Kêsia Xisto da Fonseca Ribeiro de Sena

Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones

Several 5-arylidene-4-thioxo-thiazolidine-2-ones (3a-n) were synthesized and evaluated as antimicrobial agents against representative strains, including multidrug-resistant strains of clinical isolates. Also, the antiproliferative activity was evaluated against two human carcinoma cell lines (NCI-H292 and HEp-2). The compounds containing the 5-arylidene subunit presented greater antimicrobial activities against Gram positive bacteria, including the multidrug-resistant clinical isolates, than the 4-thioxo-thiazolidine-2-one. Important SAR information was also gathered, such as the contribution of thiocarbonyl attached at 4-position on the thiazolidine heterocyclic for antimicrobial properties. None of the derivatives exhibited significant antiproliferative activity against the human carcinoma cell lines.

Antimicrobial activity of a mixture of two isomeric phenylpropanoid glycosides from Arrabidaea harleyi A.H. Gentry (Bignoniaceae)

Arrabidaea harleyi A.H. Gentry (Bignoniaceae) e uma planta ornamental, encontrada em algumas regioes da Mata Atlântica do Brasil. A partir das cascas do caule foi isolada a mistura dos isomeros verbascosideo e isoverbascosideo. A mistura mostrou-se ativa frente a Staphylococcus aureus, Micrococcus luteus, Bacillus subtilis, Bacillus mycoides, Enterococcus faecalis, Escherichia coli, Serratia marcensis e Candida albicans. Foi estabelecida a concentracao minima inibitoria (CMI) atraves do metodo de difusao em meio solido.

Antimicrobial, Antiproliferative and Proapoptotic Activities of Extract, Fractions and Isolated Compounds from the Stem of Erythroxylum caatingae Plowman

In the study, we have examined the antitumor and antimicrobial activities of the methanol extract, the fractions, a fraction of total alkaloids and two alkaloids isolated from the stem of Erythroxylum caatingae Plowman. All test fractions, except the hexane fractions, showed antimicrobial activity on gram-positive bacteria and fungi. The acetate: methanol (95:5), acetate, chloroform and hexane fractions show the highest cytotoxicity activity against the NCI-H292, HEp-2 and K562 cell lines using MTT. The absence of hemolysis in the erythrocytes of mice was observed in these fractions and 6β-Benzoyloxy-3α-(3,4,5- trimethoxybenzoyloxy) tropane (catuabine B). Staining with Annexin V-FITC and JC-1 was used to verify the mechanism of action of the compounds of E. caatingae that showed cytotoxicity less than 30 μg/mL in leukemic cells. After 48 h of incubation, we observed that the acetate: methanol (95:5), acetate, and chloroform fractions, as well as the catuabine B, increased in the number of cells in early apoptosis, from 53.0 to 74.8%. An analysis of the potential of the mitochondrial membrane by incorporation of JC-1 showed that most cells during incubation of the acetate: methanol (95:5) and acetate fractions (63.85 and 59.2%) were stained, suggesting the involvement of an intrinsic pathway of apoptosis.

Environmental factors affecting sporulation of Fuligo septica (Myxomycetes) on sugar cane bagasse

The influence of environmental factors on sporulation of Fuligo septica (L.) Wigg. and the abundance of this species on sugar cane bagasse (Saccharum officinarum L.), stored outdoors was studied.In Northeastern Brazil, between January/1997 and January/1998, a total of 29 specimens were collected through monthly collections of aethalia. The relationships between the abundance of aethalia and rainfall, temperature, relative humidity of the air and insolation were studied. Results indicated that on the substrate analyzed, F. septica was an abundant species. Sporulation occurred in all seasons of the year, with a well-defined peak at the end of winter and beginning of spring (August/September),which was strongly influenced by rainfall.

Synthesis and antimicrobial activities of 5-Arylidene-thiazolidine-2,4-dione derivatives.

Antibiotic resistance is considered one of the worlds major public health concerns. The main cause of bacterial resistance is the improper and repeated use of antibiotics. To alleviate this problem, new chemical substances against microorganisms are being synthesized and tested. Thiazolidines are compounds having many pharmacological activities including antimicrobial activities. For this purpose some thiazolidine derivatives substituted at position 5 in the thiazolidine nucleus were synthesized and tested against several microorganisms. Using a disc diffusion method, antimicrobial activity was verified against Gram-positive, Gram-negative, and alcohol acid resistant bacteria and yeast. The minimum inhibition concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined. All derivatives showed antimicrobial activity mainly against Gram-positive bacteria, with MIC values ranging from 2 to 16 µg/mL.

Biological Activity and Photostability of Biflorin Micellar Nanostructures

Capraria biflora L. is a shrub from the Scrophulariaceae family which produces in its roots a compound named biflorin, an o-naphthoquinone that shows activity against Gram-positive bacteria and fungi and also presents antitumor and antimetastatic activities. However, biflorin is hydrophobic and photosensitive. These properties make its application difficult. In this work we prepared biflorin micellar nanostructures looking for a more effective vehiculation and better preservation of the biological activity. Biflorin was obtained, purified and characterized by UV-Vis, infrared (IR) and 1H- and 13C-NMR. Micellar nanostructures of biflorin were then assembled with Tween 80®, Tween 20® and saline (0.9%) and characterized by UV-Vis spectroscopy and dynamic light scattering (DLS). The results showed that the micellar nanostructures were stable and presented an average size of 8.3 nm. Biflorin micellar nanostructures’ photodegradation was evaluated in comparison with biflorin in ethanol. Results showed that the biflorin in micellar nanostructures was better protected from light than biflorin dissolved in ethanol, and also indicated that biflorin in micelles were efficient against Gram-positive bacteria and yeast species. In conclusion, the results showed that the micellar nanostructures could ensure the maintenance of the biological activity of biflorin, conferring photoprotection. Moreover, biflorin vehiculation in aqueous media was improved, favoring its applicability in biological systems.

Influence of gamma radiation on the antimicrobial activity of crude extracts of Anacardium occidentale L., Anacardiaceae, rich in tannins

Anacardium occidentale L. Anacardiaceae, known as cashew, commonly found in northeastern of Brazil, has high levels of secondary metabolites, particularly tannins, used as raw material for herbal medicines. An efficient alternative to decontaminate plant products is the total sterilization or reduction of the initial microbial count, the process of gamma irradiation with 60Co. The objective of this study was to analyze the antimicrobial activity of crude extracts of bark and leaves of A. occidentale, based on the quantification of total phenols and tannins, before and after exposure to gamma radiation from 60Co. The extracts were obtained in the laboratory by cold maceration in ethanol, filtered and dryness. They were divided into non-irradiated control group (0 kGy) and irradiated: groups exposed to gamma radiation at doses of 5, 7.5 and 10 kGy. The total phenols was obtained by the Folin-Ciocalteau method and tannins, by the precipitation of casein. The antimicrobial potential activities of these extracts were also evaluated. The results showed that gamma radiation doses employed in this study did not influence statistically the percentage of total phenols and tannins in the bark extracts, at levels ranging from 5.73±0.14 and 5.20±0.14, respectively. The levels of metabolites in the leaves were statistically (p<0.05) influenced by radiation, observed average total phenols between 3.13±0.04 (0 kGy) and 3.50±0.08 (10 kGy), and tannin between 2.47±0.06 (0 kGy) and 2.93±0.04 (10 kGy). The extracts of bark and leaves were active against Staphylococcus aureus, Micrococcus luteus, Bacillus subtilis, Enterococcus faecalis, Mycobacterium smegmatis, Candida albicans. Gamma radiation caused an increase in antimicrobial activity of extracts against Staphylococcus aureus (Gram positive), with average inhibition zones for shells: 14.33±058 (0 kGy) and 22.33±0.58 (10 kGy), and leaves: 11.33±0.58 (0 kGy) and 19.00±1.00 (10 kGy). Exposure to radiation caused changes in physical and chemical constituents of phenolic extracts of leaves of cashew, increasing levels of tannins.

Evaluation of cytotoxic, immunomodulatory and antibacterial activities of aqueous extract from leaves of Conocarpus erectus Linnaeus (Combretaceae)

This work evaluated the antibacterial activity, cytotoxicity and immunomodulatory effect on human peripheral blood mononuclear cells (PBMCs) promoted by aqueous extract from Conocarpus erectus leaves (AELCe).

Agarose-silver particles films: Effect of calcium ascorbate in nanoparticles synthesis and film properties

New nanoparticles containing biomaterials are emerging as versatile active platforms in a great number of applications, for example, as skin substitutes and therapeutic media. The present study describes the preparation of silver nanoparticles (AgNPs) embedded in agarose films and the impact of calcium ascorbate in the formation of ANPs as well as in the final properties of the films. Colloidal AgNPs were synthetized by two chemical reduction routes: (i) applying calcium ascorbate and NaBH4 and (ii) applying only NaBH4. AgNPs synthetized using NaBH4 showed sizes ranging from 5 to 18 nm while AgNPs were calcium ascorbate was used showed micrometer from 164 to 955 nm size. Films were prepared in three formulations: agarose control film (A1); agarose + AgNPs without calcium ascorbate (A2) and agarose + AgNPs with calcium ascorbate (A3). The characterization of films by SEM and EDS showed agarose agglomerates in A2 and unreacted calcium ascorbate crystals on surface of A3. Thus, the presence of calcium ascorbate influenced the properties of A3 film. In addition, the antimicrobial analysis showed a silver particles release dependence on the film composition and only the A3 presented activity against Staphylococcus aureus. The results found in this study open an important way for development of new biomaterials, economically competitive, and with medical application.