Study of Salmonella typhimurium mutagenicity assay of (E)-piplartine by the Ames test

Phytochemical studies carried out with Piperaceae species have shown great diversity of secondary metabolites among which are several displayed considerable biological activities. The species Piper tuberculatum has been intensively investigated and a series of amides have been described. For instance, (E)-piplartine showed significant cytotoxic activity against tumor cell lines, especially human leukemia cell lines; antifungal activity against Cladosporium species; trypanocidal activity and others. Considering the popular use of P. tuberculatum and the lack of pharmacological studies regarding this plant species, the mutagenic and antimutagenic effect of (E)-piplartine was evaluated by the Ames test, using the strains TA97a, TA98, TA100 and TA102 of Salmonella typhimurium. No mutagenic activity was observed for this compound.Key words: Piperaceae, Piper tuberculatum, (Z)-piplartine, mutagenic activated, Ames test

Further monoterpene chromane esters from Peperomia obtusifolia: VCD determination of the absolute configuration of a new diastereomeric mixture

A reinvestigation of the monoterpene chromane ester enriched fraction from Peperomia obtusifolia using chiral chromatography led to the identification of a minor peak, which was elucidated by NMR and HRMS as fenchyl-3,4-dihydro-5- hydroxy-2,7-dimethyl-8-(3″-methyl-2″-butenyl)-2-(4′-methyl- 1′,3′-pentadienyl)-2H-1-benzopyran-6-carboxylate, the same structure assigned to two other fenchyl esters described previously, pointing out a stereoisomeric relationship among them. Further NMR analysis revealed that it was actually a mixture of two compounds, whose absolute configurations were determined by VCD measurements. Although, almost no vibrational transitions could be assigned to the chiral chromane, the experimental VCD spectrum was largely opposite to that obtained for the average experimental VCD [(2S,1‴R,2‴R,4‴S + 2R,1‴R,2‴R,4‴S)/2] for fenchol derivatives. These results allowed us to assign the putative compounds as a racemic mixture of the chiral chromane esterified with the monoterpene (1S,2S,4R)-fenchol, which had not been identified in our early work.Fil: Batista Junior, João Marcos. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: Batista, Andrea N. L.. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: Kato, Massuo J.. Universidade de Sao Paulo; BrasilFil: Bolzani, Vanderlan S.. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: López, Silvia Noelí. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; ArgentinaFil: Nafie, Laurence A.. Syracuse University; Estados UnidosFil: Furlan, Maysa. Universidade Estadual Paulista Julio de Mesquita Filho; Brasi

Biopiracy <i>versus </i>one-world medicine – from colonial relicts to global collaborative concepts

Background: Practices of biopiracy to use genetic resources and indigenous knowledge by Western companies without benefit-sharing of those, who generated the traditional knowledge, can be understood as form of neocolonialism.Hypothesis: : The One-World Medicine concept attempts to merge the best of traditional medicine from developing countries and conventional Western medicine for the sake of patients around the globe.Study design: Based on literature searches in several databases, a concept paper has been written. Legislative initiatives of the United Nations culminated in the Nagoya protocol aim to protect traditional knowledge and regulate benefit-sharing with indigenous communities. The European community adopted the Nagoya protocol, and the corresponding regulations will be implemented into national legislation among the member states. Despite pleasing progress, infrastructural problems of the health care systems in developing countries still remain. Current approaches to secure primary health care offer only fragmentary solutions at best. Conventional medicine from industrialized countries cannot be afforded by the impoverished population in the Third World. Confronted with exploding costs, even health systems in Western countries are endangered to burst. Complementary and alternative medicine (CAM) is popular among the general public in industrialized countries, although the efficacy is not sufficiently proven according to the standards of evidence-based medicine. CAM is often available without prescription as over-the-counter products with non-calculated risks concerning erroneous self-medication and safety/toxicity issues. The concept of integrative medicine attempts to combine holistic CAM approaches with evidence-based principles of conventional medicine.Conclusion: To realize the concept of One-World Medicine, a number of standards have to be set to assure safety, efficacy and applicability of traditional medicine, e.g. sustainable production and quality control of herbal products, performance of placebo-controlled, double-blind, randomized clinical trials, phytovigilance, as well as education of health professionals and patients

A Transmission Power Self-Optimization Technique for Wireless Sensor Networks

Wireless sensor networks (WSNs) are generally used to monitor hazardous events in inaccessible areas. Thus, on one hand, it is preferable to assure the adoption of the minimum transmission power in order to extend as much as possible the WSNs lifetime. On the other hand, it is crucial to guarantee that the transmitted data is correctly received by the other nodes. Thus, trading off power optimization and reliability insurance has become one of the most important concerns when dealing with modern systems based on WSN. In this context, we present a transmission power self-optimization (TPSO) technique for WSNs. The TPSO technique consists of an algorithm able to guarantee the connectivity as well as an equally high quality of service (QoS), concentrating on the WSNs efficiency (Ef), while optimizing the transmission power necessary for data communication. Thus, the main idea behind the proposed approach is to trade off WSNs Ef against energy consumption in an environment with inherent noise. Experimental results with different types of noise and electromagnetic interference (EMI) have been explored in order to demonstrate the effectiveness of the TPSO technique

Evaluation of mutagenicity and antimutagenicity of different fractions of Pterogyne nitens (Leguminosae), using Tradescantia pallida micronuclei assay

Pterogyne nitens (Fabaceae-Caesalpinioideae) é uma árvore nativa da América do Sul, onde é empregada na medicina popular para o tratamento da ascaridíase. Recentemente, descrevemos o efeito mutagênico do extrato etanólico das folhas de P. nitens. Dessa forma, o presente estudo teve por objetivo aprofundar a avaliação do potencial mutagênico das frações isoladas das folhas de Pterogyne nitens, acetato de etila (AcOEt), n-butanólica (BuOH) e hidroalcóolica (HA). Quando o efeito mutagênico foi observado somente nas maiores concentrações testadas, o potencial antimutagênico também foi avaliado. Os ensaios mutagênicos e antimutagênicos foram realizados utilizando ensaio de micronúcleo em Trandescantia pallida. Na avaliação de mutagenicidade, observou-se o efeito nas frações AcOEt (0,460 mg/mL), BuOH (0,142, 0,285, 0,570 e 1,14 mg/mL) e HA (0,050, 0,100, 0,200 e 0,400 mg/mL). Considerando que o efeito mutagênico da fração AcOEt foi observado somente na concentração mais elevada (0,460 mg/mL), o potencial antimutagênico da mesma foi avaliado. As concentrações de 0,115 e 0,230 mg/mL da fração AcOEt demonstraram atividade antimutagênica. A partir dos resultados do presente estudo, conclui-se que determinadas frações de P. nitens apresentam mutagenicidade (BuOH e HA), enquanto a fração AcOEt apresentou efeito antimutagênico nas maiores concentrações. Esses resultados tornam o estudo da P. nitens bastante promissor, considerando que esta planta possui distribuição geográfica ampla e tem sido pouco estudada.Pterogyne nitens (Fabaceae-Caesalpinioideae) is a tree native to South American, where it is used in folk treatment of ascaridiasis. Recently, we have been describing the mutagenic effect of the ethanol extract of leaves of P. nitens. Thus, the present study aimed at evaluating the mutagenic potential of the ethyl acetate (EtOAc), n- butanol (BuOH) and hydroalcoholic (HA) fractions. When the mutagenic effect was observed only in the highest tested concentrations, the antimutagenic activity was also evaluated. Both mutagenic and antimutagenic assays were performed using T. pallida micronuclei assay. Mutagenicity was observed between different concentrations of the P nitens fractions, EtOAc (0.460 mg/mL), BuOH (0.142, 0.285, 0.570 and 1.14 mg/mL) and HA (0.050, 0.100, 0.200 and 0.400 mg/mL). Whereas the mutagenic effect of the EtOAc fraction was observed in the highest concentration (0.460 mg/mL), its antimutagenic potential was evaluated. The 0.115 and 0.230 mg/mL concentrations of the EtOAc fraction demonstrated antimutagenic activity. Based on the results of the present study we can conclude that some P. nitens fractions (BuOH and HA) demonstrated mutagenic effects whereas the EtOAc fraction shown low mutagenicity and amtimutagenicity in the two higher concentrations. Those results stimulate the studies with P. nitens, which possess spread geographic distribution and it is still low studied

Diagnóstico da pesquisa em biodiversidade no Brasil

Biodiversity is a result of millions of years of biological evolution, and is the component of the system which supports life on our planet. Besides the intrinsic value of each species, all of them as a whole, as well as of the interactions among the species, and their interaction with the physical and chemical environment, result in ecosystem services vital for supporting life on Earth. Because of that, the science of biodiversity is largely recognized as a priority area of scientific investigation both in developed and developing countries. In Brazil, the research on biodiversity can be divided in three parts: 1) discovery and characterization of biodiversity - including marine and human-altered landscapes - systematics and taxonomy; 2) understanding the functioning of ecosystems and environmental services, including in marine and human-altered landscapes; 3) bioprospecting of the chemical diversity of the Brazilian biota.A biodiversidade resulta de milhões de anos de evolução biológica e é o componente do sistema de suporte à vida de nosso planeta. Além do valor intrínseco de cada espécie, seu conjunto, bem como o de interações entre espécies e destas com o meio físico-químico, resultam em serviços ecossistêmicos imprescindíveis para manter a vida na Terra. Sendo assim, a ciência da biodiversidade é amplamente reconhecida como área prioritária de investigação científica, tanto nos países desenvolvidos como naqueles em desenvolvimento. No Brasil, a pesquisa em biodiversidade pode ser dividida em três principais vertentes: 1) descoberta e caracterização da biodiversidade, inclusive marinha e em paisagens alteradas - sistemática e taxonomia; 2) compreensão do funcionamento de ecossistemas e serviços ambientais, inclusive marinhos e em paisagens alteradas; 3) bioprospecção da quimiodiversidade da biota brasileira

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

Anti-angiogenic effects of pterogynidine alkaloid isolated from Alchornea glandulosa

<p>Abstract</p> <p>Background</p> <p>Angiogenesis, a complex multistep process that comprehends proliferation, migration and anastomosis of endothelial cells (EC), has a major role in the development of pathologic conditions such as inflammatory diseases, tumor growth and metastasis. Brazilian flora, the most diverse in the world, is an interesting spot to prospect for new chemical leads, being an important source of new anticancer drugs. Plant-derived alkaloids have traditionally been of interest due to their pronounced physiological activities. We investigated the anti-angiogenic potential of the naturally occurring guanidine alkaloid pterogynidine (Pt) isolated from the Brazilian plant <it>Alchornea glandulosa</it>. The purpose of this study was to examine which features of the angiogenic process could be disturbed by Pt.</p> <p>Methods</p> <p>Human umbilical vein endothelial cells (HUVEC) were incubated with 8 μM Pt and cell viability, proliferation, apoptosis, invasion and capillary-like structures formation were addressed. Nuclear factor κB (NFκB), a transcription factor implicated in these processes, was also evaluated in HUVEC incubated with Pt. Quantifications were expressed as mean ± SD of five independent experiments and one-way analysis of variance (ANOVA) followed by the Dunnet test was used.</p> <p>Results</p> <p>A significant decrease in proliferation and invasion capacity and an effective increase in apoptosis as assessed by bromodeoxyuridine (BrdU), double-chamber and terminal transferase dUTP nick end labeling (TUNEL) assay, respectively, have been found. Pt also led to a drastic reduction in the number of capillary-like structures formation when HUVEC were cultured on growth factor reduced-Matrigel (GFR-Matrigel) coated plates. In addition, incubation of HUVEC with Pt resulted in reduced NFκB activity.</p> <p>Conclusion</p> <p>These findings emphasize the potential use of Pt against pathological situations where angiogenesis is stimulated as tumor development.</p