Abstract：
A novel chalcone derivative (4-(5-(pyridin-2-yl)-4,5-dihydro-1H-pyrazol-3-yl) phenol (PDP) was synthesized, characterized and investigated for its potential as a fluorescent probe. The structure of the synthesized molecule was determined by FTIR, 1H NMR, 13C NMR and LC-MS/MS. The interactions of PDP with fluorescent dyes in aqueous SDS environment and HSA were studied by using fluorescence resonance energy transfer (FRET) technique and steady-state and time-resolved fluorescence spectroscopy techniques. In addition, the cytotoxic effects of PDP against various cell lines (MCF -7, HT -29, and 3 T3-L1) as well as their corresponding healthy cell lines were tested by MTT assay and visualization of FRET efficiency of PDP in vitro was monitored by confocal microscopy. MTT assay showed that PDP has no significant cytotoxic effect on HT -29 cancer cells and moderate cytotoxicity on MCF -7 and 3 T3-L1 cells even at a concentration of 250 μM. Combining confocal microscopes with the FRET technique showed that PDP significantly stained the cytoplasm of MCF -7 cell lines. These results suggest that PDP could be used in fluorescence microscopy for cell staining.
摘要：
合成了一种新型的查耳酮衍生物(4-(5-(吡啶-2-基)-4,5-二氢-1H-吡唑-3-基)苯酚(PDP),表征和研究了其作为荧光探针的潜力。通过FTIR测定合成分子的结构,1HNMR,13CNMR和LC-MS/MS。利用荧光共振能量转移（FRET）技术以及稳态和时间分辨荧光光谱技术研究了PDP与水性SDS环境中荧光染料和HSA的相互作用。此外,通过MTT试验测试了PDP对各种细胞系（MCF-7，HT-29和3T3-L1）及其相应的健康细胞系的细胞毒性作用，并通过共聚焦显微镜监测了PDP体外FRET效率的可视化。MTT分析表明，即使浓度为250μM，PDP对HT-29癌细胞没有明显的细胞毒性作用，对MCF-7和3T3-L1细胞也没有中等的细胞毒性。将共聚焦显微镜与FRET技术相结合显示PDP显著染色MCF-7细胞系的细胞质。这些结果表明PDP可用于荧光显微镜的细胞染色。
