Characterization of phenolic compounds in Eugenia uniflora leaves by ESI(-) FT-ICR MS, analysis of cytotoxic activity on gastric adenocarcinoma (AGS cells), and anti-Helicobacter pylori activity.

Eugenia uniflora leaves are a source of flavonoids and ellagitannins, and the Brazilian population uses them to treat various diseases, including gastrointestinal disorders. This study aimed to determine if the ethanol extract and other derivatives are effective cytotoxic agents against gastric adenocarcinoma (AGS cells) and anti-H. pylori agent, its chemical composition, and mass spectrometry characterization of the more abundant compounds. The results were compared with the literature. The aqueous fraction, rich in Oenothein B and Gemin D/Hippomanin A, showed anti-H. pylori activity and higher cytotoxicity on AGS cells compared to the other samples analysed. Furthermore, the ESI(-) FT-ICR MS characterized the more abundant phenolic compounds, including Quinic Acid, Myricitrin, Gemin D/Hippomanin A, and Oenothein. Therefore, the activity of the ethanolic extract and aqueous fraction for gastric cancer and against H-pylori seems to originate from the antiproliferative and bacteriostatic effects of tannins and flavonoids.

In Vitro and In Silico Evaluation of Red Algae Laurencia obtusa Anticancer Activity.

Studies estimate that nearly 2 million new cases of gastric cancer will occur worldwide during the next two decades, which will increase mortality associated with cancer and the demand for new treatments. Marine algae of the Laurencia genus have secondary metabolites known for their cytotoxic action, such as terpenes and acetogenins. The species Laurencia obtusa has demonstrated cytotoxicity against many types of tumors in previous analyses. In this study, we determined the structure of terpenes, acetogenins, and one fatty acid of Laurencia using mass spectrometry (ESI-FT-ICR/MS). In vitro cytotoxicity assays were performed with adenocarcinoma gastric cells (AGS) to select the most cytotoxic fraction of the crude extract of L. obtusa. The Hex:AcOEt fraction was the most cytotoxic, with IC50 9.23 µg/mL. The selectivity index of 15.56 shows that the Hex:AcOEt fraction is selective to cancer cells. Compounds obtained from L. obtusa were tested by the analysis of crystallographic complexes. Molecular docking calculations on the active site of the HIF-2α protein showed the highest affinity for sesquiterpene chermesiterpenoid B, identified from HEX:AcOEt fraction, reaching a score of 65.9. The results indicate that L. obtusa presents potential compounds to be used in the treatment of neoplasms, such as gastric adenocarcinoma.

Chemical profile and cytotoxic evaluation of aerial parts of Euphorbia tirucalli L. on gastric adenocarcinoma (AGS cells).

Ethanol extract from the aerial parts of Euphorbia tirucalli L. as well as the latex of the plant suspended in water are used by the Brazilian population for the treatment of various diseases, including cancer. The purposes of this study were to determine if the ethanol extract is effective as cytotoxic agent against gastric adenocarcinoma cells (AGS) and its chemical composition by GC-MS, ESI-(-)-FT-ICR MS and (-)-ESI-LTQ-MS/MS. The results were compared with that of latex previously described by us. Hexane and aqueous fractions showed higher cytotoxicity on AGS cells. Nine triterpene compounds were detected by GC-MS in hexane fraction, including euphol and friedelin, while ellagic acid was identified as main phenolic compound in aqueous extract. Therefore, the greater cytotoxic activity of the ethanol extract of the aerial parts of Euphorbia tirucalli for gastric cancer, when compared to latex, seems to originate from the antiproliferative effects of ellagic acid and triterpenes.

Flavonoids and fractions from Saccharum officinarum L. juice: antinociceptive agents and molecular docking evaluations with µ-opioid receptor.

Opioid receptors mediate antinociceptive effects. Methanolic fractions from sugarcane varieties (MFSCf) were evaluated in classic nociception models. Interactions between bioactive compounds and the µ-opioid receptor (µOR) through docking analysis were also studied. Five methanolic fractions of sugarcane juice were obtained and analysed by LC-ESI-MS/MS. The fractions and standards of phenolic compounds were evaluated in a nociception model using the formalin test. All MFSCfs exhibited antinociceptive activity in the first phase of the formalin test. Docking analyses corroborates with the in vivo test results, suggesting that the phenolic substances are able to activate µOR. These results, for the first time, implicate phenolic constituents from sugarcane juice and other phenolic compounds in the activation of µOR. The antinociceptive activity of fractions from sugarcane juice suggests the potential pharmacological use of this species, widely cultivated in Brazil.

Analysis of Erythroxylum coca Leaves by Imaging Mass Spectrometry (MALDI-FT-ICR IMS).

Matrix-assisted laser desorption/ionization imaging mass spectrometry (MALDI IMS) can determine the chemical identity and spatial distribution of several molecules in a single analysis, conserving its natural histology. However, there are no specific studies on the spatial distribution of alkaloids in Erythroxylum coca leaves by MALDI IMS, preserving the histology of the monitored compounds. Therefore, in this work, positive-ion mode MALDI Fourier-transform ion cyclotron resonance imaging mass spectrometry (MALDI(+)FT-ICR IMS) was applied to identify and analyze the distribution of alkaloids on the surface of coca leaves, evaluating the ionization efficiency of three matrices (α-cyano-4-hydroxycinnamic acid (CHCA), 2-mercaptobenzothiazole (MBT), and 2,5-dihydroxybenzoic acid (DHB)). The last was chosen as the best matrix in this study, and it was studied in five concentrations (0.5, 1.0, 2.0, 4.0, and 8.0 mg·mL-1), where 2 mg·mL-1 was the most efficient. The washing of coca leaves with the organic solvents (acetonitrile, methanol, toluene, and dichloromethane) tested did not improve the performance of the ionization process. Finally, a tissue section, 50 µm thick, was used to study the inner part of the leaf tissue, where alkaloids and flavonoid molecules were detected.

Poly (butylene succinate) and derivative copolymer filled with Dendranthema grandiflora biolarvicide extract.

Dengue is the most important infectious disease in the world and is a severe public health problem. The chikungunya is an arbovirus, in many cases, increased, which is transmitted by the same transmitter dengue vector, Aedes aegypti. The symptoms of both diseases are similar, and infections can be lethal. Although there is no preventive vaccine against any of the two diseases, therefore, it is extremely important to control the mosquito. The eggs of A. aegypti are very resistant and hatch into larvae, which later give rise to mosquitoes in any container with water. Natural plant extracts have come from active substances with larvicidal activity against A. aegypti. However, they tend to be highly hydrophobic and need some strategy to improve its affinity for water. Because of these factors, this research aims to synthesize and characterize polymeric materials with properties suitable for the release of hydrophobic principles with larvicidal action. The synthesized polymers are poly (butylene succinate) (PBS) and PBS block copolymer with polyethylene glycol (PEG). The synthesized polymers were characterized by nuclear magnetic resonance, thermal analysis simultaneous, differential scanning calorimetry, Fourier transform infrared spectroscopy, and diffraction of X-rays analysis. The analysis results showed that the synthesized materials have chemical composition and properties suitable for use in the controlled release of actives substances. Systems were prepared using the Dendranthema grandiflora extract, which has larvicidal activity was incorporated via fusion to polymers, to evaluate its release in aqueous media. The results proved that higher amounts of PEG in the copolymer chain speed up the delivery of the larvicidal extract. Besides that, the larvicidal extract concentration required to cause death larvae of A. aegypti was achieved from the first minutes of dissolution tests, indicating that the materials developed are promising tool to fight dengue and chikungunya. This new system is a vital tool for eliminating vectors, potentially contributing to saving millions of lives worldwide.

Analytical methods to access the chemical composition of an Euphorbia tirucalli anticancer latex from traditional Brazilian medicine.

ETHNOPHARMACOLOGICAL RELEVANCE: Euphorbia tirucalli L. is widely used by Brazilian folk medicine, mainly for its anticancer activity. However, its commercialization was banned by The Brazilian National Sanitary Surveillance Agency (ANVISA) due to the presence of some compounds considered toxic, such as the diterpene esters. AIM OF THE STUDY: Chemical and biological analyses were performed with the Brazilian Euphorbia tirucalli latex to support its wide traditional use in Brazil. MATERIAL AND METHODS: Latex was collected by using two procedures, in a solution of dichloromethane: methanol (3:1, 100 mL) and in 100 mL of distilled water. The first procedure was concentrated as a crude extract and the second one was partitioned with hexane and dichloromethane. The partitions and crude extract were subjected to phytochemical analyses using three different methods: Fourier transform-ion cyclotron resonance mass spectrometry (FT-ICR MS) with electrospray ionization sources in negative mode (ESI(-)) as well as in tandem mass spectrometry ESI(-) MS/MS and Atmospheric Pressure Chemical Ionization in positive mode (APCI(+)), Gas Chromatography coupled Mass Spectrometry (GC-MS) and Nuclear Magnetic Resonance (NMR) (1H-NMR and 13C-NMR). The cytotoxic potential was evaluated using the crude extract in macrophages RAW 264.7 and Gastric Adenocarcinoma (AGS) cancer cells. The evaluation of immunomodulatory activity was made through the detection of Nitric Oxide (NO) and cytokines as Tumor necrosis factor α (TNF-α) and Interleukin-6 (IL-6). RESULTS: GC-MS showed the presence of some esters of fatty acids, for instance myristic, palmitic, stearic, oleic and linoleic acid and, mainly, triterpenes such as euphol and tirucallol. With NMR, most of the signals were related to triterpenoids euphol and tirucallol. However, when the latex was analyzed with ESI(-) FT-ICR MS, a wide variety of molecules from different classes of natural products (fatty acids, diterpenes, triterpenes, steroids) were found. On the other hand, when APCI(+)FT-ICR MS was used, the ion M+. At ratio mass-charge (m/z) 426.38567, related to triterpenes euphol and tirucallol masses, presented the most intense peak, with a mass error of -0.11, indicating high accuracy. Diterpene esters from 4-deoxyphorbol and ingenol were identified only by ESI(-)FT-ICR MS and ESI(-)FT-ICR MS/MS. When evaluated biologically, the crude latex showed immunomodulatory activity, as it reduced the production of the pro-inflammatory cytokines TNF-α, IL-6 and NO, and the effect on NO reduction was more significant, obtaining in a similar result to the N(ω)-Nitro-L-Arginine Methyl Ester (L-NAME) standards, as well as significant cytotoxic activity with half inhibitory concentration (IC50) values of 69.43 ±â€¯1.29 µg/mL against AGS without damaging healthy ones. CONCLUSION: It was verified that the Brazilian Euphorbia tirucalli latex consists mainly of the triterpenes euphol and tirucallol, which may be the main cause of the anticancer activity attributed to the plant, but many other minor compounds could have been determined by the FT-ICR MS method, such as the diterpene esters. It has antitumor potential because it acts selectively against cancer cells and it also prevents the progression of tumors, because it carries an important immunomodulatory effect.

Avocado seeds (Persea americana Mill.) prevents indomethacin-induced gastric ulcer in mice.

The long-term use of anti-inflammatory drugs is the most common cause of gastric ulcer disease, one of the major gastrointestinal disorders affecting people worldwide. Persea americana Mill. (avocado) seed is a by-product generally discarded as waste, but can be used to treat gastric disorder due to its anti-inflammatory, antioxidant and antimicrobial activities. The aim of the present study was to evaluate the potential protective effects of the ethyl acetate fraction of avocado seeds (SEAP) extracts against indomethacin-induced gastric ulcer in mice. It was found that SEAP were effective in mitigating oxidative stress through a decrease on the oxidized products levels (reduction of 90% in lipid peroxidation in plasma) and increasing superoxide dismutase enzyme (SOD) activity (4.25-fold increase compared to the indomethacin group), also preventing the rise in ulcer and lesions areas (92% of protection) and histological changes induced by indomethacin. Chemical analysis using mass spectrometry by (-)-ESI-FT-ICR MS revealed the presence of (-)-epicatechin and (+)-catechin, confirmed by HPLC-DAD, and other important phenolic compounds in avocado seeds, such as caffeoylquinic acid, flavonoids, phenylpropanoids and tannins, substances that promote inhibition of pathways involved in gastric ulcer formation. Thus, avocado seeds extract may be a suitable natural source for the prevention and treatment of gastric ulcer.

A Clinical Trial with Brazilian Arnica (Solidago chilensis Meyen) Glycolic Extract in the Treatment of Tendonitis of Flexor and Extensor Tendons of Wrist and Hand.

One of the Brazilian arnicas, Solidago chilensis Meyen, is a species of the Asteraceae family. This plant is known by this common name because it shares remarkably similar organoleptic properties with the genus Arnica L., also within the family Asteraceae. We examined the effectiveness of the S. chilensis fluid extract used externally for treating tendinitis of flexor and extensor tendons of wrist and hand in placebo-controlled double-blind clinical pharmacological studies. This study was approved by the Ethical Committee for Scientific Research in Human Beings at University Vila Velha-UVV. Two daily skin applications on the arm skin of a gel cream containing a 5% glycolic plant extract were administered to eight volunteers for 21 days. Among the volunteers, one of their arms was used as the placebo group, and the other one was used as a test group. Statistical data analyses demonstrated a significant reduction in the perception of pain in the arms in the test group, when it was compared to those receiving only the placebo.

Anti-tumor potential and acute toxicity of Jacaranda puberula Cham. (Bignoniacea).

Cancer chemotherapy is an important strategy to treat this leading cause of death worldwide and plants may constitute a source of new antineoplastic agents. This work fractionated the ethanolic extract of Jacaranda puberula leaves and studied the in vitro antitumoral action and some toxicological effects of the most bioactive fraction. Cell lines related to worldwide cancers were used. The Dichloromethane (DCM) and PP fractions were the most bioactive ones. The anti-tumoral action of the DCM fraction was higher than that of the crude EtOH extract while that of PP fraction was higher than the original one (DCM) for both breast (MCF-7), prostate (PC3) and lung (A549) tumor cells, chronic leukemia cells. The K562 cells were the most sensitive cell line. The PP fraction (20 µg/mL) cytotoxicity for these cells was similar to that of the ursolic acid triterpene or the antineoplastic ethoposide. The PP fraction inhibited K562 cell proliferation without cell cycle arrest in a specific phase or apoptosis. PP increased the mitochondrial reduction activity of lymphocytes. After a single dose by oral route, PP fraction did not induce intrinsic acute toxicity or animal death. This work demonstrated that the J. puberula fraction (PP) present high in vitro anti-tumoral effect with no cytotoxicity for immune system cells or oral acute toxicity, improving the Jacaranda puberula ethnopharmacology and reporting new biological effects for the genus Jacaranda.

Effects of natural compounds on Xenopus embryogenesis: a potential read out for functional drug discovery targeting Wnt/ß-catenin signaling.

Maternal Wnt/ß-Catenin signaling is essential to establish dorsal-specific gene expression required for axial patterning in Xenopus. Deregulation of this pathway causes axis phenotypes in frog embryos. In adult life, mutations in the Wnt pathway components are associated with many diseases, such as polyposis coli; osteoporosis-pseudoglioma syndrome (OPPG); skeletal dysplasia; neural tube defects, cancer and many others. Thus, a better understanding of Wnt/ß-catenin signaling will have great and significant impact on Biology and Medicine. In this aspect, natural compounds are potential targets as novel molecules that could modulate the Wnt pathway. For instance, flavonoids are a large group of natural compounds found in plants that modulate important cellular and molecular mechanisms related to diseases, but the specific in vivo mechanism of action of most flavonoids remain unknown. In this way, Xenopus embryos may provide an efficient model, since it is frequently used to test and identify the role of molecules that affect Wnt/ß-catenin signaling. Here, we describe a combination of approaches to outline and characterize the role of two flavonoids, quercetin and rutin, on Wnt/ß-catenin signaling, using Xenopus embryos as an experimental model. Our data support that quercetin is potential in vivo modulator of canonical Wnt signaling and that this effect might depend on the structure of this molecule, as we did not observe any effect with rutin treatment, a flavonol structurally-related to quercetin. This model is useful to analyze effects of quercetin and other flavonoids in vivo and to provide further understanding of how natural compounds can modulate signaling pathways, using Xenopus embryos as a fast and efficient reading of in vivo effects of those compounds.

Antibacterial activity and cytotoxicity analysis of halistanol trisulphate from marine sponge Petromica citrina.

OBJECTIVES: An aqueous extract and fraction from the marine sponge Petromica citrina have antibacterial activity. We performed a chemical and biological characterization of the antibiotic substance from P. citrina and investigated its mode of action on Staphylococcus aureus cells. METHODS: The inhibitory activity of the aqueous extract of P. citrina was determined against 14 bacteria belonging to type strains and clinical antibiotic-resistant strains. The aqueous extract was fractionated under bioassay guidance and the bioactive substance was identified by its (1)H-NMR, (13)C-NMR and mass spectra. The MIC and the MBC of this substance were determined. This substance was also subjected to cytotoxic bioassays. The mode of action on S. aureus cells was investigated by light and transmission electron microscopy analysis. RESULTS: P. citrina showed a large spectrum of activity against type strains and resistant-bacteria such as S. aureus, Staphylococcus epidermidis, Enterococcus faecalis, Mycobacterium fortuitum and Neisseria gonorrhoeae. The aqueous extract was fractionated and halistanol trisulphate (24ε,25-dimethylcholestane-2ß,3α,6α-triol trisodium sulphate) was isolated for the first time from P. citrina. Halistanol trisulphate had a bactericidal effect on exponentially growing S. aureus cells at the MIC (512 mg/L). Cytotoxicity biossays showed moderate toxicity against cancer cell line L929 (fibrosarcoma). This substance apparently acts by damaging the cell membrane, with subsequent cell lysis. CONCLUSIONS: Halistanol trisulphate is a broad-spectrum antibiotic isolated from P. citrina with a mode of action involving disruption of the cytoplasmic membrane. It is a new candidate for research on antibacterial substances.

Metabolite profiling of the leaves of the Brazilian folk medicine Sideroxylon obtusifolium.

Sideroxylon obtusifolium (Roem. & Schult.) T. D. Penn. (family Sapotaceae) is a tree native to Central and South America. Infusions of the bark and the leaves are used in Brazilian folk medicine as an anti-inflammatory remedy. However, information on the constituents of S. obtusifolium remains scarce, and only common pentacyclic triterpenoids have been previously reported. HPLC-DAD/MS analyses revealed that saponins and flavonoids were the main constituents of the leaves. From the butanol-soluble fraction of an ethanolic extract, a total of four saponins and ten flavonol glycosides were isolated by a combination of chromatographic methods including Sephadex LH-20, MPLC, and HPLC. Their structures were established by acid hydrolysis and spectroscopic methods, mainly MS (n), 1D and 2D NMR experiments. The compounds include the new triterpene glycoside 3-O-( ß-D-glucopyranosyl)-protobassic acid 28-O- ß-D-apiofuranosyl-(1 → 3)-O-[O- ß-D-apiofuranosyl-(1 → 3)- ß-D-xylopyranosyl-(1 → 4)]-O- α-L-rhamnopyranosyl-(1 → 2)- α-L-arabinopyranosyl ester ( 1), as well as the new flavonol glycosides, quercetin-3-O-(O- α-L-rhamnopyranosyl-(1→ 2)-O-[ ß-D-glucopyranosyl-(1 → 3)]- ß-D-galactopyranoside) ( 6) and kaempferol-3-O-(O- α-L-rhamnopyranosyl-(1 → 2)-O-[ ß-D-glucopyranosyl-(1 → 3)]- ß-D-galactopyranoside) ( 8). In addition, catechin and a glycerogalactolipid, gingerglycolipid A, were obtained from the ethyl acetate-soluble fraction. The isolated compounds could be used in the future as chemical markers for quality control of this herbal drug.

Effects of supplemental UV-A on the development, anatomy and metabolite production of Phyllanthus tenellus cultured in vitro.

Phyllanthus tenellus is widely used for its antiviral, analgesic and hepatoprotective properties. Although the production of several chemical classes of secondary metabolites is influenced by UV radiation, particularly phenolic compounds, we also know that UV radiation can result in anatomical and developmental damage. However, the morphological, anatomical and phytochemical changes in response to UV-A exposure are generally understudied in the Phyllanthaceae. Therefore, we evaluated the effects of UV-A radiation on plant development and leaf anatomy, as well as the production of secondary metabolites and the contents of carotenoids and chlorophylls a and b, in P. tenellus. To accomplish this, in vitro cultures of P. tenellus were maintained for 60 days under white light (WL) and WL plus UV-A radiation. Results showed different phenotypic responses under additional UV-A, such as high phenolic metabolite production, increasing dimensions of abaxial epidermis and thickness of palisade parenchyma. Compared to plants cultured under WL, UV-A radiation caused damage to plant morphogenesis, including a reduced number of branches and shoots, consequently reducing the rate of proliferation. On the other hand, geraniin, ellagic acid and carotenoid contents increased after UV-A exposure, indicating that this light source is an important resource for inducing phenolic compounds.

Antioxidant activity from the leaf extracts of Jacaranda puberula Cham., Bignoniaceae, a Brazilian medicinal plant used for blood depuration / Atividade antioxidante do extrato das folhas de Jacaranda puberula Cham., Bignoniaceae, uma planta medicinal Brasileira usada como depurativo do sangue

The antioxidant activity of leaf extracts from Jacaranda puberula Cham., Bignoniaceae, was assayed by the DPPH (2,2-diphenyl-1-picryl-hydrazyl) free radical scavenging method. Three phytomedicines (F1, F2, and F3) used as blood depurative, were tested by the same method. The free radical scavenger potential was measured by the discoloration of the solution. The EC50 values from Gingko bilobaEGb 761® extract and rutin, used as antioxidant for medical purposes, were used as reference. The ethanol extract (EE), ethyl acetate (EA), butanol (EB), aqueous (EAq) and the sample A (obtained from extract EB), showed lower EC50 values than other extracts and phytomedicines. The antioxidant activity (AA) of the extracts was related with the presence of the polyphenol compounds such as verbascoside (1) and cis-caffeoyl aldehyde (2). These structures were determined by chemical and spectroscopic methods and comparison with literature data.

Os extratos obtidos a partir das folhas de Jacaranda puberulaCham., Bignoniaceae, foram avaliados quanto à atividade antioxidante utilizando-se o método do radical livre DPPH (2,2-difenil-1-picril-hidrazila). Também foram incluídos na avaliação três medicamentos fitoterápicos comerciais (F1, F2 e F3) indicados como depurativos do sangue. Através da descoloração das soluções testadas, foi possível medir o potencial sequestrador do radical DPPH. Como referência, utilizou-se os dados da literatura de CE50 do extrato padronizado de Gingko bilobaEGb 761® e o flavonoide rutina, ambos empregados em medicamentos com atividade antioxidante. Entre os extratos testados, os que apresentaram valores baixos de CE50 foram os extratos etanólico bruto (EE), em acetato de etila (EA), em butanol (EB), aquoso (EAq) e da amostra A, obtida do extrato EB. Os fitoterápicos comerciais apresentaram altos valores de CE50. Com base nos resultados das análises feitas por de RMN de 13C e ¹H, CLAE-DAD e de acordo com os dados da literatura, a presença de substâncias fenólicas como o verbascosídeo (1) e o aldeído cis-caféico (2), contribuíram para a atividade antioxidante (AA) dos extratos ativos.

Ceanothane and lupane type triterpenes from Zizyphus joazeiro - an anti-staphylococcal evaluation.

The present paper describes the phytochemical and anti-staphylococcal activity investigation of the dichloromethane extract of the Brazilian plant Zizyphus joazeiro Mart. The purification steps were guided by bioassays against 17 bacterial strains of clinical sources, including methicillin-resistant (MRSA) and -sensitive (MSSA) Staphylococcus aureus as well as MRSA (ATCC 33591) and MSSA (ATCC 29213) reference strains. One of the more active fractions is comprised of three lupane-type triterpenes, the methylbetulinate (1) as well as the known betulinic (2) and alphitolic (3) acids and, for the first time in the Z. joazeiro, two ceanothane type triterpenes, the methylceanothate (4) and the epigouanic acid A (5). These substances were assayed against one clinical (PVL+) and the reference strains of S. aureus as well as the ATTC 12228 strain of S. epidermidis, in concentrations that varied from 128 to 0.125 microg/mL in order to establish the minimum inhibitory concentration (MIC) of the drugs. The minimum bactericide concentration (MBC) was also evaluated to distinguish the bactericidal from bacteriostatic activity of the crude fractions and single compounds. Compounds 3 and 4 possess the highest antibacterial activity. They inhibit all bacteria tested at 32 microg/mL and 16 microg/mL, respectively, while the other compounds showed no activity at 128 microg/mL. In contrast to single compounds, the triterpenoid fraction showed bactericidal activity at 256 microg/mL. Structural elucidations are based on 1D and 2D NMR spectroscopy as well as HR-FT-ICR-MS experiments.

Physical chemical and citotoxic evaluation of highly diluted solutions of Euphorbia tirucalli L. prepared through the fifty milesimal homeopathic method / Avaliação físico-química e citotóxica de soluções altamente diluídas de euphorbia tirucalli l. Preparada pelo método cinqüenta milesimal (lm) / Evaluación físico-química y citotóxica de soluciones altamente diluídas de Euphorbia tirucalli L. preparadas por el método homeopático cincuenta milesimal (LM)

Motivação: Embora Hahnemann tenha descrito o método LM na 6ª. Edição do Organon da Arte de Curar, poucas pesquisas tem sido feitas sobre as propriedades físico-químicas destas preparações. Além disso, ainda não existem evidências que apontem para a correlação entre propriedades físico-químicas e os efeitos biológicos das altas diluições. Objetivos: determinar características físico-químicas das preparações LM tais como condutividade elétrica, pH e índice de refração, bem como o efeito biológico em modelos experimentais. Materiais e Métodos: foi analisada uma série de diluições desde 1 lm até 10 lm de Euphorbia tirucalli L., preparada a partir do látex e do suco da planta. Para considerar as características sazonais desta planta, usamos 2 populações diferentes, colhidas uma em Junho de 2007 e outra em Maio de 2008. Além disso, o efeito citotóxico da Euphorbia tirucalli L. 5 lm foi testado em células humanas cancerosas (MCF7) através de ensaio MTT. Conclusões: Algumas diferenças entre as duas populações foram observadas. No entanto, nenhuma correlação clara pode ser observada entre as propriedades físico-químicas e a atividade biológica.(AU)

Background: although Hahnemann described the fifty-milesimal (LM) method in the 6th edition of the Organon of the Medical Art, very little research has been carried out on the physical chemical properties of these homeopathic preparations. Furthermore, there is still no evidence allowing for the correlation between the alleged physical chemical properties and the biological effects of high dilutions. Aims: to evaluate physical chemical characteristics of LM preparations including electrical conductivity, pH and refraction index, and their effect on biological experimental models. Materials and methods: preparations tested for physical chemical analysis were dilutions 1 lm to 10 lm of Euphorbia tirucalli L. prepared from the latex and the juice of the plant. To rule the seasonal characteristics of this plant, 2 different populations were used, one collected in June 2007 and the other in May 2008. Furthermore, the cytotoxic effect of Euphorbia tirucalli 5 lm was tested on human breast cancer cells (MCF7) through MTT assay. Conclusions: Some differences among the two collections were observed. However, any clear correlation could be observed between physical chemical properties and biological activity.(AU)

Motivación: Aunque Hahnemann describió el métodocincuenta milesimal (LM) en la 6 ª edición del Organon del Arte Médica, muy poca investigación se ha realizado sobre las propiedades físico-químicas de estos preparados homeopáticos. Por otra parte, todavía no hay pruebas que permitan la correlación entre las presuntas propiedades físico-químicas y los efectos biológicos, de las altas diluciones. Objetivos: evaluar las características físico-químicas de los preparados LM, incluyendo conductividad eléctrica, pH y el índice de refracción, y su efecto en modelos biológicos experimentales. Materiales y métodos: las muestras para el análisis físico-químico fueron diluciones 1 a 10 lm de Euphorbia tirucalli L. preparadas a partir del látex y el jugo de la planta. Para descartar las características sazonales de esta planta, dos poblaciones diferentes fueron utilizadas, una recogida en junio de 2007 y otro en mayo de 2008. Además, el efecto citotóxico de Euphorbia tirucalli 5 lm fue probado en células humanas de cáncer de mama (MCF7) a través del ensayo MTT. Conclusiones: Algunas diferencias entre las dos colecciones se observaron. Sin embargo, ninguna correlación clara se observó entre las propiedades físicas- químicas y actividad biológica.(AU)

Physical chemical and citotoxic evaluation of highly diluted solutions of Euphorbia tirucalli L. prepared through the fifty milesimal homeopathic method / Avaliação físico-química e citotóxica de soluções altamente diluídas de euphorbia tirucalli l. Preparada pelo método cinqüenta milesimal (lm) / Evaluación físico-química y citotóxica de soluciones altamente diluídas de Euphorbia tirucalli L. preparadas por el método homeopático cincuenta milesimal (LM)

Motivação: Embora Hahnemann tenha descrito o método LM na 6ª. Edição do Organon da Arte de Curar, poucas pesquisas tem sido feitas sobre as propriedades físico-químicas destas preparações. Além disso, ainda não existem evidências que apontem para a correlação entre propriedades físico-químicas e os efeitos biológicos das altas diluições. Objetivos: determinar características físico-químicas das preparações LM tais como condutividade elétrica, pH e índice de refração, bem como o efeito biológico em modelos experimentais. Materiais e Métodos: foi analisada uma série de diluições desde 1 lm até 10 lm de Euphorbia tirucalli L., preparada a partir do látex e do suco da planta. Para considerar as características sazonais desta planta, usamos 2 populações diferentes, colhidas uma em Junho de 2007 e outra em Maio de 2008. Além disso, o efeito citotóxico da Euphorbia tirucalli L. 5 lm foi testado em células humanas cancerosas (MCF7) através de ensaio MTT. Conclusões: Algumas diferenças entre as duas populações foram observadas. No entanto, nenhuma correlação clara pode ser observada entre as propriedades físico-químicas e a atividade biológica.

Background: although Hahnemann described the fifty-milesimal (LM) method in the 6th edition of the Organon of the Medical Art, very little research has been carried out on the physical chemical properties of these homeopathic preparations. Furthermore, there is still no evidence allowing for the correlation between the alleged physical chemical properties and the biological effects of high dilutions. Aims: to evaluate physical chemical characteristics of LM preparations including electrical conductivity, pH and refraction index, and their effect on biological experimental models. Materials and methods: preparations tested for physical chemical analysis were dilutions 1 lm to 10 lm of Euphorbia tirucalli L. prepared from the latex and the juice of the plant. To rule the seasonal characteristics of this plant, 2 different populations were used, one collected in June 2007 and the other in May 2008. Furthermore, the cytotoxic effect of Euphorbia tirucalli 5 lm was tested on human breast cancer cells (MCF7) through MTT assay. Conclusions: Some differences among the two collections were observed. However, any clear correlation could be observed between physical chemical properties and biological activity.

Motivación: Aunque Hahnemann describió el métodocincuenta milesimal (LM) en la 6 ª edición del Organon del Arte Médica, muy poca investigación se ha realizado sobre las propiedades físico-químicas de estos preparados homeopáticos. Por otra parte, todavía no hay pruebas que permitan la correlación entre las presuntas propiedades físico-químicas y los efectos biológicos, de las altas diluciones. Objetivos: evaluar las características físico-químicas de los preparados LM, incluyendo conductividad eléctrica, pH y el índice de refracción, y su efecto en modelos biológicos experimentales. Materiales y métodos: las muestras para el análisis físico-químico fueron diluciones 1 a 10 lm de Euphorbia tirucalli L. preparadas a partir del látex y el jugo de la planta. Para descartar las características sazonales de esta planta, dos poblaciones diferentes fueron utilizadas, una recogida en junio de 2007 y otro en mayo de 2008. Además, el efecto citotóxico de Euphorbia tirucalli 5 lm fue probado en células humanas de cáncer de mama (MCF7) a través del ensayo MTT. Conclusiones: Algunas diferencias entre las dos colecciones se observaron. Sin embargo, ninguna correlación clara se observó entre las propiedades físicas- químicas y actividad biológica.

Vasodilator activity of extracts of field Alpinia purpurata (Vieill) K: Schum and A. zerumbet (Pers.) Burtt et Smith cultured in vitro / Vasodilatador de extratos de Alpinia purpurata campo (Vieill) K. Schum e A. zerumbet (Pers.) Burtt et Smith cultivadas in vitro

Nowadays, the high blood pressure is one of the main causes of death and cardiovascular diseases. Vasodilator drugs are frequently used to treat arterial hypertension. Experiments were undertaken to determine whether hydroalcoholic extracts obtained from leaves of field-grown Alpinia purpurata and A. zerumbet cultured in vitro under different plant growth regulators induce a vasodilator effect on Wistar rat mesenteric vascular bed pre-contracted with norepinephrine. Plant extracts were able to induce a long-lasting endothelium-dependent vasodilation. Efficiency on activity of A. purpurata reached 87 percent at concentration of 60 μg. The extract of A. zerumbet maintained in medium containing IAA, induced the relaxation (17.4 percent) at 90 μg, as compared to the control (MS0) that showed a better vasodilator effect (60 percent). These results are in agreement with the quantification of phenolic compounds in the extracts, which were 50 percent lower for those plants cultured in IAA. A. purpurata was assayed for the first time in relation to its vasodilator activity. This paper showed a strong probability of correlation between the pharmacological activities of A. purpurata with their content in phenolic compounds.

Atualmente, a hipertensão arterial é uma das maiores causas de morte e de doenças cardiovasculares. Os vasodilatadores são freqüentemente utilizados no tratamento da hipertensão. Extratos hidroalcoólicos de Alpinia purpurata de campo e de A. zerumbet cultivada in vitro sob diferentes reguladores de crescimento vegetal foram ensaiados no leito mesentérico de ratos Wistar. Os extratos de A. purpurata e A. zerumbet produziram efeito vasodilatador com padrão de resposta dose-dependente de duração prolongada. Extratos da espécie A. purpurata tiveram efeito vasodilatador de 87 por cento na dose de 60 μg. O extrato obtido de folhas de A. zerumbet oriundas das culturas mantidas em meio contendo AIA (ácido indol acético) inibiu o relaxamento (17,4 por cento) na dose de 90 μg em relação ao controle (MS0), com o qual foi verificado melhor efeito vasodilatador (60 por cento). Estes resultados estão de acordo com a concentração de fenóis totais que foi 50 por cento menor para os extratos de plantas cultivadas in vitro em AIA. A espécie A. purpurata foi pela primeira vez ensaiada quanto à atividade vasodilatadora. Os resultados obtidos indicaram a presença de substâncias fenólicas provavelmente correlacionadas à ação terapêutica de A. purpurata.

Atividade antiviral de Musa acuminata Colla, Musaceae / Antiviral activity of Musa acuminata Colla, Musaceae

O presente trabalho avalia a atividade antiviral de extratos e frações de Musa acuminata Colla, Musaceae, coletada em duas regiões do Estado do Rio de Janeiro (Petrópolis e Santo Antônio de Pádua). As inflorescências de M. acuminata apresentaram excelente atividade para os dois vírus avaliados: herpesvírus simples humano tipo 1 e herpesvírus simples humano tipo 2, ambos resistentes ao Aciclovir. Os resultados indicam que os extratos de M. acuminata testados podem constituir alvo potencial para uso em terapias antivirais.

This study evaluates the antiviral activity of extracts and fractions of Musa acuminata Colla collected in two regions of Rio de Janeiro State (Petrópolis and Santo Antônio de Pádua). The inflorescences of M. acuminata showed excellent activity for the two virus evaluated: simple human herpesvirus type 1 and simple human herpesvirus type 2, both resistant to Acyclovir. The results indicate that the tested extracts of M. acuminata can be potential target for use in antiviral therapy.