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.223528533Bastos, J.K., Albuquerque, S., Silva, M.L.A., Evaluation of the trypanocidal activity of lignans isolated from the leaves of Zanthoxylum naranjillo (1999) Planta Med, 65, pp. 1-4Batista Jr., J.M., Lopes, A.A., Ambrósio, D.L., Regasini, L.O., Kato, M.J., Bolzani, V.S., Cicarelli, R.M., Furlan, M., Natural chromenes and chromene derivatives as potencial antitrypanosomal agents (2008) Biol Pharm Bull, 31, pp. 538-540Botsaris, A., Plants used traditionally to treat malaria in Brazil: The archives of Flora Medicinal (2007) J Ethnobiol Ethnomed, 1, p. 18Buainain, A., Giazzi, J.F., Belda Neto, F.M., Martini, A.S., Rosa, J.A., Pozetti, G.L., Estudo da atividade de extratos vegetais sobre o desenvolvimento de Trypanosoma cruzi em meio líquido de Warren (1992) Rev Cien Farm, 14, pp. 93-102Cabral, M.M., Barbosa-Filho, J.M., Maia, G.L., Chaves, M.C., Braga, M.V., de Souza, W., Neolignans from plants in northeastern Brazil (Lauraceae) with activity against (2010) Trypanosoma Cruzi. Exp Parasitol, 124, pp. 319-324Costa-Lotufo, L.V., Silveira, E.R., Barros, M.C., Lima, M.A., de Moraes, M.E., de Moraes, M.O., Pessoa, C., Antiproliferative effects of abietane diterpenes from aegiphilla lhotzkyana (2004) Planta Med, 70, pp. 180-182Cotinguiba, F., Regasini, L.O., Bolzani, V.S., Debonsi, H.M., Passerini, D.O., Cicarelli, R.M.B., Kato, M.J., Furlan, M., Piperamides and their derivatives as potential antitrypanosomal agents (2009) Med Chem Res, 18, pp. 703-711Coura, J.R., Castro, S.L., A critical review on Chagas disease chemotherapy (2002) Mem I Oswaldo Cruz, 97, pp. 3-24Coura, J.R., Present situation and new strategies for Chagas disease chemotherapy: A proposal (2009) Mem I Oswaldo Cruz, 104, pp. 549-554Fernandes, O., Souto, R.P., Castro, J.A., Pereira, J.B., Fernandes, N.C., Junqueira, A.C., Naiff, R.D., Coura, J.R., Brazilian isolates of Trypanosoma cruzi from humans and triatomines classified into two lineages using mini-exon and ribosomal RNA sequences (1998) Am J Trop Med Hyg, 58, pp. 807-811Fournet, A., Ferreira, M.E., Rojas de Arias, A., Guy, I., Guinaudeau, H., Heinzen, H., Phytochemical and antiprotozoal activity of (2007) Ocotea Lancifolia. Fitoterapia, 78, pp. 382-384Lopes, A.A., López, S.N., Regasini, L.O., Batista, J.M., Ambrósio, D.L., Kato, M.J., da Silva, B.V., Furlan, M., In vitro activity of compounds isolated from Piper crassinervium against Trypanosoma cruzi (2008) Nat Prod Res, 22, pp. 1040-1046Macedo, A.M., Oliveira, R.P., Pena, S.D.J., Chagas disease: Role of parasite genetic variation in pathogenesis (2002) Exp Mol Med, 4, pp. 1-16Muelas-Serrano, S., Nogal-Ruiz, J.J., Gómez-Barrio, A., Setting of a colorimetric method to determine the viability of Trypanosoma cruzi epimastigotes (2000) Parasitol Res, 86, pp. 999-1002Nwaka, S., Ridley, R.G., Virtual drug discovery and development for neglected diseases through publicprivate partnerships (2003) Nat Rev Drug Discov, 2, pp. 919-928Osorio, E., Arango, G.J., Jiménez, N., Alzate, F., Ruiz, G., Gutiérrez, D., Paco, M.A., Robledo, S., Antiprotozoal and cytotoxic activities in vitro of Colombian Annonaceae (2007) J Ethnopharmacol, 111, pp. 630-635Regasini, L.O., Cotinguiba, F., Passerini, G.D., Bolzani, V.S., Cicarelli, R.M.B., Kato, M.J., Furlan, M., Trypanocidal activity of Piper arboreum and Piper tuberculatum (Piperaceae) (2009) Rev Bras Farmacog, 19, pp. 199-203Saraiva, J., Vega, C., Rolon, M., da Silva, R., Silva, M.L., Donate, P.M., Bastos, J.K., de Albuquerque, S., In vitro and in vivo activity of lignan lactones derivatives against Trypanosoma cruzi (2007) Parasitol Res, 100, pp. 791-795Tibayrenc, M., Ayala, F.J., The clonal theory of parasitic protozoa: 12 years on (2002) Trends Parasitol, 18, pp. 405-410(2010), http://www.who.int/mediacentre/factsheets/fs340/en/index.html, World Health Organization 2010, accessed in Au

Avaliação das atividades antioxidante, anti e pró-hemolítica do extrato etanólico das folhas de Pterogyne nitens Tul. (Fabaceae-Caesalpinioideae) Evaluation of antioxidant, anti- and pro-hemolytic activities of ethanol extract from the leaves of Pterogynenitens Tul. (Fabaceae-Caesalpinioideae)

A pesquisa de produtos naturais permite a descoberta de novos princípios ativos, ou ainda, a descoberta de novas atividades para extratos de plantas (amplamente utilizados pela população brasileira) e princípios ativos naturais já conhecidos. Pterogyne nitens é uma planta cuja descrição das atividades é relativamente recente e, portanto, tem no extrato bruto boa fonte para pesquisas na área de produtos naturais. Desta forma, o objetivo deste trabalho foi estudar o perfil antioxidante do extrato bruto etanólico das folhas de P. nitens e possível interferência sobre a hemólise provocada pelo radical AAPH&#8226;. No estudo da ação antioxidante das espécies estudadas, ABTS&#8226;+, DPPH&#8226;, H2O2 e HOCl, encontrou-se os valores de IC50 de 5,0 µg mL-1, 17 µg mL-1, sem ação e 3,9 µg mL-1, respectivamente, valores relativamente baixos e que indicam bom potencial antioxidante. Foram encontradas atividades pró-hemolítica e anti-hemolítica para o extrato de forma concentração-dependente. O extrato estudado mostro boa fonte de moléculas naturais com potencial de ação biológica.<br>The search for natural products as a widespread practice enables the discovery of new active principles, or the discovery of new activities for plant extracts (extensively used by the population) and natural active principles already known. Pterogynenitensis is a plant whose descriptions of activities are relatively recent and therefore has in its crude extract a good source for research in the field of natural products. Thus, the aim of this study was to evaluate the antioxidant profile of crude ethanol extract from P. nitens leaves and a possible influence on the hemolysis caused by AAPH&#8226; radical. For the studied oxidant species, ABTS&#8226;+, DPPH&#8226;, HOCl and H2O2, the IC50 values were found of 5.0 µg mL-1, 17 µg mL-1, no action at all, and 3.9 µg mL-1, respectively, relatively low values, indicating a good antioxidant potential. Pro- and anti-hemolytic activities were found for the extract in a concentration-dependent way. The studied extract showed to be a good source of natural molecules with potential biological action

Avaliação das atividades antioxidante, anti e pró-hemolítica do extrato etanólico das folhas de Pterogyne nitens Tul. (Fabaceae-Caesalpinioideae)

A pesquisa de produtos naturais permite a descoberta de novos princípios ativos, ou ainda, a descoberta de novas atividades para extratos de plantas (amplamente utilizados pela população brasileira) e princípios ativos naturais já conhecidos. Pterogyne nitens é uma planta cuja descrição das atividades é relativamente recente e, portanto, tem no extrato bruto boa fonte para pesquisas na área de produtos naturais. Desta forma, o objetivo deste trabalho foi estudar o perfil antioxidante do extrato bruto etanólico das folhas de P. nitens e possível interferência sobre a hemólise provocada pelo radical AAPH•. No estudo da ação antioxidante das espécies estudadas, ABTS•+, DPPH•, H2O2 e HOCl, encontrou-se os valores de IC50 de 5,0 µg mL-1, 17 µg mL-1, sem ação e 3,9 µg mL-1, respectivamente, valores relativamente baixos e que indicam bom potencial antioxidante. Foram encontradas atividades pró-hemolítica e anti-hemolítica para o extrato de forma concentração-dependente. O extrato estudado mostro boa fonte de moléculas naturais com potencial de ação biológica.The search for natural products as a widespread practice enables the discovery of new active principles, or the discovery of new activities for plant extracts (extensively used by the population) and natural active principles already known. Pterogynenitensis is a plant whose descriptions of activities are relatively recent and therefore has in its crude extract a good source for research in the field of natural products. Thus, the aim of this study was to evaluate the antioxidant profile of crude ethanol extract from P. nitens leaves and a possible influence on the hemolysis caused by AAPH• radical. For the studied oxidant species, ABTS•+, DPPH•, HOCl and H2O2, the IC50 values were found of 5.0 µg mL-1, 17 µg mL-1, no action at all, and 3.9 µg mL-1, respectively, relatively low values, indicating a good antioxidant potential. Pro- and anti-hemolytic activities were found for the extract in a concentration-dependent way. The studied extract showed to be a good source of natural molecules with potential biological action.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP

Xylarenones C - E From An Endophytic Fungus Isolated From Alibertia Macrophylla

Xylarenones C - E (2 - 4), three new eremophilane sesquiterpenes, have been isolated from solid substrate cultures of a Camarops-like endophytic fungus isolated from Alibertia macrophylla. The structures were elucidated by analysis of spectroscopic data. Compounds were evaluated in subtilisin and pepsin protease assays, and compound 2 showed potent inhibitory activity against both proteases. © 2011 The American Chemical Society and American Society of Pharmacognosy.74613531357Rodriguez, R., Redman, R., (2008) J. Exp. Bot., 59, pp. 1109-1114Smith, S., Tank, D., Boulanger, L., Bascom-Slack, C., Eisenman, K., Kingery, D., Babbs, B., Strobel, S., (2008) PLoS ONE, 3, p. 3052Jiao, R.H., Xu, S., Liu, J.Y., Ge, H.M., Xu, H.C., Zhu, H.L., Tan, R.X., (2006) Org. Lett., 8, pp. 5709-5712Gunatilaka, A.A.L., (2006) J. Nat. Prod., 69, pp. 509-526Tomasselli, A.G., Heinrikson, R.L., (2000) Biochim. Biophys. Acta, 1477, pp. 189-214Oliveira, C.M., Silva, G.H., Regasini, L.O., Zanardi, L.M., Evangelista, A.H., Young, M.C.M., Bolzani, V.S., Araújo, A.R., (2009) Z. Naturforsch. C, 64, pp. 824-830Zhi-Yu, H., Yao-Yao, L., Yao-Jian, H., Wen-Jin, S., Yue-Mao, S., (2008) Helv. Chim. Acta, 91, pp. 46-52McDonald, L.A., Barbiere, L.R., Berman, V.S., Janso, J., Lassota, P., Carter, G.T., (2004) J. Nat. Prod., 67, pp. 1565-1567Nunes, F.M., Oliveira, M.C.F., Arriaga, A.M.C., Lemos, T.L.G., Andrade-Neto, M., Mattos, M.C., Mafezoli, J., Ferreira, A.G., (2008) J. Braz. Chem. Soc., 19, pp. 478-482Arciniegas, A., Pérez-Castorena, A.-L., Reyes, S., Contreras, J.L., Vivar, A.R., (2003) J. Nat. Prod., 66, pp. 225-229Kim, S.-K., Hatori, M., Ojika, M., Sakagami, Y., Marumo, S., (1998) Bioorg. Med. Chem., 6, pp. 1975-1982Huang, Y.F., Qiao, L., Li, L.A., Pei, Y.H., Tian, L., (2008) Chin. Chem. Lett., 19, pp. 562-564Davis, D.A., Brown, C.A., Singer, K.E., Wang, V., Kaufman, J., Stahl, S.J., Wingfield, P., Yarchoan, R., (2006) Antiv. Res., 72, pp. 89-99Ji-Qing, X., Li-Hong, H., (2009) Helv. Chim. Acta, 92, pp. 357-361Babine, R.E., Bender, S.L., (1997) Chem. Rev., 97, pp. 1359-1472Huhndorf, S.M., Miller, A.N., A new species of Camarops and phylogenetic analysis of related taxa in the Boliniaceae (2008) North Am. Fungi, 3, pp. 231-239Nannfeldt, J.A., Camarops Karst. (Sphaeriales-Boliniaceae). Svenk Botanisk Tidskrift (1972) Svensk Bot. Tidskr., 66, pp. 335-376Vasilyeva, L.N., Stephenson, S.L., Miller, A.N., Pyrenomycetes of the Great Smoky Mountains National Park. IV. Biscogniauxia, Camaropella, Camarops, Camillea, Peridoxylon and Whalleya (2007) Fungal Diversity, 25, pp. 219-231González, M.C., Anaya, A.L., Glenn, A.E., Saucedo-García, A., MacÍas-Rubalcava, M.L., Hanlin, R.T., (2007) Mycotaxon, 101, pp. 251-260Isaka, M., Srisanoh, U., Veeranondha, S., Choowong, W., Lumyong, S., (2009) Tetrahedron, 65, pp. 8808-8815Silva, G.H., Teles, H.L., Zanardi, L.M., Young, M.C.M., Eberlin, M.N., Haddad, R., Pfenning, L.H., Araujo, A.R., (2006) Phytochemistry, 67, pp. 1964-1969Sette, L.D., Passarini, M.R.Z., Delarmelina, C., Salati, F., Duarte, M.C.T., (2006) World J. Microbiol. Biotechnol., 22, pp. 1185-1195Thompson, J.D., Higgins, D.G., Gibson, T.J., Clustal, W., (1994) Nucleic Acids Res., 22, pp. 4673-4680Tamura, K., Dudley, J., Nei, M., Kumar, S., (2007) Mol. Biol. Evol., 24, pp. 1596-1599Kimura, M.J., (1980) J. Mol. Evol., 16, pp. 111-120Saitou, N., Nei, M., (1987) Mol. Biol. Evol., 4, pp. 406-42