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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
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 development of simple, efficient, and low-cost analytical methods is essential for the evaluation and monitoring of the main cannabinoids in Cannabis-based products. In this sense, the objectives of this study were to develop and validate an analytical method for obtaining and determining cannabinoids in a pool sample. Two extraction techniques were used, ultrasound and turbo-extraction, and two system-solvents, methanol:chloroform (9:1 v:v) and ethanol. The analytical method used and validated was carried out in High Performance Liquid Chromatography with Diodes Array Detector. The cannabidiol standard was characterized by a nuclear magnetic resonance. The use of the proposed method makes it possible to identify cannabinoids, both in the acid form and in the neutral form, in 7 min of analysis. The results confirmed high precision and accuracy. The detection and quantification limits were 0.19 µg/mL and 5 µg/mL, respectively. The method developed proved to be selective and robust for the evaluation of cannabinoids. It is hoped that the methods developed can be used to obtain and analyze cannabinoids, both for medicinal purposes and for forensic analysis.
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Canabidiol , Canabinoides , Cannabis , Alucinógenos , Canabinoides/análise , Cannabis/química , Canabidiol/análise , Cromatografia Líquida de Alta Pressão/métodosRESUMO
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.
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Canabinoides/análise , Cromatografia em Camada Fina , Cor , Clorofórmio , Compostos de Diazônio , Éter , Hexanos , HumanosRESUMO
BACKGROUND: Maytenus ilicifolia is a Brazilian popular medicine commonly used to treat ulcer and gastritis. Despite the absence of toxicity regarding its consumption, possible interactions when co-administrated with conventional drugs, are unknown. OBJECTIVE: This study aimed to evaluate the effects of M. ilicifolia extracts on Cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp) activities. METHODS: The extracts were obtained by infusion (MI) or turbo-extraction using hydro-acetonic solvent (MT70). The content of polyphenols in each extract was determined. To assess the modulation of M. ilicifolia on P-gp activity, the uptake of fexofenadine (FEX) by Caco-2 cells was investigated in the absence or presence of MI or MT70. The effect on CYP3A activity was evaluated by the co-administration of midazolam (MDZ) with each extract in male Wistar rats. The pharmacokinetic parameters of the drug were determined and compared with those from the control group. The content of total phenolic compounds, tannins, and flavonoids on MT70 extract was about double of that found in MI. RESULTS: In the presence of the extracts, the uptake of the P-gp marker (FEX) by Caco-2 cells increased from 1.7 ± 0.4 ng.mg-1 protein (control) to 3.5 ± 0.2 ng.mg-1 protein (MI) and 4.4 ± 0.5 ng.mg-1 protein (MT70), respectively. When orally co-administrated with MDZ (substrate of CYP3A), the extracts augmented the AUC(0-∞) (Control: 911.7 ± 215.7 ng.h.mL-1; MI: 1947 ± 554.3 ng.h.mL-1; MT70: 2219.0 ± 506.3 ng.h.mL-1) and the Cmax (Control: 407.7 ± 90.4 ng.mL-1; MI: 1770.5 ± 764.5 ng.mL-1; MT70: 1987.2 ± 544.9 ng.mL-1) of the drug in rats indicating a 50% reduction of the oral Cl. No effect was observed when midazolam was given intravenously. CONCLUSION: The results suggest that M. ilicifolia can inhibit the intestinal metabolism and transport of drugs mediated by CYP3A and P-gp, respectively, however, the involvement of other transporters and the clinical relevance of such interaction still need to be clarified.
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Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Citocromo P-450 CYP3A/metabolismo , Maytenus/química , Extratos Vegetais/farmacologia , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/agonistas , Animais , Células CACO-2 , Linhagem Celular , Inibidores do Citocromo P-450 CYP3A/farmacologia , Interações Medicamentosas , Humanos , Cetoconazol/farmacologia , Masculino , Midazolam/farmacocinética , Quinolinas/farmacologia , Ratos , Ratos Wistar , Terfenadina/análogos & derivadosRESUMO
Ethanol extract and fractions obtained from fresh and dry aerial parts of Lippia alba were examined in order to determine their phytochemical composition, antioxidant capacity and antibacterial activities. The ethanol extracts and fractions exhibited an antioxidant effect by the DPPH assay, especially samples of fresh plant. HPLC analysis of the ethyl acetate fractions identified the presence of phenolic acids and flavonoids. The ethanol extract and fractions showed activity against reference and multidrug-resistant strains of Staphylococcus aureus and Enterococcus faecalis (MIC range 2000-250 µg/mL). The hexane and dichloromethane fractions of fresh plant showed better activity against reference strains of Escherichia coli (MIC of 250 and 125 µg/mL, respectively), but all extracts and fractions were less active against multidrug-resistant strains of all the Gram-negative species evaluated. The results showed that the extract and fractions of L alba aerial parts showed antibacterial activity, even against multidrug-resistant Gram-positive bacteria, and antioxidant effect (DPPH assay).
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Antibacterianos/farmacologia , Antioxidantes/farmacologia , Lippia/química , Antibacterianos/química , Antioxidantes/química , Cromatografia Líquida de Alta Pressão , Avaliação Pré-Clínica de Medicamentos , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Enterococcus faecalis/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Escherichia coli/isolamento & purificação , Flavonoides/análise , Flavonoides/farmacologia , Testes de Sensibilidade Microbiana , Fenóis/análise , Fenóis/farmacologia , Componentes Aéreos da Planta/química , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacosRESUMO
OBJECTIVE: To evaluate the phytochemical composition of hydroethanolic extracts from powdered aerial parts of Turnera diffusa Willd (Turneraceae; T. diffusa), as well as its toxicity in astrocytes. METHODS: Chemical analyses of hydroethanolic extract from powdered aerial parts ofT. diffusa were carried out using HPLC-DAD-ESI-MS/MS.In vitro assays using astrocytes culture were performed to evaluate cell death. RESULTS: Flavone-C, O-diglycosides, such as, luteolin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside, apigenin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside and apigenin-7-O-6"-p-coumaroylglucoside were the main compounds found in this hydroethanolic extract. Concentration time-effect demonstrated the toxicity of this extract at a concentration of 1,000µg/mL in astrocyte culture, after 6 and 24 hours of incubation. CONCLUSION: In phytochemical analyses, important antioxidants (mainly flavonoids) were observed. T. diffusa extracts presented cytotoxic effect in high concentrations, leading to increased cell death in astrocyte culture.
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Antioxidantes/química , Astrócitos/efeitos dos fármacos , Extratos Vegetais/química , Turnera/química , Animais , Astrócitos/química , Morte Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão/métodos , Flavonas/análise , Flavonas/toxicidade , Extratos Vegetais/toxicidade , Ratos , Espectrometria de Massas por Ionização por Electrospray/métodosRESUMO
ABSTRACT Objective To evaluate the phytochemical composition of hydroethanolic extracts from powdered aerial parts of Turnera diffusa Willd (Turneraceae; T. diffusa), as well as its toxicity in astrocytes. Methods Chemical analyses of hydroethanolic extract from powdered aerial parts ofT. diffusa were carried out using HPLC-DAD-ESI-MS/MS.In vitro assays using astrocytes culture were performed to evaluate cell death. Results Flavone-C, O-diglycosides, such as, luteolin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside, apigenin-8-C-[6-deoxy-2-O-rhamnosyl]-xylo-hexos-3-uloside and apigenin-7-O-6”-p-coumaroylglucoside were the main compounds found in this hydroethanolic extract. Concentration time-effect demonstrated the toxicity of this extract at a concentration of 1,000µg/mL in astrocyte culture, after 6 and 24 hours of incubation. Conclusion In phytochemical analyses, important antioxidants (mainly flavonoids) were observed. T. diffusa extracts presented cytotoxic effect in high concentrations, leading to increased cell death in astrocyte culture.
RESUMO Objetivo Avaliar a composição fitoquímica do extrato hidroetanólico das partes aéreas de Turnera diffusa Willd (Turneraceae; T. diffusa) e sua toxicidade em astrócitos. Métodos Análises químicas do extrato hidroetanólico de partes aéreas de T. diffusa foram feitas por HPLC-DAD-ESI-MS/MS. Os ensaiosin vitro utilizaram culturas de astrócitos para avaliar morte celular. Resultados Flavonas-C, O-diglicosídeos, como, luteolina-8-C-[6-deoxi-2-O-raminosil]-xilo-hexos-3-ulosideo, apigenina-8-C-[6-deoxi-2-O-raminosil]-xilo-hexos-3-ulosideo e apigenina-7-O-6”-p-cumaroilglucosídeo foram os principais constituintes encontrados neste extrato hidroetanólico. Uma curva tempo-concentração demonstrou toxicidade desse extrato na concentração de 1.000µg/mL, na cultura de astrócitos após 6 e 24 horas de incubação. Conclusão Nas análises fitoquímicas, importantes antioxidantes, sobretudo flavonoides, foram observados. Extratos de T. diffusa apresentaram efeitos citotóxicos em altas concentrações, ocasionando aumento de morte celular em cultura de astrócitos.
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Animais , Ratos , Extratos Vegetais/química , Astrócitos/efeitos dos fármacos , Turnera/química , Antioxidantes/química , Extratos Vegetais/toxicidade , Astrócitos/química , Cromatografia Líquida de Alta Pressão/métodos , Morte Celular/efeitos dos fármacos , Espectrometria de Massas por Ionização por Electrospray/métodos , Flavonas/análise , Flavonas/toxicidadeRESUMO
Ethanol extract and fractions obtained from leaves of Solanum lycocarpum were examined in order to determine their phenolic composition, antioxidant, antibacterial, anti-inflammatory, and cytotoxic potential. High performance liquid chromatography coupled with DAD analysis indicated that the flavonoids apigenin and kaempferol were the main phenolic compounds present in dichloromethane and ethyl acetate fractions, respectively. The antioxidant activity was significantly more pronounced for dichloromethane, ethyl acetate, and hydroethanol fractions than that of the commercial antioxidant 2,6-di-tert-butyl-4-methylphenol. The hexane and dichloromethane fractions were more active against the tested bacteria. The hydroethanol fraction exhibited significant anti-inflammatory activity at the dose of 75 and 150 mg/kg in the later phase of inflammation. However, the antiedematogenic effect of the higher dose of the ethyl acetate fraction (150 mg/kg) was more pronounced. The ethyl acetate fraction also presented a less cytotoxic effect than the ethanol extract and other fractions. These activities found in S. lycocarpum leaves can be attributed, at least in part, to the presence of phenolic constituents such as flavonoids. This work provided the knowledge of phenolic composition in the extract and fractions and the antioxidant, antibacterial, anti-inflammatory, and cytotoxic activities of leaves of S. lycocarpum.
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Ethanol extract (EE) and fractions obtained from the ripe fruits of Solanum lycocarpum were examined in order to determine their phenolic composition, antioxidant capacity, antibacterial activities and cytotoxic potential. High-performance liquid chromatography coupled with DAD analysis indicated that caffeic and chlorogenic acids were the main phenolic compounds present in the EE, dichloromethane (DCM) and ethyl acetate (Ac) fractions. The antioxidant activity assessed by the scavenging ability on 1,1-diphenyl-2-picrylhydrazyl radical was significantly more pronounced for DCM and Ac fractions than that of the commercial antioxidant 2,6-di-tert-butyl-4-methylphenol (BHT). EE and fractions exhibited selective antibacterial activity against Gram-positive bacteria, especially the hexane (Hex) and DCM fractions. EE and fractions exhibited low toxicity towards the LLC-MK2 cell line, especially the Hex, DCM and Ac fractions. This work provides the knowledge of phenolic composition in the extract and fractions from the ripe fruits of S. lycocarpum and their antioxidant, antibacterial and cytotoxic activities.
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Antibacterianos/química , Antioxidantes/química , Frutas/química , Extratos Vegetais/química , Solanum/química , Animais , Ácidos Cafeicos/química , Linhagem Celular/efeitos dos fármacos , Ácido Clorogênico/química , Concentração Inibidora 50 , Macaca mulatta , Fenóis/químicaRESUMO
Ethanol extract and fractions obtained from aerial parts of Smilax campestris were examined in order to determine their phenolic composition, antioxidant capacity and antifungal activities. High-performance liquid chromatography coupled with DAD analysis indicated that quercetin and rutin were the main phenolic compounds present in butanol fraction and ethanol extract, respectively. The antioxidant activity assessed by the scavenging ability on 1,1-diphenyl-2-picrylhydrazyl radical was significantly more pronounced for the ethanol extract and butanol fraction than that of the commercial antioxidant 2,6-di-tert-butyl-4-methylphenol. The antifungal activity of extract and fractions was investigated by using microdilution method against five Candida and two Cryptococcus yeast strains. Ethanol extract and fractions exhibited antifungal activities against Candida albicans, Candida glabrata, Candida krusei, Candida parapsilosis, Candida tropicalis and Cryptococcus gattii. This work provides the knowledge of profile and content of flavonoids and their antioxidant and antifungal activities in the extract and fractions of aerial parts of S. campestris.
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Antifúngicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Smilax/química , Antifúngicos/química , Antifúngicos/farmacologia , Antioxidantes/química , Compostos de Bifenilo/farmacologia , Hidroxitolueno Butilado , Candida/efeitos dos fármacos , Cryptococcus/efeitos dos fármacos , Flavonoides/química , Sequestradores de Radicais Livres/química , Estrutura Molecular , Fenóis/farmacologia , Picratos/farmacologiaRESUMO
The present study aimed to assess the preclinical toxicity of two plants commonly used to treat "stomach ailments" in Brazil: Schinus terebinthifolius Raddi (S) and Myracrodruon urundeuva Allemão (M). In male rats, chronic treatment (83 days) with both pepper trees (17.6 and 13.8 mg/kg, S and M, respectively) has been shown to decrease hematocrit. However, a reduction in the number of red blood cells and hemoglobin was only seen following administration of S. terebinthifolius. None of the plants caused anatomopathological alterations following chronic treatment, and mating ability and fertility were not affected. Both pepper trees showed moderate toxicity following acute and chronic treatment by gavage, particularly S. terebinthifolius. Moreover, bone malformations were induced in fetuses, and a slight delay in recovery time of the postural reflex was observed in pups from female animals treated (18 days) with S. terebinthifolius. Given these results, a better assessment of the risks and benefits of the internal use of these plants is necessary, especially when used by women of childbearing age.
Assuntos
Anacardiaceae/toxicidade , Extratos Vegetais/toxicidade , Animais , Brasil , Eritrócitos/efeitos dos fármacos , Feminino , Fertilidade/efeitos dos fármacos , Feto/efeitos dos fármacos , Hematócrito , Hemoglobinas/análise , Masculino , Exposição Materna , Camundongos , Osteogênese/efeitos dos fármacos , Gravidez , Ratos , Testes de Toxicidade Subcrônica , Árvores/toxicidade , Aumento de PesoRESUMO
From sugarcane juice, a flavone, identified by spectroscopic methods as tricin-7-O-beta-(6''-methoxycinnamic)-glucoside, was isolated, in addition to orientin. The tricin derivative was shown to have antioxidant activity higher than Trolox by means of the DPPH assay and lower by the beta-carotene/linoleic acid system. It showed in vitro antiproliferative activity against several human cancer cell lines, with higher selectivity toward cells of the breast resistant NIC/ADR line.