Antioxidant, cytotoxic and UVB-absorbing activity of Maytenus guyanensis Klotzch. (Celastraceae) bark extracts

Maytenus guyanensis Klotzch. is an Amazonian medicinal tree species known in Brazil by the common name chichuá and in Peru and Colombia by the name chuchuhuasi. It is used in traditional medicine as stimulant, tonic, and muscle relaxant, for the relief of arthritis, rheumatism, hemorrhoids, swollen kidney, skin eruptions, and skin cancer prevention, among others. Initially, different extraction solvents and methods were applied to dried, ground bark which made possible the preparation of extracts having both significant lethality to brine shrimp larvae (Artemia franciscana Leach) as well as antioxidant activity in vitro based on tests involving reactions with 2,2,-diphenyl-1-picrylhydrazyl (DPPH). Analysis of fractions from serial extractions with solvents of increasing polarity supports the notion that antioxidant activity is associated with compounds of intermediate polarity and cytotoxicity is associated with compounds of low to intermediate polarity. Variation of extraction time and conditions revealed that hot, continuous ethanol extraction provided good yields of bark extract in several hours. Hot extraction also provided ethanol extracts having greater lethality to brine shrimp and antioxidant activity (compared to the flavonoid rutin in semi-quantitative methods based on DPPH) than extracts obtained from maceration at room temperature. Freeze-dried ethanol extracts were prepared by: 1) maceration at room temperature and 2) hot extraction (eight hours) on several hundred gram scales and the latter extract was shown to have partial screening effects on UVB light. In this work, cytotoxic, antioxidant and potential sun-screening activity are shown for the first time in M. guyanensis.

Bioactive dihydroxyfuranonaphthoquinones from the bark of Tabebuia incana A.H. Gentry (Bignoniaceae) and HPLC analysis of commercial pau d'arco and certified T.incana bark infusions

Tabebuia incana A.H. Gentry (Bignoniaceae) is a tree from the Brazilian Amazon having medicinal uses and is one several Tabebuia spp. known as pau d'arco or palo de arco in this region. Fractionation of the bark ethanolic extract afforded a mixture of 5 and 8-hydroxy-2-(1-hydroxyethyl)naphtho[2,3-b]furan-4,9-diones (1 and 2, respectively) identified on the basis of nuclear magnetic resonance (NMR), infrared (IR) and mass (MS) spectra, whose in vitro antimalarial and antitumor activity have been shown previously. This is the first study on T. incana bark, and 2 are described in this species for the first time. Also, high performance liquid chromatography (HPLC) analysis of T. incana bark tea revealed the presence of the 1 + 2 mixture peak corresponding to a concentration in the range 10-6-10-5 M. The chromatograms of teas prepared from commercial pau d' arco and T. incana bark were also studied and the presence of the 1 + 2 peak has potential for quality control of commercial plant materials.

Avaliação da toxicidade aguda pré-clínica do extrato metanólico das cascas do caule de Parahancornia amapa (Apocynaceae)

RESUMOParahancornia amapa é uma espécie endêmica do Estado do Amapá, na região Amazônica. Este estudo teve como objetivo avaliar a toxicidade aguda do extrato metanólico das cascas do caule de P. amapa. Diferentes concentrações do extrato foram adicionadas aos camarões de salmoura (Artemia salina) e a concentração letal média (CL50) foi avaliada. Os resultados desse ensaio indicaram que o extrato não era tóxico. A toxicidade aguda foi estudada em ratos Wistar (machos e fêmeas) após dose única (2000 mg kg-1) por gavagem. Ingestão de água e comida, peso corporal, alterações comportamentais e mortalidade foram anotados. Amostras de sangue foram coletadas para medições de parâmetros hematológicos e bioquímicos. Os animais foram eutanasiados e seus órgãos (coração, rins, fígado e pulmões) submetidos à análise macroscópica e histopatológica. Não houve mortalidade ou qualquer sinal de mudança de comportamento ou toxicidade observada após a administração oral do extrato. No entanto, observou-se um aumento significativo (p<0,05) sobre o consumo de água de ratas tratadas com o extrato de P. amapa (127,64 mL) quando comparadas ao grupo controle (101,93 mL). Um aumento significativo (p <0,05) na contagem das plaquetas também foi observado tanto em ratos machos (288,00x103 mm3) quanto em fêmeas (220,83x103 mm3, respectivamente) que receberam o extrato quando comparados com seus respectivos grupos controle (128,33x103 mm3; 109,50x103 mm3). Alterações histopatológicas não foram relacionadas ao tratamento com extrato em nenhum dos órgãos analisados. Estes resultados sugerem que o extrato de P. amapa tem um efeito geral não-tóxico.

Diferentes estratégias alimentares na larvicultura do acará-bandeira (Peterolophyllum scalare,Cichlidae)

RESUMOA larvicultura é uma das etapas mais críticas do desenvolvimento dos peixes e o seu sucesso está diretamente relacionado ao manejo alimentar, que pode proporcionar maiores sobrevivência e crescimento. Objetivou-se avaliar o tempo de transição alimentar e de fornecimento de meta-náuplios de Artemiaspp (MNA) na larvicultura do acará-bandeira. Dois experimentos foram conduzidos em delineamento inteiramente casualizado com cinco tratamentos e quatro repetições. Em cada experimento foram utilizados 540 peixes distribuídos em 20 aquários com 2 L. No primeiro experimento, avaliaram-se os períodos de transição alimentar (MNA + ração) por 1, 2, 3, 4 e 5 dias. No segundo experimento, avaliou-se o período de fornecimento de MNA por 5, 10, 15, 20 e 25 dias. Foram avaliados: ganho de peso, taxas de crescimento e desenvolvimento específico, sobrevivência e uniformidade do lote (apenas no experimento para avaliar o tempo de fornecimento de MNA). Não houve efeito significativo dos diferentes períodos de transição alimentar sobre as variáveis de crescimento (p>0,05), porém a sobrevivência foi maior (p<0,05) nos tratamentos compostos por 3, 4 e 5 dias de alimentação conjunta. Em relação ao tempo de fornecimento de MNA, foram observados piores resultados (p<0,05) quando o tempo de fornecimento do alimento vivo foi menor (5, 10 e 15 dias). Os animais que foram alimentados com MNA antes da transição alimentar, por mais tempo (20 e 25 dias), apresentaram os melhores resultados de crescimento (p<0,05). Portanto, recomenda-se uma transição alimentar de três dias e um fornecimento de MNA por 20 dias para realizar a substituição total do alimento vivo pela ração.

Biological screening of Brazilian medicinal plants

In this study, we screened sixty medicinal plant species from the Brazilian savanna ("cerrado") that could contain useful compounds for the control of tropical diseases. The plant selection was based on existing ethnobotanic information and interviews with local healers. Plant extracts were screened for: (a) molluscicidal activity against Biomphalaria glabrata, (b) toxicity to brine shrimp (Artemia salina L.), (c) antifungal activity in the bioautographic assay with Cladosporium sphaerospermum and (d) antibacterial activity in the agar diffusion assay against Staphylococcus aureus, Escherichia coli, Bacillus cereus and Pseudomonas aeruginosa. Forty-two species afforded extracts that showed some degree of activity in one or more of these bioassays.

Saponins from Swartzia langsdorffii: biological activities

The presence of saponins and the molluscicidal activity of the roots, leaves, seeds and fruits of Swartzia langsdorffii Raddi (Leguminosae) against Biomphalaria glabrata adults and eggs were investigated. The roots, seeds and fruits were macerated in 95% ethanol. These extracts exerted a significant molluscicidal activity against B. glabrata, up to a dilution of 100 mg/l. Four mixtures (A2, B2, C and D) of triterpenoid oleanane type saponins were chromatographically isolated from the seed and fruit extracts. Two known saponins (1 and 2) were identified as beta-D-glucopyranosyl-[alpha-L-rhamnopyranosyl-(1->3)- beta-D-glucuronopyranosyl-(1->3)]-3beta-hydroxyolean-12-ene-28 -oate, and beta-D-glucopyranosyl-(1->3)-beta-D-glucuronopyranosyl-(1 ->3)]-3beta-hydroxyolean-12-ene-28-oate, respectively. These two saponins were present in all the mixtures, together with other triterpenoid oleane type saponins, which were shown to be less polar, by reversed-phase HPLC. The saponin identifications were based on spectral evidence, including ¹H-¹H two-dimensional correlation spectroscopy, nuclear Overhauser and exchange spectroscopy, heteronuclear multiple quantum coherence, and heteronuclear multiple-bond connectivity experiments. The toxicity of S. langsdorffii saponins to non-target organisms was prescreened by the brine shrimp lethality test.

Biological activity of neosergeolide and isobrucein B (and two semi-synthetic derivatives) isolated from the Amazonian medicinal plant Picrolemma sprucei (Simaroubaceae)

In the present study, in vitro techniques were used to investigate a range of biological activities of known natural quassinoids isobrucein B (1) and neosergeolide (2), known semi-synthetic derivative 1,12-diacetylisobrucein B (3), and a new semi-synthetic derivative, 12-acetylneosergeolide (4). These compounds were evaluated for general toxicity toward the brine shrimp species Artemia franciscana, cytotoxicity toward human tumour cells, larvicidal activity toward the dengue fever mosquito vector Aedes aegypti, haemolytic activity in mouse erythrocytes and antimalarial activity against the human malaria parasite Plasmodium falciparum. Compounds 1 and 2 exhibited the greatest cytotoxicity against all the tumor cells tested (IC50 = 5-27 µg/L) and against multidrug-resistant P. falciparum K1 strain (IC50 = 1.0-4.0 g/L) and 3 was only cytotoxic toward the leukaemia HL-60 strain (IC50 = 11.8 µg/L). Quassinoids 1 and 2 (LC50 = 3.2-4.4 mg/L) displayed greater lethality than derivative 4 (LC50 = 75.0 mg/L) toward A. aegypti larvae, while derivative 3 was inactive. These results suggest a novel application for these natural quassinoids as larvicides. The toxicity toward A. franciscana could be correlated with the activity in several biological models, a finding that is in agreement with the literature. Importantly, none of the studied compounds exhibited in vitro haemolytic activity, suggesting specificity of the observed cytotoxic effects. This study reveals the biological potential of quassinoids 1 and 2 and to a lesser extent their semi-synthetic derivatives for their in vitro antimalarial and cytotoxic activities.

Uso de alimento vivo como dieta inicial no treinamento alimentar de juvenis de pirarucu

O objetivo deste trabalho foi testar a eficiência do alimento vivo como dieta inicial no treinamento alimentar de juvenis de pirarucu, Arapaima gigas. Foram usados dois tratamentos, Artemia sp. e mistura de zooplâncton nativo. O ganho de peso, a porcentagem de comedores e a sobrevivência não apresentaram diferença estatística significativa entre os tratamentos (p>0,05). A dieta inicial, à base de alimento vivo, é eficiente no treinamento alimentar de juvenis de pirarucu.

Biofiltração da água e tipos de substrato na larvicultura do pacamã

O objetivo deste trabalho foi avaliar o uso de diferentes biofiltros e substratos na qualidade da água e no desempenho de larvas de Lophiosilurus alexandri. Os tratamentos usados foram: sistema sem biofiltro (SB); biofiltro interno ao tanque com substrato de cascalho de diâmetro médio de 1,6 cm (CMe); biofiltro interno ao tanque com cascalho de diâmetro médio de 2,1 cm (CMa); biofiltro interno ao tanque com substrato constituído de uma mistura de 70% de brita (diâmetro médio de 1,3 cm) e 30% de concha (diâmetro médio de 1,1 cm) (CB); e sistema fechado (SF) com biofiltro externo aos tanques, com substrato de brita e concha. O experimento foi realizado em delineamento inteiramente casualizado, com cinco tratamentos e cinco repetições, durante 16 dias. Para íon amônio, nitrito, nitrato e ortofosfato, houve interação entre sistemas x dias de cultivo. Os sistemas SF, CMe e CB registraram menores concentrações de íon amônio e nitrito; o sistema SB, maiores concentrações de íon amônio e menores concentrações de nitrato; o SF, concentrações de ortofosfato superiores. A sobrevivência de L. alexandri foi inferior no SF. O crescimento não foi afetado pelos diferentes sistemas. Os biofiltros melhoraram a qualidade da água quanto aos compostos nitrogenados emfunção do tipo de substrato.

Antioxidant and cytotoxic activities of 'açaí' (Euterpe precatoria Mart.)

Decoction of roots of the Amazonian palm açaí (Euterpe precatoria Mart.) is widely used by Brazilian and Peruvian people as an anti-inflammatory, to heal kidney and liver diseases and against snake bites. In this study, the antioxidant activity of extracts and flavonoids (quercetin, catechin, epicatechin, rutin and astilbin) isolated from roots and leaf stalks of E. precatoria was investigated using β-carotene in TLC plates and DPPH radical scavenging in a spectrophotometric bioassay. All extracts and flavonoids showed activity. Also, the cytotoxic activity of these extracts was evaluated by the brine shrimp (Artemia salina) larvicide bioassay and was lower than that of lapachol, used as control. The presence of flavonoids and sitosterol-3-O-β-D-glucopyranoside in the extracts can justify the use of the plant in traditional medicine.

Antioxidant capacity of eugenol derivatives

Toxicity and antioxidant capacity of eugenol derivatives (E2 = 2-Methoxy-4-[1-propenylphenyl]acetate, E3 = 4-Allyl-2-methoxyphenylacetate, E4 = 4-Allyl-2-methoxy-4-nitrophenol, E5 = 5-Allyl-3-nitrobenzene-1,2-diol, E6 = 4-Allyl-2-methoxy-5-nitrophenyl acetate) were evaluated in order to determine the influence of the sustituents. E2-E6 were synthesized from eugenol (E1). E1 was extracted from cloves oil, and E2-E6 were obtained through acetylation and nitration reactions. Antioxidant capacity evaluated by DPPH (1, 1-Diphenyl-2-picrylhydrazil) and ORAC fluorescein demonstrated that E1 and E5 have a higher capacity and the minor toxicity evaluated by red blood cells haemolysis and the Artemia saline test. In accordance with our results, the compound's (E1-E5) use in the pharmaceutical, cosmetic and or food industries could be suggested.

Estudio químico y evaluación de la actividad antifouling del octocoral caribeño Eunicea laciniata

The bioassay guided purification of the octocoral Eunicea laciniata organic extract, collected at Santa Marta bay, Colombia, allowed the isolation of the new compound (-)-3β-pregna-5,20-dienyl-β-D-arabinopyranoside (1), along with the known compounds 1(S*),11(R*)-dolabell-3(E),7(E),12(18)-triene (2), 13-keto-1(S),11(R)-dolabell-3(E ),7(E),12(18)-triene (3), cholest- 5,22-dien-3β-ol (4), cholesterol (5), y brassicasterol (6). The structure and absolute configuration of 1 was determined on based spectroscopic analyses (NMR and CD). The extract showed antifouling activity against five strains of marine bacteria associated to heavy fouled surfaces. Also showed activity against the cypris of the cosmopolitan barnacle Balanus amphitrite, and low toxicity in Artemia salina test.

Efeito da temperatura do ar de secagem sobre o teor e a composição química do óleo essencial de Pectis brevipedunculata

Leaves and flower heads of P. brevipedunculata were submitted to four drying-air temperatures (room temperature, 40, 50 and 60 ºC). Room temperature (approximately 30 ºC) and higher temperature drying (50 and 60 ºC) had a deleterious effect on the essential oil content. The recommended drying-air temperature for the species is 40 ºC for it results in the same amount of essential oil observed in fresh cut plants. Overall, 13 components accounting for more than 92% of the total composition were identified. Citral was the major component, followed by α-pinene and limonene. The essential oil showed high toxicity against Artemia salina larvae.

Bioactive triterpenes and phenolics of leaves of Eugenia brasiliensis

A chemical investigation of Eugenia brasiliensis Lam. (Myrtaceae) leaves led to the isolation of α-amyrin and β-amyrin (in a mixture), betulin, 29-hydroxy-oleanolic acid, quercetin, catechin and gallocatechin. Herein, the identification of 29-hydroxy-oleanolic acid is reported for the first time in the Myrtaceae family. Moreover, in this study, the extract, fractions and six of the seven compounds were monitored for toxicity toward Artemia salina, antibacterial and acetylcholinesterase inhibitory activity. The crude ethanol extract of the leaves and fractions were found be active on A. salina toxicity bioassay.

Evaluation of antimicrobial activity and toxic potential of extracts and triterpenes isolated from Maytenus imbricata

The phytochemical study of hexane/ethyl ether (1:1) extract of the roots of M. imbricata, Celastraceae, resulted in the isolation and characterization of six known triterpenes: 11α-hydroxylup-20(29)-en-3-one, previously isolated from this species besides, 3β,11α-di-hydroxylup-20(29)-ene, 3,7-dioxofriedelane, 3-oxo-29-hydroxyfriedelane, tingenone and 6-oxo-tingenol. The chemical structures of these triterpenes were established by spectrometric data (IR, ¹H and 13C NMR) and through comparison with literature data. The hexane/ethyl ether (1:1), ethyl acetate and methanol extracts, and 11α-hydroxylup-20(29)-en-3-one, tingenone and 6-oxo-tingenol, showed antimicrobial properties on in vitro assays. All extracts and triterpenes, except 3β,11α-di-hydroxylup-20(29)-ene, presented toxicity demonstrated by the larvicidal effect test using Artemia salina.