Propolis potential activity against Candida tropicalis adhered cells and its biofilms

Objectives: Invasive fungal infections, such as candidiasis, represent a public health problem of major importance, and Candida tropicalis has been highlighted among the main agents of candidiasis. One of the major contributions to C. tropicalis virulence is its versatility in adapting to a variety of different habitats and the formation of surface attached microbial communities known as biofilms. Moreover, from the clinical perspective, the most important feature of Candida biofilms is its role in increasing tolerance to conventional antifungal therapy. This scenario encourages the search for alternative therapies. Natural matrixes, such as propolis, compromise a multitude of bioactive properties, in particular phenolic extracts have evidenced significant antimicrobial properties against a multiple of opportunist invaders, including Candida species. Thus, the main objective of the present work was to evaluate the potential antifungal effect of propolis against Candida tropicalis biofilms. Methods: This study was conducted with four strains of C. tropicalis and one reference strain, from the American Type Culture Collection (ATCC 40042). Biofilm formation were carried out on 96-well microplates containing a cellular suspension of 1x105 cells/mL and incubated for 24 h at 37°C. Pre-formed C. tropicalis biofilms were treated with propolis (ranging from 0.47 to 1.42 mg/ml), during 24 h at 37°C and its effect assessed through quantification of the number of colony forming unit (CFU). Results: It was evident that all C. tropicalis strains tested were able to form biofilm and that propolis was able to reduce around 40% and 50% of the pre-formed biofilm. Moreover, in general the propolis effect was similar among all the C. tropicalis clinical isolates strains Conclusions: These data are promising, since they open important perspectives regarding new antifungal agents, much more effective and safer than the currently available to treat and to prevent C. tropicalis infections

Genetic diversity analysis in the section Caulorrhizae (genus Arachis) using microsatellite markers

Diversity in 26 microsatellite loci from section Caulorrhizae germplasm was evaluated by using 33 accessions of A. pintoi Krapov. & W.C. Gregory and ten accessions of Arachis repens Handro. Twenty loci proved to be polymorphic and a total of 196 alleles were detected with an average of 9.8 alleles per locus. The variability found in those loci was greater than the variability found using morphological characters, seed storage proteins and RAPD markers previously used in this germplasm. The high potential of these markers to detect species-specific alleles and discriminate among accessions was demonstrated. The set of microsatellite primer pairs developed by our group for A. pintoi are useful molecular tools for evaluating Section Caulorrhizae germplasm, as well as that of species belonging to other Arachis sections

promising starting points for drug design

Medicinal chemists continue to be fascinated by chalcone derivatives because of their simple chemistry, ease of hydrogen atom manipulation, straightforward synthesis, and a variety of promising biological activities. However, chalcones have still not garnered deserved attention, especially considering their high potential as chemical sources for designing and developing new effective drugs. In this review, we summarize current methodological developments towards the design and synthesis of new chalcone derivatives and state-of-the-art medicinal chemistry strategies (bioisosterism, molecular hybridization, and pro-drug design). We also highlight the applicability of computer-assisted drug design approaches to chalcones and address how this may contribute to optimizing research outputs and lead to more successful and cost-effective drug discovery endeavors. Lastly, we present successful examples of the use of chalcones and suggest possible solutions to existing limitations.publishersversionpublishe

Nanostructured lipid systems modified with waste material of propolis for wound healing: design, in vitro and in vivo evaluation

Propolis, a natural compound that can accelerate the wound healing process, is mainly used as ethanolic extract. The extractive solution may also be obtained from the propolis by-product (BP), transforming this waste material into a pharmaceutical active ingredient. Even if propolis does not show toxicity, when used as an extract over harmed skin or mucosa, the present ethanol content may be harmful to the tissue recovering, besides hindering the drug release. This study describes the development of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) as topical propolis delivery systems and the investigation of their in vitro and in vivo activities. The extracts were evaluated to guarantee their quality, and the lipid dispersions were characterized with respect to morphology (cryo-TEM), size and diffractometry (X-ray) properties. The occlusive capacity of formulations was also evaluated by an in vitro technique, which, determines the occlusion factor. The drug entrapment efficiency (EE), as well as the in vitro drug release profile from the nanoparticulate systems was investigated as well. The size analysis performed through 90 days was favorable to a topical administration and the polydispersity index, though not ideal in all cases due to the high content of resins and gums from the extracts, were relatively stable for the SLN. The propolis extract contributes to the occlusive potential of the formulations. The human immortalized keratinocytes presented good cell viability when tested with both extracts (propolis and BP) freely or entrapped in the systems. SLN modified with propolis material provided an acceleration of the in vivo wound healing process

Design of propolis-loaded film forming systems for topical administration: The effect of acrylic acid derivative polymers

In situ film forming systems are an alternative to the conventional dosage forms for topical application, performing superior contact and adhesiveness, with a consequent sustained and efficacious therapy. Propolis (PRP) is an extremely versatile natural compound due to its constitutive complexity and in terms of biological properties and uses as healing, anti-inflammatory, anti-cancer, antimicrobial, antiviral, and antifungal activities. In this work, the thermoresponsive polymer (poloxamer 407) and bioadhesive polymers derived fromthe acrylic acid were utilized to prepare dispersed systems containing different concentrations of propolis extract, and they were evaluated in terms of film forming capability. The gelation temperature and mechanical characteristics were also investigated so that some systems could be selected from a factorial design. The selected formulations presented good mechanical and rheological structuring properties, and they could incorporate the PRP extract. These systems denoted plastic flow behavior and viscoelasticity, and the PRP extract presence evinced greater capacity of the systems to support higher shear stress. When PRP extract was present, the systems with Carpobol 974P or polycarbophil (F7 and F10) presented greater structuring, with superior flexibility and rupture resistance. Moreover, they showed easiness for topical administration, with good spreadability and softness. Its excellent film forming capacity proved ex vivo, encourages further investigations for topical application

Estimativa da área foliar de plantas daninhas: Solanum americanum Mill Leaf area determination of weeds: Solanum americanum Mill

A maria pretinha (Solanum americanum Mill) é uma planta daninha infestante de diversas culturas e além da competição pode causar outros problemas. Nos estudos envolvendo a biologia e o controle de plantas daninhas, a área foliar é uma das mais importantes características a serem avaliadas, mas tem sido pouco estudada porque sua determinação exige equipamentos sofisticados ou utiliza técnicas destrutivas. Visando obter equações que permitissem a estimativa da área foliar desta planta daninha utilizando características lineares do limbo foliar, facilmente mensuráveis em plantas no campo, foram estudadas correlações entre a área foliar real e as seguintes características das folhas: comprimento ao longo da nervura principal (C), largura máxima do limbo (L) e o produto (C x L). Para tanto, foram mensuradas 200 folhas coletadas de plantas sujeitas às mais diversas condições ecológicas em que a espécie sobrevive, considerando-se todas as folhas das plantas desde que não apresentassem deformações oriundas de fatores, tais como, pragas, moléstias e granizo. Todas as equações, lineares simples, geométricas e exponenciais, permitiram boa estimativa da área foliar (Af) da maria pretinha. Do ponto de vista prático, sugere-se optar pela equação linear simples envolvendo o produto (C x L), a qual apresentou o menor QM Resíduo. Assim, a estimativa da área foliar de S. americanum pode ser efetuada pela equação AF = 0,5632 x (C x L), com coeficiente de determinação (R2) de valor igual a 0,9516.<br>Solanum americanum is a very aggressive weed that, besides competition, can cause many other problems. Despite being one of the most important parameters to be analyzed, only few studies have been carried out concerning the leaf area mainly because its determination demands sophisticated equipment or destructive techniques. Aiming to develop equations that allow to estimate the leaf area of this weed using linear measure of the leaf surface, statistical relations between the leaf area and the following linear measures were determinded: the leaf lenght in the mid rib direction (C), maximum width (L) and the product (C x L). 200 leaves were collected from plants infesting different places and crops and showing suitable nutrition; and health conditions. All the equations, linear, geometric and exponential permitted suitable estimates of the Solanum americanum Mill leaf area (Af) . From the point of view of pratice, the linear equation (C x L) was selected because it shows the Smallest Stand Error. Thus, a estimative of Solanum americanum. Leaf area can be calculated by the equation Af = 0.5632 x (C x L), with R2 = 0.9516