In vivo antimutagenic effects of the Barbados cherry fruit (Malpighia glabra Linnaeus) in a chromosomal aberration assay.

Barbados cherry (BC) (Malpighia glabra Linnaeus) is a functional fruit that is consumed to prevent disease. It is used as an adjuvant in the treatment of several diseases, and acts as an antianemic, an appetite stimulant, a wound healer, an anti-inflammatory, a mineralizer, an antifungal, and an antioxidant agent. Several chemotherapeutic agents, such as cyclophosphamide, may result in undesirable side effects, and generate mutations in normal cells. Thus, the present study evaluated the antimutagenic potential of the fresh (BCN) and frozen (BCF) juices of BC pulp, with and without concomitant administration of cyclophosphamide, using a chromosomal aberration test system in the bone marrow cells of Wistar rats treated in vivo for 24 h. The results showed that neither the BC juice (0.4 mg/mL) alone, nor that with concomitant cyclophosphamide (1.5 mg/mL), were cytotoxic. BC has potential as an antimutagenic, and statistically reduced the percentages of chromosomal alterations induced by cyclophosphamide when administered simultaneously (BCN: 80.75%; BCF: 88.26%), pre-treatment (BCN: 86.85%; BCF: 87.32%), or post-treatment (BCN: 90.14%; BCF: 86.85%). This was due to the antioxidant activity of the fruit and the action of its bioactive compounds, which may have inhibited cyclophosphamide metabolism or scavenged the free radicals generated by this compound. Thus, attenuation of cyclophosphamide-induced mutagenicity suggests that the consumption of fresh or frozen BC should be encouraged for the prevention of disease, and for the maintenance and promotion of health.

Cytotoxic and mutagenic effects of iodine-131 and radioprotection of acerola (Malpighia glabra L.) and beta-carotene in vitro.

The radioisotope iodine-131 [(131)I] can damage DNA. One way to prevent this is to increase the amount of antioxidants via dietary consumption. The goal of this study was to evaluate the radioprotective effect of fresh acerola pulp and synthetic beta-carotene in Rattus norvegicus hepatoma cells (HTC) in response to [(131)I] exposure in vitro. Cellular DNA damage was subsequently assessed using a cytokinesis block micronucleus assay. The mutagenic and cytotoxic activities of doses of [(131)I] (0.1, 0.5, 1, 5, and 10 µCi), acerola (0.025, 0.125, and 0.25 g acerola pulp/mL), and beta-carotene (0.2, 1, and 2 µM) were evaluated. Radioprotective tests were performed by simultaneous treatment with acerola (0.25 g/mL) plus [(131)I] (10 µCi) and beta-carotene (0.2 µM) plus [(131)I] (10 µCi). Acerola, beta-carotene, and low concentrations of [(131)I] did not induce micronucleus formation in HTC cells; in contrast, high concentrations of [(131)I] (10 µCi) were mutagenic and induced DNA damage. Moreover, neither acerola nor beta-carotene treatment was cytotoxic. However, acerola reduced the percentage of [(131)I]-induced damage, although beta-carotene did not show a similar effect. Thus, our results suggest that acerola diet supplementation may benefit patients who are exposed to [(131)I] during thyroid diagnostics and therapy.

Cytotoxic/antiproliferative and nutraceutical activity of aqueous and ethanolic extracts of green and mature Averrhoa carambola.

Averrhoa carambola L. presents in its composition diversity of nutrients and vitamins. The present study aimed to extract water and fat-soluble compounds from this fruit at different stages of maturation (green and mature), perform the physical-chemical characterization as well as evaluate its cytotoxicity against hepatoma cells of Rattus norvegicus (HTC). The physicochemical results showed that the pH and molar acidity is influenced by the fruit maturation state. The fruit presented high percentage of moisture, while the percentage of total minerals (ash) increased according to its maturation stage. The results of the phytochemical screening showed that star fruits present phenolic compounds. The antioxidant activity showed greater potential for the ethanolic extracts of the green and mature star fruit. For HTC cells treated with ethanolic extract of green and mature star fruit the data show absence of cytotoxic effect. The tests with the aqueous extract showed cytotoxic/antiproliferative effect of green and mature star fruit extract, in 24, 48 and 72 hours. The presence of nutraceutical compounds and the cytotoxic/antiproliferative activity were more expressive in the aqueous extract, being an option of easily accessible solvent economic and not harmful to organisms.

Beta-carboline-3-carboxamide derivatives as promising antileishmanial agents.

Leishmaniasis has an overwhelming impact on global public health especially in tropical and subtropical countries and the currently available antileishmanial drugs have serious side effects and low efficacy. Natural and synthetic compounds have been tested in the past few years against Leishmania and the beta-carboline class of compounds have shown great results in antiparasitic chemotherapy. In the present study, three 1-substituted beta-carboline-3-carboxamides (3-5) and 1-substituted beta-carboline-3-carboxylic acid (2) were synthesized and screened for in vitro activity against L. amazonensis. Compound 5 (N-benzyl 1-(4-methoxy)phenyl-9H-beta-carboline-3-carboxamide) had the best activity against promastigote and axenic amastigote forms with IC(50) of 2·6 and 1·0 µM, respectively. Its CC(50) on macrophages cell line was higher than 2457·0 µM with an SI ratio of 930·2. Against intracellular amastigote forms, it had a dose-dependent relationship with a 50% growth inhibitory concentration of 1·0 µM. Through morphological and ultrastructure analysis of promastigote forms treated with compound 5, alterations on cell shape and number of flagella and nuclear membrane damage were observed. For this, compound 5 supports the idea for more in vitro and in vivo studies.

Parâmetros de qualidade físico-químicos e avaliação da atividade antioxidante de folhas de Plectranthus barbatus Andr. (Lamiaceae) submetidas a diferentes processos de secagem / Quality of the leaves of Plectranthus barbatus Andr. (Lamiaceae) dried in solar dryer and oven

RESUMO O presente trabalho descreve a composição físico-química, a avaliação da atividade antioxidante pelo método de sequestro de radicais livres DPPH, determinação de flavonoides e de fenóis totais dos extratos etanol, acetona e aquoso de Plectranthus barbatus Andr. (Lamiaceae), desidratadas em secador solar e em estufa de circulação de ar a 60 oC. Os valores de atividade de água encontrados para as duas secagens foram inferiores ao mínimo necessário para o crescimento e produção de toxina de patógenos de importância alimentar. Os resultados das análises físico-químicas demonstraram que ambos os processos mostraram-se eficientes na desidratação de P. barbatus. Os resultados demonstraram que os extratos acetona (estufa) e etanol (estufa e secador solar) foram os que apresentaram maior conteúdo de fenóis totais. O extrato etanólico (estufa) apresentou maior quantidade de flavonoides e melhor potencial antioxidante (IC50 = 75,71 ± 10,57 µg mL-1).

ABSTRACT This paper describes the physicochemical composition, the evaluation of the antioxidant activity by free DPPH radicals using the scavenging method, the determination of flavonoids and total phenolic compounds of ethanol, acetone and aqueous extracts of the medicinal plant Plectranthus barbatus Andr. (Lamiaceae), dehydrated in solar dryer and circulation oven at 60 °C. Water activity rates for two drying methods were below the minimum necessary for growth and toxin production of important food pathogens. Physicochemical results showed that both processes were effective in the dehydration of P. barbatus. The results demonstrated that the acetone (over) and ethanol (over and solar dryer) extracts showed the highest content of total phenols. The ethanol extract (over) showed the highest amount of flavonoids and better antioxidant activity (75.71 ± 10.57 µg L-1).

Composição centesimal, compostos bioativos e atividade antioxidante de frutos de Morinda citrifolia Linn (noni) cultivados no Paraná / Proximate composition, bioactive compounds and antioxidant activity of fruits of Morinda citrifolia L. (noni) cultivated in Paraná, Brazil

O fruto de noni (Morinda citrifolia L.) é consumido há milênios na medicina popular polinésia devido aos benefícios nutricionais e terapêuticos. O consumo de noni em outros países, incluindo o Brasil, cresceu vertiginosamente nos últimos anos em decorrência das atividades biológicas atribuídas a ingestão do suco da fruta, principalmente pela propriedade anticâncer. Contudo, a composição química da planta, que está relacionada com suas propriedades biológicas, é determinada pelo seu local de origem, e por influência do clima e do solo onde é cultivada. Neste sentido, este trabalho teve como objetivo analisar a polpa extraída de frutos maduros de noni cultivados em Maringá-PR. A análise da polpa in natura apresentou 89,16% de umidade, 0,75% de cinzas, 2,10% de proteínas, 2,19% de lipídios e 5,81% de carboidratos. Dos compostos bioativos, foram analisados antocianinas (1,39 mg.100 g-1 polpa), flavonoides amarelos (13,01 mg.100 g-1 polpa), carotenóides (0,45 mg.100 g-1 polpa) e vitamina C (12,16 mg.100 g-1 polpa). Para fenólicos totais e atividade antioxidante foram preparados diferentes extratos, sendo que os maiores teores de fenólicos totais foram encontrados no extrato aquoso (1143,56 mg equivalente de ácido gálico (EAG).100 g-1), seguido do extrato etanólico (966,96 mg EAG.100 g-1), metanol/acetona (820,88 mg EAG.100 g-1) e metanólico (306,33 mg EAG.100 g-1). Os melhores resultados para antioxidantes, determinado pelo EC50 - concentração do extrato necessária para reduzir 50% do radical DPPH, foram encontrados nos extratos metanol/acetona (EC50 de 25,18 mg.mL-1) e metanólico (EC50 de 25,96 mg.mL-1). A atividade antioxidante dos frutos pode estar relacionada com o conteúdo de vitamina C, uma vez que os extratos com um menor conteúdo de fenóis totais foram aqueles que apresentaram menores valores de EC50.

The noni fruit (Morinda citrifolia L.) has been consumed for millennia in the Polynesian folk medicine because of its nutritional and therapeutic benefits. The consumption of the noni fruit in other countries, including Brazil, has increased in recent years because of the biological activities attributed to the ingestion of noni juice, especially the anticancer effect. However, the chemical composition of the plant, which is related to its biological properties, is determined by its geographical origin and is influenced by climate and soil. Therefore, this study aimed to analyze the pulp extracted from noni fruit grown in Maringá, state of Paraná, Brazil. The fresh pulp analysis showed 89.16% of moisture, 0.75% of ash, 2.10% of protein, 2.19% of fat and 5.81% of carbohydrates. The bioactive compounds analyzed were anthocyanins (1.39 mg.100 g-1 pulp), yellow flavonoids (13.01 mg.100 g-1 pulp), carotenoids (0.45 mg.100 g-1 pulp) and vitamin C (12.16 mg.100 g-1 pulp). For the analysis of total phenols and antioxidant activity, different extracts were prepared. The highest total phenolic contents were found in the aqueous extract (1143.56 mg EAG.100 g-1), followed by the ethanol extract (966.96 mg EAG.100 g-1), methanol/acetone extract (820.88 mg EAG.100 g-1) and methanol extract (306.33 mg EAG.100 g-1). The results for the antioxidant capacity were determined by the EC50, which is concentration of extract required to reduce 50% of the DPPH radical. The best results for the antioxidant capacity were found in the methanol/acetone extract (EC50 of 25.18 mg.mL-1) and in the methanol extract (EC50 of 25.96 mg.mL-1). The antioxidant activity of the fruit may be related to its vitamin C content, since the extracts with lower total phenolic content were those that had lower EC50 values.