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ETHNOPHARMACOLOGICAL RELEVANCE: Plant vernacular names can provide clues about the popular use of a species in different regions and are valuable sources of information about the culture or vocabulary of a population. Several medicinal plants in Brazil have received names of medicines and brand-name products. AIM OF THE STUDY: The present work aimed to evaluate the chemical composition and pharmacological activity in the central nervous system of three species known popularly by brand names of analgesic, anti-inflammatory, antispasmodic, and digestive drugs. MATERIALS AND METHODS: Hydroethanolic extracts of Alternanthera dentata (AD), Ocimum carnosum (OC), and Plectranthus barbatus (PB) aerial parts were submitted to phytochemical analysis by HPLC-PAD-ESI-MS/MS and evaluated in animal models at doses of 500 and 1000 mg/kg. Mice were tested on hot plate, acetic acid-induced writing, formalin-induced licking, and intestinal transit tests. Aspirin and morphine were employed as standard drugs. RESULTS: The three extracts did not change the mice's response on the hot plate. Hydroethanolic extracts of AD and PB reduced the number of writhes and licking time, while OC was only effective on the licking test at dose of 1000 mg/kg. In addition, AD and OC reduced intestinal transit, while PB increased gut motility. CONCLUSIONS: Pharmacological tests supported some popular uses, suggesting peripheral antinociceptive and anti-inflammatory effects, while the phytochemical analysis showed the presence of several flavonoids in the three hydroethanolic extracts and steroids in PB, with some barbatusterol derivatives described for the first time in the species.
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Amaranthaceae , Analgésicos , Anti-Inflamatórios , Parassimpatolíticos , Compostos Fitoquímicos , Componentes Aéreos da Planta , Extratos Vegetais , Plectranthus , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Analgésicos/farmacologia , Analgésicos/química , Camundongos , Parassimpatolíticos/farmacologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Masculino , Amaranthaceae/química , Plectranthus/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Dor/tratamento farmacológico , Ocimum/química , Espectrometria de Massas em Tandem , Brasil , Trânsito Gastrointestinal/efeitos dos fármacosRESUMO
Introduction: The use of medical Cannabis remains unregulated in several countries due to the scarcity of clinical studies with high scientific evidence that establish safety and efficacy of Cannabis products. This study aimed to comprehensively analyze how knowledge has been created in this field, as well as perform a bibliographic mapping to identify knowledge gaps, and investigate key authors and journals that have significantly contributed to advancing our understanding of Cannabis. Method: The study protocol was registered in the International Prospective Register of Systematic Review (CRD42020223084). A systematic search was conducted in the Cochrane Central Register of Controlled Trials, Lilacs, Google Scholar, PubMed, SciELO, Scopus, and Web of Science databases. The bibliographic analysis and mapping were registered using the VOSviewer, Sci2tool, CiteSpace, and PoP software. Results: The systematic search identified 27,597 records, with 17,020 duplicates, resulting in a total of 10,577 articles included. The authors who published the most were Marilyn Ann Huestis (n=108) and Sagnik Bhattacharyya (n=71), while Elisaldo A. Carlini and Raphael Mechoulam published 8 and 22 articles, respectively. The journals Drug and Alcohol Dependence (n=297), Psychopharmacology (n=159) and Addictive Behaviors (n=150) were the ones that published the most on Cannabis. The journals suggest that the articles are correlated with the adverse and toxicological effects of recreational Cannabis use; however, most articles focus on medical Cannabis. The peak of publications was in 2021 (n=1,481). The countries that published the most were the United States (n=9,735), while Brazil occupied the 11th position (n=422). Most publications were carried out in "Pharmacology and Pharmacy" (11.31%), followed by "Psychiatry" (7.66%) and "Medicine" (5.80%). The areas of "Neurosciences" (1.59%), "Biochemistry," "Genetics," and "Molecular Biology" (0.79%) were little explored. Conclusion: This study captured the characteristics of publications about Cannabis and clinical studies in the scientific literature, yielding >10,000 articles, representing a large literature review, to date. Therefore, the most productive countries included the United States, the United Kingdom, and Canada, while the most productive authors were Marilyn Ann Huestis and Sagnik Bhattacharyya, with a peak of publications in 2021. Finally, the most chosen journals were Drug and Alcohol Dependence and Psychopharmacology.
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Bibliometria , Cannabis , Maconha Medicinal , Humanos , Maconha Medicinal/uso terapêuticoRESUMO
Brazilian Red Propolis is a resinous material produced by Apis mellifera bees through the collection of the exudates of Dalbergia ecastaphyllum, rich in flavonoids, and Symphonia globulifera and Clusia species, which are rich in polyprenylated benzophenones. More than 200 compounds, including flavonoids and polyprenylated benzophenones have been found in Brazilian red propolis. The objective of the present study was to evaluate the chemical composition and antiviral activity of an ethanolic extract of red propolis from Alagoas, Brazil, against Herpes Simplex Virus (HSV-1). In the HPLC-PDA-ESI-MS/MS analysis were detected flavanones, isoflavones, chalcones, pterocarpans and polyprenylated benzophenones. The measurement of antiviral activity of red propolis extract was performed by DNA quantification through quantitative real-time PCR assay and negative staining Electron Microscopy. The pretreatment, post-treatment, and virucide assays using ethanolic extract of red propolis with concentration of 8, 12, 24, 48, or 96 µg/mL, indicated an inhibition of the viral binding and viral entry into cells as well as the replication of HSV-1. In the electron microscopy imaging was observed the disruption of the viral membrane in the HSV-1 treated with red propolis, when compared with HSV-1 that was treated with phosphate buffered saline alone, indicating that ethanolic extract from red propolis can act directly on the viral envelope, through lipid membrane degradation and/or directly blocking the enriched proteins on the viral surface.
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Background: With the expansion of the cannabis-derived product market, there is a growing need for seedling development to produce raw material for pharmaceutical applications and medicinal research. However, cannabis cultivation is illegal in many countries, and legal producers do not sell cannabis seeds in these countries. In Brazil, cannabis is still illegal, and the only way to obtain access to cannabis plants for research or as medicine is through importation, which is costly and requires authorization from the National Health Surveillance Agency (ANVISA), or from material seized by the police from drug trafficking. Methods: Therefore, since cannabis seeds obtained from drug trafficking have never been tested regarding their viability and use in in vitro cultivation, the aim of this study was to analyze the in vitro establishment of cannabis from seeds derived from Brazilian drug trafficking seizures that were provided by the police to investigate seed disinfestation procedures and further multiplication of nodal segments, with the purpose of obtaining material for medicinal research in the country. Seeds were subjected to four disinfestation treatments. Results: The best disinfestation treatment consisted in submerging the seeds in a 2 g·L-1 Captan® solution for 30 min before following the standard procedure with 70% ethanol for 30 sec and then 20 min in 2.5% sodium hypochlorite. The in vitro establishment of cannabis from seeds originating from Brazilian drug trafficking seizures was successful. The germination rate ranged from 10% to 90% according to the sample material. Non-brick weed, which consisted of dry leaves, stalks, and flowers, was more suitable for seed extraction and germination. Clones originating from BW4b showed the best development results compared with others. Conclusions: This is the first report of in vitro cannabis use in Brazil and opens great prospects for future work on its cultivation and research for medicinal applications in the country without relying on seed importation.
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The indiscriminate use of pesticides is a worldwide concern due to the environment contamination since it can cause deleterious effects to non-target organisms including the fishes. The effects of abamectin, a pesticide from the avermectin family, were evaluated in adult zebrafish (Danio rerio) after exposure to a commercial formula commonly used in Brazil. The animals were submitted to acute (96 h) and to a short-term chronic exposure (15 days) of distinct concentrations of abamectin. LC50 was determined and a histological study followed by an immunohistochemistry analysis for P-gp and HSP70 identification were performed on livers of the animals submitted to the acute and chronic treatment, respectively. Moreover, behavior patterns were observed daily in both trials. A LC50 value of 105.68 µg/L was determined. The histological analysis revealed a morphological alteration of the hepatocytes, glycogen accumulation, degeneration, and disorganization of the cytoplasm, and a pyknotic, irregular, and laterally located nuclei. The immunohistochemistry for HSP70 and P-gp showed strong staining in the hepatocytes of the control groups and progressive decrease as the concentration of abamectin increased. Changes were observed in body posture, movement around the aquarium, opercular activity, body color and search for food in the groups treated with abamectin. The results presented suggest that abamectin can affect the behavioral pattern of the animals, promote morphological changes, and decrease the expression of HSP70 and P-gp in zebrafish liver.
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Praguicidas , Peixe-Zebra , Animais , Poluição Ambiental , FígadoRESUMO
Abstract Guarana (Paullinia cupana) is a native plant from the Amazon whose seeds contain a high concentration of caffeine. Aqueous extract of guarana is widely used in the world. In this study, the objective was to develop and validate a High-Performance Liquid Chromatography method for the determination of caffeine in extracts and commercial beverages based on guarana. A sensitive, simple, and viable high performance liquid chromatographic method without the need of an analyte extraction procedure was developed and validated according to Brazilian and international requirements. The method presented high performance, fulfilling Brazilian and international requirements, in addition to allowing product compliance tests. Results confirmed high selectivity and linearity (>0.999) between 5 to 135 ug/mL, with no significant matrix effect. Detection and quantification limits were 0.02 µg/mL and 2 µg/mL, respectively. Precision was less than 4 %, and accuracy varied from 99.9-120 %. Applicability of the method was demonstrated by conducting a limited evaluation in products containing caffeine. Commercial extracts showed quite different caffeine levels, while carbonated drinks follow Brazilian and American recommendations. Our results indicate that the developed method can be used to evaluate the quality of the guarana extract and of products containing caffeine
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Sementes/classificação , Cafeína/agonistas , Extratos Vegetais/análise , Cromatografia Líquida de Alta Pressão/métodos , Paullinia/efeitos adversos , Plantas/classificação , Bebidas/classificação , Gestão da Qualidade Total/normasRESUMO
Hibiscus sabdariffa extract (HSE) and Syzygium cumini extract (SCE) have been used in traditional medicine due to their hypoglycemic, antidiabetic, anti-obesity and antioxidant activities. This study aimed to evaluate the anti-obesity effects of these extracts, as well as to evaluate their toxicities. The phytochemical profiles were obtained by HPLC-DAD-ESI-MS/MS analyses. Pharmacological screening, motor activity, motor coordination and acute toxicity were evaluated by administering HSE or SCE (oral or intraperitoneal routes) at different doses to mice. The anti-obesity effects were examined by assessing the decrease in food intake and body weight loss in Wistar albino rats and by gastrointestinal transit in Swiss albino mice. Sibutramine was used as the positive control. Both extracts showed no toxic effects. At the end of 7 days of treatment, we observed that SCE and HSE reduced the weight gain and food intake of the treated rats in relation to the controls. Sub-chronic treatment revealed that HSE, SCE and sibutramine had the best effect 7 and 14 days after starting treatment. After 28 days, the SCE group showed less weight gain and reduced food consumption compared to the HSE group and controls. In addition, intestinal transit was increased in the HSE group, which is probably due to the high fiber content of the extract and may explain its anti-obesity properties. Myricetin glycosides were found in high levels in SCE and low levels in HSE, which may be the main compounds associated with the anti-obesity effect found in SCE. It is not possible to suggest an effective dose without conducting a preclinical toxicology study. We recommend clinical studies that evaluate the efficacy and safety, as well as the effect of discontinuing the extracts.
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Antioxidantes/farmacologia , Hibiscus , Extratos Vegetais/farmacologia , Syzygium , Animais , Antioxidantes/química , Antioxidantes/uso terapêutico , Modelos Animais de Doenças , Masculino , Medicina Tradicional , Camundongos , Obesidade/prevenção & controle , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Espectrometria de Massas em Tandem , Aumento de Peso/efeitos dos fármacosRESUMO
Midazolam (MDZ) is routinely employed as a marker compound of cytochrome P450 3A (CYP3A) activity. Despite the many HPLC-UV methods described to quantify MDZ in plasma, all of them use acetonitrile (ACN) or a mixture of methanol-isopropanol as organic solvent of the mobile phase. Since the ACN shortage in 2008, efforts have been made to replace this solvent during HPLC analysis. A simple, sensitive, accurate and repeatable HPLC-UV method (220 nm) was developed and validated to quantify MDZ in rat plasma using methanol instead. The method was applied during a herb-drug interaction study involving Maytenus ilicifolia, a Brazilian folk medicine used to treat gastric disorders. Plasma samples were alkalinized and MDZ plus alprazolam (internal standard) were extracted with diethyl ether. After solvent removal, the residue was reconstituted with methanol-water (1:1). The analyte was eluted throughout a C18 column using sodium acetate buffer (10 mm, pH 7.4)-methanol (40:60, v/v). The precision at the lower limit of quantification never exceeded 19.40%, and 13.86% at the higher levels of quality control standards, whereas the accuracy ranged from -19.81 to 14.33%. The analytical curve was linear from 50 to 2,000 ng/ml. The activity of the hepatic CYP3A enzymes was not affected by the extract.
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Cromatografia Líquida de Alta Pressão/métodos , Interações Ervas-Drogas , Maytenus/química , Midazolam/sangue , Animais , Citocromo P-450 CYP3A/metabolismo , Modelos Lineares , Masculino , Metanol , Midazolam/administração & dosagem , Midazolam/farmacocinética , Preparações de Plantas/administração & dosagem , Preparações de Plantas/sangue , Preparações de Plantas/farmacocinética , Ratos , Ratos Wistar , Reprodutibilidade dos Testes , Sensibilidade e EspecificidadeRESUMO
There are several studies investigating the effects of risperidone on autism, but many of these studies are contradictory or inconclusive. This systematic review and meta-analysis investigated the effects of risperidone on five domains of the Aberrant Behaviour Checklist (ABC) scale on Autism Spectrum Disorder (ASD), as well as weight gain and waist circumference. The protocol for the present systematic review and meta-analysis was registered on the International Prospective Register of Systematic Reviews (PROSPERO). For this study, we analysed articles (2,459), selecting them according to the PICOS strategy (Population, Intervention, Comparison, Outcome, Study design). Although risperidone is effective for the treatment of lethargy and inadequate speech, concerns about the association between weight gain, waist circumference and risperidone require a need for evaluation of the risk-benefit ratio in its use. There was a significant association between weight gain, waist circumference and risperidone. In conclusion, it was possible to suggest the efficacy of risperidone for the treatment of lethargy and inadequate speech. Finally, we emphasize that the risk-benefit in its use should be evaluated (Protocol number CRD42019122316).
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Transtorno Autístico , Adolescente , Antipsicóticos/efeitos adversos , Transtorno Autístico/tratamento farmacológico , Criança , Feminino , Humanos , Masculino , Risperidona/efeitos adversos , Resultado do Tratamento , Aumento de Peso/efeitos dos fármacos , Adulto JovemRESUMO
Cannabis sativa is the drug of abuse most cultivated, trafficked, and consumed worldwide. One of several techniques used to detect cannabinoids is based on the thin-layer chromatography (TLC). However, the designation of the colors observed can be inaccurate and not reproducible. The designation of colors goes beyond physical and physiological aspects, because what is conventionally called color is a socio-cultural construction. Thus, the objective of this paper was to evaluate the different TLC methods to detection of cannabinoids, and apply standardization method in naming of colors. TLC analysis performed using silica gel 60 F254 as a stationary phase. Three mobile phase compositions [hexane:chloroform (8:2 v:v), hexane:ethyl ether (8:2 v:v), and chloroform:hexane (8:2 v:v)], as well as, two different solutions of Fast Blue B salt (FBBS, Azoic Diazo No. 48) and Fast Blue RR (FBRR, Azoic Diazo No. 24) were evaluated. Determination of colors names was realized through the Sci-Chromus® software. The best resolution was obtained using hexane:ethyl ether (8:2 v:v) as a mobile phase. It was observed that although the cannabidiol (CBD), delta-9-tetrahydrocannabinol (Δ9 -THC), cannabinol (CBN), and cannabigerol (CBG) were detect using both the FBBS- and FBRR-acidified solutions, the best visualization was achieved using the latter reagent. To the best of our knowledge, this is the first study that applied and demonstrated a method for standardization and denomination of colors in the TLC analysis of cannabinoids. This method was able to reduce the subjectivity in naming the colors observed and presented several application possibilities.