O papel governamental como ator essencial para a P&D de medicamentos: um estudo de casos

The importance of natural products as a source of new high value-added drugs has, no doubt, transformed Brazilian megadiversity into one of the country's most valuable and strategic assets. Thus the rational exploration of the Brazilian flora on an economic basis should be considered as part of a national development strategy. In this respect, governmental mechanisms to stimulate regulation on the access, bioprospection and industrial use of natural products represent a crucial issue. The aim of this paper is to show how the incentives and institutional arrangements that led to one of the greatest breakthroughs in the pharmaceutical industry, the development and commercialization of the anti-cancer agent Taxol, could be applied to the Brazilian case.

Reações de organocatálise com aminas quirais: aspectos mecanísticos e aplicações em síntese orgânica

The philosophy of organocatalysis is based on the utilization of organic compounds to catalyze organic transformations without the intervention of metals. This area has attracted much attention of the synthetic chemistry community on the last years, which can be confirmed by the explosion of published papers dealing with this subject. Phosphorus compounds, urea and thiourea derivatives, alkaloids, guanidine derivatives, for example, have already been used as organocatalysts. In this review we have focused on the use of chiral amines as organocatalyst. We have also chosen some outstanding examples to demonstrate the potentiality of this strategy in the synthesis of natural products and biologically active compounds.

Biodiversidade: fonte potencial para a descoberta de fármacos

In economic terms, biodiversity transcends the boundaries usually given to conventional industries because it is a valuable source of biological and chemical data of great use to drug discovery. Certainly, the use of natural products has been the single most successful strategy in the discovery of novel medicines, and most of the medical breakthroughs are based on natural products. Half of the top 20 best-selling drugs are natural products, and their total sales amounted to US$ 16 billions shows the importance of natural products, which is evidenced by the new chemical entities (NCE) approved by regulatory authorities around the world in the past decade. Recently, the approval of the alkaloid galanthamine as a medicine to treat Alzheimer's disease shows that natural compounds from plants will continue to reach the market. The huge biological diversity of the Brazilian biomes, by its ability to generate new knowledge and technological innovation can be a fantastic alternative as raw material for drug discovery.

Organismos marinhos como fonte de novos fármacos: histórico & perspectivas

Though sharing only a short part on the natural products timeline, the studies on marine products has already handed in four new drugs to the clinical arsenal and brought up a long and promising list of unique molecules to pre-clinical and clinical trials. Thus, as the available analytical resources improve and the interest of large pharmaceutical companies arises, medical use of marine products has definitely become a reality.

Fotoprotetores derivados de produtos naturais: perspectivas de mercado e interações entre o setor produtivo e centros de pesquisa

Ultraviolet radiation is the major exogenous mediators of skin damage. To prevent such damage, sunscreen products are used. New research aims at both the elucidation of new sunscreen compounds, as well as new assets for supporting and synergistic action. In this article it is presented a systematic data of innovation for sunscreen and a discussion on prospects for partnership between universities and enterprises, where it is believed that the innovations in cosmetics, driven by the constant demand of the market in new products, may be a stimulus for the interactions between university and company in Brazil.

Peptídeos cíclicos de biomassa vegetal: características, diversidade, biossíntese e atividades biológicas

Natural peptides are outstanding as the most promising macromolecules in the search for new drugs, especially those of cyclic nature. The higher plants revealed a very peculiar composition of their cyclic peptides, which distinguish themselves by a "head-to-tail" cyclization. It is possible to define two groups of cyclic peptides from plant biomass. Those called in this review as Eucyclopeptides formed by 2-12 amino acid, and Cyclotides considered as circular polypeptides, composed of 29-37 amino acid that retain three disulfides bridges in an arrangement known as cyclic cystine knot. Searching for plant peptides should form into a subject for scientific research in the forefront of great importance for bioprospecting natural products macromolecular.

Metabólitos secundários de origem vegetal: uma fonte potencial de fármacos antitrombóticos

Cardiovascular diseases are responsible for the largest number of deaths among humans worldwide, including heart attacks, strokes, and thrombosis. The treatment of thrombosis is generally through the administration of anticoagulant and/or antiplatelet drugs, which have some clinical limitations. Plants synthesize a wide variety of bioactive metabolites in response to different stimuli. This review focuses on a number of molecules of vegetal origin belonging to different chemical classes, with significant anticoagulant and antiplatelet effects. Their promising antithrombotic profile confirms the potential of natural products as a source of lead molecules for drug development in the prevention and treatment of thrombosis.

Antibióticos: importância terapêutica e perspectivas para a descoberta e desenvolvimento de novos agentes

There is a continuous need for antibiotics, mainly with new mechanisms of action, since infectious diseases represent the second major cause of death in the world and bacteria resistance levels are high. This review describes the contribution of microbial natural products for the development of the major antibiotic classes, the mechanisms of action of current antibiotics, some modern approaches involving genetic tools for the discovery and development of new antibiotics from microbial products and antibiotics in clinical trials.

Fitoprodutos e desenvolvimento econômico

Natural products have been, historically, very important for Brazil. Coffee, sugar and soy were some examples that prove this economical significance. A project that involves phytoproducts should be guide by three main axis: agriculture management for the plants; pharmaceutical; support the national industry and academy. In Brazil, pharmaceutical products contribute negatively to the commerce balance showing an enormous technological dependence in this economical sector. The consolidation of the phytoproduct's chain in Brazil could contribute for the development of the pharmaceutical sector in order to help all domains in natural products area.

HIV: mecanismo de replicação, alvos farmacológicos e inibição por produtos derivados de plantas

The AIDS epidemy has spread out and led to the diversification on the research for new antiviral drugs. Natural products, especially those derived from plants, are well-recognized as excellent sources of new drugs. Several of them have inhibitory activity against HIV replication, and some have been already clinically tested, with favorable results. This review presents the biochemical basis of the viral cycle and the research up to date on the identification, determination of the mechanism of biological action together with the therapeutical potential of plants-derived natural products, in the inhibition of HIV.

Curiosidades sobre a reação aldólica utilizada como etapa chave na síntese Brasileira dos ácidos pterídicos A e B

This work describes an overview of our synthesis of pteridic acids A and B and discloses some interesting results related to the lithium enolate-mediated aldol reaction used as key step to set up the C5-C15 fragment of these natural products. This first example, as far we know, of an aldol reaction between a chiral enolate of a (Z) enone and a chiral aldehyde has driven us to a series of experiments showing the remarkable relation between enolization selectivity and reaction conditions.

Glicerol: um breve histórico e aplicação em sínteses estereosseletivas

Presently glycerol is considered a co-product of biodiesel industry. As the biodiesel production is exponentially increasing, glycerol generated from the transesterification of vegetable oils and fats is also being produced on a large scale, and turned out to be essential seeking for novel alternatives to the consumption of the extra volume, in crude and/or as derivatives high added value. This review mainly deals with chemical and enzymatic transformations of glycerol to obtain chiral building blocks for synthesis of pharmaceuticals and natural products.

Irradiação de micro-ondas aplicada à síntese orgânica: uma história de sucesso no Brasil

This review article shows the publications in the field of microwave irradiation published by Brazilian researchers over the past 10 years. In South America, Brazil leads the publication of articles with the use of microwave irradiation possessing a large advantage in number of articles published over the others countries. The works were divided into four major areas: Catalysis, Reactions without Solvent, Heterocycles Chemistry, Natural Products and Other, and some could be classified in more than one category.

Utilização de detecção por espalhamento de luz evaporativo para a análise de produtos naturais

The interest in the use of evaporative light scattering detector (ELSD) for the analysis of different classes of natural products has grown over the years. This is because this detector has become an excellent alternative compared to other types of detectors, such as the refractive index detector and the ultraviolet (UV) detector. This review describes the basic principles of ELSD functioning and discusses the advantages and disadvantages in using an ELSD for the analysis of organic compounds. Additionaly, an overview, covering the last 23 years, of ELSD applications in natural products analysis (saponins, terpenes, carbohydrates, glycosides, alkaloids, steroids, flavonoids, peptides, polyketides, coumarins and iridoids) is presented and discussed.

Químico-Biologia Quantitativa: um novo paradigma?

Disconcerting environmental problems, for which no solutions exist yet, appear daily. Despite this, many believe countries such as Brazil, biologically rich and not yet belonging to the First World, should be restricted to collecting information. Counteracting this opinion, that precludes rationally influencing the environment, we have sought to better understand the language of nature based on Quantitative Chemo-Biology. This multidisciplinary endeavor tackles a range of issues from basic questions such as the origin of life, to more urgent problems such as mapping the chemical and biological diversity of specific regions. We believe this is the right way to prepare younger generations to deal with the unpredictable future.