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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
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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
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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.
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