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Application of a kind of iridoid glycoside compound in preparation of β-glucuronidase inhibitor

An aldolidase and compound technology, applied in the field of biomedicine, can solve the problems of drug-induced diarrhea, affecting the chemotherapy process, delayed diarrhea, etc., and achieve the effect of significant inhibitory activity and broad application prospects

Active Publication Date: 2021-10-15
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When it enters the human body, it will be metabolized into inactive SN-38 glucuronide (SN-38G) in the liver, and then SN-38G will be excreted into the intestinal tract through the bile duct, and will be absorbed by intestinal bacteria β-glucuronide Enzymatic hydrolysis into SN-38, when SN-38 accumulates in the intestinal tract, it will cause severe delayed diarrhea and intestinal damage, which will seriously affect the chemotherapy process
In addition, many NSAIDs containing carboxylic acids, such as ketoprofen, diclofenac, and indomethacin, can cause similar intestinal toxicity, which can cause severe drug-induced diarrhea

Method used

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  • Application of a kind of iridoid glycoside compound in preparation of β-glucuronidase inhibitor
  • Application of a kind of iridoid glycoside compound in preparation of β-glucuronidase inhibitor
  • Application of a kind of iridoid glycoside compound in preparation of β-glucuronidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Screening of EcGUS inhibitors

[0022] (1) Preparation of EcGUS:

[0023] Inoculate Escherichia coli BL21 (DE3) stored at -80°C into 200 mL of LB liquid medium containing 30 μg / mL kanamycin (trypsin 10 g / L, yeast extract 5 g / L, sodium chloride 10g / L, the solvent is water, pH7.0), cultivated at 200rpm, 37°C until the OD600 reaches 0.5, and then add isopropyl-β-D-thiogalactopyranoside (IPTG) at a final concentration of 100mM, Cultivate overnight at 200 rpm and 30°C to induce the expression of EcGUS (SDS-PAGE electrophoresis can detect the expression of the enzyme). After the expression is completed, centrifuge the culture solution at 4°C and 9000rpm for 5 minutes to collect the bacteria, then wash the bacteria with PBS (pH 7.4) 2-3 times, and then press the volume of the original bacteria solution (culture solution before centrifugation) 1 / 10 of lysate (20mM 4-hydroxyethylpiperazineethanesulfonic acid (HEPES), 300mM NaCl, 5mM imidazole (imidazole), volume con...

Embodiment 2

[0044] Example 2: Research on the type of inhibition of EcGUS by compounds 7, 8, 9, and 10

[0045] The four compounds with the best inhibitory activity in rescreening were selected, namely compounds 7, 8, 9, and 10. Their structures were all similar, and compound 9 had the best inhibitory activity. Inhibitors were prepared with PBS into solutions with a series of concentration gradients, and substrates were also prepared with PBS into solutions with concentrations of 2, 3, 5, and 10 mM, that is, the final concentrations were 200, 300, 500, and 1000 μM. Taking compound 7 as an example to make Table 2, the prepared solubility gradient is 0, 100, 200, 300, 400 μM, that is, the final concentration is 0, 10, 20, 30, 40 μM (see Table 2);

[0046] Table 2 The permutation and combination table of different solubility points of substrate and compound 7

[0047]

[0048] Note: C PNPG Indicates the final solubility of the substrate, C In Indicates the final solubility of the inhib...

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PUM

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Abstract

The invention discloses an application of an iridoid glycoside compound in the preparation of an inhibitor of β-glucuronidase activity. The iridoid glycoside compound extracted from baobab pulp in the present invention is effective against Escherichia coli β-glucuronidase activity inhibitor. ‑Glucuronidase inhibitory activity significant, IC 50 The value range is 20.7‑34.0 μM, and it has broad application prospects in the research and development of drugs for the treatment of drug-induced diarrhea caused by irinotecan or non-steroidal anti-inflammatory drugs.

Description

(1) Technical field [0001] The present invention relates to a new application of baobab fruit pulp extract, in particular to the application of iridoid glycosides in the preparation of β-glucuronidase inhibitors, which is helpful for the treatment of irinotecan or non-steroidal The research and development of drugs for drug-induced diarrhea caused by body-like anti-inflammatory drugs belongs to the field of biomedical technology. (2) Background technology [0002] Irinotecan (CPT-11), is a commonly used drug for the treatment of colon cancer. When it enters the human body, it will be metabolized into inactive SN-38 glucuronide (SN-38G) in the liver, and then SN-38G will be excreted into the intestinal tract through the bile duct, and will be absorbed by intestinal bacteria β-glucuronide Enzymatic hydrolysis into SN-38, when SN-38 accumulates in the intestinal tract, it will cause severe delayed diarrhea and intestinal damage, seriously affecting the chemotherapy process. I...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61P1/12
CPCA61K31/7048A61P1/12Y02A50/30
Inventor 魏斌周涛顺李行诺华露霞
Owner ZHEJIANG UNIV OF TECH
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