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

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

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 This work describes the establishment of procedures to induce in vitro callogenesis from Poincianella pyramidalis (Tul.) L. P. Queiroz, Fabaceae, explants. Nodal, internodal and leaf segments were isolated from in vitro germinated seedlings and cultured in MS medium with 0, 2.5, 5 and 10 mg l-1 of 2,4-dichlorophenoxyacetic acid. After 30 days, the explants with induced callus showed a quadratic response for the segments nodal, internodal and leaf, with increasing the callus formation in 2,4-dichlorophenoxyacetic acid concentrations of 6.28, 6.49 and 4.91 mg l-1, respectively. In 30 days there was a linear oxidation rise with the increase to the 2,4-dichlorophenoxyacetic acid. After 60 days, oxidation values were minimum, at 2,4-dichlorophenoxyacetic acid concentrations of 5.13 mg l-1 (internodal) and 3.98 mg l-1 (leaf). The highest callus production was observed after 30 days in the presence of 6.09 mg l-1, 5.82 mg l-1 and 4.91 mg l-1 of 2,4-dichlorophenoxyacetic acid in nodal, internodal and leaf segments, respectively. After 60 days these segments showed peaks of production at 7.0 mg l-1 (nodal), 6.15 mg l-1 (internodal) and 5.08 mg l-1 (leaf) of 2,4-dichlorophenoxyacetic acid. For callus induction the intake of 2,4-dichlorophenoxyacetic acid was essential. The greater intensity in callus formation was observed in 4.91 mg l-1 in leaf segments after 30 days.

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

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

RESUMEN

BACKGROUND: Volatile oils from fresh roots, stems, leaves and seeds of Piper klotzschianum (Piperaceae) were obtained by hydrodistillation and analysed by GC-FID and GC-MS. In total, 25 components, representing more than 95% of the examined oils, were identified. The essential oils were evaluated against Artemia salina Leach nauplii and fourth-instar Aedes aegypti larvae. RESULTS: The major chemical constituents that were identified from various parts of this plant were 1-butyl-3,4-methylenedioxybenzene and 2,4,5-trimethoxy-1-propenylbenzene in the root, 1-butyl-3,4-methylenedioxybenzene in the stems and leaves and 1-butyl-3,4-methylenedioxybenzene, limonene and α-phellandrene in the seeds. The biological activities of these essential oils generally exhibited high toxicity against A. salina, with LC50 values that ranged from 7.06 to 15.43 µg mL(-1), and significant larvicidal activity against fourth-instar A. aegypti larvae was observed in the essential oils from the seeds (LC50 of 13.27 µg mL(-1)) and roots (LC50 of 10.0 µg mL(-1)) of the plant. CONCLUSION: The present study indicates that both essential oil of P. klotzsdhianum and the isolate 1-butyl-3,4-methylenedioxybenzene are potential resources for A. aegypti larva control. This is the first report of the biological activities of the oil and isolated compound.

Asunto(s)

Insecticidas/química , Insecticidas/farmacología , Larva/efectos de los fármacos , Aceites Volátiles/química , Aceites Volátiles/farmacología , Piper/química , Aceites de Plantas/química , Aceites de Plantas/farmacología , Aedes/efectos de los fármacos , Aedes/crecimiento & desarrollo , Animales , Artemia/efectos de los fármacos , Control de Insectos , Larva/crecimiento & desarrollo , Estructura Molecular

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

Betulinic, ursolic and oleanolic acids isolated from the aerial parts of Eriope blanchetii (Lamiaceae) were subjected to different esterification reactions, yielding 12 C-3 position ester derivatives. All compounds were identified using spectroscopic techniques, such as IR, 1H-NMR and MS. The derivatives were further investigated for their antioxidant level, Artemia salina lethality and antimicrobial activity.

Asunto(s)

Ácido Oleanólico/farmacología , Triterpenos/farmacología , Animales , Artemia/efectos de los fármacos , Ésteres/química , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/farmacología , Lamiaceae/química , Resonancia Magnética Nuclear Biomolecular , Ácido Oleanólico/química , Triterpenos Pentacíclicos , Extractos Vegetales/química , Triterpenos/química , Ácido Betulínico , Ácido Ursólico

RESUMEN

Approximately 600-700 species of Ipomoea, Convolvulaceae, are found throughout tropical and subtropical regions of the world. Several of those species have been used as ornamental plants, food, medicines or in religious ritual. The present work reviews the traditional uses, chemistry and biological activities of Ipomoea species and illustrates the potential of the genus as a source of therapeutic agents. These species are used in different parts of the world for the treatment of several diseases, such as, diabetes, hypertension, dysentery, constipation, fatigue, arthritis, rheumatism, hydrocephaly, meningitis, kidney ailments and inflammations. Some of these species showed antimicrobial, analgesic, spasmolitic, spasmogenic, hypoglycemic, hypotensive, anticoagulant, anti-inflammatory, psychotomimetic and anticancer activities. Alkaloids, phenolics compounds and glycolipids are the most common biologically active constituents from these plant extracts.

RESUMEN

This work reports isolation of an unusual lignan with a bicyclic [2.2.2] octene skeleton, named rufescenolide (1), from stems of Cordia rufescens, along with ß-sitosterol, stigmasterol, syringaldehyde, 3-ß-O-D-glucopyranosyl-sitosterol, methyl caffeate, 4-methoxy-protocatechuic acid and methyl rosmarinate. Structural characterizations employed IR spectroscopic, ESIHRMS and mono and dimensional NMR spectroscopy.

Asunto(s)

Compuestos Bicíclicos con Puentes/aislamiento & purificación , Ácidos Cafeicos/química , Cordia/química , Lignanos/química , Octanos/química , Compuestos Bicíclicos con Puentes/química , Hidroxibenzoatos/química , Lignanos/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Estructura Molecular , Octanos/aislamiento & purificación , Tallos de la Planta/química , Sitoesteroles/química , Sitoesteroles/aislamiento & purificación , Estigmasterol/química , Estigmasterol/aislamiento & purificación

RESUMEN

Bergenin (1) is a C-glucoside of 4-O-methylgallic acid with known antiarthritic activity attributed to modulation of cytokine production. The present study was undertaken to evaluate whether 1 has antinociceptive properties in models of inflammatory pain and to investigate its possible mechanisms of action. Pretreatment with 1 (12.5-100 mg/kg, ip) produced a dose-related inhibition of acetic acid-induced writhing in mice. Furthermore, treatment with 1 (50 and 100 mg/kg) inhibited both the early and late phases in a formalin test. In addition, 1 (50 and 100 mg/kg, ip) inhibited mechanical hyperalgesia, edema, and paw production of hyperalgesic cytokines (TNF-α and IL-1ß) induced by complete Freund's adjuvant. However, the local production of IL-10, an anti-inflammatory cytokine, was not altered by 1 (100 mg/kg, ip). Treatment with 1 produced a similar profile of antinociception in wild-type and IL-10-deficient mice. Mice treated with 1 did not show any motor performance alterations or apparent systemic toxicity. The results presented herein demonstrate that bergenin has consistent antinociceptive and anti-inflammatory properties, acting by the inhibition of IL-1ß and TNF-α production, and suggest its potential for the control of inflammatory pain.

Asunto(s)

Analgésicos/farmacología , Antiinflamatorios no Esteroideos/farmacología , Benzopiranos/farmacología , Dolor/tratamiento farmacológico , Analgésicos/química , Animales , Antiinflamatorios no Esteroideos/química , Benzopiranos/química , Relación Dosis-Respuesta a Droga , Edema/inducido químicamente , Edema/tratamiento farmacológico , Ácido Gálico/análogos & derivados , Ácido Gálico/química , Interleucina-10/antagonistas & inhibidores , Interleucina-10/biosíntesis , Interleucina-10/genética , Masculino , Ratones , Dolor/inducido químicamente , Dimensión del Dolor , Factor de Necrosis Tumoral alfa/antagonistas & inhibidores , Factor de Necrosis Tumoral alfa/biosíntesis

RESUMEN

Phytochemical investigation of the aerial parts of Eriope blanchetii and E. latifolia (Lamiaceae) yielded podophyllotoxin, as well as the aryltetralin lignans α- and ß-peltatin and yatein. Oleanolic, ursolic and epikatonic acids were also isolated. This is the first occurrence of podophyllotoxin in the family.

Asunto(s)

Lamiaceae/química , Lignanos/aislamiento & purificación , Podofilotoxina/farmacología , Tetrahidronaftalenos/aislamiento & purificación , Cromatografía en Capa Delgada , Espectroscopía de Resonancia Magnética , Espectrometría de Masa por Ionización de Electrospray

RESUMEN

Rutaceae is a taxon with species very well distributed in Brazilian semi-arid area, commonly used in folk medicine. Species from this genus have diverse biological activity described in literature. In this work, immunomodulatory and bactericidal activity are described for chloroform and ethyl acetate extracts of three of them (Esenbeckia grandiflora Mart., Pilocarpus spicatus A.St.-Hil. and Galipea simplicifolia Schult.). Initially all the samples had their cytotoxicity evaluated, aiming to determine the LC50. The immunomodulatory potential was evaluated in cultures of murine splenocytes stimulated or not with concanavalin A and in a mixed lymphocyte reaction (MLR) using splenocytes from BALB/c (H-2d) mice immunized with splenocytes from C57Bl/6 (H-2b) mice. Four samples had higher values of lymphoproliferation inhibition in concanavalin A-stimulated cultures and were evaluated in MLR. The antibacterial activity of extracts was also evaluated and the minimal inhibitory concentrations (MIC) for two active samples were 1.0 and 5.0 mg/ml for extracts from Esenbeckia grandiflora Mart. and Galipea simplicifolia Schult., respectively. Thus, our results reinforce data of literature relating biological activity for many species of the Rutaceae family and encourage studies with these species aiming to discover active compounds, candidates to new medicines.

---

A família Rutaceae apresenta espécies vegetais muito bem distribuídas no Semi-Árido Brasileiro e comumente usadas em medicina popular. Espécies dessa família tem diversas atividades biológicas descritas na literatura. Neste trabalho, atividades imunomoduladora e bactericida são descritas para o extrato acetato de etila e clorofórmico de três espécies da família (Esenbeckia grandiflora Mart., Pilocarpus spicatus A.St.-Hil. e Galipea simplicifolia Schult.). Todas as amostras foram inicialmente avaliadas quanto à sua citotoxicidade, com objetivo de determinar a LC50. O potencial imunomodulador foi avaliado em culturas de esplenócitos murinos estimulados ou não com concanavalina A e também em reação mista linfocitária (RML), usando também esplenócitos de camundongos BALB/c (H-2d) imunizados com esplenócitos de camundongos C57Bl/6 (H-2b). Quatro amostras tiveram os mais elevados valores percentuais de inibição da proliferação de linfócitos ativados pela concanavalina A e foram avaliados em RML. A atividade antibacteriana dos extratos foi também avaliada e a concentração mínima inibitória (CMI) para duas amostras ativas foi de 1.0 e 5.0 mg/mL, respectivamente para as espécies Esenbeckia grandiflora Mart. and Galipea simplicifolia Schult. Assim, os dados aqui apresentados reforçam informações da literatura científica relacionados à atividade biológica para muitas espécies da família Rutaceae e incentivam outros estudos com estas visando descobrir substâncias ativas, potenciais candidatas a novos fármacos.

RESUMEN

Chemical investigation of the leaves of Waltheria brachypetala Turks (Sterculiaceae) resulted in the isolation of quinolinone alkaloids, waltherione-A, waltherione-B (N-methylwaltherione-A), 8-methoxyflindersine, and the cyclic peptide alkaloid waltherine. The inhibition of activity of acetylcholinesterase (AChE) by the alkaloids was evaluated. Waltherione-A, waltherione-B and waltherine showed significant activity.

Asunto(s)

Acetilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/farmacología , Malvaceae/química , Péptidos Cíclicos/farmacología , Hojas de la Planta/química , Quinolinas/farmacología , Relación Dosis-Respuesta a Droga , Estructura Molecular , Péptidos Cíclicos/química , Quinolinas/química

RESUMEN

The family Boraginaceae is widely distributed in Brazil and in the Northeastern region some species are popularly used to treat symptoms of rheumatism, painful menstruation and dyspepsia. In this work we studied Cordia superba Cham. and C. rufescens A. DC., native from Brazilian Semi-arid region, in order to investigate their immunomodulatory activity. Six extracts were prepared from aerial parts of C. superba and C. rufescens. The cytotoxicity was evaluated using splenocytes from BALB/c mice. The immunomodulatory activity was determined by in vitro assays using activated mouse macrophages and lymphocytes. Peritoneal macrophages obtained from BALB/c mice were stimulated with IFN-gamma and LPS in the presence/absence of the samples. The NO production was measured indirectly through Griess method. Three samples inhibited the production of nitric oxide in values near 50 percent at a concentration of 100 µg/mL. To evaluate the effects of the extracts on lymphocytes, splenocytes from BALB/c mice were incubated with the samples and concanavalin A. Proliferation inhibition was determined by analysis of ³H-thymidine uptake. Samples from the two species had a strong inhibitory activity on lymphocyte proliferation and IL-2 production. Two chloroform extracts prepared from aerial parts of C. rufescens had the lowest IC50 values (7.6 and 11.0 µg/mL).

---

A família Boraginaceae é amplamente distribuída no Brasil e na região nordeste algumas espécies são usadas popularmente no tratamento de reumatismo, dores menstruais e dispepsias. Neste trabalho foram estudadas as espécies Cordia superba Cham. and C. rufescens A. DC., nativas da região semi-árida brasileira, objetivando investigar a atividade imunomoduladora. Seis extratos foram preparados a partir de partes aéreas das espécies. A citotoxicidade foi avaliada usando culturas de esplenócitos de camundongos BALB/c. A atividade imunomoduladora foi determinada por ensaios in vitro usando macrófagos e linfócitos murinos ativados. Macrófagos peritoneais obtidos de camundongos BALB/c foram estimulados com IFN-gama and LPS na presença/ausência das amostras. A produção de NO foi medida indiretamente através do método de Griess. Três amostras inibiram a produção de NO em valores próximos a 50 por cento (100 µg/mL). Os efeitos das amostras sobre os linfócitos foram avaliados cultivando esplenócitos de camundongos BALB/c em presença destas amostras e de concanavalina A. A proliferação foi determinada pela análise da incorporação de ³H-tritiada. Amostras de duas espécies apresentaram uma forte atividade inibidora sobre a proliferação de linfócitos e sobre a produção de IL-2. Dois extratos clorofórmicos (partes aéreas de C. rufescens) tiveram os menores valores de IC50 (7,6 and 11,0 µg/mL).

Asunto(s)

Boraginaceae/inmunología , Cordia/inmunología , Extractos Vegetales