首页> 外国专利> FLUORESCENT PROBE SUBSTRATE FOR DETECTING ACTIVITY OF HUMAN INTESTINE CARBOXYLESTERASE, AND USES THEREOF

FLUORESCENT PROBE SUBSTRATE FOR DETECTING ACTIVITY OF HUMAN INTESTINE CARBOXYLESTERASE, AND USES THEREOF

机译:荧光探针基质,用于检测人肠道羧化酶的活性,及其用途

摘要

A fluorescent probe substrate for detecting the activity of human intestine carboxylesterase and uses thereof, which relate to the technical field of pharmaceuticals. The specific probe substrate is an aromatic ester (TCFE for short) of (E)-2-(4-(4-hydroxybenzene vinyl)-3-cyan-5,5-dimethylfuran-2(5H)-subunit)malononitrile (TCF for short). The substrate can be used for quick quantitative detection of the activity of the human intestine carboxylesterase and for quick screening and estimation of an inhibitor of the human intestine carboxylesterase. The process of the quick quantitative detection of the activity of the human intestine carboxylesterase comprises: selecting a TCFE hydrolysis reaction as a probe reaction, adding a proper substrate into a buffer system comprising hCE2, and determining the actual activity of hCE2 enzyme in each in-vitro organism sample by quantitatively detecting the production of a hydrolysis metabolism product TCF in a unit time in a linear reaction interval. The probe has good selectivity, the hydrolysis product TCF has a long fluorescence emission wavelength (612 nm), and the probe can reduce background fluorescence of the organism sample and increase the sensitivity, and has good practicability and application prospect.
机译:一种用于检测人肠道羧酸酯酶活性的荧光探针底物及其用途,涉及药物技术领域。特定的探针底物是(E)-2-(4-(4-羟基苯乙烯基)-3-氰基-5,5-二甲基呋喃-2(5H)-亚基)丙二腈(TCF)的芳族酯(简称TCFE)简称)。该底物可用于快速定量检测人肠羧酸酯酶的活性,并用于快速筛选和估计人肠羧酸酯酶的抑制剂。快速定量检测人肠羧酸酯酶活性的过程包括:选择TCFE水解反应作为探针反应,向包含hCE2的缓冲系统中添加合适的底物,并确定每种in-hCE2酶的实际活性。通过在线性反应间隔内单位时间内定量检测水解代谢产物TCF的产生来获得体外生物样品。该探针具有良好的选择性,水解产物TCF具有较长的荧光发射波长(612nm),可减少生物样品的背景荧光并提高灵敏度,具有良好的实用性和应用前景。

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