Glycosomal Targets for Anti-Trypanosomatid Drug Discovery

Glycosomes are peroxisome-related organelles found in all kinetoplastid protists, including the human pathogenic species of the family Trypanosomatidae: Trypanosoma brucei, Trypanosoma cruzi and Leishmania spp. Glycosomes are unique in containing the majority of the glycolytic/gluconeogenic enzymes, but they also possess enzymes of several other important catabolic and anabolic pathways. The different metabolic processes are connected by shared co-factors and some metabolic intermediates, and their relative importance differs between the parasites or their distinct life-cycle stages, dependent on the environmental conditions encountered. By genetic or chemical means, a variety of glycosomal enzymes participating in different processes have been validated as drug targets. For several of these enzymes, as well as others that are likely crucial for proliferation, viability or virulence of the parasites, inhibitors have been obtained by different approaches such as compound libraries screening or design and synthesis. The efficacy and selectivity of some initially obtained inhibitors of parasite enzymes were further optimized by structure-activity relationship analysis, using available protein crystal structures. Several of the inhibitors cause growth inhibition of the clinically relevant stages of one or more parasitic trypanosomatid species and in some cases exert therapeutic effects in infected animals. The integrity of glycosomes and proper compartmentalization of at least several matrix enzymes is also crucial for the viability of the parasites. Therefore, proteins involved in the assembly of the organelles and transmembrane passage of substrates and products of glycosomal metabolism offer also promise as drug targets. Natural products with trypanocidal activity by affecting glycosomal integrity have been reported.

Associação de variedades de goiaba, bioinseticidas e o parasitóide Diachasmimorpha longicaudata no controle de Anastrepha fraterculus

Pós-graduação em Agronomia (Produção Vegetal) - FCAV

Antimalarial activity of piperidine alkaloids from Senna spectabilis and semisynthetic derivatives

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

New drugs with antiprotozoal activity from marine algae: a review

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

Estudo de espécies de Chrysobalanaceae com ação citotóxica: análise metabolômica visando ao entendimento de associações sinérgicas e da complexidade micromolecular

Pós-graduação em Química - IQ

Investigação química e biológica dos metabólitos secundários derivados de macroalgas marinhas e microrganismos associados

Pós-graduação em Química - IQ

Dimeric Flavonoids from Arrabidaea brachypoda and Assessment of Their Anti-Trypanosoma cruzi Activity

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

In Vitro Antibacterial Activity of Prenylated Guanidine Alkaloids from Pterogyne nitens and Synthetic Analogues

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

HPLC-DAD method for metabolic fingerprinting of the phenotyping of sugarcane genotypes

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Antimicrobial activity of essential oils

Natural products have been studied aiming to understand their biological properties. Thus, this study aimed to investigate the antimicrobial activity of twenty-seven essential oils (EOs) used in aromatherapy procedures, a natural therapy with great emphasis currently used against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa strains. The agar dilution method was carried out and minimal inhibitory concentration against 50% and 90% of strains (MIC50% and MIC90% values) were reported. The S.aureus strains were highly susceptible with MIC90% from 0.21mg/mL to black pepper (Piper nigrum) and tea tree (Melaleuca alternifolia) to 26.52mg/mL with copaiba (Copaifera officinalis) EO. Cinnamon (Cinnamomum cassia) and clove (Syzygium aromaticum) EOs were effective against E.coli (2.0mg/mL) while the S.aromaticum EO was against P.aeruginosa (8.29mg/mL). Thus, the higher susceptibility of Gram-positive bacteria when compared with Gram-negative strains was found, and a large variability in the potential antibacterial has also been observed.

Tumor venéreo transmissível canino com enfoque nos diversos tratamentos

The canine Transmissible Venereal Tumor (TVT) is a neoplasm of round cells that primarily affects the external genitalia of both male and female dogs with high casuistry. Its transmission occurs by the tumor cells’ implementation in the mucous membranes during the coitus or in other body parts through licking, scratching or direct contact with the tumor. The clinical manifestations vary according to the location. Despite being a malignant neoplasm, TVT’s metastatic potential is low. The diagnosis is based on macroscopic characteristics, clinical signs, cytology and/or histopathology exam, among which cytology is considered the best method. There are several treatment protocols for the TVT, among which, surgical excision, radiotherapy, immunotherapy and chemotherapy. Chemotherapy with vincristine sulfate is the elected treatment. However, more and more new alternatives have been developed, as the usage of natural products, homeopathy and ivermectina. They can be used as a unique treatment to neoplasm or combined to the chemotherapy in order to decrease the dose and the application number of the chemotherapic and its side effects

Estudo do potencial de associações de ZnO com os produtos naturais ácido cafeico e ferúlico como filtros solares híbridos: [recurso eletrônico]

In this work were studied associations of ZnO with the natural products caffeic and feluric acids. Two preparation methods were used, that is, the sol-gel and a reflux procedure. In the sol-gel method, ZnO is produced by the basics hydrolysis of precursors in the presence of the organic filters (caffeic and feluric acids), which results in 30 nm (or less) ZnO particles with the organic filters (in dissociated form) bonded to the surface of ZnO. In the reflux method, a dispersion of ZnO in a water/ethanol mixture was kept under reflux (50oC/4h) in the presence of the organic acids. The ZnO particles used in the reflux method have a higher diameter than sol-gel ZnO particles, but the prepared associated product ZnO/Organic acids were similar. Despite of the difference in relation to crystallinity between the products, the preparation methods resulted in analogous associations with respect to the interaction of the organic filters with the ZnO surface. The caffeic/ZnO associations presented low photostability, which lead to the degradation of the organic filter. The other associations (feluric acid/ZnO) presented satisfactory results. The FT-IR spectroscopy confirmed the formation of the association, and the nature of the bond formed compared with the Zn-O bond in Zn2+/Felutic acid complexes. The isolated organic and inorganic filters, along with the associations were analyzed by diffuse reflectance spectroscopy and Uv-vis spectroscopy. The absorption edges and the critical wavelengths were analyzed and the effects of Zn-O bonds in feluric acid/ZnO associations described as a function of the relative position of the π/π* system of the organic filter. Finally the performance of the hybrid filters were investigated in terms of the absorption of UVA and UVB radiations, with the UVA/UVB ratio, an efficiency parameter largely used in the description of solar filters, sunscreen and suncare products

Espectroscopia de infravermelho e suas aplicações

Infrared spectroscopy (IR spectroscopy) explores the infrared region of the electromagnetic spectrum. Like any other spectroscopic technique, it can be used to identify a compound or the composition of investigate a sample. Spectroscopy (IR) is a very important technique in qualitative chemical analysis, widely used in the chemistry of natural products, organic synthesis and transformations. In this work we study of the theoretical foundations of infrared spectroscopy, the different vibration modes, experimental techniques, and the identification and characterization of solids. Were studied as applications: their use in thermograph and remote sensing satellites

Avaliação dos efeitos do cogumelo do sol (Agaricus blazei) sobre o colesterol plasmático em coelhos com hipercolesterolemia induzida

Prophylactic or therapeutic treatments administered with medicinal plants and natural products are used in popular medicine of diverse people since prehistoric times to the present days. Species with medicinal properties are increasingly studied in an attempt to understand their possible effects on organisms and their functioning. This study aimed to analyze the effect of the mushroom Agaricus blazei (aqueous extract) in rabbits subjected to experimental hypercholesterolemia. The animals were divided into two groups (control and treated with the mushroom) whose experimental protocol was divided into three phases: Phase 1, the animals were fed a normal diet to evaluate the physiological level of cholesterol; phase 2, the animals were fed a supplemented diet to induce hypercholesterolemia and in phase 3, the animals of control group continued to take high-cholesterol diet and the animals of treated group high-cholesterol diet including treatment with the mushroom. Weekly, after fasting of 14 hours, blood samples were collected from the animals and its plasma was stored for later measurement of plasmatic cholesterol. In the first phase, the cholesterol level was, on average, 31,30  7,34 mgdL-1. In the second phase, there was a significant increase (p<0,05) in cholesterol level of both groups. During the last phase of the experiment, the mushrooms didn’t cause reduction in plasmatic cholesterol of treated rabbits, however, prevent disease progression, maintaining the cholesterol level established at the beginning of treatment, whereas, in the control group, total serum cholesterol increased significantly at this stage