a-130a and Inflammation

Oxyprenylated secondary metabolites from plants, fungi, and bacteria, and their semisynthetic derivatives have been subject of growing interest during the last decade. Such natural products in fact have been discovered as potentially novel lead compounds for a series of pharmacological activities, mainly in terms of anti-cancer and anti-inflammatory ones. Especially during the last 5 years, a wider panel of prenyloxy secondary metabolites have been investigated from chemical and biological points of view and these include benzoic acids, alcohols, aldehydes, chalcones, anthraquinones, 1,4-naphthoquinones, other than the well known oxyprenylated ferulic acid and coumarin derivatives. The aim of this comprehensive review is to focus on the anti-inflammatory properties and related mechanisms of action of selected classes of oxyprenylated naturally occurring compounds and their semisynthetic analogues covering the literature period from 2011 to 2017. In vitro and in vivo data on their pharmacological activity triggering different pathways of the overall inflammatory machinery as well as structure activity relationship acquisitions will be summarized in order to make a detailed survey of the most recent reports on the potential of the title compounds as a novel class of anti-inflammatory agents.

Topics: Animals; Anthraquinones; Anti-Inflammatory Agents; Benzoates; Biological Products; Chalcones; Cinnamates; Coumarins; Drug Discovery; Humans; Inflammation; Naphthoquinones; Prenylation; Secondary Metabolism

This protocol describes microsphere-based protease assays for use in flow cytometry and high-throughput screening. This platform measures a loss of fluorescence from the surface of a microsphere due to the cleavage of an attached fluorescent protease substrate by a suitable protease enzyme. The assay format can be adapted to any site or protein-specific protease of interest and results can be measured in both real time and as endpoint fluorescence assays on a flow cytometer. Endpoint assays are easily adapted to microplate format for flow cytometry high-throughput analysis and inhibitor screening.

Topics: Animals; Biotinylation; Flow Cytometry; Fluorescence Resonance Energy Transfer; Green Fluorescent Proteins; High-Throughput Screening Assays; Humans; Inflammation; Kinetics; Microspheres; Peptide Hydrolases; Peptides; Reproducibility of Results; Temperature