Betulinic Acid from Zizyphus Joazeiro Bark Using Focused Microwave-Assisted Extraction and Response Surface Methodology.

BACKGROUND: The effect of the extraction time (min) and temperature (°C) on the yield of betulinic acid (BA) from Zizyphus joazeiro barks using focused microwave-assisted extraction was investigated. MATERIALS AND METHODS: The ethyl acetate was used as extractor solvent because it was shown to provide a betulinic acid-clean extract. A full two-level statistical factorial design was applied to determine the important effects and interactions of these independent variables upon the yield of BA. RESULTS: The conditions that produced the highest yield of BA were at temperature of 70°C and an extraction time of 15 min (3.33 mg per gram of plant). CONCLUSION: The BA has drawn attention due to its use as a raw material in the synthesis of active compounds against the Human Immunodeficiency Virus (HIV). SUMMARY: The extraction of betulinic acid (BA) from Zizyphus joazeiro barks using focused microwave was investigatedA full two-level statistical factorial design was applied to determine the effects and interactions of the independent variables (time and temperature) upon the yield of BAThe reversed-phase high-performance liquid chromatography with diode-array detector was used for quantification. Abbreviation used: BA: Betulinic acid; FMAE: Focused microwave assisted extraction; HPLC: High-performance liquid chromatography; RSD: Relative standard deviations.

Antinociceptive effect of Encholirium spectabile: A Bromeliaceae from the Brazilian caatinga biome.

BACKGROUND: Encholirium spectabile is a species found in outcrops rocky throughout the Brazilian Caatinga. OBJECTIVE: This study was carried out to evaluate the antinociceptive effects of ethanolic extract of the leaves from E. spectabile (Es-EtOH) in mice using chemical and thermal models of nociception. MATERIAL AND METHODS: HPLC was used to determine the fingerprint chromatogram. The Es-EtOH was examined for its antinociceptive activity at the doses of 100, 200 and 400 mg/kg intraperitoneal (i.p.). The evaluation of antinociceptive activity was carried out by the acetic acid-induced writhing, formalin and hot plate tests in mice. Rota-rod test was used for the evaluation of motor coordination. RESULTS: In the acetic acid-induced writhing test, the Es-EtOH (100, 200 and 400 mg/kg, i.p.) reduced the number of writhings by 68.59, 79.33 and 65.28%, respectively. Additionally, Es-EtOH (100, 200 and 400 mg/kg, i.p.) decreased by 34.14, 52.61 and 60.97% the paw licking time in the first phase, as well as 89.56, 79.90 and 96.71% in the second phase of the formalin test, respectively. Es-EtOH also showed effect in the hot plate test, since increased the latency time at dose of 100 mg/kg after 60 minutes. In addition, Es-EtOH did not impair motor coordination. The presence of phenolic compounds in the extract was confirmed using HPLC. These results indicate that Es-EtOH has antinociceptive activity, probably of peripheral origin. The mechanism involved is not completely understood but, at least in part there is the participation of opioid receptors.

Avaliação de formulações tópicas magistrais para o tratamento da acne / Assessment of topical formulations for the treatment of acne

A acne é uma afecção inflamatória que atinge 80% da população entre 11 e 30 anos de idade. A seleção do tratamento dependerá do tipo de pele e da gravidade da acne que o paciente apresenta, sendo as formulações tópicas magistrais as mais indicadas devido à vantagem de serem realizadas de acordo com as necessidades dos pacientes. O objetivo deste trabalho foi avaliar a composição das formulações tópicas para o tratamento da acne aviadas em cinco farmácias de manipulação da cidade de Feira de Santana - BA. Os dados foram obtidos através das informações contidas na ordem de manipulação sendo avaliado um total de 402 formulações. Na análise dos dados, verificou-se que o ácido retinoico foi o ativo mais empregado. As formas farmacêuticas mais prescritas foram o gel (39,1%) e o creme (29,6%). Pode-se perceber uma variedade de ativos antiacneicos empregados, sendo que 31% das formulações continham associações de dois ou mais ativos. A avaliação das faixas de concentração de alguns ativos indicou valores acima das adequações às concentrações usuais. Na maioria das formulações, as associações entre os ativos não apresentaram incompatibilidades, sendo que 96,5% das formulações avaliadas apresentaram-se corretas quanto aos aspectos relacionados à concentração, à associação dos ativos, veículos ou excipientes empregados, apresentando-se confiáveis para utilização no tratamento da acne. Pelo exposto faz-se necessária a constante atuação e capactação do profissional farmacêutico com intuito de evitar possíveis incopatibilidades nas formulações evitando danos maiores a saúde do paciente.

Acne is a chronic inflammatory disorder affecting 80% of the population between 11 and 30 years of age. The treatment depends on skin type and severity of the acne that the patient presents, so that topical formulations are highly recommended, having the advantage of being made up according to the specific needs of the patient. The objective of this study was to assess the composition of topical formulations for the treatment of acne dispensed in five pharmacies in the city of Feira de Santana in Bahia, Brazil. The data were obtained from information contained in the compounding prescriptions for the 402 formulations assessed. In analyzing the data, it was found that the active principle used most frequently was retinoic acid. The commonest vehicles prescribed were gel (39.1%) and cream (29.6%). A wide variety of anti-acne active ingredients were found, and 31% of the formulations contained combinations of two or more. Analysis of the concentration ranges of the active principles revealed some values above the usual recommended concentrations. In most formulations, the combinations of active substances showed no incompatibilities, as 96.5% of the formulations studied were correct with respect to concentration, the active combination used, vehicles and excipients, and thus were safe for use in the treatment of acne. This study confirmed the need for the constant performance and training of the pharmacist, so as to avoid incompatibilities in compounded medicines and thus prevent further damage to the patient´s health.

Fenóis totais, flavonoides totais e atividade antioxidante de Selaginella convoluta (Arn. ) Spring (Selaginellaceae) / Total phenols, total flavonoids and antioxidant activity of Selaginella convoluta (Arn. ) Spring (Selaginellaceae)

Selaginella convoluta é uma espécie conhecida no Nordeste do Brasil como “jericó”, e bastante utilizada na medicina popular para tratamento de doenças. Este estudo teve como objetivo determinar o teor de compostos fenólicos e avaliar a atividade antioxidante in vitro do extrato etanólico e das frações obtidas por partição de S. convoluta. O conteúdo de fenóis totais foi determinado pelo método de Folin-Ciocalteu. O teor de flavonoides totais também foi avaliado. A atividade antioxidante dos extratos foi avaliada usando o método do sequestro do radical DPPH e inibição da auto-oxidação do sistema β-caroteno-ácido linoleico e comparada com os compostos de referência ácido ascórbico, BHA, BHT, quercetina e pirogalol. O conteúdo fenólico total foi de 209,90 ± 19,84 e 61,13 ± 2,50 mg equivalente de ácido gálico/g para os extratos AcOEt e EEB, respectivamente. O conteúdo de flavonoides totais foi de 155,70 ± 6,21 e 62,13 ± 4,10 para os dois extratos, respectivamente. Os extratos AcOEt e EEB apresentaram boas atividades antioxidantes. BHA foi o antioxidante mais efetivo, com um valor de IC50 de 1,62 ± 0,69 μg/mL. Os resultados obtidos mostram que S. convoluta pode ser uma boa fonte de compostos fenólicos antioxidantes. Estudos posteriores serão realizados para se chegar ao isolamento e identificação dos principais constituintes fenólicos dos extratos.

Selaginella convoluta is a species of "spike moss" (an order of pteridophytes) known in Northeast Brazil as "jericó" and widely used in popular medicine to treat several diseases. Phenolic compounds were determined in extracts of whole Selaginella convoluta plants. The total phenolics content was determined by the Folin-Ciocalteu method. Total flavonoid content was also measured. Antioxidant activities of the extracts were assayed by DPPH radical scavenging and inhibition of β-carotene-linoleic acid bleaching and compared with ascorbic acid, BHA, BHT, quercetin and pyrogallol, used as reference compounds. The total phenolics contents of ethyl acetate (EtOAc) and crude ethanol extract (CEE) were 209.90 ± 19.84 and 61.13 ± 2.50 mg of gallic acid equivalent/g, respectively. The total flavonoids contents were 155.70 ± 6.21 and 62.13 ± 4.10 mg of catechin equivalent/g for the two extracts, respectively. The EtOAc and CEE extracts exhibited good antioxidant activities. BHA was the most effective antioxidant, with an IC50 of 1.62 ± 0.69 μg/ml. The results show that S. convoluta could be a good source of antioxidant phenolics. Further research will be carried out to achieve the isolation and identification of the main phenolic constituents of the extracts.

Antinociceptive effect of ethanolic extract of Selaginella convoluta in mice.

BACKGROUND: Selaginella convoluta (Arn.) Spring (Selaginellaceae), commonly known as "jericó", is a medicinal plant found in northeastern Brazil. S. convoluta is used in folk medicine as an antidepressant, aphrodisiac, diuretic, analgesic, anti-inflammatory and it is used to combat amenorrhea, coughing and bleeding. This study was performed to evaluate the antinociceptive effects of ethanolic extract from S. convoluta in mice exposed to chemical and thermal models of nociception. METHODS: Preliminary phytochemical analysis of the ethanolic extract was performed. The ethanolic extract from Selaginella convoluta (Sc-EtOH) was examined for its intraperitoneal (i.p.) antinociceptive activity at the doses of 100, 200 and 400 mg/kg body weight. Acetic acid-induced writhing, formalin injection and hot plate tests were used to evaluate the antinociceptive activity of Sc-EtOH extract. The rota-rod test was used to evaluate motor coordination. RESULTS: A preliminary analysis of Sc-EtOH revealed that it contained phenols, steroids, terpenoids and flavonoids. In the acetic acid-induced writhing test, mice treated with Sc-EtOH (100, 200 and 400 mg/kg, i.p.) exhibited reduced writhing (58.46, 75.63 and 82.23%, respectively). Secondly, Sc-EtOH treatment (100, 200 and 400 mg/kg, i.p.) decreased the paw licking time in mice during the first phase of the formalin test (by 44.90, 33.33 and 34.16%, respectively), as well as during the second phase of the test (by 86.44, 56.20 and 94.95%, respectively). Additionally, Sc-EtOH treatment at doses of 200 and 400 mg/kg increased the latency time in the hot plate test after 60 and 90 minutes, respectively. In addition, Sc-EtOH did not impair motor coordination. CONCLUSION: Overall, these results indicate that Sc-EtOH is effective as an analgesic agent in various pain models. The activity of Sc-EtOH is most likely mediated via the inhibition of peripheral mediators and central inhibitory mechanisms. This study supports previous claims of traditional uses for S. convoluta.