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Specificity probe substrate of cytochrome P450-3A4 enzyme and application thereof

A technology of cytochrome and probe substrate, which is applied to the specific probe substrate of cytochrome P450_3A4 enzyme and its application field, which can solve the problem of inability to clearly analyze the metabolic clearance ability of cytochrome P4503A4, confusion of the catalytic ability of cytochrome P4503A4, etc. problems, to achieve the effect of good UV absorption characteristics

Active Publication Date: 2015-10-14
GENERAL HOSPITAL OF PLA
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Problems solved by technology

However, recent studies have found that the catalytic ability of cytochrome P4503A5 in some individuals is even comparable to that of cytochrome P4503A4 (Williams, et.al., 2002). Confuse the catalytic ability of cytochrome P4503A4 and 3A5, so that the metabolic clearance ability of cytochrome P4503A4 for a drug cannot be clearly analyzed

Method used

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  • Specificity probe substrate of cytochrome P450-3A4 enzyme and application thereof
  • Specificity probe substrate of cytochrome P450-3A4 enzyme and application thereof
  • Specificity probe substrate of cytochrome P450-3A4 enzyme and application thereof

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Embodiment Construction

[0025] The following examples are intended to further illustrate the invention without limiting its scope.

[0026] Tenuifoliside A was used to detect the effect of ketoconazole on CYP3A4 activity in human liver microsomes

[0027] Using Tenuifoliside A to detect the inhibitory effect of ketoconazole as a CYP3A specific inhibitor on CYP3A4, the specific steps are as follows:

[0028] (1) In 200 μL in vitro metabolic reaction system, 10 mM glucose-6-phosphate, 1 unit of glucose-6-phosphate dehydrogenase, and 4 mM MgCl 2 , the concentration of human liver microsomes is 0.2 mg / ml, the concentration of Tenuifoliside A is 10 μM, and the concentration of ketoconazole is 1 μM, pre-incubated at 37°C for 5 minutes;

[0029] (2) Add 20μl NADP to the reaction system + (final concentration 1mM) initial reaction;

[0030] (3) After 20 minutes, add 100 μl of acetonitrile, shake vigorously, and terminate the reaction;

[0031] (4) Using a high-speed refrigerated centrifuge, under the con...

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Abstract

The invention provides a specificity probe substrate Tenuifoliside A of cytochrome P450-3A4 enzyme and application thereof in CYP3A4 enzyme activity measurement. The enzyme activity measurement includes the following operation processes: (1) with the Tenuifoliside A as the high-specificity probe substrate, carrying out a CYP catalytic reaction of a specificity substrate by means of a CYP in-vitro incubation system; and (2) quantitatively detecting the product generation amount or substrate consumption amount in unit time for determining the activity of the CYP3A4 enzyme in various bio-samples and cells. The specificity probe substrate can be used for quantitative evaluation of the CYP3A4 enzyme activity in the bio-samples from different individual sources, and quantitative measurement of the CYP3A4 single-enzyme activity of cell culture fluids and cell prepared products from different animal tissue cell sources.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an oligosaccharide ester compound Tenuifoliside A, which can be used as a specific probe substrate for cytochrome P4503A4 enzymes for quantitative determination of cytochrome P4503A4 enzyme activities in biological samples from different sources, in order to achieve Assessment of the ability of the important drug-metabolizing enzyme CYP3A4 to dispose of drugs. Background technique [0002] The cytochrome P450 enzyme (Cytochrome P450, CYP) superfamily includes the most important drug-metabolizing enzymes in the body, and participates in the metabolism of more than 80% of marketed drugs, of which about 50% are metabolized by the cytochrome P4503A subfamily. Four isoforms of cytochrome P4503A are expressed in the human body, namely cytochrome P4503A4, P4503A5, P4503A7 and P4503A43. Cytochrome P450 3A4 accounts for 30-60% of the total cytochrome P450 enzyme content (Huk...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12Q1/26
Inventor 刘屏董瑞华李照亮董宪喆穆丽华王东晓
Owner GENERAL HOSPITAL OF PLA
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