Mutagenic Activity of Glycoallkaloids from Solanum palinacanthum Dunal (Solanaceae) in the Brazilian cerrado

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Antioxidant Activity and Total Phenols from the Methanolic Extract of Miconia albicans (Sw.) Triana Leaves

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

Dietary intervention with narrow-leaved cattail rhizome flour (Typha angustifolia L.) prevents intestinal inflammation in the trinitrobenzenesulphonic acid model of rat colitis

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

Analysis of Bothrops jararacussu venomous gland transcriptome focusing on structural and functional aspects: I - gene expression profile of highly expressed phospholipases A(2)

Snake venom glands are a rich source of bioactive molecules such as peptides, proteins and enzymes that show important pharmacological activity leading to in local and systemic effects as pain, edema, bleeding and muscle necrosis. Most studies on pharmacologically active peptides and proteins from snake venoms have been concerned with isolation and structure elucidation through methods of classical biochemistry. As an attempt to examine the transcripts expressed in the venom gland of Bothrops jararacussu and to unveil the toxicological and pharmacological potential of its products at the molecular level, we generated 549 expressed sequence tags (ESTs) from a directional cDNA library. Sequences obtained from single-pass sequencing of randomly selected cDNA clones could be identified by similarities searches on existing databases, resulting in 197 sequences with significant similarity to phospholipase A(2) (PLA(2)), of which 83.2% were Lys49-PLA(2) homologs (BOJU-1), 0.1% were basic Asp49-PLA(2)s (BOJU-II) and 0.6% were acidic Asp49-PLA(2)s (BOJU-III). Adjoining this very abundant class of proteins we found 88 transcripts codifying for putative sequences of metalloproteases, which after clustering and assembling resulted in three full-length sequences: BOJUMET-I, BOJUMET-II and BOJUMET-III; as well as 25 transcripts related to C-type lectin like protein including a full-length cDNA of a putative galactose binding C-type lectin and a cluster of eight serine-proteases transcripts including a full-length cDNA of a putative serine protease. Among the full-length sequenced clones we identified a nerve growth factor (Bj-NGF) with 92% identity with a human NGF (NGHUBM) and an acidic phospholipase A2 (BthA-I-PLA(2)) displaying 85-93% identity with other snake venom toxins. Genetic distance among PLA(2)s from Bothrops species were evaluated by phylogenetic analysis. Furthermore, analysis of full-length putative Lys49-PLA(2) through molecular modeling showed conserved structural domains, allowing the characterization of those proteins as group II PLA(2)s. The constructed cDNA library provides molecular clones harboring sequences that can be used to probe directly the genetic material from gland venom of other snake species. Expression of complete cDNAs or their modified derivatives will be useful for elucidation of the structure-function relationships of these toxins and peptides of biotechnological interest. (C) 2004 Elsevier SAS. All rights reserved.

Biological properties of medicinal plants: a review of their antimicrobial activity

Plants have been used for thousands of years to flavor and conserve food, to treat health disorders and to prevent diseases including epidemics. The knowledge of their healing properties has been transmitted over the centuries within and among human communities. Active compounds produced during secondary vegetal metabolism are usually responsible for the biological properties of some plant species used throughout the globe for various purposes, including treatment of infectious diseases. Currently, data on the antimicrobial activity of numerous plants, so far considered empirical, have been scientifically confirmed, concomitantly with the increasing number of reports on pathogenic microorganisms resistant to antimicrobials. Products derived from plants may potentially control microbial growth in diverse situations and in the specific case of disease treatment, numerous studies have aimed to describe the chemical composition of these plant antimicrobials and the mechanisms involved in microbial growth inhibition, either separately or associated with conventional antimicrobials. Thus, in the present work, medicinal plants with emphasis on their antimicrobial properties are reviewed.

Biosurfactants in food industry

The increasing environmental concern about chemical surfactants triggers attention to microbial-derived surface-active compounds essentially due to their low toxicity and biodegradable nature. At present, biosurfactants are predominantly used in remediation of pollutants; however, they show potential applications in many sectors of food industry. Associated with emulsion forming and stabilization, antiadhesive and antimicrobial activities are some properties of biosurfactants, which could be explored in food processing and formulation. Potential applications of microbial surfactants in food area and the use of agroindustrial wastes as alternative substrates for their production are discussed.

Rhamnolipid surfactants: An update on the general aspects of these remarkable biomolecules

Pseudomonas strains are able to biosynthesize rhamnose-containing surfactants also known as rhamnolipids. These surface-active compounds are reviewed with respect to chemical structure, properties, biosynthesis, and physiological role, focusing on their production and the use of low-cost substrates such as wastes from food industries as alternative carbon sources. The use of inexpensive raw materials such as agroindustrial wastes is an attractive strategy to reduce the production costs associated with biosurfactant production and, at same time, contribute to the reduction of environmental impact generated by the discard of residues, and the treatment costs. Carbohydrate-rich substrates generated low rhamnolipid levels, whereas oils and lipid-rich wastes have shown excellent potential as alternative carbon sources.

The use of biodiversity as source of new chemical entities against defined molecular targets for treatment of malaria, tuberculosis, and T-cell mediated diseases: a review

The modern approach to the development of new chemical entities against complex diseases, especially the neglected endemic diseases such as tuberculosis and malaria, is based on the use of defined molecular targets. Among the advantages, this approach allows (i) the search and identification of lead compounds with defined molecular mechanisms against a defined target (e.g. enzymes from defined pathways), (ii) the analysis of a great number of compounds with a favorable cost/benefit ratio, (iii) the development even in the initial stages of compounds with selective toxicity (the fundamental principle of chemotherapy), (iv) the evaluation of plant extracts as well as of pure substances. The current use of such technology, unfortunately, is concentrated in developed countries, especially in the big pharma. This fact contributes in a significant way to hamper the development of innovative new compounds to treat neglected diseases. The large biodiversity within the territory of Brazil puts the country in a strategic position to develop the rational and sustained exploration of new metabolites of therapeutic value. The extension of the country covers a wide range of climates, soil types, and altitudes, providing a unique set of selective pressures for the adaptation of plant life in these scenarios. Chemical diversity is also driven by these forces, in an attempt to best fit the plant communities to the particular abiotic stresses, fauna, and microbes that co-exist with them. Certain areas of vegetation (Amazonian Forest, Atlantic Forest, Araucaria Forest, Cerrado-Brazilian Savanna, and Caatinga) are rich in species and types of environments to be used to search for natural compounds active against tuberculosis, malaria, and chronic-degenerative diseases. The present review describes some strategies to search for natural compounds, whose choice can be based on ethnobotanical and chemotaxonomical studies, and screen for their ability to bind to immobilized drug targets and to inhibit their activities. Molecular cloning, gene knockout, protein expression and purification, N-terminal sequencing, and mass spectrometry are the methods of choice to provide homogeneous drug targets for immobilization by optimized chemical reactions. Plant extract preparations, fractionation of promising plant extracts, propagation protocols and definition of in planta studies to maximize product yield of plant species producing active compounds have to be performed to provide a continuing supply of bioactive materials. Chemical characterization of natural compounds, determination of mode of action by kinetics and other spectroscopic methods (MS, X-ray, NMR), as well as in vitro and in vivo biological assays, chemical derivatization, and structure-activity relationships have to be carried out to provide a thorough knowledge on which to base the search for natural compounds or their derivatives with biological activity.

Characterization of two novel polyfunctional mastoparan peptides from the venom of the social wasp Polybia paulista

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

In vitro Trypanocidal Activity of Phenolic Derivatives from Peperomia obtusifolia

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

Bioactive Metabolites Produced by Penicillium sp.1 and sp.2, Two Endophytes Associated with Alibertia macrophylla (Rubiaceae)

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

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)

Purification of an antibacterial compound from Lantana lilacina

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids

Five new piperidine alkaloids were designed from natural (-)-3-O-acetyl-spectaline and (-)-spectaline that were obtained from the flowers of Senna spectabilis (sin. Cassia spectabilis, Leguminosae). Two semi-synthetic analogues (7 and 9) inhibited rat brain acetylcholinesterase, showing IC50 of 7.32 and 15.1 mu M, and were 21 and 9.5 times less potent against rat brain butyrylcholinesterase, respectively. Compound 9 (1 mg/kg, ip) was fully efficacious in reverting scopolamine-induced amnesia in mice. The two active compounds (7 and 9) did not show overt toxic effects at the doses tested in vivo. (c) 2005 Elsevier Ltd. All rights reserved.

Production of Pseudomonas aeruginosa LBI rhamnolipids following growth on Brazilian native oils

Oils from Buriti (Mauritia flexuosa), Cupuacu (Theobroma grandiflora), Passion Fruit (Passiflora alata), Andiroba (Carapa gitianensis), Brazilian Nut (Bertholletia excelsa) and Babassu (Orbignya spp.) were evaluated as carbon sources for rhamnolipid production by Pseudomonas aeruginosa LBI. The highest rhamnolipid concentrations were obtained from Brazilian Nut (9.9 l(-1)) and Passion Fruit (9.2 g l(-1)) oils. Surface tension varied from 29.8 to 31.5 mN m(-1), critical micelle concentration from 55 to 163 mg l(-1) and the emulsifying activity was higher against toluene (93-100%) than against kerosene (70-92%). Preliminary characterization of the surfactant mixtures by mass spectrometry revealed the presence of two major components showing m/z of 649 and 503, which corresponded to the dirhamnolipid (Rha(2)C(10)C(10)) and the monorhamnolipid (RhaC(10)C(10)), respectively. The monorhamnolipid detected as the ion of m/z 503 is predominant in all samples analyzed. (c) 2005 Elsevier Ltd. All rights reserved.