In vitro evaluation of the enzymatic activity profile of non-albicans Candida species isolated from patients with oral candidiasis with or without diabetes

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Nanostructured Lipid Systems as a Strategy to Improve the in Vitro Cytotoxicity of Ruthenium(II) Compounds

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

Uso de extratos vegetais no controle in vitro do Colletotrichum gloeosporioides penz. Coletado em frutos de mamoeiro (Carica papaya L.)

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

Nanostructured Lipid Carriers as a Strategy to Improve the In Vitro Schistosomiasis Activity of Praziquantel

Praziquantel (PZQ) is a pyrazinoisoquinoline anthelmintic that was discovered in 1972 by Bayer Germany. Currently, due to its efficacy, PZQ is the drug of choice against all species of Schistosoma. Although widely used, PZQ exhibits low and erratic bioavailability because of its poor water solubility. Nanostructured lipid carriers (NLC), second-generation solid lipid nanoparticles, were developed in the 1990s to improve the bioavailability of poorly water soluble drugs. The aim of this study was to investigate nanostructured lipid carriers as a strategy to improve the efficacy. of PZQ in S. mansoni treatment. We prepared NLC2 and NLC4 by adding seventy percent glycerol monostearate (GMS) as the solid lipid, 30% oleic acid (OA) as the liquid lipid and two surfactant systems containing either soybean phosphatidylcholine/poloxamer (PC/P-407) or phosphatidylcholine/Tween 60 (PC/T60), respectively. The carriers were characterized by nuclear magnetic resonance, differential scanning calorimetry, thermogravimetric analysis and Fourier transform-infrared spectroscopy. The safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. The results showed that the encapsulation of PZQ in NLC2 or NLC4 improved the safety profile of the drug. Treatment efficacy was evaluated on the S. mansoni BH strain. PZQ-NLC2 and PZQ-NLC4 demonstrated an improved efficacy in comparison with free PZQ. The results showed that the intestinal transport of free PZQ and PZQ-NLC2 was similar. However, we observed that the concentration of PZQ absorbed was smaller when PZQ was loaded in NLC4. The difference between the amounts of absorbed PZQ could indicate that the presence of T60 in the nanoparticles (NLC4) increased the rigid lipid matrix, prolonging release of the drug. Both systems showed considerable in vitro activity against S. mansoni, suggesting that these systems may be a promising platform for the administration of PZQ for treating schistosomiasis.

Antitumor Activity of Kielmeyera Coriacea Leaf Constituents in Experimental Melanoma, Tested in Vitro and in Vivo in Syngeneic Mice

Purpose: The antitumor activity of Kielmeyera coriacea (Clusiaceae), a medicinal plant used in the treatment of parasitic, as well as fungal and bacterial infections by the Brazilian Cerrado population, was investigated. Methods: A chloroform extract (CE) of K. coriacea was tested in the murine melanoma cell line (B16F10-Nex2) and a panel of human tumor cell lines. Tumor cell migration was determined by the wound-healing assay and the in vivo antitumor activity of CE was investigated in a melanoma cell metastatic model. 1H NMR and GC/MS were used to determine CE chemical composition. Results: We found that CE exhibited strong cytotoxic activity against murine melanoma cells and a panel of human tumor cell lines in vitro. CE also inhibited growth of B16F10- Nex2 cells at sub lethal concentrations, inducing cell cycle arrest at S phase, and inhibition of tumor cell migration. Most importantly, administration of CE significantly reduced the number of melanoma metastatic nodules in vivo. Chemical analysis of CE indicated the presence of the long chain fatty compounds, 1-eicosanol, 1-docosanol, and 2-nonadecanone as main constituents. Conclusion: These results indicate that K. coriacea is a promising medicinal plant in cancer therapy exhibiting antitumor activity both in vitro and in vivo against different tumor cell lines.

Análise in vitro da atividade antimicrobiana, citotoxicidade e genotoxicidade de um princípio ativo (Timol) e de um enxaguatório bucal (LISTERINE® ZERO™)

Pós-graduação em Biopatologia Bucal - ICT

In vitro antibacterial and chemical properties of essential oils including native plants from Brazil against pathogenic and resistant bacteria

The antimicrobials products from plants have increased in importance due to the therapeutic potential in the treatment of infectious diseases. Therefore, we aimed to examine the chemical characterisation (GC-MS) of essential oils (EO) from seven plants and measure antibacterial activities against bacterial strains isolated from clinical human specimens (methicillin-resistant Staphylococcus aureus (MRSA) and sensitive (MSSA), Escherichia coli, Pseudomonas aeruginosa, Salmonella Typhimurium) and foods (Salmonella Enteritidis). Assays were performed using the minimal inhibitory concentration (MIC and MIC90%) (mg/mL) by agar dilution and time kill curve methods (log CFU/mL) to aiming synergism between EO. EO chemical analysis showed a predominance of terpenes and its derivatives. The highest antibacterial activities were with Cinnamomun zeylanicum (0.25 mg/mL on almost bacteria tested) and Caryophyllus aronzaticus EO (2.40 mg/mL on Salmonella Enteritidis), and the lowest activity was with Eugenia uniflora (from 50.80 mg/mL against MSSA to 92.40 mg/mL against both Salmonella sources and P aeruginosa) EO. The time kill curve assays revealed the occurrence of bactericide synergism in combinations of C. aromaticus and C. zeylanicum with Rosmarinus. officinalis. Thus, the antibacterial activities of the EO were large and this can also be explained by complex chemical composition of the oils tested in this study and the synergistic effect of these EO, yet requires further investigation because these interactions between the various chemical compounds can increase or reduce (antagonism effect) the inhibitory effect of essential oils against bacterial strains.

Structural characterization and in vitro antioxidant activity of kojic dipalmitate loaded W/O/W multiple emulsions intended for skin disorders

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

New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Avaliação do potencial biológico de extratos hidroetanólicos de Astronium sp incorporados ou não em sistemas nanoestruturados: in vitro e in vivo: in vitro e in vivo

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

Análise do efeito in vitro de acridonas na replicação do Vírus da Hepatite C

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)