Marina Scopel

Dipeptide cis-cyclo(Leucyl-Tyrosyl) produced by sponge associated Penicillium sp. F37 inhibits biofilm formation of the pathogenic Staphylococcus epidermidis.

Infections associated to microbial biofilms are involved in 80% of human infections and became a challenge concerning public health. Infections related to Staphylococcus epidermidis biofilms are presently commonly associated to medical devices, increasing treatment costs for this type of infection. Alternatives to eliminate this kind of disease have been employed in screening programs using diverse marine-derived fungi source of bioactive compounds capable to combat biofilm formation. In this work was isolated the dipeptide cis-cyclo(Leucyl-Tyrosyl) from a sponge associated Penicillium sp. possessing a remarkable inhibition up to 85% of biofilm formation without interfering with bacterial growth, confirmed by scanning electron microscopy. This is the first demonstration that cis-cyclo(Leucyl-Tyrosyl) is able to specifically inhibit biofilm formation adding another aspect to the broad spectrum of bioactivities of cyclic dipeptides.

Anti-Trichomonas vaginalis activity of marine-associated fungi from the South Brazilian Coast.

Trichomonas vaginalis is the causative agent of trichomonosis, the most common non-viral sexually transmitted disease. Infection with this protozoan may have serious consequences, especially for women. Currently, 5-nitroimidazole drugs are the treatment of choice for trichomonosis, but the emergence of resistance has limited the effectiveness of this therapy. In this context, this study aimed to evaluate the anti-T. vaginalis activity of marine-associated fungi found in the South Brazilian Coast. A total of 42 marine-associated fungal species (126 filtrate samples) isolated from 39 different marine organisms, mainly sponges, were selected to be screened against T. vaginalis. Of these, two filtrate samples from Hypocrea lixii F02 and Penicillium citrinum F40 showed significant growth-inhibitory activity (up to 100%) against ATCC 30236 and fresh clinical isolates, including a metronidazole-resistant isolate. Minimum inhibitory concentration (MIC) values of H. lixii F02 and P. citrinum F40 samples for all isolates tested, including the metronidazole-resistant isolate, were 2.5 mg/mL. The kinetic growth curve showed that the filtrate samples were able to reduce the density of parasites to zero within 24 h of incubation, which was confirmed by microscopy. Both fungal filtrate samples exhibited no hemolytic activity, and the P. citrinum F40 filtrate sample showed low cytotoxicity against Vero cells. These data suggest that marine-associated fungi from the South Brazilian Coast may produce potential candidates for further investigation and possible use in the treatment of metronidazole-resistant trichomonosis.

Mevalonolactone: an inhibitor of Staphylococcus epidermidis adherence and biofilm formation.

Staphylococcus epidermidis, a commensal microorganism at the human skin and mucosae, is nowadays considered an important opportunistic pathogen related to nosocomial infections on indwelling medical devices due biofilm formation. Bacterial biofilms are the worst aspect in the treatment of infections and now efforts have been made in the search for new molecular entities to overcome this situation. In this work, a compound isolated from marine associated fungi was capable to interfere with the adherence and biofilm formation of S. epidermidis. This compound, identified as mevalonolactone, showed significant inhibition of S. epidermidis ATCC 35984 biofilm formation, without antibacterial activity, evaluated by crystal violet assay, turbidimetric assay and scanning electron microscopy. When assayed against 12 clinical isolates of S. epidermidis, this compound exhibited both biofilm inhibition and antimicrobial activity, but no activity against gram-negative bacteria was observed. Therefore, when this constitutive molecule is added in the antibiofilm and antibacterial assays, it might act as an important agent against this pathogen, contributing to the arsenal of antibiofilm compounds.

Comparative Analysis of Sambucus nigra and Sambucus australis Flowers: Development and Validation of an HPLC Method for Raw Material Quantification and Preliminary Stability Study

This work was designed to develop a simple, effective, and reliable LC system to identify a chemical marker and compare Sambucus nigra L. and Sambucus australis Cham. et Schltdl. flower extracts (American and European elder). Rutin was the main constituent of both species. The developed method showed a linear response in the range of 10 to 45 microg x mL(-1) for rutin and 1.75 to 3.25 microg x mL(-1) for samples of the Sambucus species. Precision was determined and the relative standard deviations were 1.75 % for HSN and 1.28 % for HSA for intraday precision and 1.28 % and 1.51 % for inter-day precision, respectively, while accuracy was 97.9 % for HSN and 99.41 % for HSA. Quantification and detection limits as well as robustness were determined, presenting adequate results. The LC method showed an adequate performance for the separation of flavonoid glycosides in S. nigra and S. australis extracts, since the presence of interference had been previously evaluated. The analysis of thirty different samples of S. NIGRA and S. australis of different origins did not show significant variability among them. An accelerated stability study revealed a significant decrease in the first 30 days reaching 57 % in 90 days for S. australis samples and a total decrease of 25 % in 90 days for S. nigra samples, considering rutin as the chemical marker. These results will contribute to quality control analysis routines of these raw materials in pharmaceutical production facilities.

Caracterização farmacobotânica das espécies de Sambucus (Caprifoliaceae) utilizadas como medicinais no Brasil: Parte II. Sambucus australis Cham. & Schltdl.

Sambucus australis Cham. & Schltdl. (sabugueiro-do-rio-grande, Caprifoliaceae) is a medicinal plant described only in the first edition of Brazilian Pharmacopoeia. This species is native to Brazil, and its flowers are used in the folk medicine, with diuretic purpose, antipiretic, anti-inflammatory, mild laxative and to treat respiratory diseases, on infusions or decoctions forms. Aiming at elaborating an updated pharmacopoeical monograph and comparing it with the monograph of Sambucus nigra L., from Europe, it was established the macro and microscopic botanical characters, through the classic methodology used in plant morpho-anatomy. The macroscopic characters are: morphologic monoclin flowers; corolla with seven to ten millimeters of diameter; petals with five, rarely four parallel veins; shorter and longer stamens; ovary oftenly with five locules. The main microscopic characters are: thickned and striated cuticule; absense of idioblasts with calcium oxalate sandy cristals; anomocytic stomatas; amphystomatic bracts; hypostomatic sepals; amphi-hypostomatic petals; wavy and straight epidermal cells in the lower surface of sepals and petals; filaments epidermal cells with narrow and straight walls; glandular and non-glandular trichomes of different types; homogeneous mesophyll in bracts, sepals and petals; vascular system represented by both collateral bundles and xylematic elements; volatile and non volatile oil globules in all structures.

Caracterização farmacobotânica das espécies de Sambucus (Caprifoliaceae) utilizadas como medicinais no Brasil. Parte I. Sambucus nigra L.

The Elder tree (Sambucus nigra L., Caprifoliaceae) is a medicinal plant described in international pharmacopoeias, not yet mentioned in the Brazilian Pharmacopoeia. The flowers of this European species are commercialized in natura by the pharmacopeial name of Sambuci flos, with diuretic, antipyretic, anti-inflammatory and mild laxative purposes, and to treat respiratory diseases, through infusions or decoctions forms. Aiming at elaborating an updated pharmacopeial monograph, the macro and microscopic botanic characters were established, with the classic methodology used in plant morpho-anatomy. The macroscopic characters are: monoclin and equal flowers; corolla with three to five millimeters of diameter; petals with three to four parallel veins; equal stamens; ovary often with three locules. The main microscopic characters are: thickened and striated cuticle; anomocytic stomatas; bracts, sepals and petals with sandy crystals of calcium oxalate idioblasts; hypostomatic bracts; amphystomatic sepals; amphi-hypostomatic petals; strongly wavy epidermal cells in the lower surface of sepals and petals; filaments epidermal cells with narrow and straight walls; glandular and non-glandular trichomes of different types in all pieces; homogeneous mesophyll in bracts, sepals and petals; vascular system represented by both collateral bundles and xylematic elements; volatile and non-volatile oil globules in all structures.

Hydroxypropyl‐β‐cyclodextrin‐containing hydrogel enhances skin formononetin permeation/retention

This study was aimed to investigate the in vitro permeation potential of hydrogel formulations containing the isoflavones formononetin and biochanin A and cyclodextrins in different combinations.