Robust SERS Platforms Based on Annealed Gold Nanostructures Formed on Ultrafine Glass Substrates for Various (Bio)Applications

In this study, stable gold nanoparticles (AuNPs) are fabricated for the first time on commercial ultrafine and nonconductive glass coverslips coated with gold thin layers (2 nm, 4 nm, 6 nm, and 8 nm) at 25 \ub0C and annealed at high temperatures (350 \ub0C, 450 \ub0C, and 550 \ub0C) on a hot plate for different periods of time. Such gold nanostructured coverslips were systematically tested via surface enhanced Raman spectroscopy (SERS) to identify their spectral performances in the presence of different concentrations of a model molecule, namely 1,2-bis-(4-pyridyl)-ethene (BPE). By using these SERS platforms, it is possible to detect BPE traces (10 1212 M) in aqueous solutions in 2 min (120 s)

Quartz Crystal Microbalance Genosensing of Brettanomyces bruxellensis Yeast in Wine Using a Rapid and Efficient Drop and Collect Protocol

A miniaturized quartz crystal microbalance (QCM) genosensor is proposed for sensitive and real-time detection of short ssDNA sequences (53 bp) or DNA extracted from Brettanomyces bruxellensis (Brett) yeast cells. The presence of Brett yeast causes a depreciation of the quality of aged fine wines, producing molecules of unpleasant odors and biogenic amines that are harmful to human health. More specifically, standard quartz crystal (S-QCM) and homemade 4 nm gold transmission electron microscopy (TEM)-grid patterned quartz (multi-TEM QCM) are herein proposed for biofunctionalization steps with different ssDNA sequences. By employing a rapid and efficient drop and collect protocol, the specific detection of 1 pg/µL ssDNA Brett of a short sequence and 100 ng/μL DNA of B. bruxellensis extracted from a wine sample (VR2008) is reported

Quinazoline based \u3b11-adrenoreceptor antagonists with potent antiproliferative activity in human prostate cancer cell lines

New \u3b11-adrenoreceptor (\u3b11-AR) antagonists related to prazosin and doxazosin were synthesized by replacing piperazine ring with (S)- or (R)-3-aminopiperidine. Binding studies indicated that the S configuration at the 3-C position of the piperidine ring is crucial for an optimal interaction of the compounds at all three \u3b11-AR subtypes. Quinazolines 9 and 10, bearing a quinone ring on the lateral chain, exhibited also potent antiproliferative activity in LNCaP androgen-sensitive prostate cancer cell lines, higher than that of doxazosin. Compound 10 increased apoptosis, in terms of DNA fragmentation, without triggering cell necrosis. The prooxidant activity found in compound 10 may underlie its ability to inhibit cell proliferation in synergy with the effect mediated by \u3b11-AR antagonism. Due to its better biological profile compared to doxazosin for LNCaP cell line, compound 10 might be a valuable lead compound for the design of new prostate antitumor agents

Doxazosin-Related a1-Adrenoceptor Antagonists With Prostate Antitumor Activity

Doxazosin analogues 1-3 and 1a were synthesized and investigated at alpha1-adrenoceptors and PC-3, DU-145, and LNCaP human prostate cancer cells. Compound 1 (cyclodoxazosin) was a potent alpha(1B)-adrenoceptor antagonist displaying antiproliferative activity higher than that of doxazosin in cancer cells in vitro and in vivo, respectively. Because of its antitumor efficacy at low concentrations, lower apoptotic activity in NHDF vs tumor cells, and antiangiogenetic effect, 1 showed a better therapeutic profile relative to doxazosin

Discovery of a new series of 5-HT1A receptor agonists

Starting from compounds previously disclosed as \uf0611-adrenoceptor antagonists which were also found to bind to 5-HT1A receptor, in the attempt to separate the two activities, a new series of 5-HT1A receptor agonist was identified. They were shown to have high potency and/or high selectivity. Among them compound 13 that combine high selectivity (5-HT1A/\uf0611= 151) and good agonist potency (pD2= 7.82; Emax=76) turned out to be the most interesting of the series