chemical composition and antimicrobial activity of the essential oil from the bark of xylopia hypolampra

Hydrodistillation of Xylopia hypolampra Mildbr. stem bark afforded 39 mg (dry weight basis) of a pale yellow fragrant essential oil; gas chromatography-flame ionization detector and gas chromatogra..

Protein-Labs on Separative Analytical Scale in Medicinal Chemistry: from the Proof of Concept to Applications

Coupling of a macromolecule such as an enzyme or a receptor to a chromatographic support has revealed a powerful analytical tool to face different aspects related to drug discovery. Chromatographic systems with immobilized macromolecules have been developed to be used for different applications in pharmaceutical analysis including enzyme inhibitor screening, biopharmaceutics structural analysis, chiral separations and binding studies. These areas of research are very challenging both for the technological and for the applicative aspects. This review offers an overview of general strategies and references that can be considered in order to develop innovative and reliable “protein-labs” for specific separative analytical applications of pharmaceutical interest

Affinity-based separation methods for the study of biological interactions: The case of peroxisome proliferator-activated receptors in drug discovery

Affinity-based methods using immobilized proteins are important approaches for understanding the interactions between small molecules and biological targets. This review is intended to provide an overview of different affinity based separation methods that have been applied to the study of peroxisome proliferator activated receptors (PPARs). The screening of compound to increase screening rates for synthetic and natural ligands of PPAR are reported. Pros and cons of the approaches in ligand discovery initiatives are discusse

Optimum extraction process of polyphenols from Bridelia grandis stem bark using experimental design

Euphorbiaceae barks are known to contain an appreciable amount of polyphenolic compounds responsible for several biological activities. Preliminary extraction from Bridelia grandis stem bark afforded high content of polyphenols, determined by spectrophotometric methods such as Folin–Ciocalteu (for total phenols, TP) and n-butanol-HCl (for condensed tannins, CT). A preliminary Plackett–Burman screening design was used to identify the key factors that influence the TP and CT extraction. Between all the variables known to influence the extraction from vegetable matrixes, six were selected; maceration was chosen as traditional extraction methodology. To investigate the effect of solvents and extraction method, methanol, acetone 70% (v/v in water), centrifugation and ultrasound were chosen. A full factorial design 23 was applied to optimize the extraction procedure. The responses were obtained analyzing the extracts for their TP and CT contents determined by the above-mentioned spectrophotometric methods. The results confirm that, within the explored domain, the optimum solvent is methanol and the optimum method is one-cycle centrifugation. Finally, it was also compared with the effect of maceration on the considered responses. It has never given results better than centrifugation, whereas in the case of CT it represents an advantage to employ a threecycle centrifugation instead of one