Effect of Ershiwuwei Zhenzhu Tablets on Microvascular Function in Zebrafish / 中国实验方剂学杂志

Objective:To explore the effect of Ershiwuwei Zhenzhu tablets (EZT) on microvascular function. Method:The zebrafish models of thrombosis, microvascular defect and vascular endothelial injury were induced by using arachidonic acid, simvastatin and ponatinib respectively, and treated with EZT, astragaloside or asprin. To evaluate the protective effect of EZT on vascular endothelium and its effect on thrombus formation, zebrafish heart output and blood flow velocity were counted, and the vascular area of the zebrafish intestine and the intervascular diameter were calculated. The thrombus in the tail vein was observed under microscope. Result:Compared with model group,EZT improved the cardiac output (PP-1, and promoted angiogenesis in zebrafish at concentrations of 0.11, 0.33, 1 mg·L-1. Compared with the model group, the vascular diameter of the zebrafish internode was significantly increased at the concentrations of 33 mg·L-1 (P-1 (P-1(PConclusion:EZT could improve microvascular dysfunction, and its mechanism may be related to the reduction of vascular endothelial damage to promote its angiogenesis and the improvement of microvascular hemodynamics to reduce thrombus formation.

Design, synthesis and biological evaluation of pyrrolo-pyridine derivatives as HIV-1 integrase inhibitors / 国际药学研究杂志

Objective To design and synthesze novel pyrrolopyridine as integrase inhibitors. Method The launched anti-HIV drug raltegravir was selected as template compounds. According to the concept of bioisosterism and molecular docking, a series of pyrrolopyridine compounds (6a-6t) were designed, synthesized and their anti-integrase 3’-processing activity were analyzed. Results The designed compounds were successfully synthesized and the structures of these compounds were confirmed by 1H NMR, 13C NMR and ESI-HRMS. The anti-IN 3’-P activity of these compounds were also measured. The binding mode and docking energy of representative compounds were analyzed. Conclusion The structure-activity relationships of these compounds were also analyzed by the results of docking. These results lay the foundation for the further optimization of these compounds.

Design,synthesis and biological evaluation of pyrrolo-pyridine derivatives as HIV-1 integrase inhibitors / 国际药学研究杂志

Objective To design and synthesze novel pyrrolopyridine as integrase inhibitors. Method The launched anti-HIV drug raltegravir was selected as template compounds. According to the concept of bioisosterism and molecular docking ,a series of pyrrolopyridine compounds(6a-6t)were designed,synthesized and their anti-integrase 3′-processing activity were analyzed. Re?sults The designed compounds were successfully synthesized and the structures of these compounds were confirmed by 1H NMR,13C NMR and ESI-HRMS. The anti-IN 3′-P activity of these compounds were also measured. The binding mode and docking energy of rep?resentative compounds were analyzed. Conclusion The structure-activity relationships of these compounds were also analyzed by the results of docking. These results lay the foundation for the further optimization of these compounds.