Safety and Photoprotective Efficacy of a Sunscreen System Based on Grape Pomace (Vitis vinifera L.) Phenolics from Winemaking.

In winemaking, a large amount of grape pomace is produced that is rich in polyphenolics and highly beneficial for human health, as phenols are useful for skin ultraviolet (UV) protection. In this investigation, we evaluated the safety and clinical efficacy of a sunscreen system containing a grape pomace extract from Vitis vinifera L. as a bioactive ingredient. The recovery of phenolics in the waste was performed by percolation. Nine emulsions were developed using a factorial design and two were evaluated clinically: Formulation E, containing only UV filters (butylmethoxydibenzoyl methane, ethylhexyl methoxycinnamate and ethylhexyl dimethyl PABA), and F, with the extract at 10.0% w/w + UV filters. The antioxidant activity was determined by the DPPH assay and the in vitro efficacy was established by sun protection factor (SPF) measurements (Labsphere UV-2000S). Clinical tests were performed to determine safety (human repeated insult patch test) and to confirm efficacy (photoprotective effectiveness in participants). The results showed a synergistic effect between the sunscreen system and the extract on UVB protection and antioxidant activity. Both samples were considered safe. Formulation F was 20.59% more efficient in protecting skin against UVB radiation, taking approximately 21% more time to induce erythema compared to the extract-free sample.

Antiulcerogenic potential activity of free and nanoencapsulated Passiflora serratodigitata L. extracts.

This paper provides evidence that the leaves and stem of Passiflora serratodigitata L. dry crude extract (DCE), ethylacetate fraction (EAF), and residual water fraction show potential antiulcerogenic activity. Interestingly, the polymeric nanocapsule loaded with EAF had 10-fold more activity than the free EAF. Furthermore, the polymer nanoparticles provided homogeneous colloidal drug delivery systems and allowed overcoming challenges such as poor aqueous solubility as well as the physical-chemical instability of the organic extract, which presented 90% (w/w) of the flavonoid content. The entrapment efficiency of the total flavonoid was 90.6 ± 2.5% (w/v) for the DCE and 79.9 ± 2.7% (w/v) for the EAF. This study shows that nanoencapsulation improves both the physicochemical properties and the efficacy of the herbal formulations. Therefore, free and encapsulated extracts have the potential to be suitable drug design candidates for the therapeutic management of ulcer.

Phytochemical study and evaluation of the antimicrobial activity and cytotoxicity of Cuscuta racemosa

Cuscuta racemosa Mart. is a parasitic plant of the Convolvulaceae family, used in popular medicine as an anti-inflammatory and a diuretic, for stomach and hepatic disorders, and for treating fresh wounds. This plant is popularly known as "cipó-chumbo" and "fios-de-ovos". In this study, it was chemically investigated and tested for its antimicrobial activity and cytotoxicity. The flavonoid and tannin content of the dried plant were 2.79 percent and 2.01 percent, respectively. Furthermore, the 4'-methoxyquercetin flavanoid compound was isolated from the ethanolic fraction. The minimum inhibiting concentration in the antimicrobial test was 2.0 mg/ml for Staphylococcus aureus, and a DL50 of 0.231 mg/mL was obtained in the cytotoxicity experiment. The fraction directed to alkaloids was able to eliminate 100 percent of the brine shrimp used for the test.

Atividades antiúlcera e antioxidante do extrato de folhas de Syzygium jambos (L) Alston (Myrtaceae) / Antiulcerogenic and antioxidant activities of leaf extract of Syzygium jambos (L) Alston (Myrtaceae)

Syzygium jambos (L.) Alston, Myrtaceae, é empregado na medicina popular como digestivo e antiinflamatório. A triagem fitoquímica da droga pulverizada (folhas) indicou a presença de flavonóides, taninos e óleo volátil. O extrato hidroetanólico a 70 por cento das folhas de S. jambos foi preparado por percolação e liofilizado. O conteúdo de taninos das folhas e do extrato foi calculado, respectivamente, em 21,9 por cento e 43,3 por cento. O teor de flavonóides foi de 0,6 por cento (folhas) e 1,2 por cento (extrato). A administração oral prévia do extrato (400 mg/kg) a ratos Wistar reduziu significativamente as lesões gástricas induzidas por etanol acidificado. No modelo de úlcera subcrônica, com indução de lesão gástrica utilizando ácido acético a 30 por cento, o tratamento com o extrato (400 mg/kg) não apresentou resultado significativo. A atividade antioxidante do extrato foi avaliada através dos modelos de lipoperoxidação e de medida de capacidade seqüestrante de radicais DPPH. Os valores obtidos de Q1/2 (MDA) e CE50 (DPPH) foram, respectivamente, 0,17 μg/mL e 5,68 μg/mL.

Syzygium jambos (L.) Alston, Myrtaceae, is commonly employed in folk medicine as digestive and anti-inflammatory. Phytochemical screening of the powdered dried leaves indicates the presence of flavonoids, tannins and essential oil. Hydroethanol extracts (70 percent) were prepared by percolation and freeze-drying. The tannin content of dried leaves and extract was, respectively, 21.9 percent and 43.3 percent. The flavonoid content was 0.6 percent (dried leaves) and 1.2 percent (extract). Previous oral administration of S. jambos leaves extract (400 mg/kg) to rats reduced significantly gastric injury induced by HCl/ethanol. At the subcronic ulcer model by induction with 30 percent acetic acid the results were not significant. In vitro antioxidant activity of S. jambos extract was evaluated by malondialdehyde (MDA) and DPPH free radical method. The Q1/2 for MDA assay was 0.17 μg/mL and the EC50 for DPPH assay was 5.68 μg/mL.

Atividades antiúlcera e antioxidante Baccharis trimera (Less) DC (Asteraceae) / Antiulcerogenic and antioxidant activities of Baccharis trimera (Less) DC (Asteraceae)

A "carqueja", Baccharis trimera (Less) DC (Asteraceae), é uma espécie vegetal característica de regiões tropicais, muito utilizada na medicina popular como antiinflamatória, hipoglicemiante e em tratamento de problemas digestivos. A avaliação da atividade antiúlcera do extrato bruto liofilizado e do extrato liofilizado da "resina" (porção que durante a concentração dos extratos ficava depositada no fundo do recipiente com aspecto viscoso e pegajoso) foi realizada através de indução aguda por etanol acidificado. O extrato bruto liofilizado, na dose de 400 mg/ kg, reduziu a área de lesão em 90 por cento, 200 mg/kg, 87 por cento, 100 mg/kg, 66 por cento e o fármaco controle (lansoprazol), 66 por cento. O extrato liofilizado da "resina", administrado na dose de 400 mg/kg, reduziu a área de lesão em 82 por cento, 200 mg/kg, 82 por cento, 100 mg/kg, 53 por cento e o fármaco controle (lansoprazol), 70 por cento. A atividade antioxidante foi ensaiada com extrato bruto liofilizado, extrato liofilizado da "resina", pó da droga e frações clorofórmica, acetato de etila, etanol e etanol 50 por cento através do método que reduz o radical 2,2'-difenil-1-picril-hidrazil (DPPH), permitindo após o equilíbrio da reação, calcular a quantidade de antioxidante gasta para reduzir 50 por cento do DPPH, apresentando resultado evidente, comparado à vitamina E. Não foram verificados sinais de alteração aparente no ensaio de toxicidade na dose única de 5g/kg, em camundongos.

Baccharis trimera (Less) DC (Asteraceae) is a medicinal Brazilian plant well-known by "carqueja". Natural from tropical regions, used as home-made medicine as anti-inflammatory, hypoglycemiant and for the treatment of digestive problems. The evaluation of the antiulcer activity of the extract and the "resin" (portion which during the extracts concentration was settled at the bottom of the recipient, showing a viscous and clammy aspect), was accomplished through the acute induction by acidified ethanol. The lyophilized extract, at a dose of 400 mg/kg, reduced the lesion area at 90 percent; 200 mg/kg, at 87 percent; 100 mg/kg, at 66 percent; and the control (lansoprazol) at 66 percent. The "resin" administered at the 400 mg/kg dose reduced the lesion area at 82 percent; 200 mg/kg, at 82 percent, 100 mg/kg, at 53 percent and the control (lansoprazol), at 70 percent. The antioxidant activity of the lyophilized extract, of the "resin" of the powdered drug, of the chloroform, ethyl acetate, ethanol and 50 percent ethanol fractions was tested following the method which reduces the 2,2-dipheny l-1 -picrylhydrazyl (DPPH) radical, permitting after the reaction balance, to calculate the amount of antioxidant spent to reduce 50 percent of the DPPH. The result was meaningful, when compared with the vitamin E result. The acute toxicity test performed in mice showed no apparent alteration.

Estudo farmacognóstico do caule e raízes de Microgramma squamulosa (Kaulf.) Sota (Polypodiaceae) / Pharmacognostic and phytochemical study of the stem and roots from Microgramma squamulosa (Kaulf.) Sota (Polypodiaceae)

Microgramma squamulosa (Polypodiaceae) tem sido tradicionalmente empregada como agente contra úlceras estomacais. Trabalhos realizados anteriormente confirmaram a atividade antiúlcera do extrato bruto de caule/raízes e de suas frações preparadas com os caules e as raízes dessa planta. Foi também demonstrado que o extrato não é tóxico no modelo de toxicidade aguda, em ratos. Devido a esses resultados, considerou-se importante providenciar instrumentos capazes de orientar a caracterização da droga vegetal. M. squamulosa é uma epífita com caule escandente, portando folhas na porção adaxial e raízes adventícias na porção abaxial. As principais características histológicas para identificação são: escamas lanceoladas, peltadas e com tricomas, esclereídes, meristelos (feixes anficrivais) e traqueídes com espessamento espiralado no caule; pêlos em fita e esclereídes, na raiz. A análise fitoquímica e o perfil cromatográfico realizados com o extrato bruto de caule/raízes e frações ativas mostraram a presença de flavonóides e taninos, que podem estar relacionados à atividade antiúlcera. Os resultados obtidos auxiliam a identificação da planta e possibilitam a caracterização da droga vegetal fragmentada e também sob forma de pó ou extrato.

Pharmacognostic and phytochemical study of the stem and root of Microgramma squamulosa (Kaulf.) Sota. Erva silvina, or Microgramma squamulosa (Kaulf.) Sota belongs to the family Polypodiaceae and is traditionally used as an antiulcer agent. Previous assays showed results that confirm the antiulcer action of the ethanolic extract and some fractions of the stem of M. squamulosa and results showing no significant toxicity in the acute model, both made in rats. Due to the significant results obtained in this previous work, it becomes important to furnish tools to identify the vegetal drug. The species is an epiphyte that bears lanceolate scales totally covering the long-creeping brown-colored stem. Adventicious roots can be seen in the abaxial portion of the stem, while the leaves appear in the adaxial portion. Elements which contribute to the histological identification are: peltate lanceolate -haired scales, sclereids, meristeles (amphicribal bundles) and scalariform tracheids in the stem; strip hairs and sclereids in the roots. Phytochemical screening and TLC analysis showed the presence of flavonoids and tannins which may be related to the antiulcer activity. Results shown may help the identification of the plant as well as the characterization of the fragmented vegetal drug and if it is presented as powder or as extract.

Optimization of Pothomorphe umbellata (L.) Miquel topical formulations using experimental design.

Pothomorphe umbellata is a native plant widely employed in the Brazilian popular medicine. This plant has been shown to exert a potent antioxidant activity on the skin and to delay the onset and reduce the incidence of UVB-induced skin damage and photoaging. The aim of this work was to optimize the appearance, the centrifuge stability and the permeation of emulsions containing P. umbellata (0.1% 4-nerolidylchatecol). Experimental design was used to study ternary mixtures models with constraints and graphical representation by phase diagrams. The constraints reduce the possible experimental domain, and for this reason, this methodology offers the maximum information while requiring the minimum investment. The results showed that the appearance follows a linear model, and that the aqueous phase was the principal factor affecting the appearance; the centrifuge stability parameter followed a mathematic quadratic model and the interactions between factors produced the most stable emulsions; skin permeation was improved by the oil phase, following a linear model generated by data analysis. We propose as optimized P. umbellata formulation: 68.4% aqueous phase, 26.6% oil phase and 5.0% of self-emulsifying phase. This formulation displayed an acceptable compromise between factors and responses investigated.

Lipid metabolism in trained rats: effect of guarana (Paullinia cupana Mart.) supplementation.

BACKGROUND AND AIMS: Guarana is widely consumed by athletes, either in supplements or in soft drinks, under the belief that it presents ergogenic and "fat burning" effects. We examined the effect of guarana supplementation (14 days) upon aspects of lipid metabolism in sedentary (C) and trained rats (T). METHODS: To isolate the effect of caffeine from that of other components of guarana, we adopted two different doses of whole extract (G1-0.130 g/kg; G2-0.325 g/kg) or decaffeinated extract (DG1, DG2). Body weight, food and water intake; muscle fat content, oleate incorporation, glycogen content, and carnitine palmitoyltransferase I (CPT I) activity and mRNA expression; along with plasma lactate concentration, were assessed. RESULTS: Muscle oleate incorporation was decreased in rats receiving decaffeinated guarana in relation to G1 and G2; as was CPT I mRNA expression in the gastrocnemius. Whole extract supplementation, but not DG induced reduced plasma lactate concentration in trained rats. G1 showed higher muscle glycogen content compared with all other groups. The results show an effect of guarana on aspects of lipid metabolism, which is abolished by decaffeination. CONCLUSION: The changes in lipid metabolism of supplemented rats herein reported are associated with the methylxanthine content of guarana.

Caracterização Farmacognóstica de Polygonum persicaria L / Pharmacognostic characterization of Polygonum persicaria L

Polygonum persicaria L.(Polygonaceae)é uma planta empregada na medicina popular brasileira como anti-hemorroidal, antiúlcera e vermífuga. As folhas e os caules foram estudados sob os aspectos macro e microscópicos. Fotografias ilustram as descrições. O perfil cromatográfico em camada delgada do extrato foi obtido comparativamente com substâncias de referência. Esses dados em conjunto fornecem parâmetros de controle de qualidade da droga vegetal inteira ou fragmentada auxiliando a detecção de fraudes ou adulterações

Atividade antimicrobiana de Leonorus sibiricus L.

A espécie vegetal Leonurus sibiricus L. (Lamiaceae) é utilizada pela população brasileira para os mais diversos fins, principalmente como anti-inflamatória. No presente trabalho é estudada a atividade antimicrobiana do extrato hidroalcodico a 70 por cento liofilizado (extrato bruto) de Leonurus sibiricus L.O extrato foi testado frente a Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans e Aspergillus niger, pela determinação da concentração minima inibitória, atraves do método de diluicão em tubos. O extrato bruto de Leonurus sibiricus L. inibiu o crescimento de Candida albicans, Staphylococcus aureus e Pseudomonas aeruginosa.

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