Novel carbohydrate-triazole derivatives as potential α-glucosidase inhibitors / 中国天然药物

A series of novel pyrano[2, 3-d]trizaole compounds were synthesized and their α-glucosidase inhibitory activities were evaluated by in vitro enzyme assay. The experimental data demonstrated that compound 10f showed up to 10-fold higher inhibition (IC74.0 ± 1.3 μmol·L) than acarbose. The molecular docking revealed that compound 10f could bind to α-glucosidase via the hydrophobic, π-π stacking, and hydrogen bonding interactions. The results may benefit further structural modifications to find new and potent α-glucosidase inhibitors.

Recent advance in carbohydrate-based cancer vaccines / 药学学报

The abnormal glycans expressing on the surface of tumor cells are good targets to develop carbohydrate-based anti-cancer vaccines. However, one of the major problems is that carbohydrate antigens possess weak immunogenicity. This review summarizes the recent efforts to overcome this problem: glycoconjugates produced by coupling the carbohydrate antigens and proper carrier proteins improve their immunogenicity, many glycoconjugates have entered clinical trials; the vaccines become chemically well-defined when coupling the carbohydrate antigens with a T-cell peptide epitope and an immunostimulant to form fully synthetic multi-component glycoconjugate vaccines; the modification of carbohydrate antigens in combination with the technology of metabolic oligosaccharide engineering of tumor cells induces a strong immune response; and the fact that the antibodies elicited against the unnatural carbohydrate antigens can recognize the native carbohydrate antigens on tumor cells provides a new promising strategy for the development of anti-cancer vaccines.

Aminoglycoside mimetics as small-molecule drugs targeting RNA.

The potential of RNA as a new drug target has recently come to the fore, with the recognition that RNA molecules can adopt complex three-dimensional structures that, as with proteins, enable the design of specific ligands. Another reason for the present interest comes from the fact that many pathogenic agents, such as retroviruses, encode their genetic information in RNA strands. Unfortunately, the high toxicity and rapid emergence of high-level resistance have severely limited the usefulness of naturally occurring aminoglycoside antibiotics. To tackle these problems, it is an important concern to design new synthetic compounds with smaller, simpler structures which possess higher RNA binding affinity, better selectivity, better antibiotic activity, and stronger resistance against the aminoglycoside-modifying enzymes compared to their parent structures. Here, we will attempt a survey of current efforts to develop aminoglycoside mimetics or derivatives that target RNA. The latest advances in this field including rational design, synthetic strategy, and structure activity relationships are reviewed.