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In this study, we investigated the influence of mixture design on the chemical profile of Eugenia unifloraleaves, evaluating the antioxidant and antimicrobial activities, the toxic and hemolytic potential, with the focus on the improvement of the polyphenol’s extraction for incorporation of the extract in semi-solid forms with antifungal action. The chemical analysis was evaluated by UV-Vis and HPLC. The antimicrobial, antioxidant, and hemolytic activities were monitored. The flavonoid content ranged from 2.63-7.98 %w/w and tannins from 5.42-18.29 %w/w. The extract consisted of gallic acid (0.09-1.29%; w/w), ellagic acid (0.09-0.37%; w/w), and myricitrin (0.18-1.20%; w/w). The most successful solvent system with the highest level of active extract was water: ethanol: propylene glycol. The extracts showed fungicidal properties (3.9 μg/mL), high antioxidant activity (IC50: 9.50 μg/mL), and low toxicity. These solvent mixtures can improve the in vitro bioactivities when compared to pure solvents and this result demonstrates the importance of mixture designs as useful tools for creating high-quality herbal products and elucidate the potential of E. unifloraglycolic extracts as active herbal pharmaceutical ingredients in topical delivery systems.

Croton blanchetianus Baill, commonly known as “marmeleiro”, is native to the Brazilian Caatinga is traditional used to treat joint pain and gastrointestinal disorders. The aim of the study was identify the chemical constituents by HPLC-DAD and determine the antioxidant activity of the spray-dried extract (SDE) aqueous (AqF) and ethyl acetate (EAF) fractions obtained from the leaves of C. blanchetianus; and to determine the acute (single dose, 2000 or 5000 mg/kg, p.o) and subacute (repeated dose, 250, 500 and 1000 mg/kg, p.o) toxicities, and genotoxicity (1000 and 2000 mg/kg, p.o) of the EAF in mice. In the acute oral toxicity assay the LD50 was determined as > 5000 mg/kg. In the subacute toxicity, changes in weight gain, food and water intake, hematological, organ coefficients, oxidative stress parameters were not observed; however, changes in transaminases and leukocyte infiltration in the liver were observed at the highest dose. The genotoxicity test showed that high concentrations of EAF were not genotoxic in micronucleus and comet assays. The enrichment process was confirmed by HPLC and five flavonoids were identified. Our results provide evidence that the EAF was safe to use, although a long-term dose of 1000 mg/kg in should be avoided.

This study investigated the phytochemical characteristics of the aerial parts of Acanthospermum hispidum, by chromatographic and spectrophotometric methods, and evaluated the antioxidant and antifungal activities of the crude extract and polyphenol-enriched fractions of the species. The phytochemical prospection showed the presence of polyphenols from the groups of hydroxycinnamic derivatives and flavonoids in the crude extract (CE) and fractions of the aerial parts of A. hispidum . In the chromatographic analysis, it was possible to observe that the fractionation process of the CE with hexane and ethyl acetate was efficient in enriching the fractions in phenolic compounds. This enrichment provided an increase in antioxidant activity by the DPPH and ABTS methods, in which it was observed a higher antioxidant activity for EAF in the DPPH test and higher activity against the ABTS radical by the fractions AqF and RAqF. The extract and fractions were effective against Candida non- Candida albicans strains, mainly against C. glabrata , C. parapsilosis and C. krusei , acting predominantly fungicidal. The results indicate that the aerial parts of A. hispidum can serve as a basis for the development of new antioxidant and antifungal products. Moreover, the fractionation process can contribute to increasing the biological potential of the species.

Aedes aegypti can transmit dengue, chikungunya, zika and yellow fever. Its control represents the main strategy for reducing the spreading of these diseases. In the present work, Plectranthus barbatus leaf saline extract (SE), decoction and infusion were studied for their effects on the survival of A. aegypti third instar larvae (L3), as well as for the presence of secondary metabolites, lectins, and trypsin inhibitors. The effects of SE (non-heated or heated) on digestive proteases, permeability of peritrophic membrane, morphophysiology, microbiota growth and melanogenesis of L3 are reported. SE killed L3 (LC50 of 0.48%, w/v), while decoction and infusion were not larvicides. HPLC analysis identified caffeic acid and flavonoids in SE, decoction, and infusion. SE also contained a ribose/galactose-binding lectin, trypsin inhibitor activities and polypeptides (34, 63 and 66 kDa) resistant to hydrolysis by L3 gut proteases. The incubation of SE with larval proteases did not alter lectin and trypsin inhibitor activities. Treatment of L3 with SE (at LC50) increased the permeability of peritrophic membrane and prevented the larvae from passing into the fourth instar. The morphology of larval midgut was not affected by SE, but the content of neutral polysaccharides in epithelial cells was reduced. SE stimulated in vitro the proliferation of L3 midgut microbiota and increased in vivo the production of melanin by larvae. The heating (100°C, 5 h) of SE increased lectin, trypsin inhibitor and larvicidal activities. In conclusion, SE larvicidal activity may be linked to the presence of lectin and trypsin inhibitor and involves the inhibition of digestive proteases, damage to larval midgut morphophysiology and induction of dysbiosis.

This study aims to determine a suitable artificial neural network (ANN) regression model for quantification of polyphenols from herbal matrices through thin-layer chromatography (TLC) images. Galli...

Annona muricata (soursop) is a native American plant and is well known for its leafy canopy and its fruits, widely consumed in South America and Southeast Asia. The objective of this work was to obtain Annona muricata leaf extracts and to evaluate their antioxidant activities, which were obtained by four different extraction methods: Soxhlet, maceration, ultrasound, and pressurized hot (subcritical) water. In order to assess and compare the extracts bioactivities, total polyphenol contents of the extracts were evaluated by the Folin-Ciocalteu method and the antioxidant activities were determined by DPPH and ABTS methods. High performance liquid chromatography was used to identify and quantify rutin, a special flavonoid, which was found to be the most representative component, for all extracts obtained. Rutin is known for its benefits has a potential natural antioxidant. Among all extraction methods investigated, extracts obtained by the Soxhlet method using ethanol as solvent showed a higher total polyphenol content, 2.83% of gallic acid equivalent/g plant material, as well as higher antioxidant activity. A correlation between rutin content and antioxidant activity was found. Soxhlet extractions revealed samples with the highest rutin content of 0.130 ± 0.003 g g-1, what may explain the high antioxidant activity of the obtained A. muricata leaf extracts. Annona muricata (soursop) is a native American plant and is well known for its leafy canopy and its fruits, widely consumed in South America and Southeast Asia. The objective of this work was to obtain Annona muricata leaf extracts and to evaluate their antioxidant activities, which were obtained by four different extraction methods: Soxhlet, maceration, ultrasound, and pressurized hot (subcritical) water. In order to assess and compare the extracts bioactivities, total polyphenol contents of the extracts were evaluated by the Folin-Ciocalteu method and the antioxidant activities were determined by DPPH and ABTS methods. High performance liquid chromatography was used to identify and quantify rutin, a special flavonoid, which was found to be the most representative component, for all extracts obtained. Rutin is known for its benefits has a potential natural antioxidant. Among all extraction methods investigated, extracts obtained by the Soxhlet method using ethanol as solvent showed a higher total polyphenol content, 2.83% of gallic acid equivalent/g plant material, as well as higher antioxidant activity. A correlation between rutin content and antioxidant activity was found. Soxhlet extractions revealed samples with the highest rutin content of 0.130 ± 0.003 g g-1, what may explain the high antioxidant activity of the obtained A. muricata leaf extracts.

Eugenia uniflora Linn (Myrtaceae) is the native species of Brazil. The leaves of this species are used in folk medicine to treat different inflammatory and gastrointestinal disorders. However, research on the safety of using E. uniflora leaves has been poorly explored.This approach aims to investigate the phytochemical composition as well as the acute, subacute toxicity, and in vivo genotoxic profile of the aqueous extract of E. uniflora leaves.The chemical composition of E. uniflora leaf extract was determined by Fingerprint by High-Performance Thin Layer and High-Performance Liquid Chromatography. The acute toxicity in vivo was evaluated for 14 days after the administration of E. uniflora leaves extract (2000 mg/kg). For the evaluation of subacute toxicity, mice were daily treated for 28 days with E. uniflora extract (250, 500, or 1000 mg/kg). Signs of behavioral toxicity and biochemical and hematological alterations, including the multiple organ toxicities were investigated. In addition, the micronucleus assay was used to evaluate the in vivo genotoxicity of the leaves extract in murine erythrocytes.The phytochemical analysis showed the majority presence of phenolic compounds (gallic acid, ellagic acid, and myricitrin). Single or repeated doses of the aqueous extract of E. uniflora leaves did not reveal any signs of in vivo toxicity. Daily doses of the extract for 28 days induced a slight reduction in cholesterol and triglyceride levels. Furthermore, E. uniflora leaves extract (1000-2000 mg/kg) showed no genetic damage in the micronucleus assay, indicating the absence of genotoxicity of the herbal species.The aqueous extract of E. uniflora leaves showed a predominance of phenolic compounds, with non-toxic and non-genotoxic action in vivo. This approach sheds light on the chemical composition of the leaves of E. uniflora and suggests a high margin of safety in the popular use of the leaves of this plant species.

The chemical composition, the antioxidant and antimicrobial potential of crude extract from leaves Cinnamomum verum and their enriched fractions was studied. Phytochemical analyses were performed by TLC and HPLC, and the antioxidant capacity was verified by DPPH• and ABTS•+. The Minimal Inhibitory/Bactericidal Concentration was conducted against twenty-two bacteria to select five strains susceptible to extracts/fractions and resistant to the antibiotics tested. Interference of Ethyl Acetate Fraction (EAF) in resistance to synthetic antibiotic was assayed by modulatory and checkerboard model. The chromatographic data showed phenolic compounds in crude extract, as well the flavonoid enrichment in the EAF. The combination of EAF and synthetic antibiotics (ampicillin, azithromycin, ciprofloxacin, or gentamicin) provides a synergistic effect against multidrug resistant strains). The results are useful to obtain multi-targeting in a single therapy solution, which on antioxidants molecules plant-derivatives can act synergistically in antimicrobial combinations, a valuable aid as bacterial resistance modifying compounds.

Microgramma vacciniifolia is broadly used in folk medicine but safety information is unavailable. Therefore, we evaluated the toxicity of a saline extract and a lectin-rich fraction of M. vacciniifolia rhizome. The extract showed hemolytic activity on mice erythrocytes at 1000 μg/mL, whereas the fraction promoted hemolysis (8.57–26.15%) at all tested concentrations (10–1000 μg/mL). Acute toxicity test in mice indicated an LD50 of >5000 mg/kg. Hematological alterations and increased serum alkaline phosphatase level were observed in the treated animals. Transaminases and urea levels increased in the groups treated with the extract or fraction at 5000 mg/kg. Leukocyte infiltration was observed in the liver of extract-treated animals and in the liver and lungs of mice treated with the fraction. The kidneys of animals treated with the fraction at 5000 mg/kg presented hydropic degeneration. The extract and fraction did not induce oxidative stress in the liver and did not show genotoxicity, as examined by micronucleus and comet assays. In conclusion, the preparations were not lethal to mice but caused some signs of toxicity, mainly the fraction. The results indicated the need to evaluate the toxicity of M. vacciniifolia rhizome in other models and in chronic assays.

Background: Efavirenz is the most used medication in the treatment of Acquired Immunodeficiency Syndrome (AIDS). The limited number of pediatric antiretroviral formulations approved by regulatory agencies is the most significant obstacle to adequate and efficient pharmacotherapy for this group of patients. The efavirenz has excellent therapeutic potential, but has low aqueous solubility/bioavailability. Methods: To minimize these limitations, multicomponent systems with β-cyclodextrin and polyvinylpyrrolidone K-30 were obtained. Due to the limited number of pediatric antiretroviral formulations, the development of a pediatric orodispersible tablet is an alternative that is thought easy to administer, since it disintegrates rapidly in the oral cavity. The multicomponent systems were obtained by the method of kneading and characterized by solubility test, X-ray diffraction, differential scanning calorimetry and infrared absorption spectroscopy by Fourier transform. The orodispersible tablets were prepared by direct compression. The quality control of hardness, friability, disintegration, and dissolution was performed. The influence of the components of the formulation on the characteristics of the tablets was evaluated through a 22 factorial design added with three central points, to compare the effect of the dependent variables on the responses. Results: An increase in drug solubility was observed, with a decrease in crystallinity. Besides that, an excellent dissolution profile presented with more than 83% of the drug's content dissolved in less than 15 minutes. Satisfactory disintegration time and friability were observed. Conclusion: It was observed that reduced concentrations of mannitol decreased the hardness and disintegration time of the formulations. The orodispersible tablet composed of efavirenz: β- cyclodextrin: polyvinylpyrrolidone, favors greater absorption and bioavailability. It has several advantages for pediatric patients, as the dosage form disintegrates quickly in the mouth and does not require water for administration, thereby improving patient compliance with the treatment.

In this study, the toxicity and antinociceptive effects of the ethanolic extract of Croton blanchetianus leaves were investigated in mice. Phytochemical analysis was performed by thin layer chromatography (TLC) and high–performance liquid chromatography (HPLC) revealed the presence of alkaloids, reducing sugars, cinnamic derivatives, flavonoids, saponins, condensed tannins, terpenes, and steroids. Acute toxicity was evaluated by administration of a single dose of 2000 or 5000 mg/kg b.w. (per os or i.p.). The extract (50, 100, and 200 mg/kg per os) was evaluated for genotoxicity through micronucleus and comet assays, and antinociceptive effects using different tests. No death was observed but increased serum levels of hepatic and renal markers, hematological changes, and histological alterations in the lung and kidney were observed exclusively with intraperitoneal administration. Oral administration did not result in genotoxicity in bone marrow or peripheral blood cells. The extract reduced the number of abdominal writhings by 47.16–88.81%, increased the latency time (up to 2.13 times) in the tail–immersion test, and decreased the paw licking time by as much as 74.07% and 97.76% in the first and second phases of the formalin test, respectively. This work contributes to the determination of safety and pharmacological potential for C. blanchetianus leaves.

Objective: The development of medicinal plants for clinical use represents an important direction in biomedical research, despite the technological difficulties.Significance: The aim of this study ...

Moringa oleifera Lam. leaves infusion and powder are widely used by population due the nutritional and medicinal potentials, however data regarding safety of use are still inconclusive, leading to prohibition of this plant in some countries.The present work investigated the nutritional and phytochemical composition, acute and 28-day repeated dose toxicity, and genotoxicity of M. oleifera leaves infusion and powder.For nutritional characterization of leaf powder, it was determined: humidity; mineral residue (ash); total lipid, protein, carbohydrate, and crude fiber contents; and total caloric value. Phytochemical composition was determined by high performance liquid chromatography (HPLC). The acute toxicity assay used Swiss female albino mice and oral administration in a single dose at 2000 and 5000 mg/kg of infusion or powder. The 28-day repeated dose toxicity assay employed female and male mice, with oral administration of infusion or powder at the doses 250, 500 and 1000 mg/kg. The animals were evaluated for body weight, water and feed consumption, biochemical and hematological parameters, and histology of the liver, spleen, and kidneys. In vivo genotoxicity and mutagenicity (2000 mg/kg) were evaluated by the comet assay and the micronucleus test, respectively.Nutritional characterization confirmed that M. oleifera leaves are rich in proteins, carbohydrates, lipids, minerals, and fiber. HPLC indicated the presence of flavonoids and cinnamic derivatives as major polyphenols. Acute toxicity did not reveal alterations in weight gain and water and feed consumptions and no change in biochemical, hematological, and histological parameters. Behavior alterations was observed in the first 2 h after administration at 5000 mg/kg in both treatments. Infusion did not present toxicity when administered for 28 days. Conversely, the powder at 500 and 1000 mg/kg promoted liver and kidney damages observed through biochemical parameters and histopathology. Genotoxicity and mutagenicity were not detected at 2000 mg/kg.The present study reveals that M. oleifera leaves are an important source of polyphenols and nutrients. Indiscriminate use of both infusion and crude leaf powder above 2000 mg/kg and powder at 500 and 1000 mg/kg are not recommended. Chronic toxicological studies and establishment of preparation protocols are suggested aiming to guarantee the safety in the use of M. oleifera leaves as nutraceutical by population.

The genus Croton, belonging to the Euphorbiaceae family, is a plant with shrubby characteristics, with the ability to regrow in times of rain, develops wildly, especially in deforestation areas, being reported mainly in the Caatinga and Forest region. One of the main characteristics of this genus is that several species are rich in chemical constituents of importance for medicine. In this way, this review of the literature, has an objective that findings regarding the biological activities and chemical composition of Croton species. This study is a literature review, carried out in the following databases: SciELO, BVS, MEDLINE, LILACS, PubMed and ScienceDirect, with a time frame between 1997 and 2020. The articles studied have shown different activities for Croton species, such as anti-inflammatory, antihypertensive, antifungal, antimicrobial, antidiabetic, antioxidant, antinociceptive and anti-tumor. Regarding toxicological aspects, the findings suggest caution in the use of Croton species, as some are toxic. While, regarding the chemical composition, in most species the presence of several secondary metabolites is observed, such as alkaloids, terpenoids, flavonoids and other phenolic compounds. Therefore, the results described in this article suggest that the therapeutic application of Croton species is supported by the literature, however we point out that caution is required in the use of Croton species, some present due to toxicity. El género Croton, perteneciente a la familia Euphorbiaceae, es una planta de características arbustivas, con capacidad de rebrote en épocas de lluvia, se desarrolla salvajemente, especialmente en áreas de deforestación, siendo reportada principalmente en la región de Caatinga y Bosques. Una de las principales características de este género es que varias especies son ricas en componentes químicos de importancia para la medicina. De esta forma, esta revisión de la literatura, tiene como objetivo que los hallazgos sobre las actividades biológicas y la composición química de las especies de Croton. El presente estudio es una revisión de la literatura, realizada en las siguientes bases de datos: SciELO, BVS, MEDLINE, LILACS, PubMed y ScienceDirect, con un período de tiempo comprendido entre 1997 y 2020. inflamatorio, antihipertensivo, antifúngico, antimicrobiano, antidiabético, antioxidante, antinociceptivo y antiinflamatorio. En cuanto a los aspectos toxicológicos, los hallazgos sugieren precaución en el uso de especies de Croton, ya que algunas son tóxicas. Mientras que, en cuanto a la composición química, en la mayoría de especies se observa la presencia de varios metabolitos secundarios, como alcaloides, terpenoides, flavonoides y otros compuestos fenólicos. Por lo tanto, los resultados descritos en este artículo sugieren que la aplicación terapéutica de las especies de Croton está respaldada por la literatura, sin embargo, señalamos que se requiere precaución en el uso de las especies de Croton, algunas presentes por toxicidad. O gênero Croton, pertencente à família Euphorbiaceae, é uma planta com características arbustivas, com capacidade de rebrota em épocas de chuva, desenvolve-se de forma selvagem, principalmente em áreas de desmatamento, sendo relatada principalmente na Caatinga e na região da Floresta. Uma das principais características desse gênero é que várias espécies são ricas em constituintes químicos de importância para a medicina. Desta forma, esta revisão da literatura, tem como objetivo obter descobertas a respeito das atividades biológicas e composição química das espécies de Croton. Este estudo é uma revisão da literatura, realizada nas seguintes bases de dados: SciELO, BVS, MEDLINE, LILACS, PubMed e ScienceDirect, com período compreendido entre 1997 e 2020. Os artigos estudados mostraram diferentes atividades para espécies de Croton, como anti-inflamatório, anti-hipertensivo, antifúngico, antimicrobiano, antidiabético, antioxidante, antinociceptivo e antitumoral. Em relação aos aspectos toxicológicos, os achados sugerem cautela no uso de espécies de Croton, pois algumas são tóxicas. Já quanto à composição química, na maioria das espécies observa-se a presença de diversos metabólitos secundários, como alcaloides, terpenóides, flavonoides e outros compostos fenólicos. Portanto, os resultados descritos neste artigo sugerem que a aplicação terapêutica de espécies de Croton é suportada pela literatura, porém ressaltamos que é necessário cautela no uso de espécies de Croton, devido à toxicidade.

Senna occidentalis Link (Fabaceae), known as “fedegoso”, is used in folk medicine due to its anti-inflammatory, antioxidant, muscle relaxant and inhibiting lipid peroxidation imputed to flavonoids contained in its composition. The species is also a constituent of processed products are commercialized in various parts of the world including Brazil, although there are few reports in the literature about the development of an analytical method for quantification of flavonoids in it. The main purpose of this research was the evaluation of an analytical methodology to determinate the content of total flavonoids in leaves of S. occidentalis, for quality control. The parameters evaluated were: drug: solvent ratio, concentration of aluminum chloride and reaction time. The quantification of total flavonoids was obtained after reaction with aluminum chloride by UV/Vis spectrophotometry. The results revealed a maximum absorption peak (λ = 392 nm) was the amount of 0.5 g of a plant raw in 100 mL of solvent and there were no significant influences between the concentrations of aluminum chloride or hydroalcoholic solutions analyzed. The evaluation of reaction time allowed to characterize the kinetics as slow, stabilizing from 60 min, choosing this as reading time. The method was specific, linear, precise, accurate and robust, according to the specifications set in RDC n. 166/2017. Finally, the results of the study showed that the measured methodology is simple and accurate and can be applied for quality assessment of the species S. occidentalis. Senna occidentalis Link (Fabaceae), conocido como “fedegoso”, se utiliza en la medicina popular por su acción antiinflamatoria, antioxidante, relajante muscular e inhibidora de la peroxidación lipídica imputada a los flavonoides contenidos en su composición. La especie también es un constituyente de productos procesados que se comercializan en diversas partes del mundo incluido Brasil, aunque existen pocos informes en la literatura sobre el desarrollo de un método analítico para la cuantificación de flavonoides en ella. El objetivo principal de esta investigación fue la evaluación de una metodología analítica para determinar el contenido de flavonoides totales en hojas de S. occidentalis, para control de calidad. Los parámetros evaluados fueron: relación fármaco: disolvente, concentración de cloruro de aluminio y tiempo de reacción. La cuantificación de los flavonoides totales se obtuvo tras la reacción con cloruro de aluminio mediante espectrofotometría UV/Vis. Los resultados revelaron que un pico de absorción máximo (λ = 392 nm) fue la cantidad de 0.5 g de una planta cruda en 100 mL de solvente y no hubo influencias significativas entre las concentraciones de cloruro de aluminio o soluciones hidroalcohólicas analizadas. La evaluación del tiempo de reacción permitió caracterizar la cinética como lenta, estabilizándose a partir de 60 min, eligiendo este como tiempo de lectura. El método fue específico, lineal, preciso, exacto y robusto, de acuerdo con las especificaciones establecidas en RDC n. 166/2017. Finalmente, los resultados del estudio mostraron que la metodología medida es simple y precisa y se puede aplicar para la evaluación de la calidad de la especie S. occidentalis. Senna occidentalis Link (Fabaceae), conhecido como “fedegoso”, é utilizado na medicina popular por ser anti-inflamatório, antioxidante, relaxante muscular e inibidor da peroxidação lipídica imputada aos flavonoides contidos em sua composição. A espécie também é constituinte de produtos processados, sendo comercializados em várias partes do mundo inclusive no Brasil, embora existam poucos relatos na literatura sobre o desenvolvimento de um método analítico para quantificação de flavonoides na mesma. O objetivo principal desta pesquisa foi a avaliação de uma metodologia analítica para determinação do teor de flavonoides totais em folhas de S. occidentalis, para controle de qualidade. Os parâmetros avaliados foram: relação fármaco: solvente, concentração de cloreto de alumínio e tempo de reação. A quantificação dos flavonoides totais foi obtida após reação com cloreto de alumínio por espectrofotometria UV/Vis. Os resultados revelaram que um pico máximo de absorção (λ = 392 nm) foi a quantidade de 0,5 g de uma planta crua em 100 mL de solvente e não houve influências significativas entre as concentrações de cloreto de alumínio ou soluções hidroalcóolicas analisadas. A avaliação do tempo de reação permitiu caracterizar a cinética como lenta, estabilizando a partir de 60 min, escolhendo-se este como tempo de leitura. O método foi específico, linear, preciso, exato e robusto, de acordo com as especificações estabelecidas na RDC n. 166/2017. Por fim, os resultados do estudo mostraram que a metodologia de medição é simples e precisa e pode ser aplicada para avaliação da qualidade da espécie S. occidentalis.

Historicamente, o conhecimento tradicional tem sido ponto de partida para pesquisas inovadoras na área de medicamentos. Contudo, o potencial etnofarmacológico relacionado ao uso de algumas espécies, como alecrim-de-caboclo pelo povo Pankararu segue ignorado pela comunidade científica. Diante do exposto, esse artigo teve como objetivo realizar a compilação de estudos que relatem a utilização do alecrim-de-caboclo pelos indígenas da etnia Pankararu, especulando suas potencialidades farmacológicas baseada nos conhecimentos tradicionais. Foi realizada revisão da literatura nas bases de dados PubMed, Scielo e Google Acadêmico. Apenas 13 artigos foram considerados relevantes para o presente estudo, sendo 10 diretamente relacionados com o uso tradicional do alecrim-de-caboclo pelo povo Pankararu; e 3 relacionados a divergências na classificação botânica da espécie em outros contextos étnicos. Em 10 trabalhos foram relatados o uso tradicional do alecrim-de-caboclo para fins ritualísticos (80% dos estudos); além de uso medicinal (70% dos trabalhos). Apesar de não serem descritas as indicações terapêuticas, a utilização na forma de lambedor sugere indicação tradicional para gripes e resfriados. Dos 10 estudos, apenas 2 identificaram a espécie utilizada pelos indígenas Pankararu como Baccharis sylvestris. Outros 3 trabalhos, realizados em outros contextos étnicos, identificaram o alecrim-de-caboclo como Lippia thymoides ou Turnera diffusa. Estudos complementares precisam ser conduzidos no intuito de realizar uma descrição etnofarmacológica mais detalhada do alecrim-de-caboclo no contexto do povo Pankararu, incluindo indicações tradicionais, confirmação taxonômica, caracterização fitoquímica, estudos de toxicidade, além da investigação de potenciais farmacológicos.

The aim of this study was to evaluate the phytochemical composition, antioxidant, and antimicrobial potential of crude extract and fractions of Punica granatum leaves. The extract was produced by turbo extraction, after which hexanic, ethyl acetate, and aqueous fractions were obtained by partitioning. The chemical analyses were performed by thin layer chromatography and high-performance liquid chromatography, and the antioxidant activities were assayed by DPPH. and ABTS.+ . Minimal inhibitory and bactericidal concentrations (MIC/MBC) were applied to twenty-two bacteria. Most strains susceptible to extract/fractions and resistant to antibiotics were selected, and ampicillin, azithromycin, ciprofloxacin, and gentamicin were associated with the ethyl acetate fraction (EAF) against multidrug-resistant strains in modulatory and checkboard models. The data from chromatographic analyses showed flavonoids and tannins in the extract, as well as the enrichment of EAF in phenols, mainly flavonoids. The flavonoids were connected to the electron transfer activity demonstrated in the DPPH. and ABTS.+ assays. Gram-positive strains are more susceptible to EAF. The subinhibitory concentrations of P. granatum enhanced the antimicrobial activity of the agents and reduced the EAF individual MIC, and the combination of EAF and antibiotics demonstrated a synergistic effect. These results present a promising approach for developing a therapy in which antioxidant extracts and fractions can be used in combination with antibiotics.

This study aimed to evaluate the performance of polyphenolic extraction from leaves of Eugenia uniflora by using solvent systems and different extractive conditions. The solvent systems containing water, methanol, ethanol, and acetone (binary, ternary, or quaternary mixtures) were used to produce extracts by turbo-extraction in accordance with a simplex centroid. The extraction performances were determined by dry residue, total tannin, and flavonoid contents, which were used to calculate the extractive efficiency, and content of markers gallic acid, ellagic acid, and myricitrin. Fingerprints were also obtained by high-performance liquid chromatography and high-performance thin layer chromatography. The mixture of H2O to MeOH to EtOH to acetone (46:13:18:23) demonstrate a larger extractive efficiency and was used as solvent to evaluate the influences of drug amount and extraction method. A 32-design with response surface methodology allowed to optimize the extraction conditions, showing better extraction at 5% (w/v) of the herbal drug and by turbo-extraction, standardized condition for extracts from Eugenia uniflora leaves.

Eugenia uniflora (Myrtaceae) is a species native to Brazil and has a traditional use in the treatment of inflammation.To evaluate the anti-inflammatory and antinociceptive effects, and the involvement of opioid receptors in the antinociceptive activity of extract and fractions from Eugenia uniflora leaves.TLC and HPLC were used to characterize the spray-dried extract (SDE) and fractions. In the in vivo assays, Swiss (Mus musculus) mice were used. Carrageenan-induced hind-paw edema and carrageenan-induced peritonitis models were used to determine the anti-inflammatory effect of the extract (50, 100, or 200 mg/kg). Acetic acid-induced writhing, tail-flick, and formalin tests were used to determine the antinociceptive effect of the extract (50, 100, or 200 mg/kg). The aqueous (AqF) and ethyl acetate (EAF) fractions (6.25, 12.5, and 25 mg/kg) were then combined with naloxone to evaluate the involvement of opioid receptors in the antinociceptive activity.In this work, the TLC and HPLC analysis evidenced the enrichment of EAF, which higher concentration of gallic acid (5.29 ± 0.0004 %w/w), and ellagic acid (1.28 ± 0.0002 %w/w) and mainly myricitrin (8.64 ± 0.0002 %w/w). The extract decreased the number of total leukocytes and neutrophils in the peritoneal cavity (p 0.05), at doses of 100 and 200 mg/kg and showed significant inhibition in the increase of paw edema volume (p 0.05). The treatment per oral route (doses of 50, 100, and 200 mg/kg) significantly reduced the nociceptive response in acetic acid-induced abdominal writhing (p 0.05). The effect of the extract on the tail-flick test showed a significant increase in latency time of animals treated at doses of 200 and 100 mg/kg (p 0.05). The extract and ethyl acetate fraction reduced the nociceptive effect in both phases of formalin at all tested doses. The naloxone reversed the antinociceptive effect of EAF, suggesting that opioid receptors are involved in mediating the antinociceptive activity of EAF of E. uniflora in the formalin test.The current study demonstrates the anti-inflammatory and analgesic activities of water: ethanol: propylene glycol spray-dried extract from E. uniflora leaves using in vivo pharmacological models in mice. Our findings suggest that spray-dried extract and ethyl acetate fraction exhibit peripheral and central antinociceptive activity with the involvement of opioid receptors that may be related to the presence of flavonoids, mainly myricitrin.

This study describes for the first time the effect of saline extract and Parkia pendula seed fraction on Biomphalaria glabrata adult embryos and molluscs well as the reproductive parameters (fecundity and fertility) and survival, in addition to cytotoxicity and genotoxicity through the profile of blood cells after exposure to sublethal concentrations. Furthermore, we analyzed the action of both preparations against the cercariae of Schistosoma mansoni and their environmental safety using the bioindicator Artemia salina. The saline extract and fraction showed toxic effects for embryos (CL

The aim of this study was evaluate the in vitro antifungal activity of crude extracts from Eugenia uniflora, Libidibia ferrea and Psidium guajava. The extracts were obtained by turbo-extraction using water (AQ) or acetone-water (AC-W) (7:3, v/v) as solvents and lyophilized to obtain the crude extracts (CE). The CE were characterized by UV-Vis, TLC and HPLC. The activity of CEs was investigated against clinical isolates of Candida spp. and the Minimum Inhibitory Concentration (MIC), MIC50 and MIC90 were determinated. The analysis by TLC showed that all CEs presented polyphenols (flavonoids and tannins). The CEs from E. uniflora showed higher amount of polyphenols (30.35 ± 2.15%, AC-W) and the HPLC analysis revealed the tannins in all extracts. The CEs of E. uniflora showed MIC range from 1.9 to 500.0 µg/mL, and lower values of MIC50 and MIC90 against non-albicans Candida isolates. Regarding L. ferrea and P. guajava, the results showing MIC from 3.9 to 1000.0 µg/mL (CE-AQ) against C. albicans. The results demonstrate antifungal performance from CE against various species of Candida spp., suggesting that the herbal species may be use as new potential antifungal agents. Additionally, the polyphenol content can play a pivotal role in the antifungal properties of CE.

Plectranthus barbatus Andrews (Lamiaceae) is widely distributed in the world and has a range of popular therapeutic indications. This work aimed to evaluate the phytochemical characterization of two leaf extracts of P. barbatus, and their antimicrobial, antineoplastic and immunomodulatory potential. After collection, herborization and obtainment of the P. barbatus aqueous extract (PBA) and acetone:water 7:3 P. barbatus organic extract (PBO), the phytochemical characterization was performed by high-performance liquid chromatography (HPLC). The antimicrobial activity was performed to determine the minimum inhibitory concentration (MIC) against eight bacterial strains using the microdilution test and the fungus Trichophyton rubrum by disc diffusion assay and microdilution test. Cytotoxicity was assessed by MTT and trypan blue methods in normal peripheral blood mononuclear cells (PBMCs) at concentrations ranged between 0.1 to 100 µg.mL-1 and in neoplastic cell lines Toledo, K562, DU-145 and PANC-1 at 1, 10 and 100 µg.mL-1 . Immunomodulatory activity, was evaluated by sandwich ELISA of proinflammatory cytokines at BALB/c mice splenocytes cultures supernatant. Both extracts presented flavonoids, cinnamic derivatives, steroids and ellagic acid. PBO showed bacteriostatic activity against Acinetobacter baumannii (MIC = 250 µg.mL-1) clinical isolate and PBA fungistatic activity against Trichophyton rubrum (MIC = 800 µg.mL-1). The extracts did not exhibit toxicity to PBMCs and neoplastic cells (IC50 > 100 µg.mL-1). Additionally, PBO at 100 µg.mL-1 significantly inhibited IFN-γ and IL-17A cytokines (p = 0.03). Plectranthus barbatus is a potential candidate for therapeutic use due to its low toxicity in healthy human cells and exhibits biological activities of medical interest as bacteriostatic, fungistatic and immunomodulatory. Resumo Plectranthus barbatus Andrews (Lamiaceae) é amplamente distribuída no mundo e com uma série de indicações terapêuticas populares. Este trabalho teve como objetivo avaliar a caracterização fitoquímica de dois extratos da folha de P. barbatus e seu potencial antimicrobiano, antineoplásico e imunomodulador. Após coleta, herborização e obtenção do extrato aquoso (PBA) e acetona: água 7: 3 (orgânico) (PBO) de P. barbatus, a caracterização fitoquímica foi realizada por cromatografia líquida de alta eficiência (CLAE). A atividade antimicrobiana foi realizada para determinar a concentração inibitória mínima (CIM) contra oito cepas bacterianas usando o teste de microdiluição e o fungo Trichophyton rubrum por ensaio de difusão em disco e teste de microdiluição. A citotoxicidade foi avaliada por métodos MTT e azul de tripan em células normais mononucleares do sangue periférico (CMSP) em concentrações variadas entre 0,1 a 100 µg.mL-1 e nas linhagens celulares neoplásicas Toledo, K562, DU-145 e PANC-1 em 1, 10 e 100 µg.mL-1 . A atividade imunomoduladora foi avaliada por ELISA sanduíche de citocinas pró-inflamatórias em sobrenadante de culturas de esplenócitos de camundongos BALB/c. Ambos os extratos apresentaram flavonoides, derivados cinâmicos, esteróides e ácido elágico. O PBO mostrou atividade bacteriostática contra Acinetobacter baumannii (CIM = 250 µg.mL-1) e atividade fungistática do PBA contra Trichophyton rubrum (CIM = 800 µg.mL-1). Os extratos não apresentaram toxicidade para CMSP e células neoplásicas (IC50 > 100 µg.mL-1). Além disso, o PBO a 100 µg.mL-1 inibiu significativamente as citocinas IFN-γ e IL-17A (p = 0,03). Plectranthus barbatus é um candidato potencial para uso terapêutico devido à sua baixa toxicidade em células humanas saudáveis e exibe atividade de interesse médico como bacteriostática, fungistática e imunomoduladora.