Plasma protein binding plays a critical role in drug therapy, being a key part in the characterization of any compound. Among other methods, this process is largely studied by ultrafiltration based on its advantages. However, the method also has some limitations that could negatively influence the experimental results. The aim of this study was to underline key aspects regarding the limitations of the ultrafiltration method, and the potential ways to overcome them. The main limitations are given by the non-specific binding of the substances, the effect of the volume ratio obtained, and the need of a rigorous control of the experimental conditions, especially pH and temperature. This review presents a variety of methods that can hypothetically reduce the limitations, and concludes that ultrafiltration remains a reliable method for the study of protein binding. However, the methodology of the study should be carefully chosen.
Non-steroidal anti-inflammatory drugs (NSAIDs) are an important pharmacological class of drugs used for the treatment of inflammatory diseases. They are also characterized by severe side effects, such as gastrointestinal damage, increased cardiovascular risk and renal function abnormalities. In order to synthesize new anti-inflammatory and analgesic compounds with a safer profile of side effects, a series of 2,6-diaryl-imidazo[2,1-b][1,3,4]thiadiazole derivatives 5a–l were synthesized and evaluated in vivo for their anti-inflammatory and analgesic activities in carrageenan-induced rat paw edema. Among all compounds, 5c showed better anti-inflammatory activity compared to diclofenac, the standard drug, and compounds 5g, 5i, 5j presented a comparable antinociceptive activity to diclofenac. None of the compounds showed ulcerogenic activity. Molecular docking studies were carried out to investigate the theoretical bond interactions between the compounds and target, the cyclooxygenases (COX-1/COX-2). The compound 5c exhibited a higher inhibition of COX-2 compared to diclofenac.
The study provides information about separation and identification of natural bioactive compounds from beech (Fagus sylvatica L.) bark with potential therapeutic applications such as antibacterial activity against human pathogens. Beech is a common material used in the wood industry, but its bark is separated from the wood and is considered a by-product. In this study, natural compounds with biological activity were obtained from beech bark by hot water extraction. The high-performance liquid chromatography (HPLC) was used to analyze the phenolic compounds in the beech bark extracts. Spectrophotometric methods were employed for the determination of total phenolic content. Microdilution technique was used for testing the antimicrobial activity of the extract. The following strains were tested: Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus, Klebsiella pneumoniae, Escherichia coli and Pseudomonas aeruginosa. The yield of extracted polyphenols was of 22.952 mg gallic acid/g dry bark. The compounds identified by HPLC were vanilic acid, catechin, taxifolin and syringin. The extracts were active against Staphylococcus aureus and Methicillin-resistant Staphylococcus aureus. The effect of polyphenolic extract on Gram-negative bacteria was absent at a concentration of 30 mg/mL beach bark extract. Altogether, the use of pure water for extraction of polyphenols from beech bark proved to be an effective eco-friendly method. This method sustains the concept of "green" chemistry by involving the use of renewable plant resources and also by using water as solvent.
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