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Application of deacetylated cinobufagin as a specific probe substrate for ugt1a4-catalyzed o-glucuronide conjugation

A technology of deacetylated cinobufagin and UGT1A4, which is used in the field of application of deacetylated cinobufagin as a specific probe substrate for UGT1A4 catalyzed O-glucuronic acid conjugation reaction, which can solve the problems of inability to catalyze , to achieve the effect of low toxic and side effects, single metabolite, and strong specificity

Active Publication Date: 2017-06-16
DALIAN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

That is, the prior art clearly shows that the UGT subtype cannot catalyze the glucuronidation reaction of the 3-hydroxyl group of deacetylated cinobufagin

Method used

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  • Application of deacetylated cinobufagin as a specific probe substrate for ugt1a4-catalyzed o-glucuronide conjugation
  • Application of deacetylated cinobufagin as a specific probe substrate for ugt1a4-catalyzed o-glucuronide conjugation
  • Application of deacetylated cinobufagin as a specific probe substrate for ugt1a4-catalyzed o-glucuronide conjugation

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Embodiment Construction

[0017] Experiment 1: Deacetylated cinobufagin used in the determination of UGT1A4 enzyme activity in human liver microsomes

[0018] Different concentrations of deacetylated cinobufagin (5, 10, 20, 50, 100, 150, 200, 300, 400, 600, 800 μM) were incubated with human liver microsomes (5.0 mg / ml) at 37°C (the incubation system contained 50 mM Tris-Hcl, 50 mM MgCl 2 , 2mM UDPGA, pH 7.4; the total volume is 200 μl;) 60 min, stop the reaction with 1 / 2 volume methanol, 20000 g Centrifuge for 20 minutes, take the supernatant and inject samples to analyze the amount of metabolites generated, calculate the reaction rate as the ordinate, and take the substrate concentration as the abscissa to obtain the following formula: figure 1 The kinetic curve of deacetylated cinobufagin in mixed human liver microsomes is shown, and then the curve in the inset is obtained by the Eadie–Hofstee plotting method, and the deacetylation of human liver microsomes is obtained by linear fitting. Cinobufagin...

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Abstract

The invention discloses an application of deacetylate cinobufagin used as a specific probe substrate for catalysis of UGT1A4 for binding reaction of O-glucuronic acid. The application can be used for calibrating the activities of catalyzing the binding reaction of O-glucuronic acid by UGT1A4 single enzymes from various sources, and quantitatively determining the activity of catalyzing the binding reaction of O-glucuronic acid by the UGT1A4 in prepared products such as microsomes and S-9 from various mammal tissue and organ sources. The application can be applied to predication and evaluation of a compound taking the mode of catalyzing the binding reaction of O-glucuronic acid by the UGT1A4 as a main way in searches on the metabolic clearance rate of a specific organism and the medicine-medicine interactions induced by the binding reaction of O-glucuronic acid mediated by the UGT1A4, and has the advantages of higher specificity, single metabolite, low toxic and side effects, low price, availability and the like.

Description

technical field [0001] The invention relates to a new application of deacetylated cinobufagin, especially the application of deacetylated cinobufagin as a specific probe substrate for UGT1A4 catalyzed O-glucuronic acid binding reaction. Background technique [0002] UDP-glucuronosyltransferases (UDP-glucuronosyltransferases, UGT) are a class of phase II metabolic enzymes that catalyze the binding reaction between the substrate and the endogenous cofactor uridine diphosphate-glucuronic acid (UDPGA), making it Increased water solubility facilitates elimination from the body. UGT is mainly expressed in liver, kidney, intestine and other important metabolic and excretory organs of the body, not only involved in the metabolism of endogenous substances such as bilirubin, steroid hormones, thyroid hormones, bile acids and fat-soluble vitamins, but also , analgesics, non-steroidal anti-inflammatory drugs and anticonvulsants and other drugs play an important role in the metabolism p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C12Q1/48
Inventor 马骁驰霍晓奎王超田象阁姜丽王长远张宝璟黄珊珊邓卅
Owner DALIAN MEDICAL UNIVERSITY
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