oxygenated terpenes, it can have antibacterial activity against Staphylococcus aureus and toxic action against Drosophila melanogaster; we aimed to verify these activities. The broth microdilution tests determined the minimum inhibitory concentration (MIC) of benzaldehyde alone and in association with antibiotics and ethidium bromide (EtBr). Toxicity against Drosophila melanogaster was determined by fumigation tests that measured lethality and damage to the locomotor system. The results indicated that there was an association of norfloxacin and ciprofloxacin with benzaldehyde, from 64 µg/mL to 32 µg/mL of ciprofloxacin in the strain K6028 and from 256 µg/mL to 128 µg/mL of norfloxacin in the strain 1199B; however, the associations were not able to interfere with the functioning of the tested efflux pumps. In addition, benzaldehyde had a toxic effect on flies. Thus, the results proved the ability of benzaldehyde to modulate quinolone antibiotics and its toxic effects on fruit flies, thus enabling further studies in this area.

Myorelaxant Effect of the Dysphania ambrosioides Essential Oil on Sus scrofa domesticus Coronary Artery and Its Toxicity in the Drosophila melanogaster Model.

PURPOSE: Alternative methods for the use of animals in research have gained increasing importance, due to assessments evaluating the real need for their use and the development of legislation that regulates the subject. The principle of the 3R's (replacement, reduction and refinement) has been an important reference, such that in vitro, ex vivo and cord replacement methods have achieved a prominent place in research. METHODS: Therefore, due to successful results from studies developed with these methods, the present study aimed to evaluate the myorelaxant effect of the Dysphania ambrosioides essential oil (EODa) using a Sus scrofa domesticus coronary artery model, and the toxicity of both the Dysphania ambrosioides essential oil and its major constituent, α-terpinene, against Drosophila melanogaster in toxicity and negative geotaxis assays. RESULTS: The EODa relaxed the smooth muscle of swine coronary arteries precontracted with K+ and 5-HT in assays using Sus scrofa domesticus coronary arteries. The toxicity results presented LC50 values of 1.546 mg/mL and 2.282 mg/mL for the EODa and α-terpinene, respectively, thus showing the EODa and α-terpinene presented toxicity to these dipterans, with the EODa being more toxic. CONCLUSIONS: Moreover, the results reveal the possibility of using the EODa in vascular disease studies since it promoted the relaxation of the Sus scrofa domesticus coronary smooth muscle.

Antiedematogenic and Anti-Inflammatory Activity of the Monoterpene Isopulegol and Its ß-Cyclodextrin (ß-CD) Inclusion Complex in Animal Inflammation Models.

Isopulegol (ISO) is an alcoholic monoterpene widely found in different plant species, such as Melissa officinalis, and has already been reported to have a number of pharmacological properties. Like other terpenes, ISO is a highly volatile compound that is slightly soluble in water, so its inclusion into cyclodextrins (CDs) is an interesting approach to increase its solubility and bioavailability. Thus, our aim was to evaluate the antiedematogenic and anti-inflammatory activity of isopulegol and a ß-cyclodextrin-isopulegol inclusion complex (ISO/ß-CD) in rodent models. For the anti-inflammatory activity evaluation, antiedematogenic plethysmometry and acute (peritonitis and pleurisy), as well as chronic (cotton pellet-induced granuloma) anti-inflammatory models, were used. The docking procedure is used to evaluate, analyze, and predict their binding mode of interaction with H1 and Cox-2 receptors. The animals (n = 6) were divided into groups: ISO and ISO/ß-CD, negative control (saline), and positive control (indomethacin and promethazine). ISO and ISO/ß-CD were able to reduce acute inflammatory activity by decreasing albumin extravasation, leukocyte migration, and MPO concentration, and reducing exudate levels of IL-1ß and TNF-α. ISO and ISO/ß-CD significantly inhibited edematogenic activity in carrageenan- and dextran-induced paw edema. Moreover, both significantly reduced chronic inflammatory processes, given the lower weight and protein concentration of granulomas in the foreign body granulomatous inflammation model. The results suggest that the inclusion of ISO in ß-cyclodextrins improves its pharmacological properties, with the histamine and prostaglandin pathways as probable mechanisms of inhibition, and also reinforces the anti-inflammatory profile of this terpene.

Evidence of insulin-dependent signalling mechanisms produced by Citrus sinensis (L.) Osbeck fruit peel in an insulin resistant diabetic animal model.

Citrus sinensis (L.) Osbeck is extensively cultivated worldwide and one of the most consumed fruits in the world. We evaluated the therapeutic properties of the methanol extract from Citrus sinensis fruit peel (CSMe) in high-fat diet-fed streptozotocin-induced insulin-resistant diabetic rats. Body weight, food intake, and water consumption were analysed. Biochemical and molecular biologic indices, and the expression of insulin receptor-induced signalling molecules were assessed to identify possible mechanisms. In addition, we conducted histology of pancreatic and adipose tissues. UHPLC-MS/MS analysis showed the presence of 17 dietary phenolics at substantial concentrations. High-fat diet-fed streptozotocin-induced diabetic rats administered CSMe (50 and 100 mg/kg) had reduced fasting blood glucose (56.1% and 55.7%, respectively) and plasma insulin levels (22.9% and 32.7%, respectively) compared with untreated diabetic control rats. CSMe reversed the biochemical abnormalities in diabetic rats, showed cytoprotective activity, and increased the intensity of the positive immunoreactions for insulin in pancreatic islets. CSMe treatment increased the expression of PPARγ in the adipose tissue and signalling molecules GLUT4 and insulin receptor. Our data suggest that CSMe could optimize glucose uptake of adipose tissues through the insulin-dependent signalling cascade mechanism and it should be investigated in the management of individuals with type 2 diabetes mellitus.

Perfil Epidemiológico de Usuários de um Centro de Atenção Psicossocial em Pernambuco, Brasil / Epidemiological Profile of a Psychosocial Care Center's Users in Pernambuco, Brazil

Para garantir a ressocialização e a cidadania de pacientes, com doenças psíquicas, é preciso conhecê-los em seu contexto familiar, social e comunitário e, assim, traçar uma rede de atenção que assista às suas necessidades. A presente pesquisa teve por objetivo identificar o perfil epidemiológico dos usuários de um C entro de Atenção Psicossocial CAPS I, em Exu, Pernambuco, Brasil. Os dados foram coletados de formulários sociais, epidemiológicos e clínicos disponíveis no serviço. As informações colhidas foram analisadas se utilizando o pacote estatístico SPSS versão 21.0 e os dados foram apresentados, por meio de gráficos e tabelas de frequências simples absolutas e relativas, com variáveis sociais e epidemiológicas e clínicas. Houve entre 35,6% dos pacientes com internações psiquiátricas antes da adesão ao serviço oferecido no CAPS, ocorrendo após o início do tratamento uma significativa redução (89,8%) nos casos de reinternação. A maioria (64,4%) dos pacientes possui antecedentes familiares com diagnóstico positivo. A patologia prevalente, tanto na hipótese diagnóstica (13,6%), quanto no diagnóstico atual (11,9%) foi F 20 - Esquizofrenia. O total de 79,7% dos pacientes permanece ativo no serviço e 64,4% sob modalidade semi-intensiva. As variáveis clínicas indicam a importância do tratamento na melhoria das condições clínicas dos usuários. A característica de antecedentes familiares indica a hereditariedade dos distúrbios mentais. Apesar da lacuna nas informações, constatou-se a Esquizofrenia e suas formas como doença mais prevalente. As informações dos prontuários precisam ser anotadas, valorizadas e utilizadas para traçar o plano terapêutico mais apropriado para cada indivíduo. (AU)

To ensure the rehabilitation and citizenship of patients with mental illness, it is necessary to know them in their family, social and community context, and thus define a care network to assist their needs. This study aimed to identify the Users' epidemiological profile of the Psychosocial Care Center (PCC) in Exú, Pernambuco, Brazil. Data were collected through socio-demographic and clinical forms available on the service. The information collected was analyzed using the statistical package SPSS version 21.0, and the data were presented through graphs and tables of simple absolute and relative frequencies, with socio-epidemiological and clinical variables. There was between 35.6% of psychiatric hospitalizations before subscribing to the service offered in PCC, occurring after the beginning of the treatment a significant reduction (89.8%) in cases of readmission. The majority (64.4%) of the patients had a family history with a positive diagnosis. The prevalent pathology in diagnostic hypothesis (13.6%) and the current diagnosis (11.9%) was F 20 - Schizophrenia. The total of 79.7% of patients remain active in service and 64.4% under semi-intensive mode. The clinical variables indicate the importance of treatment in improving the users' clinical conditions. The characteristic of family history indicates the inheritance of mental disorders. Despite the gaps in information, it was found Schizophrenia and their forms the most prevalent disease. The information from medical records need to be valued and used to define the most appropriate treatment plan for each user. (AU)

Gastroprotective and ulcer healing effects of hydroethanolic extract of leaves of Caryocar coriaceum: Mechanisms involved in the gastroprotective activity.

This work aimed to determine the chemical fingerprint of hydroethanolic extract of leaves of Caryocar coriaceum (HELCC) and the gastroprotective activity. The chemical fingerprint of HELCC was analyzed by HPLC-DAD, to quantify total phenols and flavonoids were carried out by Folin-Ciocalteu reagent and aluminum chloride assay, while in vitro antioxidant activity was evaluated by the DPPH method. The methods used to determine pharmacological activity were: gastroprotective screening test in classical models of induced acute and chronic gastric lesions and physical barrier test. Further assays were performed to demonstrate the involvement of NO, prostaglandins, ATP-dependent potassium channels, TRPV, noradrenergic α2 receptors, histamines, and opioids. The DPPH method demonstrated the antioxidant activity of the extract, in vitro, explained by the presence of polyphenols and flavonoids. Oral administration of the extract, previously dissolved in deionized water, at a dose of 100 mg/kg decreased the lesions induced by indomethacin, acidified ethanol, ethanol and acetic acid by 75.0, 72.8, 69.4 and 86.2% respectively. It was demonstrated that opioid receptors, α2-adrenergic receptors and primary afferent neurons sensitive to capsaicin were involved in the mechanism of gastric protection, in addition to the contribution of NO and prostaglandins. The results show that extract is a promising candidate for the treatment of gastric ulcers.

Uso etnofarmacológico de plantas medicinais em infecções geniturinárias por moradoras da Chapada do Araripe, Crato, Ceará - Brasil / Ethnopharmacological usage of medicinal plants in genitourinary infections by residents of Chapada do Araripe, Crato, Ceará - Brazil

Objective: To determine the ethnopharmacological use of plants in the treatment of urogenital tract infections (UTIs) by women living in the city of Crato, located in Chapada do Araripe, in the interior of the State of Ceará, Brazil. Methods: A cross-sectional study, with a quantitative approach, performed from September to November, 2010, with 25 residents of Chapada do Araripe, who use and/or recommend plants for the treatment of UTIs. Results: The prevalent characteristics of the informants were: age-group between 56 and 60 years old, married, all of them farmers with a monthly income of minimum wage, and most of them with incomplete schooling. Nine plant species were identified as being used by the population against infection, inflammation and pain. The most common forms of usage are the decoction, cooking and the maceration of leaves and barks. Barbatimão and mallow were the most reported species by informants. Conclusion: Popular medicine is greatly adopted by traditional communities and represents an incalculable cultural wealth which should be preserved and evaluated to assure sustainable development. Information brought out by this research may be useful in further pharmacological studies.

Objetivo: Conhecer o uso etnofarmacológico de plantas no tratamento de infecções do trato geniturinário (ITU) por mulheres residentes no município de Crato, na Chapada do Araripe, no interior do Estado do Ceará, Brasil. Métodos: Estudo transversal com abordagem quantitativa, realizado entre setembro e novembro de 2010, com 25 moradoras da Chapada do Araripe que utilizam e/ou recomendam plantas para o tratamento de ITU. Resultados: As características prevalentes das informantes foram: faixa etária de 56 a 60 anos, casadas e com renda mensal de um salário mínimo, todas agricultoras e a maior parte delas com ensino fundamental incompleto. Foram identificadas nove espécies vegetais empregadas pela população contra processos infecciosos, inflamatórios e álgicos. As principais formas de uso são o decocto, o cozimento e a maceração de folhas e cascas. Barbatimão e malva foram as espécies mais citadas pelas informantes. Conclusão: A medicina popular é amplamente adotada por comunidades tradicionais e representa uma riqueza cultural inestimável que deve ser preservada e valorizada para garantia do desenvolvimento sustentável. As informações levantadas nesta pesquisa podem ser aplicadas em futuros estudos farmacológicos.