Natural products from Brazilian biodiversity as a source of new models for medicinal chemistry

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

Tropical biodiversity: has it been a potential source of secondary metabolites useful for medicinal chemistry?

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

Estabilidade e eficácia de fotoprotetores contendo filtros inorgânicos e quercetina

A exposição ao sol traz benefícios à saúde, no entanto, o excesso pode ocasionar danos cutâneos dentre os quais se destacam as neoplasias. A fotoproteção é um método para a prevenção dos efeitos danosos da radiação ultravioleta (UV) e a biodiversidade Brasileira é campo fértil para pesquisas nesta área. Dessa forma, os objetivos deste estudo envolveram o desenvolvimento de formulações fotoprotetoras contendo quercetina (composto bioativo) e filtros solares físicos (dióxido de titânio e óxido de zinco), com posterior caracterização das formulações e avaliação da sua estabilidade. As formulações contendo o composto bioativo, isolado ou em associação com os filtros físicos, possuíram valores de pH biocompatíveis com a pele,intervalo de viscosidade aparente entre 10550 e 23600 cP; fator de proteção solar (FPS) estimado entre 2.1 e 22.5; e amplo espectro de proteção, com comprimentos de onda crítico acima de 379 nm. Constatou-se que não foi adequado utilizar a quercetina associada aos filtros solares físicos devido às interações negativas que ocorreram entre o composto e os metais, somente identificadas ao longo do estudo de estabilidade. No entanto, em função da eficácia estimada in vitro apresentada pelo flavonoide, seu uso ainda pode ser explorado como substituto alternativo aos filtros solares clássicos.

Community perceptions of four protected areas in the Northern portion of the Cerrado hotspot, Brazil

Establishing effective networks of protected areas (PAS) is one of the major goals of conservation strategies worldwide. However, the success of PAS in promoting biodiversity conservation depends on their integration to local and regional contexts, reducing and mitigating human impacts originating from buffer zones. Community perceptions affect interactions between residents and PAS, and thereby conservation effectiveness. Research at Tocantins state (northern Brazilian Cerrado), aimed to analyse local community perceptions of four PAs, discussing how different factors may influence these. Perceptions were assessed through standardized interviews applied to PA employees and 275 local inhabitants. There was modest community participation in PA establishment and management. Residents were aware of the PAS` existence, but were unfamiliar with their goals. Length of residency and occupation of inhabitants influenced their PA perceptions, shaping different people-park relations in each of the four studied PAs. Involvement of local residents in PA planning and management represents a central strategy to strengthen local support for PAS over the long term. In those areas that still have settlements inside their boundaries, community relocation should follow a careful participatory process to avoid significant changes in local perceptions and attitudes towards these PAS, crucial for conserving Brazilian biodiversity.

Ensaios em opções reais e investimento sob incerteza

Esta tese é composta por três artigos, nos quais são apresentadas extensões e aplicações da Teoria das Opções Reais, todas de interesse para formuladores de política econômica no Brasil. O primeiro faz uma análise original da questão da bioprospecção, ou a exploração da diversidade biológica para fins econômicos. Duas estruturas alternativas para o desenho do mecanismo de concessão, visando o uso sustentável da biodiversidade brasileira, são sugeridas: (i) um modelo de projetos de P&D com maturidade incerta, no qual a intensidade do processo de Poisson que governa o tempo de maturação é explicitamente dependente do nível da biodiversidade no local concedido; (ii) um modelo de Agente-Principal, onde o Estado delega o exercício da opção de investimento à empresa de pesquisa biotecnológica. O segundo artigo avança a analogia entre opções de venda (“put options”) e cotas de importação. Os parâmetros relevantes para apreçar as licenças são agora obtidos endogenamente, a partir da interação entre a firma importadora e os produtores domésticos. Por fim, no terceiro, é feita análise pioneira do mercado paralelo de títulos precatórios no Brasil. Um modelo para a valoração de tais títulos é construído e proposto, tendo por base o arcabouço institucional existente sobre o assunto, tanto no governo central, como nos estados e municípios.

Caracterização e composição florística de uma comunidade savânica no Rio Grande do Norte, Brasil : subsídios para a conservação

Studies on Brazilian biodiversity are still very few and can observe the difference of knowledge between the different regions of the country. This affirmation can be verified in the investigation to identify the rare species in Brazil and the key biodiversity areas (ACBs). In that study were identified for Brasil 2.256 rare species and 752 ACBs. The Rio Grande do Norte (RN) was the only Brazilian state that has not been identified any rare species and no ACBs, possibly due to the lack of floristic studies in this state. A particular area was selected for this study: an area of ecological tension with savanna physiognomy in Rio do Fogo, RN. This savanna community is represented in RN in a fragment and immersed in restinga and caatinga and was identified and described only through of radar imagens there are no studies to date in loco . We have prepared the following questions about this community savanna: 1) The region delimited and described by through of radar images by the RADAMBRASIL, 1976, can be associated of the Cerrado, in terms of floristic ?; 2) What is the floristic composition of this area? This area includes rare species, endemic or endangered? 3) What is the geographical and phytogeographical distribution of plant species registered in this area? 4) Those plant species registered are endemic or have affinity with other areas phytoecological Brazilian? To answer these questions we performed a floristic inventory of the August 2007 to September/2009. The results are presented in two chapters (manuscripts). The first chapter, titled "The Savannah Rio Grande do Norte: floristic links with other plant formations in the Northeast and Center-West Brazil" was submitted to the Revista Brasileira de Botância. Chapter 1 discusses the phytogeographical distribution of the species, by comparing floristic studies conducted in the Cerrado, Caatinga and Restinga in the Northeast and Cerrado of the Central Brazil. The analysis of data of this study and compilation with other studies indicated that: i) the record of 94 plant species; ii) of total species, about 64% are associated with the Cerrado, the second specialized bibliography, and about 78% as the List of Species of Flora of Brazil. However, about 73% of total species (94) are also distributed in the Caatinga, the Atlantic forest 64%, the Amazon forest 64%, the Pantanal 15% and the Pampa 12%. Floristically the data show that the community studied is influenced by other floras, has a structure where grasses dominate and also because of his appearance the same savanna then be classified as a Savana gramíneo-lenhosa do tabuleiro . Chapter 2, titled "Considerations on the flora of a savanna community in Rio Grande do Norte, northeastern Brazil: Subsidy key area for conservation" was submitted to the Revista Natureza e Conservação. This has the objective of improve the knowledge of flora of Rio Grande do Norte and to identify possible rare species and consequently increase the key areas of biodiversity in Brazil. The data indicated that: i) of 94 species registered in the study area, 40 were new records for the Rio Grande do Norte state; ii) These citations to unpublished state, Stylosanthes montevidensis Vogel (Fabaceae) and Aristida laevis (Nees) Kunth (Poaceae) are indicated for the first time to the Northeast of Brazil; iii) are registered in the area 24 species endemic to Brazil and 63 non-endemic; iv) Aspilia procumbens Baker (Asteraceae) registered in the area is considered a restricted species and micro endemic Rio Grande do Norte, ie rare species; v) Aspilia procumbens is also cited in the category of critically endangered species and Stilpnopappus cearensis Hubber (Asteraceae) a species vulnerable to extinction. This study shows a new area phytoecological in Rio Grande do Norte and indicates the area's potential to contribute with the sites of global significance for biodiversity conservation, either locally, regionally and nationally. This will certainly contribute to respond some targets set by the Global Strategy for Plant Conservation and the Convention on Biological Diversity such as the inventory of vegetal diversity in a region with little collection, which will provide data that contributes to questions and themes related to biodiversity.

Antinociceptive profile of 2,3,6-trisubstituted piperidine alkaloids: 3-O-acetyl-spectaline and semi-synthetic derivatives of (-)-spectaline

In early studies, we have reported the antinociceptive profile of (-)-spectaline, a piperidine alkaloid from Cassia spectabilis. The present study describes the synthesis, the antinociceptive and anti-inflammatory activities of a series of 2,3,6-trialkyl-piperidine alkaloids: the natural (-)-3-O-acetyl-spectaline (LASSBio-755) and ten semi-synthetic spectaline derivatives. Structure-activity relationship (SARs) studies were performed. The structures of all synthesized derivatives were confirmed by means of nuclear magnetic resonance. Compounds were evaluated for their analgesic (acetic acid-induced mouse abdominal constrictions, hot-plate test, formalin-induced pain test) and some of them for the anti-inflammatory activities (carrageenan-induced rat paw edema test). The pharmacological results showed that several of the new compounds given orally at a dose of 100 mu mol/kg significantly inhibited the acetic acid-induced abdominal constrictions, but they were less active than (-)-spectaline. LASSBio-755 and LASSBio-776 were the most actives with 37% and 31.7% of inhibition. In the formalin-induced pain only LASSBio-776 was able to inhibit by 34.4% the paw licking response of the inflammatory phase, (-)-spectaline and LASSBio-755 did show any activity. In the carrageenan-induced rat paw edema, only (-)-spectaline exhibited an anti-inflammatory profile, showing an ED(50) value of 56.6 mu mol/kg. Our results suggest different mechanisms of action for the analgesic activity observed for LASSBio-776 (3-O-Bocspectaline), LASSBio-755 (3-O-acetyl-spectaline) and (-)-spectaline (LASSBio-754). The antinociceptive profile of some of the semi-synthetic spectaline derivatives extends our research concerning the chemical and pharmacological optimization of isolated natural products in the search of new drug candidates from brazilian biodiversity.