Hop leaves: From waste to a valuable source of bioactive compounds - A multidisciplinary approach to investigating potential applications.

After harvesting of cones used for beer production, the remaining hop vegetative biomass requires disposal. The hop plant contains bioactive compounds in all its parts-cones, leaves, and roots-exhibiting interesting antioxidant, antiviral, and antibacterial properties. In this work, extracts obtained from hop leaves, a plant material often neglected in the hop cultivation, have been investigated; the qualitative UHPLC-MS/MS and GC-TOF-MS characterization revealed the presence of bioactive compounds such as polyphenols, α- and β-acids and terpenes are present.

Inhibition of polymorphic MexXY-OprM efflux system in Pseudomonas aeruginosa clinical isolates by Berberine derivatives.

The MexXY-OprM multidrug efflux pump (EP) in aminoglycosides resistant Pseudomonas aeruginosa is one of the major resistance mechanisms, which is often overexpressed in strains isolated from pulmonary chronic disease such as cystic fibrosis. In this research, we focused on the design of potential efflux pumps inhibitors, targeting MexY, the inner membrane component, in an allosteric site. Berberine has been considered as lead molecule since we previously demonstrated its effectiveness in targeting MexY in laboratory reference strains.

Identification of a novel nitroflavone-based scaffold for designing mutant-selective EGFR tyrosine kinase inhibitors targeting T790M and C797S resistance in advanced NSCLC.

The inhibition of the Epidermal Growth Factor (EGFR) represents one of the most promising strategies in non-small cell lung cancer (NSCLC) therapy. The recently identified C797S mutation causes resistance of EGFR against osimertinib, the latest approved third generation EGFR inhibitor. The identification of small molecules capable of selectively inhibiting the T790M mutations also in the late-onset C797S mutation is a desirable strategy and novel chemical structures might provide new insight in the overcoming resistance mechanisms.

Salt effects on mixed composition membranes containing an antioxidant lipophilic edaravone derivative: a computational-experimental study.

The protection of lipid membranes against oxidation avoids diseases associated with oxidative stress. As a strategy to contrast it, functionalized lipids with antioxidant activity are used to become part of membranes thus protecting them. For this purpose, a lipophilic edaravone derivative has been synthesized, adding a C18 saturated chain to the original structure.

Berberine Derivatives as MexXY-OprM Inhibitors: Activity and In Silico Insights.

The natural alkaloid berberine has been demonstrated to inhibit the multidrug efflux system MexXY-OprM, which is responsible for tobramycin extrusion by binding the inner membrane transporter MexY. To find a structure with improved inhibitory activity, we compared by molecular dynamics investigations the binding affinity of berberine and three aromatic substituents towards the three polymorphic sequences of MexY found in (PAO1, PA7, and PA14). The synergy of the combinations of berberine or berberine derivatives/tobramycin against the same strains was then evaluated by checkerboard and time-kill assays.

Ethnopharmacognostic survey on the natural ingredients used in folk cosmetics, cosmeceuticals and remedies for healing skin diseases in the inland Marches, Central-Eastern Italy.

An ethnopharmaceutical study focused on domestic cosmetics, cosmeceuticals, and remedies to heal skin diseases traditionally used in the inland part of the Marches region (Central-Eastern Italy) has been conducted. At present, traditional knowledge concerning home-made phytocosmetics is represented by both the remnants of an orally transmitted folk heritage and also by new forms of knowledge, sometimes coming from popular phytotherapeutical books and the mass media (out of the scope of this survey), but also as a result of recent migration trends from Eastern Europe. We recorded approximately 135 cosmetic or cosmeceutical preparations prepared from more than 70 botanical species and a very few animal or mineral ingredients.