Screening of Brazilian plants for antimicrobial and dnadamaging activities: I. Atlantic rain forest . Ecological station juréia-itatins

(Triagem de plantas nativas do Brasil para atividades antimicrobiana e de Danos no DNA I. Mata Atlântica . Estação Ecológica Juréia-Itatins). Oitenta e oito espécies nativas do estado de São Paulo foram coletadas numa região de Mata Atlântica e ensaiadas quanto a sua atividade antimicrobiana e capacidade de causar danos no DNA. Dos 114 extratos submetidos aos ensaios para atividade antibacteriana, apenas os extratos de folhas e galhos de Aspidosperma ramiflorum (Apocynaceae) apresentaram uma atividade fraca contra Escherichia coli. No ensaio antifúngico com Candida albicans, não foram observados extratos ativos. Por outro lado, no ensaio de bioautografia com Cladosporium sphaerospermum e C. cladosporioides 12% dos extratos apresentaram atividade. Contudo, nesse ensaio, somente o extrato dos ramos de Psychotria mapoureoides (Rubiaceae) inibiu fortemente o crescimento de ambas espécies do fungo. O ensaio para danos no DNA com cepas mutantes de Saccharomyces cerevisiae apresentou 17.5 % de extratos ativos. A maioria dos extratos ativos (55 %) apresentou resultados seletivos para danos dependentes da topoisomerase II como mecanismo de reparo do DNA e somente 20 % foram seletivos para o mecanismo da topoisomerase I.

Screening for antifungal, DNA-damaging and anticholinesterasic activities of Brazilian plants from the Atlantic Rainforest: Ilha do Cardoso State Park

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Trypanocidal activity of Brazilian plants against epimastigote forms from Y and Bolivia strains of Trypanosoma cruzi

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Comparison of Brazilian plants used to treat gastritis on the oxidative burst of helicobacter pylori -stimulated neutrophil

Ten Brazilian medicinal plants used to treat gastritis and ulcers were carefully selected on the basis of ethnopharmacological importance and antiulcerogenic activity previously described. The antioxidant activity of the methanolic extracts was determined in analysis conditions that simulate a real biological activity on inhibition of the oxidative burst induced in neutrophils using Helicobacter pylori as activator, by a luminol-amplified chemiluminescence assay. The extracts, at low concentration (5 g/mL), exhibited a large variation in inhibitory effects of H. pylori-induced oxidative burst ranging from 48% inhibition to inactive, but all extracts, excluding Byrsonima intermedia, had inhibitory activity over 80% at the concentration of 100 g/mL. The total suppressive antioxidant capacity measured as the effective concentration, which represents the extract concentration producing 50% inhibition of the chemiluminescence induced by H. pylori, varies from 27.2 to 56.8 g/mL and was in the following order: Qualea parviflora > Qualea multiflora > Alchornea triplinervia > Qualea grandiflora > Anacardium humile > Davilla elliptica > Mouriri pusa > Byrsonima basiloba > Alchornea glandulosa > Byrsonima intermedia. The main groups of compounds in tested extracts are presented. Differences in the phytochemical profile, quantitatively and qualitatively, of these plants can explain and justify their protective effect on the gastric mucosa caused by the neutrophil-generated ROS that occurs when H. pylori displays its evasion mechanisms. © 2013 Cibele Bonacorsi et al.

Natural compounds isolated from Brazilian plants are potent inhibitors of hepatitis C virus replication in vitro

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Trypanocidal activity of Brazilian plants against epimastigote forms from Y and Bolivia strains of Trypanosoma cruzi

Chagas disease is one of the main public health problems in Latin America. Since the available treatments for this disease are not effective in providing cure, the screening of potential antiprotozoal agents is essential, mainly of those obtained from natural sources. This study aimed to provide an evaluation of the trypanocidal activity of 92 ethanol extracts from species belonging to the families Annonaceae, Apiaceae, Cucurbitaceae, Lamiaceae, Lauraceae, Moraceae, Nyctaginaceae, and Verbenaceae against the Y and Bolivia strains of Trypanosoma cruzi. Additionally, cytotoxic activity on LLCMK2 fibroblasts was evaluated. Both the trypanocidal activity and cytotoxicity were evaluated using the MTT method, in the following concentrations: 500, 350, 250, and 100 µg/mL. Benznidazole was used for positive control. The best results among the 92 samples evaluated were obtained with ethanol extracts of Ocotea paranapiacabensis (Am93) and Aegiphila lhotzkiana (Am160). Am93 showed trypanocidal activity against epimastigote forms of the Bolivia strain and was moderately toxic to LLCMK2 cells, its Selectivity Index (SI) being 14.56, while Am160 showed moderate trypanocidal activity against the Bolivia strain and moderate toxicicity, its SI being equal to 1.15. The screening of Brazilian plants has indicated the potential effect of ethanol extracts obtained from Ocotea paranapiacabensis and Aegiphila lhotzkiana against Chagas disease.

New Brazilian Floristic List Highlights Conservation Challenges

A comprehensive new inventory of Brazilian plants and fungi was published just in time to meet a 2010 Convention on Biological Diversity target and offers important insights into this biodiversity's global significance. Brazil is the home to the world's richest flora (40,989 species; 18,932 endemic) and includes two of the hottest hotspots: Mata Atlantica (19,355 species) and Cerrado (12,669 species). Although the total number of known species is one-third lower than previous estimates, the absolute number of endemic vascular plant species is higher than was previously estimated, and the proportion of endemism (56%) is the highest in the Neotropics. This compilation serves not merely to quantify the scale of the challenge faced in conserving Brazil's unique flora but also serves as a key resource to direct action and monitor progress. Similar efforts by other megadiverse countries are urgently required if the 2020 targets of the Convention on Biological Diversity and the Global Strategy for Plant Conservation are to be attained.

Gene expression during early somatic embryogenesis in Brazilian pine (Araucaria angustifolia (Bert) O. Ktze)

Brazilian pine (Araucaria angustifolia (Bert) O. Ktze) is the only native conifer species with economic importance in Brazil. Recently, due to intensive exploitation Brazilian pine was included in the official list of endangered Brazilian plants, under the "vulnerable" category. Biotechnology tools like somatic embryogenesis (SE) are potentially useful for mass clonal propagation and ex situ conservation strategies of commercial and endangered plant species. In spite of that, numerous obstacles still hamper the full application of SE technology for a wider range of species, including Brazilian pine. To enhance somatic embryogenesis in Brazilian pine and to gain a better understanding of the molecular events associated with somatic embryo development, we analyzed the steady-state transcript levels of genes known to regulate somatic embryogenesis using semiquantitative reverse transcription polymerase chain reaction (sqRT-PCR). These genes included Argonaute (AaAGO), Cup-shaped cotyledon1 (AaCUC), wushel-related WOX (AaWOX), a S-locus lectin protein kinase (AaLecK), Scarecrow- like (AaSCR), Vicilin 7S (AaVIC), Leafy Cotyledon 1 (AaLEC), and a Reversible glycosylated polypeptide (AaRGP). Expression patterns of these selected genes were investigated in embryogenic cultures undergoing different stages of embryogenesis, and all the way to maturation. Up-regulation of AaAGO, AaCUC, AaWOX, AaLecK, and AaVIC was observed during transition of somatic embryos from stage I to stage II. During the maintenance phase of somatic embryogenesis, expression of AaAGO and AaSCR, but not AaRPG and AaLEC genes was influenced by presence/ absence of plant growth regulators, both auxins and cytokinins. The results presented here provide new insights on the molecular mechanisms responsible for somatic embryo formation, and how selected genes may be used as molecular markers for Brazilian pine embryogenesis.

On the relationships between molecular conformations and intermolecular contacts toward crystal self-assembly of mono-, di-, tri-, and tetra-oxygenated xanthone derivatives

Oxygenated xanthones have been extensively investigated over the years, but there are few reports concerning their crystal structure. Our chemical investigations of Brazilian plants resulted in the isolation of four natural products named 1-hydroxyxanthone (I), 1-hydroxy-7-methoxyxanthone (II), 1,5-dihydroxy-3-methoxyxanthone (III), and 1,7-dihydroxy-3,8-dimethoxyxanthone (IV). The structures of these compounds were established on the basis of single crystal X-ray diffraction. The xanthone nucleus conformation is essentially planar with the substituents adopting the orientations less sterically hindered. In addition, classical intermolecular hydrogen bonds (O-H center dot center dot center dot O) present in III and IV give rise to infinite ribbons. However, the xanthone I does not present any intermolecular hydrogen bonds, meanwhile the xanthone II presents only a non-classical one (C-H center dot center dot center dot O). The crystal packing of all xanthone structures is also stabilized by pi-pi interactions. The fingerprint plots, derived from the Hirshfeld surfaces, exhibited significant features of each crystal structures.

Avaliação da atividade mutagênica do extrato etanólico bruto de Paepalanthus latipes (Eriocaulaceae) e dos compostos flavonoídicos 7-metoxilados relacionados

Paepalanthus latipes (Silveira) é uma das plantas brasileiras nativas da Serra do Cipó, Minas Gerais, conhecida como sempre-vivas e muito exportada para os Estados Unidos, Europa e Japão, por seu valor ornamental. Poucos resultados são relatados quanto à atividade biológica destas plantas. Este trabalho teve como objetivo avaliar a atividade mutagênica do extrato etanólico bruto de P. latipes e de dois flavonóides 7-metoxilados dele isolados (7-metilquercetagetina e 7-metilquercetagetina-4'-O-β-D-glicopiranosídeo), através do teste de Ames, utilizando linhagens mutantes de Salmonella typhimurium TA98 e TA100. A atividade mutagênica das amostras testadas, em concentrações variando de 62,5 a 375 μg/placa, foi determinada com ativação metabólica (utilizando-se a fração microssomal S9) e na ausência dessa. Os resultados demonstraram que, tanto o extrato etanólico bruto de P. latipes quanto os flavonóides 7-metoxilados testados, não induziram atividade mutagênica nas linhagens TA98 e TA100.

Estudo químico de Zollernia ilicifolia (Fabaceae), Wilbrandia ebracteata (Cucurbitaceae) e Caesalpinia ferrea (Caesalpiniaceae)

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

A Catuama e o bilobalide na regeneração nervosa periférica de ratos submetidos à secção do nervo isquiático

The Catuama((R)) is composed of four Brazilian plants extracts (Paullinia cupana, Trichilia catigua, Ptychopetalum olacoides e Zingiber officinale). The Catuama((R)) is known as having neuroprotector, anti-inflammatory, antioxidant and antidepressant effects. Bilobalide, extracted from leaves of Ginkgo biloba, is known by its neuroprotective effect in the central and peripheral nervous systems. The present study evaluates the effect of Catuama((R)) and bilobalide on peripheral nerve regeneration in rats following a sciatic nerve section. Sciatic nerve of forty adult rats was transected with a 10-mm gap and the proximal and distal nerve stumps were fixed in a silicone tube filled with liquid collagen. The animals were divided into four groups: the control group (A), two groups treated with Catuama((R)) by gavage along 28 days after the surgery in different doses of 100 (B) and 400mg. kg(-1) (C) and the group using 200 mu M bilobalide (D) associated with the liquid collagen in the silicone tube. Evaluations were done by a walk test on the first, fifth and tenth week after the surgery. Electrophysiological stimulation and quantitative and qualitative histological analyses of the sciatic nerve and gastrocnemius muscle were also performed on the tenth week after the surgery. All groups showed good regeneration but no statistical difference was found between treatments and control groups (P > 0.05).

Evaluation of the anti-mycobacterium tuberculosis activity and in vivo acute toxicity of annona sylvatic

Background The recent emergence of extensively multidrug-resistant Mycobacterium tuberculosis strains has further complicated the control of tuberculosis. There is an urgent need for the development of new molecular candidates antitubercular drugs. Medicinal plants have been an excellent source of leads for the development of drugs. The aim of this study was to evaluate the in vitro activity of 28 alcoholic extracts and essential oils of native and exotic Brazilian plants against Mycobacterium tuberculosis and to further study these extracts through chemical fractionation, the isolation of their constituents, and an evaluation of the in vivo acute toxicity of the active extracts. To the best of our knowledge this is the first chemical characterization, antituberculosis activity and acute toxicity evaluation of Annona sylvatica. Methods The anti-mycobacterial activity of these extracts and their constituent compounds was evaluated using the resazurin reduction microtiter assay (REMA). To investigate the acute toxicity of these extracts in vivo, female Swiss mice were treated with the extracts at doses of 500, 1000 and 2000 mg · kg-1 of body weight. The extracts were characterized by LC-MS, and the constituents were isolated and identified by chromatographic analysis of spectroscopic data. Results Of the 28 extracts, the methanol extract obtained from the leaves of Annona sylvatica showed anti-mycobacterial activity with an minimal inhibitory concentration (MIC) of 184.33 μg/mL, and the ethyl acetate fraction (EAF) resulting from liquid-liquid partitioning of the A. sylvatica extract showed an MIC of 115.2 μg/mL. The characterization of this extract by LC-MS identified flavonoids and acetogenins as its main constituents. The phytochemical study of the A. sylvatica EAF resulted in the isolation of quercetin, luteolin, and almunequin. Conclusions Among the compounds isolated from the EAF, luteolin and almunequin were the most promising, with MICs of 236.8 μg/mL (827.28 μM) and 209.9 μg/mL (328.48 μM), respectively. The acute administration of the EAF fraction in doses of 500, 1000, and 2000 mg · kg-1 of body weight did not cause signs of toxicity in the treated animals.