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.

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.

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.

High dilutions of euphorbia tirucalli L. (aveloz) modify the viability and glycolytic metabolism of cell lines / Altas diluições de Euphorbia tirucalli L. (aveloz) modificam a viabilidade e o metabolismo glicolítico de linhas celulares

The latex of Euphorbia tirucalli L. (Aveloz) is popularly used to treat cancers from diverse sources such as: breast, prostate, lung and kidney. Furthermore, high dilutions of this latex (latex-HDs) have been successfully used in the treatment of tumors, although the mechanisms involved in this antitumoral activity are not yet known [...] Latex-HDs were obtained through the interaction of two procedures: 1:100 dilution in mass and agitation, using 2 solvents, water and 70% ethanol in homeopathic preparations 5, 15 and 30cH, following the Brazilian Homeopathic Pharmacopeia. Cell lines were incubated with 1 % and 10 % of latex-HDs for 24 hours. Controls treated with similar preparations without latex were incubated under the same conditions. Cell viability was analyzed by MTT assay and morphological features were assessed by May-Grunwald-Giemsa method. Cell ultrastructure was analyzed by transmission electron microscopy. Metabolic alterations were detected by spectrophotometric assay for the enzyme 6-phosphofructo-1-kinase (PFK-1) activity. 1% of ethanolic latex-HDs induced no alterations in MelanA cells viability, however Aveloz 15cH induced an increase in MCF7 cells viability. After aqueous treatment, MelanA cells viability decreased in almost all systems, whereas in MCF7 cells, an increase was detected in dynamized water systems and Aveloz 15CH. However, only water 15cH increased cell viability in comparison to control and non-dynamized water. No alterations in MCF7 morphology and ultrastructure were visualized through light microscopy or electronic microscopy, respectively. Interesting results were detected when we studied the glycolytic metabolism of both cells, giving support to evidences showing that HDs interfere in the metabolism of cell lines. Further studies are needed to better understand the mechanisms involved in this in vitro biological response to HDs.(AU)

O látex de Ephorbia tirucalli L. (aveloz) é usado popularmente no tratamento de diversos tipos de câncer incluindo mama, próstata, pulmão e rim. Além do mais, altas diluições desse látex (latex-HDs) têm sido utilizadas com sucesso no tratamento de tumores, embora o mecanismo dessa ação ainda seja desconhecido [...] As látex-HDs foram obtidas através de 2 procedimentos: diluição 1:100 em massa e agitação, com 2 solventes, água e etanol 70%, nas diluições homeopáticas 5, 15cH e 30cH de acordo com a Farmacopéia Homeopática Brasileira. As linhas celulares foram incubadas com látex-HDs 1% e 10% por 24 horas. Foram preparados controles similares sem o látex e incubados sob as mesmas condições. A viabilidade celular foi analisada através do método May-grunwald-Giemsa. A ultrastrutura celular foi analisada através de microscopia eletrônica de transmissão. As alterações metabólicas foram detectadas por ensaio de espectrofotometria para a atividade da anzima 6-fosfofructo-1-quinase (PFK-1). Látex-Hds em etanol 1% não induziram qualquer alteração na viabilidade das células MelanA, mas Aveloz 15cH induziu aumento da viabilidade das células MCF7. Após tratamento, a viabilidade das células MelanA diminuiu em quase todos os sistemas, enquanto que nas células MCF7 foi detectado aumento nos sistemas aquosos e Aveloz 15cH, mas só água 15cH aumentou a viabilidade celular por comparação ao controle e agua não dinamizada. Não foram detectadas alterações na morfologia celular por microscopis de luz quando se estudou o metabolismo glicolítico em ambas as células, demonstrando que os padrões de resposta celular dependem do tipo de solvente, metabolismo celular e procedimento de diluição. esa é a primeira vez que se mostra que as altas diluições interferem no metabolismo de linhas celulares. Outros estudos são necessários para se compreender melhor os mecanismos envolvidos nesta resposta in vitro a altas diluições de aveloz.(AU)

High dilutions of Euphorbia tirucalli L. (aveloz) modify the viability and glycolytic metabolism of cell lines / Altas diluições de Euphorbia tirucalli L. (aveloz) modificam a viabilidade e o metabolismo glicolítico de linhas celulares

The latex of Euphorbia tirucalli L. (Aveloz) is popularly used to treat cancers from diverse sources such as: breast, prostate, lung and kidney. Furthermore, high dilutions of this latex (latex-HDs) have been successfully used in the treatment of tumors, although the mechanisms involved in this antitumoral activity are not yet known [...] Latex-HDs were obtained through the interaction of two procedures: 1:100 dilution in mass and agitation, using 2 solvents, water and 70% ethanol in homeopathic preparations 5, 15 and 30cH, following the Brazilian Homeopathic Pharmacopeia. Cell lines were incubated with 1 % and 10 % of latex-HDs for 24 hours. Controls treated with similar preparations without latex were incubated under the same conditions. Cell viability was analyzed by MTT assay and morphological features were assessed by May-Grunwald-Giemsa method. Cell ultrastructure was analyzed by transmission electron microscopy. Metabolic alterations were detected by spectrophotometric assay for the enzyme 6-phosphofructo-1-kinase (PFK-1) activity. 1% of ethanolic latex-HDs induced no alterations in MelanA cells viability, however Aveloz 15cH induced an increase in MCF7 cells viability. After aqueous treatment, MelanA cells viability decreased in almost all systems, whereas in MCF7 cells, an increase was detected in dynamized water systems and Aveloz 15CH. However, only water 15cH increased cell viability in comparison to control and non-dynamized water. No alterations in MCF7 morphology and ultrastructure were visualized through light microscopy or electronic microscopy, respectively. Interesting results were detected when we studied the glycolytic metabolism of both cells, giving support to evidences showing that HDs interfere in the metabolism of cell lines. Further studies are needed to better understand the mechanisms involved in this in vitro biological response to HDs.

O látex de Ephorbia tirucalli L. (aveloz) é usado popularmente no tratamento de diversos tipos de câncer incluindo mama, próstata, pulmão e rim. Além do mais, altas diluições desse látex (latex-HDs) têm sido utilizadas com sucesso no tratamento de tumores, embora o mecanismo dessa ação ainda seja desconhecido [...] As látex-HDs foram obtidas através de 2 procedimentos: diluição 1:100 em massa e agitação, com 2 solventes, água e etanol 70%, nas diluições homeopáticas 5, 15cH e 30cH de acordo com a Farmacopéia Homeopática Brasileira. As linhas celulares foram incubadas com látex-HDs 1% e 10% por 24 horas. Foram preparados controles similares sem o látex e incubados sob as mesmas condições. A viabilidade celular foi analisada através do método May-grunwald-Giemsa. A ultrastrutura celular foi analisada através de microscopia eletrônica de transmissão. As alterações metabólicas foram detectadas por ensaio de espectrofotometria para a atividade da enzima 6-fosfofructo-1-quinase (PFK-1). Látex-Hds em etanol 1% não induziram qualquer alteração na viabilidade das células MelanA, mas Aveloz 15cH induziu aumento da viabilidade das células MCF7. Após tratamento, a viabilidade das células MelanA diminuiu em quase todos os sistemas, enquanto que nas células MCF7 foi detectado aumento nos sistemas aquosos e Aveloz 15cH, mas só água 15cH aumentou a viabilidade celular por comparação ao controle e água não dinamizada. Não foram detectadas alterações na morfologia celular por microscopis de luz quando se estudou o metabolismo glicolítico em ambas as células, demonstrando que os padrões de resposta celular dependem do tipo de solvente, metabolismo celular e procedimento de diluição. Esta é a primeira vez que se mostra que as altas diluições interferem no metabolismo de linhas celulares. Outros estudos são necessários para se compreender melhor os mecanismos envolvidos nesta resposta in vitro a altas diluições de aveloz.

Potential use of Piper nigrum ethanol extract against pyrethroid-resistant Aedes aegypti larvae.

Fractionation of Piper nigrum ethanol extract, biomonitored by assays on pyrethroid-resistant Aedes aegypti larvae yielded isolation of the larvicidal amides piperolein-A and piperine. Comparing LC50 values, the ethanol extract (0.98 ppm) was the most toxic, followed by piperolein-A (1.46 ppm) and piperine (1.53 ppm).

Potential use of Piper nigrum ethanol extract against pyrethroid-resistant Aedes aegypti larvae

Fractionation of Piper nigrum ethanol extract, biomonitored by assays on pyrethroid-resistant Aedes aegypti larvae yielded isolation of the larvicidal amides piperolein-A and piperine. Comparing LC50 values, the ethanol extract (0. 98 ppm) was the most toxic, followed by piperolein-A (1. 46ppm) and piperine (1. 53ppm).

O fracionamento do extrato etanólico de Piper nigrum biomonitorado por ensaios em larvas de Aedes aegypti resistentes a piretróides resultou no isolamento das amidas larvicidas piperoleína-A e piperina. Comparando-se os valores de CL50, o extrato etanólico (0. 98ppm) foi o mais tóxico, seguido pela piperoleína-A (1. 46ppm) e piperina (1. 53ppm).

Hypoglycemic activity of two Brazilian Bauhinia species: Bauhinia forficata L. and Bauhinia monandra Kurz.

The hypoglycemic activity of aqueous extracts from Bauhinia forficata L. and Bauhinia monandra Kurz leaves (10 percent w/v) was evaluated in normoglycemic mice. Both extracts have shown hypoglycemic activity using this methodology. It was also possible to isolate two flavonoids from B. forficata L., 3,7-di-O-alpha-rhamnopyranosylquercetin and 3,7-di-O-alpha-rhamnopyranosylkaempferol (kaempferitrin), whose structures were elucidated by usual NMR techniques. Only the quercetin derivative was identified in B. monandra aqueous extract by HPLC.

Extratos aquosos das folhas de Bauhinia forficata L. e Bauhinia monandra Kurz (10 por cento p/v) foram testados em camundongos normoglicêmicos, objetivando averiguar a sua atividade hipoglicemiante. Ambos os extratos mostraram atividade hipoglicemiante na metodologia empregada. Ainda, foi possível isolar de B. forficata L. dois flavonóides, quercetina-3,7-O-dirhamnosido e kaempferol-3,7-O-dirhamnosido, sendo as estruturas estabelecidas por técnicas clássicas de RMN. Apenas o derivado da quercetina foi identificado no extrato aquoso de Bauhinia monandra por CLAE.

Tabebuia avellanedae naphthoquinones: activity against methicillin-resistant staphylococcal strains, cytotoxic activity and in vivo dermal irritability analysis.

BACKGROUND: Methicillin-resistant Staphylococcus aureus (MRSA) and coagulase-negative staphylococcus infections are a worldwide concern. Currently, these isolates have also shown resistance to vancomycin, the last therapy used in these cases. It has been observed that quinones and other related compounds exhibit antibacterial activity. This study evaluated the antibacterial activity, toxicity and in vivo dermal irritability of lapachol extracted from Tabebuia avellanedae and derivatives against methicillin-resistant staphylococcal isolates. In addition, its mechanism of action was also analyzed. METHODS: The compounds beta-lapachone, 3-hydroxy beta N lapachone and alpha-lapachone were tested to determine the MIC values against methicillin-resistant S. aureus, S. epidermidis and S. haemolyticus strains, being the two last ones hetero-resistant to vancomycin. Experiments of protein synthesis analysis to investigate the naphthoquinones action were assessed. In vitro toxicity to eukaryotic BSC-40 African Green Monkey Kidney cell cultures and in vivo primary dermal irritability in healthy rabbits were also performed. RESULTS: The compounds tested showed antibacterial activity (MICs of 8, 4/8 and 64/128 microg/mL to beta-lapachone, 3-hydroxy beta N lapachone and alpha-lapachone, respectively), but no bactericidal activity was observed (MBC > 512 microg/mL for all compounds). Although it has been observed toxic effect in eukaryotic cells, the compounds were shown to be atoxic when applied as topic preparations in healthy rabbits. No inhibition of proteins synthesis was observed. CONCLUSION: Our results suggest that quinones could be used in topic preparations against wound infections caused by staphylococci, after major investigation of the pharmacological properties of the compounds. Studies about the use of these compounds on tumoral cells could be carried on, due to their effect in eukaryotic cells metabolism.

Brazilian phytopharmaceuticals--evaluation against hospital bacteria.

Pharmaceutical companies have demonstrated renewed interest in investigating higher plants as sources for new lead structures and also for the development of standardized phytotherapeutic agents of proven efficacy, safety and quality. This work analysed three commercial phytopharmaceuticals against multi-resistant bacteria of medical importance, including methicillin-resistant Staphylococcus aureus isolates from the Brazilian endemic clone. From the phytopharmaceuticals assayed, plants from the products 'Astmoflora' and 'Kókolos' were considered active, while plants from 'Uva do Mato' were not active in the tested concentrations, which ranged from 62.5 to 500 microg/mL. Among fractions of Aristolochia cymbifera and Myroxylon balsamum, the hexane extracts showed the best results against Staphylococcus spp. and Pseudomonas aeruginosa. These fractions showed growth inhibition of all methicillin-sensitive and -resistant Staphylococcus aureus strains and the majority of the Pseudomonas aeruginosa strains at a concentration of 500 microg/mL. Bioassay-guided fractionation of hexane extracts of Aristolochia cymbifera and Myroxylon balsamum led to the identification of the diterpene 2-oxo-populifolic acid and of the chalcone isoliquiritigenin, respectively, as antimicrobial compounds.