Mini-Reviews in Organic Chemistry - Volume 13, Issue 2, 2016

The fruit of Cnidium monnieri (L) Cusson is an important traditional medicine employed in Taiwan and China as the treatments of impotence, sterilization, renal disease, dermatosis, colpitis, inflammation and gynecological disease. Peroxisome Proliferator-activated Receptor γ (PPARγ) and Farnesoid X receptor (FXR) are the members of nuclear receptor superfamily that have been targeted for developing treatments for chronic liver diseases. In this study, the furocoumarins isolated from the fruit of Cnidium monnieri (L) Cusson were evaluated for their PPARγ and FXR agonism. Indeed, in transient transfection reporter assays, these furocoumarins transactivated PPARγ and FXR to respectively modulate promoter action including ABCA1 and SHP promoters in dose-dependent manner. Through the molecular modeling docking studies these furocoumarins were shown to bind to PPARγ or FXR ligand binding pocket fairly well. All these results indicate that Cnidium monnieri (L) Cusson might possess therapeutic effects through the activation of PPARγ and FXR pathways.

Nuclear receptors (NRs) are ligand-activated transcription factors modulating significant biological functions including cell growth, lipid metabolism, and glucose homeostasis, so they are frequently to be utilized as important drug targets to develop therapeutic reagents. Farnesoid X receptor (FXR) with bile acids as the natural ligands, plays an essential role in regulation of bile acid and glucose metabolism, and is involved in the pathologies of human diseases including diabetes and chronic liver diseases. Thus, FXR is a promising pharmacological target for these diseases. Synthetic FXR agonists like INT-747 developed by Intercept Pharmaceutical Company is in the clinical trial phase III for non-alcoholic steatohepatitis and can be approved as the treatment of primary biliary cirrhosis in 2016. Due to the promising clinical trial results of INT-747, the naturally occurring FXR ligands may be utilized as the preventive nutraceuticals or treatments of the chronic liver diseases and diabetes. In this review, the natural FXR agonists are summarized and their possible interactions with FXR ligand binding region are discussed.

Cationic polyacrylamide (CPAM) is a polyelectrolyte whose monomeric unit contains ionizable cationic groups. In recent years, CPAM has received increasing attention owing to its unique properties and superior performance compared with those of other conventional inorganic coagulants and organic polymeric flocculants. This review examined the recent advances in CPAM synthesis. The synthetic mechanisms include direct copolymerization and post-polymerization functionalization, and direct copolymerization mainly includes aqueous solution polymerization, micellar copolymerization, dispersion polymerization, inverse emulsion polymerization, and template polymerization. In addition, various choices for initiator preparation are summarized in this paper. In conclusion, we propose a future research prospect relating to CPAM synthesis and its application in water treatment.

Magnetic polymer microspheres with unique magnetic properties and excellent physical chemical properties, such as strong stability, high biocompatibility, and exclusive adsorption properties, are widely used in biology and medicine, as well as show unique advantages in environmental fields. This article aims to provide recent preparation and characterization methods of magnetic polymer microspheres and their applications in environmental fields. Conclusions and future trends are also presented.

Natural products bearing a triazaspirocyclic motif have received significant attention in recent years. These compounds, which feature three nitrogen atoms attached to one quaternary carbon forming a spirocyclic scaffold, exhibit a wide range of biological activity and have promising applications in materials as well as in drug discovery. In this review article, we will discuss triazaspirocycles in Nature, their biological activity, and applications. Methods for the synthesis of triazaspirocycles as well as the reactivity of triazaspirocyclic scaffolds will be reviewed.

β-Aminocarbonyl compounds are useful building blocks for the synthesis of biologically and medicinally important molecules. They are important intermediates for molecules like β-amino alcohols, β-amino acids and lactams which have applications in various pharmaceutical and natural product syntheses. The derivatives of β-aminocarbonyl compounds have found applications as diverse therapeutic agents such as antimicrobial, anti-inflammatory, anticonvulsant, anticancer, etc. Due to the wide diversity of applications, the methods for their synthesis are focus of research. In the present review, we have compiled some of the important catalysts and reagents used for the synthesis using Mannich reaction and their potential pharmaceutical applications.

Chitosan is an ideal biomaterial due to its excellent comprehensive properties. Cyclodextrins bearing the cavity structure and amphiphilic properties have become the focus of supramolecular chemistry. The chemical immobilization of cyclodextrin on the chitosan skeleton can be a feasible means to generate supramolecular host material. However, cyclodextrin is usually immobilized on the 2-NH2 group of chitosan, which suppresses the activities of the amino group such as physiological activities, functionalization, modification, and so on. Therefore, efforts have been made to immobilize cyclodextrin at the 6-OH position of chitosan to maintain the functions of the 2-NH2 group, and thus to achieve materials with the excellent supramolecular inclusion properties of cyclodextrin and the remarkable advantages of chitosan in membrane formation, immobilization, functionalization and biochemical properties, especially the prominent bioactivity derived from its 2-NH2. In the present paper, various recently reported synthesis routes for chitosan 6-OH immobilized cyclodextrin derivatives (CTS-6-CD) were introduced in detail. The applications of CTS-6-CD in drug delivery, absorbents, the corrosion inhibition of metal and biosensor due to the unique properties of CTS-6-CD was reviewed. The perspectives on the developing of particular derivatives were also discussed.