Inhibitory Effects of Euphorbia tirucalli Lineu (Euphorbiaceae) Diluted Latex on Human and Canine Melanoma Cells.

Euphorbia tirucalli Lineu (Euphorbiaceae) is a tropical and subtropical ornamental and toxic plant. E. tirucalli produces a latex that is commonly used to treat neoplasms. This study aimed to evaluate the effects of diluted E. tirucalli latex (DETL) on human (SK-MEL-28) and canine (CBMY) melanoma cells. SK-MEL-28 (3 × 103 cells/well) and CBMY (6 × 103 cells/well) were cultivated in 96-well plates. The cells were treated with 50 µl/well of dilutions (1/2, 1/4, 1/8, 1/16, 1/32, 1/64, 1/128, 1/256, and 1/512) of a standard solution containing 1 mg/mL of the E. tirucalli latex (ETL) in DMEM. Control group cells received 50 µl/well of DMEM. After 24, 48, and 72 h of treatment, cell viability was assessed by the MTT assay. There was a significant decrease in viability at 48 and 72 hours after treatment for human melanoma cells and at 24, 48, and 72 hours for canine cells, mainly in higher dilutions of ETL. Human melanoma cells presented a typical U shape curve, characteristic of hormesis. To our knowledge, this is the first study showing inhibitory effects of DETL on canine melanoma cells. Therefore, DETL is a potentially new antineoplastic drug.

The Synergistic Behavior of Antioxidant Phenolic Compounds Obtained from Winemaking Waste's Valorization, Increased the Efficacy of a Sunscreen System.

Grape pomace retains polyphenols in the peels and in the seeds after winemaking, which is indicative of the high valorization potential of this industrial waste. There is strong evidence that phenolics are robust antioxidants and confer photoprotection; thus, it is rational to apply these active compounds from winemaking waste to sunscreens, in order to increase UV protection. Despite the importance of this class of cosmetics to public health, more efficacious strategies are still needed to overcome the problems caused by the photoinstability of some UV filters. The hydroethanolic extract of Vitis vinifera L. grapes was obtained by percolation and then lyophilized. Six formulations were developed: Type I-cosmetic base and UV filters; Type II-cosmetic base and extract; and Type III-cosmetic base, extract and UV filters. Each formulation was prepared in the pHs 5 and 7. The antioxidant activities of the samples were measured by DPPH• and expressed in Trolox® equivalents (TE), and their photostability and in vitro sun protection factor (SPF) were analyzed by diffuse reflectance spectrophotometry. The anti-radical efficiencies observed in the formulations with grape extract were: (II) 590.12 ± 0.01 µmol TE g-1 at pH 5 and 424.51 ± 0.32 µmol TE g-1 at pH 7; (III) 550.88 ± 0.00 µmol TE g-1 at pH 5 and 429.66 ± 0.10 µmol TE g-1, at pH 7, demonstrating that the UV filters, butylmethoxydibenzoyl methane, ethylhexyl methoxycinnamate and ethylhexyl dimethyl 4-aminobenzoic acid had no influence on this effect. The photoprotective efficacy and the photostability of formulation III containing the extract and UV filters at pH 5 suggested that a synergism between the active molecules provided an 81% increase in SPF. Additionally, this was the only sample that maintained a broad spectrum of protection after irradiation. These results confirmed that the grape pomace extract has multifunctional potential for cosmetic use, mainly in sunscreens, granting them superior performance.

Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam. ) Pers

ABSTRACT Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE50=41.91 µg/mL) by DPPH in comparison with Trolox(r) and 11.33 mmol Trolox(r) equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids.

Evaluation of gastroprotective activity of Passiflora alata

AbstractPassiflora alata Curtis, Passifloraceae, is a liana popularly known in Brazil as ‘maracujá-doce’ that has been used for treating different illnesses. Its leaves are described in the Brazilian Pharmacopoeia, but the gastroprotective activity has never been investigated. In the present study a freeze-dried crude 60% ethanol–water extract of P. alata aerial parts was prepared. Total flavonoid content, expressed as vitexin, was 0.67% ± 0.01. The hemolytic activity was 32 units for P. alata, using Saponin (Merck®) as reference. P. alata presented EC50 of 1061.2 ± 8.5 µg/ml in the 2,2-diphenyl-1-picryhydrazyl assay and 1076 ± 85 µmol Trolox/g in the Oxygen Radical Absorbance Capacity assay. P. alata, its solvent fractions and a P. alatananopreparation were investigated for gastroprotective activity. The test samples exhibited gastroprotective activity on HCl/ethanol induced gastric mucosal lesions in rats. P. alata at doses of 100, 200 and 400 mg/kg, using the necrotizing agent at 150 mmol/l, inhibited 100% of ulcer formation (compared to the negative control), while lansoprazole (30 mg/kg) 77%. When tested against a more concentrated necrotizing agent (300 mmol/l), fractions of P. alata at 100 mg/kg reduced 57% (n-hexane), 34% (ethyl acetate) and 72% (aqueous fraction) the ulcer formation. In this assay, lansoprazole (30 mg/kg) inhibited 47%. When encapsulated, P. alata inhibited ulcer formation at 55%, 94% and 90% for dosages of 25, 50 and 100 mg/kg. These results suggest the potential use of P. alata as a gastroprotective herbal medicine.

Applying design of experiments (DOE) to flavonoid extraction from Passiflora alata and P. edulis

The Passifloraceae family is extensively used in native Brazilian folk medicine to treat a wide variety of diseases. The problem of flavonoid extraction from Passiflora was treated by application of design of experiments (DOE), as an experiment with mixture including one categorical process variable. The components of the binary mixture were: ethanol (component A) and water (component B); the categorical process variable: extraction method (factor C) was varied at two levels: (+1) maceration and (-1) percolation. ANOVA suggested a cubic model for P. edulis extraction and a quadratic model for P. alata.These results indicate that the proportion of components A and B in the mixture is the main factor involved in significantly increasing flavonoid extraction. In regard to the extraction methods, no important differences were observed, which indicates that these two traditional extraction methods could be effectively used to extract flavonoids from both medicinal plants. The evaluation of antioxidant activity of the extract by ORAC method showed that P. edulis displays twice as much antioxidant activity as P. alata. Considering that maceration is a simple, rapid and environmentally friendly extraction method, in this study, the optimized conditions for flavonoid extraction from these Passiflora species is maceration with 75% ethanol for P. edulis and 50% ethanol for P. alata.

Cytotoxicity of cashew flavonoids towards malignant cell lines.

The leaves of the Cashew plant (Anacardium occidentale L.) are used by the folk medicine in South America and West Africa. This plant is rich in flavonoids, which are polyphenolic compounds widespread in plants, and that have diverse physiological effects. In a sub-acute toxicity assay it was found that an ethanolic extract of Cashew leaves elicited lymphopenia in rats. The extract was also found to be cytotoxic and to induce apoptosis in Jurkat (acute lymphoblastic leukemia) cells. The crude ethanolic extract was fractionated and resolved by HPLC. One of the four fractions obtained led to the isolation of the biflavonoid agasthisflavone. [(3)H]-thymidine incorporation assays and flow cytometry analysis showed that the isolated compound displayed a high anti-proliferative effect in Jurkat cells with an IC(50) of 2.4 µg/ml (4.45 µM). The effect of agathisflavone on the acute promyelocytic leukemia cell line HL60, Burkitt lymphoma Raji cells and Hep-2 laryngeal carcinoma cells was also tested. The two latter ones were only mildly affected by agathisflavone. It is also shown that agathisflavone induces apoptosis in Jurkat cells and it this proposed that this is the likely mechanism of agathisflavone specific cytotoxicity.

Passiflora alata Curtis: a Brazilian medicinal plant: [review] / Passiflora alata Curtis: una planta medicinal brasileña: [revisión]

This review describes botanical, chemical, pharmacological and phytotechnological properties of Passiflora alata Curtis, with emphasis on analytical methods. Native to Brazil, P. alata is featured in several pharmaceutical preparations registered by the regulatory agency ANVISA. In four of the five editions of the Brazilian Pharmacopoeia, P. alata leaves have been included under the designation of “maracujᔠor “maracujá doce” (sweet passion fruit). This species is cited as Passiflora alata Curtis and was originally published in 1788 in the Botanical Magazine. In the last decade, phytochemical and pharmacological studies of Brazilian researchers related to this plant have increased. Despite several studies, the substances responsible for the anxiolytic, sedative, antioxidative and antiulcer activities attributed to passifloras remain unknown. Analytical methods for the quantification of markers are being developed in order to improve quality control analysis and to better understand the relationship between chemical markers and their pharmacological effects. Those methods include spectrophotometry, high performance thin-layer chromatography (HPTLC) and high performance liquid chromatography (HPLC). There is also great interest in the technological processes involved in the production of dry extracts of this native medicinal plant with the primary goal of assuring the quality of phytopharmaceutical products.

En esta revisión se describen las características botánicas, químicas, farmacológicas y fitotecnologicas de Passiflora alata Curtis, con énfasis en los métodos analíticos. Originaria de Brasil, varias preparaciones farmacéuticas de P. alata son registradas por el organismo regulador ANVISA. En tres de las cinco ediciones de la Farmacopea Brasileña, las hojas de P. alata se han incluido bajo la denominación de "maracuyá" (fruta de la pasión). Esta especie debe ser citada como Passiflora alata Curtis, publicada originalmente en 1788 en “Botanical Magazine”. En la última década, los estudios fitoquímicos y farmacológicos de investigadores brasileños relacionados con esta planta han aumentado substancialmente. A pesar de varios estudios, las sustancias responsables de las actividades ansiolítica, sedante, antioxidante y antiulcerosa atribuidas a la passiflora continúan siendo desconocidos. Los métodos analíticos para la cuantificación de los marcadores están siendo desarrollados con el fin de mejorar el análisis de control de calidad y para comprender mejor la relación entre marcadores químicos y sus efectos farmacológicos. Estos métodos incluyen espectrometría de alto rendimiento, cromatografía en capa fina (HPTLC) y la cromatografía líquida de alta resolución (HPLC). También existe un gran interés en los procesos tecnológicos envueltos en la producción de extractos secos con el objetivo principal de asegurar la calidad de los productos fitosanitarios.

Evaluation of gastroprotective activity of Plinia edulis (Vell.) Sobral (Myrtaceae) leaves in rats.

Plinia edulis, an arboreous species popularly known as "cambucá", is native to the Brazilian Atlantic Rain Forest. Despite its traditional uses, no reports are available on the safety of this utilization or on the relationship between the antiulcer activity of its extract and its phytochemical compounds. This paper reports on the investigation of the acute toxicity and gastroprotective effect of the aqueous ethanol extract of leaves of Plinia edulis on HCl/ethanol-induced ulcers. In order to correlate the secondary metabolites and the efficacy of the crude drug in traditional medicine, the extract was submitted to chromatographic fractionation after solvent partition. The extract did not show acute toxicity in mice treated with 5 g/kg p.o., but exhibited significant antiulcer activity in rats at doses of 100, 200, and 400mg/kg p.o., more active than the reference drug lansoprazole.The ethyl acetate fraction yielded beta-amyrin, oleanolic acid, ursolic acid, and maslinic acid, which were identified based on spectrometric analyses. Since antiulcerogenic activity is not restricted to one class of compounds in plants, the triterpenoids isolated in the extract can be associated with the observed effect.

Antiulcerogenic effect and acute toxicity of a hydroethanolic extract from the cashew (Anacardium occidentale L.) leaves.

The antiulcerogenic effect of a hydroethanolic extract of Anacardium occidentale L. leaves was investigated. The extract inhibited gastric lesions induced by HCl/ethanol in female rats. A dose-response effect study showed that the ED50 was 150 mg/kgb.w. Extract doses higher than 100 mg/kgb.w. were more effective than 30 mg/kg of lansoprazol in inhibiting gastric lesions. A methanolic fraction (257.12 mg/kg) which reduced gastric lesion at 88.20% is likely to contain the active principle of the antiulcer effect. No signs of acute toxicity were observed when mice were treated with extract dose up to 2000 mg/kgb.w. A chemical analysis of the extract allowed the identification of phenolic compounds as the major components. Glycosylated quercetin, amentoflavone derivate and a tetramer of proanthocyanidin were identified by liquid chromatography coupled to mass spectrometry. The level of total phenolics in the extract was evaluated at 35.5% and flavonoid content was 2.58%.

Acute, subacute toxicity and genotoxic effect of a hydroethanolic extract of the cashew (Anacardium occidentale L.).

Anacardium occidentale L. (Anacardiaceae), popularly known as cajueiro is a native plant to Brazil, and largely used in popular medicine to treat ulcers, hypertension and diarrhea. In the present study, acute, 30-day subacute toxicity and genotoxicity assays were carried out. The crude extract did not produce toxic symptoms in rats in doses up to 2000 mg/kg. Based on biochemical analyses of renal and hepato-biliary functions, such as the level of urea, creatinine, transaminases and alkaline phosphatase, we determined that the extract is generally tolerated by rats. This was also confirmed by hematological and histopathological exams. Genotoxicity was accessed by the Ames test in Salmonella typhimurium strains TA97, TA98, TA100, TA102 and by the bone marrow micronucleus test in mice. The extract was shown to induce frameshift, base pair substitution and damage to the chromosomes. However, this effect was less deleterious than the clastogenic effect of ciclophosphamide.

Antiulcerogenic effects of Campomanesia xanthocarpa.

Campomanesia xanthocarpa O. Berg., popularly known as "gabiroba", is used in Brazilian folk medicine for ulcer treatment. The hydroalcoholic extract of Campomanesia xanthocarpa leaves was evaluated for antiulcerogenic activity, acute toxicity and phytochemical profile. Oral administration of the extract at 400 mg/kg proved to be effective in preventing gastric ulceration in rats and did not produce toxic symptoms in mice in doses up to 5 g/kg. TLC screening methods revealed the presence of flavonoids, saponins and tannins.

Antiulcer activity of Sapindus saponaria L. in the rat.

Extracts of leaves and fruits of Sapindus saponaria L. were orally administered to rats and the parameters of gastric secretion (volume, pH and acidity) were evaluated after pylorus ligature. The inhibitory effect of the extracts on lesions induced by stress was compared to that of cimetidine. The volume and concentration of hydrochloric acid were reduced after oral administration of the extracts. A significant reduction of the lesion index was observed in the acute assays. No significant alteration in body or organ weight was detected in animals treated orally for 30 days with the extracts. These results suggest that S. saponaria fruits have an anti-gastric ulcer potential.

Antibacterial activity of Apocynaceae extracts and MIC of Tabernaemontana angulata stem organic extract

Trinta e oito extratos orgânicos e aquosos obtidos de 11 espécies de Apocynaceae foram submitidos a triagem utilizando o método da microdiluiçäo em caldo contra Staphylococcus aureus, Pseudomonas aeruginosa e Candida albicans. O extrato orgânico obtido do caule de Tabernaemontana angulata apresentou atividade contra a bactéria Gram positiva S. aureus. A concentraçäo inibitória mínima verificada para esse extrato variou de 2,50 a 1,25 mg/mL. Cloranfenicol foi utilizado como antimicrobiano padräo. A análise fitoquímica indicou a presença de triterpenos e alcalóides no extrato ativo.

Determinação do valor de ocncentração mínima inibitória de tinturas vegetais pelo método de diluição em meio líquido utilizando microplacas / Determination of minimum inhibitory concentration (MIC) of plant tinctures by the method of dilution in broth medium using microplates

Foram determinados os valores de concentração mínima inibitória de tinturas hidroalcoólicas a 70 por cento de folhas de araçá-pêra (Psidium acutangulum), guabiju (Myrcianthes pungens), jaboticaba (Myrciaria cauliflora), murta (Myrtus communis) e uvaia (Eugenia pyriformis) pelo método de diluição em meio de cultura líquido, utilizando tubos e microplacas. Os valores obtidos pelos dois métodos foram equivalentes, nos testes realizados com S. aureus, E.coli, C.albicans e A.niger.

Extração por fluido supercrítico

Acima de uma certa temperatura e pressão repre­sentados pelo ponto crítico, os gases não mais podem ser liquefeitos e em função do aumento da densidade passam para o que alguns consideram um estado intermediário entre o líquido e o gasoso: tornam-se "supercríticos" e podem então agir em par­te como solventes. 0 dióxido de carbono em estado supercrítico pode dissolver ou incorporar a maioria das moléculas orgânicas. Já utilizado na indústria agroalimentar, está agora entrando na indústria farmacêutica. O presente trabalho tem como objetivo apresentar o atual estágio de utilização, as vantagens e desvantagens, princípios e perspectivas de aplicação da tecnologia de extração por fluidos supercríticos, principalmente dióxido de carbono , de uma manei­ra ampla, na obtenção de insumos farmacêuticos e fitoterápicos.

The present study evaluated the antimicrobial activity of the 70 percent hydroalcoholic extract from Leonurus sibiricus l., Lamiaceae. The antimicrobial activity was determined throught the minimum inhibitory concentration (MIC). The extract of Leonurus sibiricus l. was active against Candida albicans, Staphylococcus aureus and Pseudomonas aeruginosa.

Identificacao cromatografica e acao farmacologica de extratos de Styrax camporum Pohl e Caesalpinia ferrea Martius / Chromatographic identification and pharmacologic action of Styrax camporum Pohl and Caesalpina ferrea Martius

As cascas das especies vegetais Styrax camporum Pohl, conhecida popularmente por estoraque do campo ou cuia do brejo, e Caesalpinia ferrea Martius ou pau-ferro, sao ha muito utilizadas em medicina popular como cicatrizantes e no tratamento de ulceras gastroduodenais, recentemente comprovados em trabalhos de experimentacao animal. Em funcao da dificuldade de caracterizacao dos extratos destas especies, foram padronizadas condicoes cromatograficas, que poderao ser uteis em sua identificacao. Tendo em vista que o local da ulceracao encontra-se geralmente inflamado, propoe o presente trabalho verificar se os extratos, alem da acao antiulcera, apresentam tambem acao antiinflamatoria. Como na ulceracao podem estar envolvidos tambem receptores H2 e H1, realizou-se teste de permeabilidade vascular, em que ha envolvimento de histamina, com o objetivo de verificar o possivel mecanismo de acao destes extratos

Analgesicos e antipireticos / Analgesic and antipyretic

Revisao sobre os analgesicos e antipireticos existentes no mercado com os respectivos mecanismos de acao, bem como a perspectiva do uso de plantas medicinais brasileiras.

Açäo anti-úlcera e cicatrizante de algumas plantas brasileiras / Anti-ulcer and cicatrization action of some brazilian plants

Apresentamos uma revisäo de algumas plantas brasileiras, existentes na regiäo de Säo Paulo, conhecida por sua açäo anti-ulcera e cicatrizante. As espécies citadas neste trabalho säo: sucupira, jucá, erva de bugre, taiuiá, cipó-chumbo, cipó caboclo, carobinha, saiäo, cordäo de frade, aroeira e estoraque do campo