Application of oxymetazoline as special substrate for glucuronyl transferase UGT1A9

A technology of glucuronic acid and oxymetazoline, applied in the field of medicine, can solve the problem that the substrate does not have enzyme specificity, and achieve the effects of remarkable technical performance, good industrialization prospect and easy detection.
CN104178554AInactive Publication Date: 2014-12-03JINAN UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
JINAN UNIVERSITY
Publication Date
2014-12-03
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses application of oxymetazoline as a special substrate for glucuronyl transferase UGT1A9. The oxymetazoline used as the substrate is subjected to glucuronatation reaction in a biological system, and the elimination quantity of the substrate or the generation quantity of the glucuronatation product in unit time is quantitatively detected to determine the UGT1A9 enzyme activity in the biological system. The oxymetazoline can also be used for evaluating the disposition capacity of the UGT1A9 enzyme for the drugs in the human liver microsome. The oxymetazoline has high UGT metabolizing enzyme selectivity (only metabolized by UGT1A9), thereby preventing the oxymetazoline from being influenced by other metabolizing enzymes when being used as the special substrate. Besides, the glucuronatation of the oxymetazoline has the characteristics of metabolite singleness, and easy detection of the metabolites and the like.
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Description

technical field

[0001] The invention belongs to the technical field of medicine, and specifically relates to the application of a compound oxymetazoline as a specific substrate of glucuronosyltransferase UGT1A9. Background technique

[0002] The glucuronidation reaction catalyzed by glucuronosyltransferases (UDP-glucuronosyltransferases, UGTs) is the main way of metabolism of exogenous and endogenous substances in the human body. After the glucuronidation reaction of the substrate, the polarity will generally increase, the activity will decrease, and it will be excreted from the body. Therefore, the glucuronidation reaction is an important detoxification method for the human body. The human glucuronosyltransferase family is systematically divided into four families, including UGT1, UGT2, UGT3 and UGT8. Among them, the most important UGT families related to drugs are UGT1 and UGT2.

[0003] The glucuronidation reaction is catalyzed by glucuronosyltransferase to transfer the...

Claims

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