RESUMEN

Agathisflavone is a flavonoid with anti-neuroinflammatory and myelinogenic properties, being also capable to induce neurogenesis. This study evaluated the therapeutic effects of agathisflavone-both as a pharmacological therapy administered in vivo and as an in vitro pre-treatment aiming to enhance rat mesenchymal stem cells (r)MSCs properties-in a rat model of acute spinal cord injury (SCI). Adult male Wistar rats (n = 6/group) underwent acute SCI with an F-2 Fogarty catheter and after 4 h were treated daily with agathisflavone (10 mg/kg ip, for 7 days), or administered with a single i.v. dose of 1 × 106 rMSCs either unstimulated cells (control) or pretreated with agathisflavone (1 µM, every 2 days, for 21 days in vitro). Control rats (n = 6/group) were treated with a single dose methylprednisolone (MP, 60 mg/kg ip). BBB scale was used to evaluate the motor functions of the animals; after 7 days of treatment, the SCI area was analyzed after H&E staining, and RT-qPCR was performed to analyze the expression of neurotrophins and arginase. Treatment with agathisflavone alone or with of 21-day agathisflavone-treated rMSCs was able to protect the injured spinal cord tissue, being associated with increased expression of NGF, GDNF and arginase, and reduced macrophage infiltrate. In addition, treatment of animals with agathisflavone alone was able to protect injured spinal cord tissue and to increase expression of neurotrophins, modulating the inflammatory response. These results support a pro-regenerative effect of agathisflavone that holds developmental potential for clinical applications in the future.

RESUMEN

The present work describes the acetylcholinesterase inhibitory activity of Ocotea pomaderroides extracts besides the chemical composition of chromatographic fractions. The hexane, dichloromethane and ethyl acetate extract soluble fractions showed high Electrophorus electricus acetylcholinesterase (EelAChE) inhibition (92.18, 71.86 and 74.25%, respectively) while the butanolic and aqueous extracts showed moderate to low activities (44.48 and 20.74%, respectively). The high-performance liquid chromatography coupled with electrospray ionization multiple-stage mass spectrometry (HPLC-ESI-MSn) analysis led to the identification of the alkaloids and flavonol glycoside derivatives present in these extracts. The binding profile of the alkaloids and their atomic effect on 3D structure of Electrophorus electricus AchE (EelAChE) were assessed with molecular modeling.

Asunto(s)

Inhibidores de la Colinesterasa/farmacología , Ocotea , Extractos Vegetales , Acetilcolinesterasa/metabolismo , Cromatografía Líquida de Alta Presión , Ocotea/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Espectrometría de Masa por Ionización de Electrospray , Espectrometría de Masas en Tándem

RESUMEN

Erythroxylaceae is a family composed of four genera, with Erythroxylum being the only one represented in the Neotropical region. Chemical studies indicate the presence of alkaloids, terpenes, flavonoids, and phenolic compounds as main compounds. The incorporation of cytotoxic activity assays of natural products using cell cultures assists in the selection of potential chemotherapeutic agents. In this work, we describe a revision of the cytotoxicity evaluation studies performed with extracts or pure substances obtained from Erythroxylum species through an integrative review. We found studies that evaluated the cytotoxic activity of 21 species of Erythroxylum against 45 different cell lines. The analysis of the chemical composition of these species shows that the metabolites present in each species influence their cytotoxic potential, especially the presence of disubstituted tropane alkaloid species with the highest cytotoxic potential. MTT and Sulforrodamine B assays were the main in vitro tests used for the evaluation of the cytotoxic activities. From the total species, less than 10% of the Erythroxylum species have already been evaluated for cytotoxic activity. Four of them showed high cytotoxic activity according to the criteria of the NCI plant screening program. Thus, this genus represents a potential source of natural products with antitumor activity.

Asunto(s)

Erythroxylaceae/química , Tropanos/farmacología , Antineoplásicos/farmacología , Productos Biológicos/farmacología , Extractos Vegetales/farmacología

RESUMEN

Trichilia ramalhoi Rizz. is a species from Meliaceae family and its chemical composition and biological activities are still unknown. This work describes the chemical composition and biological activities of the organic extracts of this plant. Therefore, methanolic extract of stem barks and leaves were prepared and submitted to chromatographic procedures. Besides, T. ramalhoi extracts biological evaluation showed antioxidant, antinociceptive and, anti-inflammatory activities. Usual chromatographic procedures of the active extracts permitted to isolate methyl 5-O-caffeoylquinate, apocynin C, cinchonains Ia and Ib, besides ß-sitosterol, stigmasterol and lupeol. The identification of the isolates was based on 13C and 1H NMR (1 D and 2 D) spectroscopic data and mass spectrometry. Although the flavalignans cinchonains Ia and Ib were previously isolated from T. catigua, this is the first occurrence of apocynin C in the Meliaceae family.

Asunto(s)

Antioxidantes , Meliaceae , Analgésicos/farmacología , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Extractos Vegetales/farmacología

RESUMEN

Glioblastoma is the most lethal tumor of the central nervous system, presenting a very poor prognostic, with a survival around 16 months. The interaction of mesenchymal stem cells and tumor cells has been studied, showing a bias in their role favoring or going against aggressiveness. Natural products such as flavonoids have showed their anticancer properties and the synergic potential with the activation of microenvironment cells to inhibit tumor progression. Agathisflavone is a flavonoid studied in neurodegenerative diseases and cancer. The present study investigated the effect of flavonoid in the viability of heterogeneous glioblastoma (GBM) cells considering a coculture or conditioned medium of mesenchymal stem cells (MSCs) effect, as well as the dose-dependent effect of this flavonoid in tumor migration and differentiation via STAT3. Agathisflavone (3-10 µM) induced dose-dependent toxicity to GL-15 and U373 human GBM cells, since 24 h after treatments. It was not toxic to human MSC but modified the pattern of interaction with GBM cells. Agathisflavone also inhibited migration and increased differentiation of human GBM cells, associated with the reduction on the expression of STAT3. These results demonstrate that the flavonoid agathisflavone had a direct anti-glioma effect. However, could be observed its effect in MSCs response that may have an impact in controlling GBM growth and aggressiveness, an important factor to consider for new therapies.

Asunto(s)

Antineoplásicos/farmacología , Biflavonoides/farmacología , Neoplasias Encefálicas/tratamiento farmacológico , Glioblastoma/tratamiento farmacológico , Células Madre Mesenquimatosas/metabolismo , Neoplasias Encefálicas/patología , Diferenciación Celular/efectos de los fármacos , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Técnicas de Cocultivo , Medios de Cultivo Condicionados/farmacología , Glioblastoma/patología , Humanos , Factor de Transcripción STAT3/metabolismo

RESUMEN

Passiflora alata or passion fruit is a native flowering plant from Amazon, geographically spread from Peru to Brazil. The plant has long been used in folks medicine for its pharmacological properties and is included in the Brazilian Pharmacopoeia since 1929. The aim of this study was to evaluate the potential cytotoxic and antitumor activities of Passiflora alata leaf extract (PaLE) in S180-tumor bearing mice. The percentage of cell proliferation inhibition (% CPI) and IC50 in relation to 4 tumor cell lines were determined in PC3, K-562, HepG2 and S180 cell lines using the MTT assay. PaLE showed a CPI > 75% and greater potency (IC50 < 30 µg/mL) against PC3 and S180 cell lines. PaLE showed antitumor activity in treatments intraperitoneally (36.75% and 44.99% at doses of 100 and 150 mg/kg/day, respectively). Toxicological changes were shown in the reduced body mass associated with reduced food consumption, increased spleen mass associated with histopathological increase in the white pulp of the spleen and increased number of total leukocytes with changes in the percentage relationship between lymphocytes and neutrophils. Our outcomes corroborate the conclusion that PaLE has antitumor activity in vitro and in vivo with low toxicity.

Asunto(s)

Flavonoides/farmacología , Neoplasias/tratamiento farmacológico , Passiflora/química , Extractos Vegetales/farmacología , Animales , Antineoplásicos/química , Antineoplásicos/farmacología , Brasil , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Flavonoides/química , Xenoinjertos , Humanos , Ratones , Neoplasias/patología , Perú , Extractos Vegetales/química , Hojas de la Planta/química

RESUMEN

Diabetic neuropathy is a frequent complication of diabetes. Symptoms include neuropathic pain and sensory alterations-no effective treatments are currently available. This work characterized the therapeutic effect of bergenin in a mouse (C57/BL6) model of streptozotocin-induced painful diabetic neuropathy. Nociceptive thresholds were assessed by the von Frey test. Cytokines, antioxidant genes, and oxidative stress markers were measured in nervous tissues by ELISA, RT-qPCR, and biochemical analyses. Single (3.125-25 mg/kg) or multiple (25 mg/kg; twice a day for 14 days) treatments with bergenin reduced the behavioral signs of diabetic neuropathy in mice. Bergenin reduced both nitric oxide (NO) production in vitro and malondialdehyde (MDA)/nitrite amounts in vivo. These antioxidant properties can be attributed to the modulation of gene expression by the downregulation of inducible nitric oxide synthase (iNOS) and upregulation of glutathione peroxidase and Nrf2 in the nervous system. Bergenin also modulated the pro- and anti-inflammatory cytokines production in neuropathic mice. The long-lasting antinociceptive effect induced by bergenin in neuropathic mice, was associated with a shift of the cytokine balance toward anti-inflammatory predominance and upregulation of antioxidant pathways, favoring the reestablishment of redox and immune homeostasis in the nervous system. These results point to the therapeutic potential of bergenin in the treatment of painful diabetic neuropathy.

Asunto(s)

Benzopiranos/farmacología , Homeostasis/efectos de los fármacos , Sistema Inmunológico/efectos de los fármacos , Sistema Nervioso/efectos de los fármacos , Neuralgia/tratamiento farmacológico , Oxidación-Reducción/efectos de los fármacos , Animales , Antiinflamatorios/farmacología , Antioxidantes/metabolismo , Citocinas/metabolismo , Diabetes Mellitus Experimental/inducido químicamente , Diabetes Mellitus Experimental/complicaciones , Diabetes Mellitus Experimental/metabolismo , Neuropatías Diabéticas/inducido químicamente , Neuropatías Diabéticas/complicaciones , Neuropatías Diabéticas/metabolismo , Glutatión Peroxidasa/metabolismo , Sistema Inmunológico/metabolismo , Masculino , Malondialdehído/metabolismo , Ratones , Ratones Endogámicos C57BL , Factor 2 Relacionado con NF-E2/metabolismo , Sistema Nervioso/metabolismo , Neuralgia/etiología , Neuralgia/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Estrés Oxidativo/efectos de los fármacos , Estreptozocina/farmacología

RESUMEN

Traumatic brain injury (TBI) is a critical health problem worldwide, with a high incidence rate and potentially severe long-term consequences. Depending on the level of mechanical stress, astrocytes react with complex morphological and functional changes known as reactive astrogliosis. In cases of severe tissue injury, astrocytes proliferate in the area immediately adjacent to the lesion to form the glial scar, which is a major barrier to neuronal regeneration in the central nervous system. The flavonoid agathisflavone has been shown to have neuroprotective, neurogenic, and immunomodulatory effects and could have beneficial effects in situations of TBI. In this study, we investigated the effects of agathisflavone on modulating the responses of astrocytes and neurons to injury, using the in vitro scratch wound model of TBI in primary cultures of rat cerebral cortex. In control conditions, the scratch wound induced an astroglial injury response, characterized by upregulation of glial fibrillary acidic protein (GFAP) and hypertrophy, together with the reduction in proportion of neurons within the lesion site. Treatment with agathisflavone (1 µM) decreased astroglial GFAP expression and hypertrophy and induced an increase in the number of neurons and neurite outgrowth into the lesion site. Agathisflavone also induced increased expression of the neurotrophic factors NGF and GDNF, which are associated with the neuroprotective profile of glial cells. These results demonstrate that in an in vitro model of TBI, the flavonoid agathisflavone modulates the astrocytic injury response and glial scar formation, stimulating neural recomposition.

Asunto(s)

Astrocitos/efectos de los fármacos , Biflavonoides/farmacología , Biflavonoides/uso terapéutico , Lesiones Traumáticas del Encéfalo/tratamiento farmacológico , Neuronas/efectos de los fármacos , Animales , Astrocitos/fisiología , Lesiones Traumáticas del Encéfalo/patología , Células Cultivadas , Relación Dosis-Respuesta a Droga , Femenino , Ratones , Neuronas/fisiología , Embarazo , Ratas , Ratas Wistar

RESUMEN

Neoflavonoids, which are classified as 4-arylcoumarin (neoflavone), 3,4-dihydro-4-arylcoumarin and neoflavene, have been the subject of a number of studies with respect to their therapeutic potential and, despite promising in vitro, ex vivo and in vivo pharmacological activities, there is a lack of studies demonstrating their toxicological properties. Therefore, this study aims to evaluate the acute (14 days) and repeated-dose (28 days) toxicity of synthetic neoflavonoid 7-acetoxy-4-aryl-3,4-dihydrocoumarin in Swiss mice through parameters related to changes in body weight, food and water intake, hematological and biochemical parameters. Toxicity studies using acute doses (300 and 2000 mg/kg) and repeated doses (250, 500 and 1000 mg/kg) orally were carried out as per Organization for Economic Co-operation and Development (OECD) guidelines 423 and 407, respectively. Based on the results of this study, treatment with 7-acetoxy-4-aryl-3,4-dihydrocoumarin was found to not cause clinical adverse symptoms and mortality in any animal used in the acute and repeated-dose toxicity study. In addition, no significant changes were observed in body weight and internal organs, food and water intake, hematological and biochemical parameters, compared to control group. Therefore, these results provide an initial understanding regarding the toxicity profile of 7-acetoxy-4-aryl-3,4-dihydrocoumarin, which can be considered a neoflavonoid with toxicity seen at doses higher than 2000 mg/kg in Swiss mice.

Asunto(s)

Cumarinas/toxicidad , Animales , Artemia/efectos de los fármacos , Femenino , Masculino , Ratones , Pruebas de Toxicidad Aguda , Pruebas de Toxicidad Subaguda

RESUMEN

ABSTRACT The profile of volatile organic compounds, the glandular and non-glandular trichomes of Plectranthus ornatus, obtained by in vitro cultivation, was evaluated in plants grown in Murashide and Skoog medium supplemented with benylaminopurine at 4.5, 9.0, and 18.0 µM + naphthaleneacetic acid at 5.37 µM, kinetin at 4.7, 9.3 and 18.5 µM + naphthaleneacetic acid (5.37 µM) or Murashide and Skoog 0 medium (as a control). Scanning Electron Microscopy was performed on samples of the third leaf node of the 90 days old plants obtained from treatment with 4.5 or 9.0 µM benylaminopurine, and 4.7 or 9.3 µM kinetin. Headspace Solid Phase Micro-Extraction of the 30, 60 and 90 days old in vitro plants permitted to determinate by GC/MS the composition comprised of 62 compounds. The data were analyzed using Principal Component Analysis and Hierarchical Clustering Analysis and, the major constituents of these oils after treatment and aging were monoterpenes and sesquiterpenes. Morphoanatomical analysis of trichomes, by Scanning Electron Microscopy, enabled the identification of non-glandular trichomes and four types of glandular trichomes, which comprised capitate and peltate glandular trichomes that were distributed on both sides of the leaf. We observed that the regulators influenced qualitative and quantitative profiles of the volatile organic compounds and the number and distribution of hairs on the leaf surface.

RESUMEN

ABSTRACT Natural steroids and triterpenes such as b-sitosterol, stigmasterol, lupeol, ursolic and betulinic acids were transformed into its hexanoic and oleic esters, to evaluate the influence of chemical modification towards the cytotoxic activities against tumor cells. The derivatives were evaluated against five tumor cell lines [OVCAR-8 (ovarian carcinoma); SF-295 (glioblastoma); HCT-116 (colon adenocarcinoma); HL-60 (leukemia); and PC-3 (prostate carcinoma)] and the results showed only betulinic acid hexyl ester exhibits cytotoxic potential activity.

Asunto(s)

Humanos , Triterpenos/farmacología , Lamiaceae/química , Triterpenos Pentacíclicos/farmacología , Fabaceae/química , Antineoplásicos/farmacología , Triterpenos/aislamiento & purificación , Triterpenos/química , Ensayos de Selección de Medicamentos Antitumorales , Lamiaceae/clasificación , Concentración 50 Inhibidora , Línea Celular Tumoral , Ésteres , Triterpenos Pentacíclicos/aislamiento & purificación , Triterpenos Pentacíclicos/química , Fabaceae/clasificación , Antineoplásicos/aislamiento & purificación , Antineoplásicos/química

RESUMEN

Natural steroids and triterpenes such as b-sitosterol, stigmasterol, lupeol, ursolic and betulinic acids were transformed into its hexanoic and oleic esters, to evaluate the influence of chemical modification towards the cytotoxic activities against tumor cells. The derivatives were evaluated against five tumor cell lines [OVCAR-8 (ovarian carcinoma); SF-295 (glioblastoma); HCT-116 (colon adenocarcinoma); HL-60 (leukemia); and PC-3 (prostate carcinoma)] and the results showed only betulinic acid hexyl ester exhibits cytotoxic potential activity.

Asunto(s)

Antineoplásicos/farmacología , Fabaceae/química , Lamiaceae/química , Triterpenos Pentacíclicos/farmacología , Triterpenos/farmacología , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Ésteres , Fabaceae/clasificación , Humanos , Concentración 50 Inhibidora , Lamiaceae/clasificación , Triterpenos Pentacíclicos/química , Triterpenos Pentacíclicos/aislamiento & purificación , Triterpenos/química , Triterpenos/aislamiento & purificación , Ácido Betulínico , Ácido Ursólico

RESUMEN

BACKGROUND: Bergenin, a compound derived from gallic acid, is a secondary metabolite of the plant Peltophorum dubium (Spreng.) Taub. OBJECTIVE: In this study, we aimed to characterize the ability of bergenin to eliminate the radicals in non-biological systems. METHODS: We evaluated bergenin's ability to protect erythrocytes from oxidative damage in a biological system. We have elucidated bergenin structure using nuclear magnetic resonance, X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry. We then evaluated its antioxidant capacity in vitro against DPPH•, ABTS•+, hydroxyl radicals, and nitric oxide, and determined its ability to transfer electrons owing to its reduction potential and ability to chelate iron. We also evaluated its protective capacity against oxidative damage produced by AAPH in erythrocytes, its hemolytic properties, its ability to inhibit hemolysis, and its ability to maintain intracellular reduced glutathione homeostasis. RESULTS: Bergenin concentrations between 0.1 and 3mM significantly (p < 0.05) and dose dependently decreased formation of ABTS•+, DPPH•, nitrite ions, OH•, reduced formation ferricyanide, ferrozine-Fe2+complex, inhibited AAPH-induced oxidative hemolysis of erythrocytes, raised GSH levels in the presence of AAPH, inhibited AAPH-induced lipid peroxidation in erythrocytes. CONCLUSION: Bergenin may represent a novel alternative antioxidant, with potential applications in various industries, including drugs, cosmetics, and foods.

Asunto(s)

Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Benzopiranos/aislamiento & purificación , Benzopiranos/farmacología , Eritrocitos/efectos de los fármacos , Fabaceae/química , Animales , Antioxidantes/química , Benzopiranos/química , Benzotiazoles/química , Compuestos de Bifenilo/química , Transporte de Electrón/efectos de los fármacos , Eritrocitos/metabolismo , Femenino , Glutatión/metabolismo , Hemólisis/efectos de los fármacos , Homeostasis/efectos de los fármacos , Radical Hidroxilo/química , Espacio Intracelular/efectos de los fármacos , Espacio Intracelular/metabolismo , Hierro/química , Peroxidación de Lípido/efectos de los fármacos , Modelos Moleculares , Conformación Molecular , Nitritos/química , Picratos/química , Ratas , Ratas Wistar , Ácidos Sulfónicos/química

RESUMEN

An unusually substituted coumarin, named poligalen, was isolated from a chloroform extract of the aerial parts of Polygala boliviensis. This coumarin was identified by one- and two-dimensional NMR techniques, and the structure of the compound was confirmed by X-ray diffraction. Poligalen exhibits immunomodulatory effects, reducing the levels of IL-6 and TNF after LPS stimulation in peritoneal macrophages. However, poligalen potentiates NF-kB activation.

Asunto(s)

Cumarinas/química , Interleucina-6/metabolismo , Macrófagos Peritoneales/efectos de los fármacos , Polygala/química , Factor de Necrosis Tumoral alfa/metabolismo , Animales , Cumarinas/aislamiento & purificación , Regulación hacia Abajo , Masculino , Ratones , Ratones Endogámicos C57BL , Estructura Molecular , FN-kappa B/metabolismo , Componentes Aéreos de las Plantas/química , Cultivo Primario de Células , Células RAW 264.7

RESUMEN

The bark of Mimosa tenuiflora (Willd.) Poiret (Leguminosae family), popularly known as "jurema preta" in Brazil, is used by the population of Contendas of Sincorá (Bahia State, Brazil) for the treatment of coughs and wound healing. Thus, the aim of this study was to evaluate the antinociceptive and anti-inflammatory activities of the bark ethanol extract (EEMT) and solvent soluble fractions (hexane-H, DCM-D, EtOAc-E and BuOH-B) of the extract in vivo. Additionally, we synthesized 5,7-dihidroxy-4'-methoxyflavanone (isosakuranetin) and isolated the compound sakuranetin, and both compounds were also tested. The anti-inflammatory and antinociceptive assays performed were: writhing test; nociception induced by intraplantar formalin injection; leukocyte recruitment to the peritoneal cavity; evaluation of vascular permeability (Evans blue test); and evaluation of mechanical hypernociception (von Frey test). Production of TNF-α, IL-10, myeloperoxidase and the expression of ICAM-1 were also evaluated. Statistical analysis was performed by one-way ANOVA followed by the Bonferroni post-test (n = 8), with P < 0.05. The EEMT showed antinociceptive activities in writhing test (100-200 mg/kg), in the second phase of the formalin test (50-200 mg/kg), and in mechanical hypernociception (100 mg/kg). EEMT showed an anti-inflammatory effect by reducing neutrophil migration to the peritoneal cavity and in the plantar tissue detected by the reduction of myeloperoxidase activity (100 mg/kg), reduction of IL-10 levels and expression of ICAM-1 in the peritoneal exudate and the mesentery (100 mg/kg), respectively. The four soluble EEMT fractions showed good results in tests for antinociceptive (H, D, E, B) and anti-inflammation (H, D, E). Only sakuranetin showed reduction of the writhing and neutrophil migration (200 mg/kg). Thus, the EEMT and soluble fractions of M. tenuiflora bark demonstrated great antinociceptive and anti-inflammatory activities, as also sakuranetin. More studies should be conducted to elucidate the mechanism of action of this compound. To the best of our knowledge, this is the first report on the antinociceptive activity of the M. tenuiflora fractions and the bioactive isolated compound sakuranetin in vivo.

Asunto(s)

Analgésicos/farmacología , Antiinflamatorios/farmacología , Flavonas/farmacología , Mimosa/química , Extractos Vegetales/farmacología , Analgésicos/química , Analgésicos/aislamiento & purificación , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Permeabilidad Capilar/efectos de los fármacos , Quimiotaxis de Leucocito/efectos de los fármacos , Citocinas/biosíntesis , Edema/inducido químicamente , Edema/tratamiento farmacológico , Flavonas/química , Flavonas/aislamiento & purificación , Expresión Génica , Hiperalgesia/inducido químicamente , Hiperalgesia/tratamiento farmacológico , Molécula 1 de Adhesión Intercelular/genética , Molécula 1 de Adhesión Intercelular/metabolismo , Masculino , Ratones , Neutrófilos/efectos de los fármacos , Neutrófilos/fisiología , Peroxidasa/metabolismo , Extractos Vegetales/química

RESUMEN

Flavanones (hesperidin, naringenin, naringin, and poncirin) in industrial, hand-squeezed orange juices and from fresh-in-squeeze machines orange juices were determined by HPLC/DAD analysis using a previously described liquid-liquid extraction method. Method validation including the accuracy was performed by using recovery tests. Samples (36) collected from different Brazilian locations and brands were analyzed. Concentrations were determined using an external standard curve. The limits of detection (LOD) and the limits of quantification (LOQ) calculated were 0.0037, 1.87, 0.0147, and 0.0066 mg 100 g(-1) and 0.0089, 7.84, 0.0302, and 0.0200 mg 100 g(-1) for naringin, hesperidin, poncirin, and naringenin, respectively. The results demonstrated that hesperidin was present at the highest concentration levels, especially in the industrial orange juices. Its average content and concentration range were 69.85 and 18.80-139.00 mg 100 g(-1). The other flavanones showed the lowest concentration levels. The average contents and concentration ranges found were 0.019, 0.01-0.30, and 0.12 and 0.1-0.17, 0.13, and 0.01-0.36 mg 100 g(-1), respectively. The results were also evaluated using the principal component analysis (PCA) multivariate analysis technique which showed that poncirin, naringenin, and naringin were the principal elements that contributed to the variability in the sample concentrations.

RESUMEN

Garcinielliptone FC (GFC) isolated from hexanic fraction seed extract of species Platonia insignis Mart. It is widely used in folk medicine to treat skin diseases in both humans and animals as well as the seed decoction has been used to treat diarrheas and inflammatory diseases. However, there is no research on GFC effects in the central nervous system of rodents. The present study aimed to evaluate the GFC effects at doses of 25, 50 or 75 mg/kg on seizure parameters to determine their anticonvulsant activity and its effects on amino acid (γ-aminobutyric acid (GABA), glutamine, aspartate and glutathione) levels as well as on acetylcholinesterase (AChE) activity in mice hippocampus after seizures. GFC produced an increased latency to first seizure, at doses 25mg/kg (20.12 ± 2.20 min), 50mg/kg (20.95 ± 2.21 min) or 75 mg/kg (23.43 ± 1.99 min) when compared with seized mice. In addition, GABA content of mice hippocampus treated with GFC75 plus P400 showed an increase of 46.90% when compared with seized mice. In aspartate, glutamine and glutamate levels detected a decrease of 5.21%, 13.55% and 21.80%, respectively in mice hippocampus treated with GFC75 plus P400 when compared with seized mice. Hippocampus mice treated with GFC75 plus P400 showed an increase in AChE activity (63.30%) when compared with seized mice. The results indicate that GFC can exert anticonvulsant activity and reduce the frequency of installation of pilocarpine-induced status epilepticus, as demonstrated by increase in latency to first seizure and decrease in mortality rate of animals. In conclusion, our data suggest that GFC may influence in epileptogenesis and promote anticonvulsant actions in pilocarpine model by modulating the GABA and glutamate contents and of AChE activity in seized mice hippocampus. This compound may be useful to produce neuronal protection and it can be considered as an anticonvulsant agent.

Asunto(s)

Conducta Animal , Pilocarpina/toxicidad , Convulsiones/metabolismo , Triterpenos/farmacología , Animales , Femenino , Masculino , Ratones , Convulsiones/inducido químicamente , Convulsiones/psicología

RESUMEN

This study describes the isolation and identification of apigenin-7-O-ghicopyranoside, a flavonoid isolated from the flowers of Bellis perennis L., Asteraceae, an species with a broad spectrum of biological activities. The in vitro antioxidant activity and the inhibition of the enzyme acetylcholinesterase were evaluated. The flavonoid showed strong in vitro antioxidant potential, because of the capacity of removal of hydroxyl radicals and nitric oxide, and also prevented the formation of thiobarbituric acid-reactive substances. These parameters were inhibited at the highest concentration of ApG at rates of 77.7%, 72% and 73.4%, respectively, in addition to inhibiting acetylcholinesterase, suggesting potential use in the treatment of neurodegenerative diseases.

Asunto(s)

Antioxidantes/farmacología , Asteraceae/química , Inhibidores de la Colinesterasa/farmacología , Flores/química , Extractos Vegetales/farmacología , Acetilcolinesterasa/efectos de los fármacos , Asteraceae/clasificación , Peroxidación de Lípido/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación

RESUMEN

Plectranthus spp (Lamiaceae) are plants of economic importance because they are sources of aromatic essential oils and are also cultivated and several species of this genus are used as folk medicines. This paper describes the effects of different concentrations of the 2,4-dichlorophenoxyacetic acid (2,4-D) and 1-naphthaleneacetic acid (NAA) on the induction of callus from nodal segments of Plectranthus ornatus Codd and in the production of volatile organic compounds (monoterpenes and sesquiterpenes). The 20 and 40 day calli were subjected to solid phase micro extraction (HS-SPME) and submitted to GCMS analysis. Variations in VOCs between the samples were observed and, a direct relationship was observed between of the major constituent detected (α-terpinyl acetate) and the monoterpenes α-thujene, α-pinene, ß-pinene, camphene, sabinene and α-limonene that were present in the volatile fractions. Besides α-terpinyl acetate, isobornyl acetate and α-limonene were also major constituents. Variations were observed in VOCs in the analyzed periods. The best cultivation media for the production of VOCs was found to be MS0 (control). Moderate success was achieved by treatment with 2.68 µM and 5:37 µM NAA (Group 2). With 2,4-D (9.0 µM), only the presence of α-terpinyl acetate and isocumene were detected and, with 2.26 µM of 2,4-D was produced mainly α-terpinyl acetate, α-thujene and ß-caryophyllene (16.2%). The VOC profiles present in P. ornatus were interpreted using PCA and HCA. The results permitted us to determine the best cultivation media for VOC production and, the PCA and HCA analysis allowed us to recognize four groups among the different treatments from the compounds identified in this set of treatments.

Asunto(s)

Monoterpenos/aislamiento & purificación , Componentes Aéreos de las Plantas/química , Plectranthus/química , Sesquiterpenos/aislamiento & purificación , Compuestos Orgánicos Volátiles/aislamiento & purificación , Cromatografía de Gases y Espectrometría de Masas , Monoterpenos/química , Monoterpenos/metabolismo , Aceites Volátiles/química , Aceites Volátiles/aislamiento & purificación , Componentes Aéreos de las Plantas/crecimiento & desarrollo , Componentes Aéreos de las Plantas/metabolismo , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Aceites de Plantas/química , Aceites de Plantas/aislamiento & purificación , Plectranthus/crecimiento & desarrollo , Plectranthus/metabolismo , Sesquiterpenos/química , Sesquiterpenos/metabolismo , Microextracción en Fase Sólida , Compuestos Orgánicos Volátiles/química , Compuestos Orgánicos Volátiles/metabolismo

RESUMEN

CONTEXT: Cratylia mollis Martius ex Benth. and Cenostigma macrophyllum Tul. (Leguminosae) are both endemic Brazilian plants and they are used by the natives as medicinal plants, and the leaves of C. mollis are also employed as forage for cattle during the dry season of region. OBJECTIVE: Isolation of the compounds responsible for the acetylcholinesterase (AChE) inhibition from the CHCl3 active extract. MATERIALS AND METHODS: Two peptidic compounds were isolated by chromatographic techniques from the CHCl3 extract of the leaves of C. mollis and C. macrophyllum. They were identified by spectrometric data analysis (MS and NMR) and they were subjected to AChE inhibition employing Ellman's test. RESULTS: The peptides were identified as N-benzoylphenylalaninoyl-phenlyalaninolacetate (aurentiamide acetate) (1) and N-benzoylphenylalaninyl-N-benzoylphenylalaninate (2). Both peptides 1 and 2 exhibit AChE inhibition, with IC50 values equal to 111.34 µM and 137.6 µM, respectively. DISCUSSION AND CONCLUSION: Compound 1 (aurentiamide acetate) has rarely been isolated from the Leguminosae family, and N-benzoylphenylalaninyl-N-benzoylphenylalaninate (2) is a compound that has never previously been isolated from this family. Compound 1 is shown to be a potent inhibitor of AChE, with IC50 values similar to the physostigmine control (141.51 µM).

Asunto(s)

Acetilcolinesterasa/efectos de los fármacos , Inhibidores de la Colinesterasa/farmacología , Fabaceae/química , Extractos Vegetales/farmacología , Acetatos/administración & dosificación , Acetatos/aislamiento & purificación , Acetatos/farmacología , Acetilcolinesterasa/metabolismo , Compuestos de Bencilo/administración & dosificación , Compuestos de Bencilo/aislamiento & purificación , Compuestos de Bencilo/farmacología , Inhibidores de la Colinesterasa/aislamiento & purificación , Dipéptidos/administración & dosificación , Dipéptidos/aislamiento & purificación , Dipéptidos/farmacología , Concentración 50 Inhibidora , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Fisostigmina/farmacología , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Hojas de la Planta