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Oral medication with activity specifically at the inflamed sites throughout the gastrointestinal tract and limited systemic exposure would be a major advance in our therapeutic approach to inflammatory bowel disease (IBD). For this purpose, we have designed a prodrug by linking active drug moiety to phospholipid (PL), the substrate of phospholipase A

Therapeutics with activity specifically at the inflamed sites throughout the gastrointestinal tract (GIT) would be a major advance in our therapeutic approach to inflammatory bowel disease (IBD). We aimed to develop the prodrug approach that can allow such site-specific drug delivery. Currently, using cyclosporine as a drug of choice in IBD is limited to the most severe cases due to substantial systemic toxicities and narrow therapeutic index of this drug. Previously, we synthesized a series of a phospholipid-linker-cyclosporine (PLC) prodrugs designed to exploit the overexpression of phospholipase A

Polymeric coatings with micro-spherical morphology have a high surface area, which is advantageous for resins for heterogeneous chemical catalysis, for adsorption processes, nano-reactors, and anti-fouling coatings for water treatment membranes. The fabrication of stable, non-leachable micro-spherical polymers on solid surfaces is challenging. Here we introduce a straightforward method for fabricating polymeric particles with micro-spherical morphology on poly(ethylene terephthalate) fibers used as media for water filtration in microfiber technology. UV-initiated grafting with poly(ethylene glycol) methacrylate (PEGMA) monomers using benzophenone in aqueous solutions resulted in stable spherical particles coated on poly(ethylene terephthalate) threads, as revealed by FTIR, gravimetric degree of grafting, and SEM analyses. The micro-spherical morphology was unique to grafting with PEGMA monomers, whereas other types of methacrylate monomers resulted in smooth coatings. Grafting with PEGMA on high-flux water filtration cassette made of poly(ethylene terephthalate) fibers lead to enhanced performance and better dust removal capacity of the filter. The improved performance in coarse filtration is beneficial for treatment of water for agriculture, pretreatment facilities for freshwater supply, cooling water systems, and wastewater treatment. The protocol developed in this study is highly promising for both industrial and medical applications.

Lysine deacetylases (KDACs) are enzymes that catalyze the hydrolysis of acyl groups from acyl-lysine residues. The recent identification of thousands of putative acylation sites, including specific acetylation sites, created an urgent need for biochemical methodologies aimed at better characterizing KDAC-substrate specificity and evaluating KDACs activity. To address this need, we utilized genetic code expansion technology to coexpress site-specifically acylated substrates with mammalian KDACs, and study substrate recognition and deacylase activity in live Escherichia coli. In this system the bacterial cell serves as a “biological test tube” in which the incubation of a single mammalian KDAC and a potential peptide or full-length acylated substrate transpires. We report novel deacetylation activities of Zn2+-dependent deacetylases and sirtuins in bacteria. We also measure the deacylation of propionyl-, butyryl-, and crotonyl-lysine, as well as novel deacetylation of Lys310-acetylated RelA by SIRT3, SIRT5, SIRT6, and HDAC8. This study highlights the importance of native interactions to KDAC-substrate recognition and deacylase activity.

A novel bioinspired iron-catalyzed oxidative cross-coupling reaction between phenols and conjugated alkenes was developed. This method enables the direct coupling of phenols with styrene, α-alkyl- and α-arylstyrenes, β-alkyl styrenes, and stilbenes, thereby providing a new strategy for the preparation of the pharmacologically important 2,3-dihydrobenzofuran motif. In addition, this study revealed that under a different set of conditions an oxidative/addition dearomatization reaction of 1,1′-bi-2-naphthol (BINOL) with styrene can take place.

A novel bioinspired iron-catalyzed oxidative cross-coupling reaction between phenols and conjugated alkenes was developed. This method enables the direct coupling of phenols with styrene, α-alkyl- and α-arylstyrenes, β-alkyl styrenes, and stilbenes, thereby providing a new strategy for the preparation of the pharmacologically important 2,3-dihydrobenzofuran motif. In addition, this study revealed that under a different set of conditions an oxidative/addition dearomatization reaction of 1,1′-bi-2-naphthol (BINOL) with styrene can take place.

A chemo-, regio-, and stereoselective FeCl(3)/1,10-phenanthroline-catalyzed cross dehydrogenative coupling (CDC) reaction between phenols and α-substituted β-ketoesters was developed. The reaction creates a new quaternary carbon center within a polycyclic hemiacetal or polycyclic spirolactone architecture. The applicability of the new method to the synthesis of natural products was demonstrated by a possible biomimetic synthesis of the lachnanthospirone core.