Analgesic, Anti-Inflammatory, and Antioxidant Activities of Byrsonima duckeana W. R. Anderson (Malpighiaceae).

Background. Byrsonima is a promising neotropical genus, rich in flavonoids and triterpenes, with several proven pharmacological properties. Nevertheless, Byrsonima duckeana W. R. Anderson is an Amazonian species almost not studied. Objective. To assess the antioxidant, anti-inflammatory, and analgesic activities of Byrsonima duckeana leaves. Materials and Methods. We analyzed an ethanol extract and its fractions for polyphenol content and UHPLC-MS/MS, phosphomolybdenum, DPPH, TBARS antioxidant tests, formalin-induced pain, carrageenan-induced peritonitis, acetic acid-induced abdominal writhings, and hot plate assays. Results. All the samples showed high polyphenol content and antioxidant capacity in the phosphomolybdenum, DPPH, and TBARS tests. We identified ethyl gallate, quinic acid, gallic acid, catechin, epicatechin, quercetrin, and quercetin in the samples. B. duckeana was able to reduce leukocyte migration in the carrageenan-induced peritonitis by 43% and the licking time in the formalin test by 57%. In the acetic acid-induced writhing test, the chloroform (FCL) and ethyl acetate (FEA) fractions were the most active samples. FEA was selected for the hot plate test, where all the dosages tested (5, 50, and 200 mg·kg-1) showed significant analgesic activity. Conclusion. B. duckeana has interesting analgesic and antioxidant activities, due to its high phenolic content, especially phenolic acids.

Chemical composition, antioxidant activity and hepatoprotective potential of Rourea induta Planch. (Connaraceae) against CCl4-induced liver injury in female rats.

OBJECTIVES: The aim of this study was to evaluate the flavonoid content of an ethanolic leaf extract from the medicinal plant Rourea induta Planch. (RIEE) and to investigate its hepatoprotective potential and in vivo antioxidant effects. METHODS: Using samples from carbon tetrachloride-treated Wistar female rats treated orally with or without RIEE, we evaluated the aspartate aminotransferase, alanine aminotransferase, and total bilirubin levels in plasma; the levels of the hepatic oxidative stress markers catalase, superoxide dismutase, glutathione peroxidase, and reduced glutathione in liver homogenates; and the thiobarbituric acid reactive substance levels. A histopathology study was performed. A quantitative analysis of the RIEE extract was performed using high-performance liquid chromatography to evaluate its flavonoid content. RESULTS: Oral administration of RIEE significantly reduced carbon tetrachloride-induced elevations in the levels of plasma markers of hepatic damage and lipid peroxidation. It also rescued histopathologic alterations observed in the liver and levels of oxidative stress markers. CONCLUSIONS: RIEE exhibits antioxidant and hepatoprotective activities in vivo, which may be attributable to its flavonoids composition [hyperin (2), quercetin-3-O-ß-xyloside (4), quercetin-3-O-α-arabinofuranoside (5), and quercetin (6)].

Chemical composition and antinociceptive effect of aqueous extract from Rourea induta Planch. leaves in acute and chronic pain models.

ETHNOPHARMACOLOGICAL RELEVANCE: Rourea induta Planch. is a small tree or shrub growing wild in Brazil and belonging to the Connaraceae family. It is used for the treatment of Chagas disease and as antirheumatic in folk medicine. This study was designed to investigate the antinociceptive activity of the aqueous extract (AERi) of Rourea induta leaves in rodents, as well as isolate and identify components that can be responsible for its effect. MATERIAL AND METHODS: The antinociceptive effect of orally administered AERi was evaluated in behavioral models of acute (formalin) and chronic [complete Freund׳s adjuvant (CFA)] pain in mice. We also investigated the possible involvement of opioid receptors and proinflammatory cytokines (interleukin-1ß and tumor necrosis factor-α) in the antinociceptive effect of the AERi. In addition, a nonspecific effect of AERi was evaluated by measuring locomotor activity and corporal temperature. Finally, we performed a phytochemical analysis of AERi. RESULTS: HPLC titration revealed the presence of hyperin (21.6 mg/g), quercetin-3-O-ß-xyloside (4.4 mg/g), quercetin-3-O-α-arabinofuranoside (12.0 mg/g), and quercetin (2.1 mg/g). It was also possible to isolate minor constituents׳ chlorogenic acid, neochlorogenic acid and procyanidin C1. The oral administration of AERi (100 mg/kg) significantly inhibited the neurogenic (37 ± 5%) and inflammatory (34 ± 7%) phases of formalin-induced pain. Acute and repeated treatment of animals with AERi (100 mg/kg, p.o.) once a day markedly reduced the mechanical hypersensitivity response induced by CFA, and this effect was evident until the day 10. Moreover, repeated treatment with AERi (100 mg/kg, p.o.) significantly reduced the levels of IL-1ß and TNF-α in the paw (22 ± 7% and 50 ± 19%) and in the spinal cord (100% and 100%) when compared to the CFA group. The AERi (100 mg/kg, p.o.) markedly reduced biting behavior induced by intrathecal injection of TNF-α (81 ± 11%). Finally, the effect of AERi was not associated with changes in locomotor activity or the corporal temperature of animals. CONCLUSION: These data show that aqueous extract of Rourea induta has significant antinociceptive action, which seems to be associated with an inhibition of pro-inflammatory cytokines activated pathways. These findings support the ethnomedical uses of this plant.

Avaliação da atividade antibacteriana das cascas das raízes de Xylosma ciliatifolia (Clos) Eichler (Flacourtiaceae/Salicaceae sensu lato) / Validación de la actividad antibacteriana de corteza de raíces de Xylosma ciliatifolia (Clos) Eichler (Flacourtiaceae/Salicaceae sensu lato) / Validation of the antibacterial activity of root bark of Xylosma ciliatifolia (Clos) Eichler (Flacourtiaceae/Salicaceae sensu lato)

Introdução: Xylosma ciliatifolia (Clos) Eichler (Flacourtiaceae/Salicaceae sensu lato), espécie conhecida popularmente como sucará, açucará ou espinho-de-judeu é uma árvore de pequeno porte, que se desenvolve em regiões de vegetação de mata ciliar. Objetivos: avaliar o potencial antibacteriano de frações e substância isolada das cascas das raízes de Xylosma ciliatifolia sobre Staphylococcus aureus, Staphylococcus epidermidis, Salmonella typhimurium e Escherichia coli. Métodos: o material vegetal seco foi extraído em etanol 96 % em aparelho de Soxhlet com aquecimento. O extrato etanólico obtido foi submetido à partição líquido-líquido em hexano, clorofórmio e acetato de etila e, após, concentrados em banho-maria, obtendo-se, respectivamente, as frações hexano, clorofórmio e acetato de etila. Por cromatografia em coluna da fração hexano obteve-se o composto ugandensidial. A atividade antibacteriana foi avaliada pelo ensaio da difusão em disco e pela medida da concentração inibitória mínima. Resultados: a atividade antibacteriana foi evidenciada nas frações hexano e clorofórmio sobre as bactérias: Staphylococcus aureus e Staphylococcus epidermidis. O composto ugandensidial mostrou-se ainda mais bioativo sobre as cepas Staphylococcus aureus e Staphylococcus epidermidis com inibição do crescimento bacteriano na concentração de 62,5 µg/mL. Conclusão: os ensaios antibacterianos realizados neste trabalho com as cascas das raízes de Xylosma ciliatifolia foram capazes de inibir o crescimento de duas cepas gram positivas. Estes resultados contribuem para o conhecimento fitoquímico dessa espécie vegetal que ainda não apresenta dados em literaturas científicas.

Introducción: Xylosma ciliatifolia (Clos) Eichler (Flacourtiaceae/Salicaceae sensu lato), especie conocida en la población como sucará, acucará o espinho-de-judeu es un árbol de pequeño porte, que se desarrolla en las regiones de vegetación de ribera. Objetivos: evaluar la actividad antibacteriana de las fracciones y sustancias aisladas de la corteza de raíces de Xylosma ciliatifolia sobre Staphylococcus aureus, Staphylococcus epidermidis, Salmonella typhimurium y Escherichia coli. Métodos: el material seco se extrajo en etanol 96 % en un aparato de Soxhlet con calentamiento. El extracto etanólico obtenido se sometió a partición líquido-líquido en hexano, cloroformo y acetato de etilo; después se concentró en un baño de agua, produciendo, respectivamente, las fracciones hexano, cloroformo y acetato de etilo. Por cromatografía de columna de la fracción hexano se obtuvo el compuesto ugandensidial. La actividad antibacteriana se evaluó mediante la prueba de la difusión en disco y mediante la medición de la concentración inhibitoria mínima. Resultados: la actividad antibacteriana se observó en las fracciones hexano y cloroformo sobre las bacterias: Staphylococcus aureus y Staphylococcus epidermidis. El compuesto ugandensidial resultó aún más bioactivo sobre las bacterias Staphylococcus aureus y Staphylococcus epidermidis, con inhibición del crecimiento bacteriano en la concentración de 62,5 µg/mL. Conclusiones: los ensayos antibacterianos realizados en este estudio con corteza de raíces de Xylosma ciliatifolia fueron capaces de inhibir el crecimiento de ambas cepas grampositivas. Estos resultados contribuyen al conocimiento fitoquímico de esa especie vegetal que aún no presenta datos en la literatura científica.

Introduction: Xylosma ciliatifolia (Clos) Eichler (Flacourtiaceae/Salicaceae sensu lato), a species known by the general public as sucara, acucara or espinho-de-judeu, is a small tree growing in riverside areas. Objectives: evaluate the antibacterial activity of fractions and substances isolated from root bark of Xylosma ciliatifolia against Staphylococcus aureus, Staphylococcus epidermis, Salmonella typhimurium and Escherichia coli. Methods: the dry material was extracted into 96% ethanol in a Soxhlet device with heating. The ethanolic extract thus obtained was subjected to liquid-liquid partition in hexane, chloroform and ethyl acetate. It was then concentrated in a water bath to obtain hexane, chloroform and ethyl acetate fractions, respectively. The ugandensidial compound was obtained by column chromatography of the hexane fraction. Antibacterial activity was evaluated by the disc diffusion test and by measurement of the minimum inhibitory concentration. Results: antibacterial activity against Staphylococcus aureus and Staphylococcus epidermis was observed in the hexane and chloroform fractions. The ugandensidial compound was found to be even more bioactive against the bacteria Staphylococcus aureus and Staphylococcus epidermis, with inhibition of bacterial growth in the 62.5 µg/mL concentration. Conclusions: the antibacterial assays conducted in this study with root bark of Xylosma ciliatifolia revealed inhibition in the growth of both gram-positive strains. These results provide phytochemical information about this plant species, for which there are no data in the scientific literature.

Phytochemical constituents and preliminary toxicity evaluation of leaves from Rourea induta Planch. (Connaraceae) / Constituintes fitoquímicos e avaliação preliminar de toxicidade folhas de Rourea Induta Planch. (Connaraceae)

Most active plants are toxic at high doses and it is therefore important to investigate the preliminary toxicity of plant extracts. The Rourea induta species is a potential drug with no phytochemical or biological studies registered in the literature. Thus, a phytochemical study and a toxicity analysis of the ethanolic extract obtained from the leaves of Rourea induta Planch., Connaraceae, was run. A long chain hydrocarbon, n-tetracosane, and four flavonoids were identified: quercetin, and three glycosylated derivates, quercetin-3-O-α-arabinofuranoside, quercetin-3-O-β-xyloside and quercetin-3-O-β-galactoside. This is the first time these have been isolated in this species. The structures were elucidated by 13C NMR, ¹H NMR, UV and IR spectroscopy. The toxicity evaluation of extracts was performed by the brine shrimp method and determination of hemolytic activity. The samples demonstrated no toxic potential by the analyzed methods.

A maioria das plantas ativas é tóxica em doses elevadas, portanto, é importante a investigação da toxicidade preliminar dos extratos das plantas. A espécie Rourea induta é uma droga potencial que não apresenta estudo fitoquímico ou biológico descrito na literatura. Assim, um estudo fitoquímico e análises toxicológicas foram realizados com o extrato etanólico obtido das folhas de Rourea induta Planch., Connaraceae. Foram obtidos um hidrocarboneto de cadeia longa, n-tetracosano, e quatro flavonóides, quercetina e três derivados glicosilados, quercetina-3-O-α-arabinofuranosideo, quercetina-3-O-β-xilosideo e quercetina-3-O-β-galactosideo. Esta é a primeira vez que estes compostos são isolados nesta espécie. As estruturas foram elucidadas por espectroscopia de RMN-13C, RMN-¹H, ultravioleta e infravermelho. A avaliação da toxicidade dos extratos foi analisada pelo método da Artemia salina e atividade hemolítica. Nenhuma das amostras testadas apresentou um potencial tóxico pelos métodos analisados.