Design, synthesis and study of anti-tumor activity of thiazolinone urea derivatives bearing aryloxypyridinone fragments / 药学学报

Taking cabozantinib as leading compound, 13 novel small molecular c-Met inhibitors were designed and synthesized based on the obtained structure-activity relationships (SARs) of c-Met inhibitors. The structures of compounds were confirmed by 1H NMR, 13C NMR and HR-MS. In vitro anti-tumor activity was evaluated by MTT method, and the mechanism was preliminarily disclosed by real-time dynamic living cell imaging and flow cytometry analysis. The results indicated that most of compounds showed good inhibition activity against human non-small-cell carcinoma cell A549 and human colorectal cancer cell HT-29 which was superior to cabozantinb. Compounds showed excellent cytotoxity and anti-proliferative activity against HT-29, and promoted cell apoptosis.

Research progress of roles of Toxoplasma gondii profilin in invading host cells and inducing immune response / 中国人兽共患病学报

Toxoplasma gondii is a kind of worldwide obligate intracellular parasitic protozoa,which can live in almost all nucleated cells besides red blood cells and cause zoonosis.Toxoplasma gondii is mainly transmitted by the fecal-oral route;damaged skin,mucous membrane and the placenta are the secondary pathway.After infection,the parasite need to invade host cells and formate parasitophorous vacuole to complete reproductive cycle,while many studies have shown that actin binding protein profilin of Toxoplasma gondii(TgPRF) play important roles in regulating actin polymerization and invading host cells.At the same time,TgPRF can be used as a dominant antigen to induce host immune response,especially innate immunity through Toll like receptor (TLR).In this paper,the structural characteristics of TgPRF and its roles in the invasion of the host and inducing the host immune responses were reviewed,which would provide profound understanding of Toxoplasma gondii pathogenic mechanism and a reference for immune prevention.