RESUMEN
In this study, twenty-four oleanolic acid (OA) derivatives were rationally designed based on molecule docking studies and their VEGFR-2 inhibitory activities were tested by Homogeneous time-resolved fluorescence (HTRF) method in vitro. All of the synthesized compounds were identified as new compounds, and the structures of these compounds were determined by 1H-NMR and ESI-MS. In the screening for VEGFR-2 inhibitors, compounds I6 and I7 exhibited excellent inhibitory effect. The results indicated that insertion of phenylurea group with a linker at position C-28 of OA can increase the activity against VEGFR-2 significantly. [Formula: see text].
Asunto(s)
Ácido Oleanólico , Proliferación Celular , Diseño de Fármacos , Simulación del Acoplamiento Molecular , Estructura Molecular , Ácido Oleanólico/farmacología , Relación Estructura-Actividad , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismoRESUMEN
Surface plasmon resonance (SPR) technology has effectively bolstered optic fiber sensing in fields of life science, clinical diagnosis, medicine, food safety and so on. The current review outlines the research status of fiber optic biosensor based on SPR, and the merits of optical fiber sensor and the development of optical fiber sensor based on SPR are completely covered. An in-depth review of four devices for generating SPR is presented, and optical fiber is finally adopted for a substrate to generate SPR. Different prototypes of optical fiber biosensor based on SPR are meticulously outlined: optical fiber grating biosensor based on SPR and optical fiber structured type biosensor based on SPR, and representative instances from literature are presented to verify the latest advancements in this potentially valuable research avenue. In addition, the sensing performance of different optical fiber structured type biosensor based on SPR are compared. What's more, simultaneous multi-parameter detection and improvement of sensitivity are discussed and summarized. The article concludes identify key challenges and develop orientation of optical fiber biosensor based on SPR.