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A new rigid and symmetrical tetracarboxylic ligand 2,3,5,6-tetrakis(4-carboxyphenyl)pyrazine (H4TCPP) ligand was employed in the construction of a new Zn(II)-based metal–organic framework [Zn3(OH)2(H2TCPP)2](DMF)3 (1). Complex 1 not only displays bright blue luminescence arising from the matrix coordination-induced emission effect of the TCPP2− ligand, but also exhibits effective detection for picric acid in the solution with the quenching constant of 3.59 × 104 M−1. In the biological study, we investigated the effect of compound on Hep laryngeal cancer cell viability and proliferation with CCK8 assay, analyzed the production of autophagy in Hep cells by flow cytometer, and the western blot was also used to detect the expression of autophagy-related proteins. Moreover, the autophagy inhibitor 3-MA was used in this study to explore the role of autophagy in the anti-cancer activity of compound. [ABSTRACT FROM AUTHOR]

Strigolactones (SLs) are a novel class of plant hormones with enormous potential for the prevention and treatment of inflammation. To further investigate the anti-inflammatory activities of SLs, a representative SL, GR24, and the reductive products of its D-ring were synthesized and their anti-inflammatory activities were fully evaluated on both in vitro and in vivo models. Among these compounds, the two most active optical isomers ( 2a and 6a ) demonstrated strong inhibitory activity on the release of inflammatory cytokines, including nitric oxide (NO), tumor necrosis factor-alpha (TNF-α), and interleukin-6 (IL-6) by blocking the nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways; they also greatly inhibited the migration of neutrophils and macrophages in fluorescent protein labeled zebrafish larvae. These results identified the promising anti-inflammatory effects of SLs, and suggested that both the absolute configuration of SL and the α,β-unsaturated D-ring structure are essential for the observed anti-inflammatory activity.

Factor IXa (FIXa), a blood coagulation factor, is specifically inhibited at the initiation stage of the coagulation cascade, promising an excellent approach for developing selective and safe anticoagulants. Eighty-four amidinobenzothiophene antithrombotic derivatives targeting FIXa were selected to establish three-dimensional quantitative structure-activity relationship (3D-QSAR) and three-dimensional quantitative structure-selectivity relationship (3D-QSSR) models using comparative molecular field analysis and comparative similarity indices analysis methods. Internal and external cross-validation techniques were investigated as well as region focusing and bootstrapping. The satisfactory q (2) values of 0.753 and 0.770, and r (2) values of 0.940 and 0.965 for 3D-QSAR and 3D-QSSR, respectively, indicated that the models are available to predict both the inhibitory activity and selectivity on FIXa against Factor Xa, the activated status of Factor X. This work revealed that the steric, hydrophobic, and H-bond factors should appropriately be taken into account in future rational design, especially the modifications at the 2'-position of the benzene and the 6-position of the benzothiophene in the R group, providing helpful clues to design more active and selective FIXa inhibitors for the treatment of thrombosis. On the basis of the three-dimensional quantitative structure-property relationships, 16 new potent molecules have been designed and are predicted to be more active and selective than Compound 33, which has the best activity as reported in the literature.

Objective: To study the oldly people's hearing screening and dynamic monitoring mode, and to discuss the new diseases and health management mode in current information network era., Methods: To establish the network connection between the hospital and the communities in the internet through the function expansion of the Hospital Information Systems and to realize "dual systems, double platforms" integrated management modes and establish the audiology workstation. The routine physical examination, pure tone hearing threshold tests and middle ear analysis were performed on four hundred and twenty elderly people from the fourteen communities every three months, and the changes of hearing and related symptoms were observed., Results: Resources sharing was established between the hospital and these fourteen communities. Health records were established for all the aged people, the hearing screening lasted only half a day each time. Fourteen hearing loss cases were found during one year. A statistically significant difference (P < 0.01) were found, the ratio of hearing loss with diabetes, high blood pressure and other diseases were much higher than people without concomitant., Conclusion: The advantage of disease management mode under the Hospital Information System is convenient, the work efficiency and qualities are improved, which is worthy of popularizing.