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Application of a kind of diterpenoid compound in the preparation of β-glucuronidase activity inhibitor

An activity inhibitor, the technology of aldolase, which is applied in the field of biomedicine and achieves broad application prospects and significant inhibitory activity.

Active Publication Date: 2022-05-24
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no relevant literature report on whether the above-mentioned compounds have β-glucuronidase inhibitory activity; Still a research blank area

Method used

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  • Application of a kind of diterpenoid compound in the preparation of β-glucuronidase activity inhibitor
  • Application of a kind of diterpenoid compound in the preparation of β-glucuronidase activity inhibitor
  • Application of a kind of diterpenoid compound in the preparation of β-glucuronidase activity inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Preparation and identification of compound 1 of Example 1

[0033] 1. Preparation of compound 1

[0034](1) Dried iron begonia (3kg) after cutting and crushing with 95% ethanol 18 liters (25-30 °C) maceration for seven days, filter, filter cake repeated extraction twice (18 liters each time, each time for seven days), combined with the extract and concentrated to dry by reduced pressure, to give extract extract 364.5g;

[0035] (2) Dissolve 364.5g of extract extract extract in 1 liter of chloroform in the above step (1), re-extract 3 times with water (3 liters each), and concentrate the chloroform extract (222g) after taking the organic phase under reduced pressure to dry.

[0036] (3) Step (2) Chloroform extract dissolved with 200mL of dichloromethane, open silica gel column chromatography (silica gel 200-300 mesh, silica gel column diameter d = 13 cm, high h = 60 cm), sequentially in the volume ratio of 20:1, 15:1, 10:1, 7:1, 5:1, 4:1, 3:1, 2:1, 1:1 petroleum ether: ethyl...

Embodiment 2

[0043] Example 2 Compound 1 inhibits EcGUS

[0044] 1. Preparation of β-glucuronidase (EcGUS):

[0045] LB liquid medium: trypsin 10 g / L, yeast extract 5 g / L, sodium chloride 10 g / L, solvent is water, pH 7.0.

[0046] Lysate: 20 mM 4-hydroxyethylpiperazine ethanesulfonic acid (HEPES), 300 mM NaCl, 5 mM imidazole (imidazole), volume concentration 10% glycerol (glycerol), solvent is water, pH 7.4.

[0047] NTA-0 buffer: 20 mM Tris-HCl, 0.5 M sodium chloride, volume solubility 10% glycerol, pH 7.9.

[0048] NTA-20 buffer: 20 mM Tris-HCl, 0.5 M sodium chloride, volume solubility 10% glycerol, 20 mM imidazole, pH 7.9.

[0049]NTA-250 buffer: 20 mM Tris-HCl, 0.5 M sodium chloride, volume solubility 10% glycerol, 250 mM imidazole, pH 7.9.

[0050] E. coli (Escherichia coli BL21 (de3), stored at -80 °C) inoculated into 200 mL lb liquid medium containing 30 μg / mL kanamycin, cultured at 200 rpm, 37 °C to OD600 to reach 0.5, followed by the addition of a final concentration of 100 mM of isop...

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Abstract

The invention relates to the application of a diterpene compound in the preparation of an inhibitor of β-glucuronidase activity. The diterpenoid compound of the present invention is euphominoid C, and described compound has obvious inhibitory action to Escherichia coli β-glucuronidase activity, IC 50 The value is 45.87±1.94 μg / mL, and it has broad application prospects in drug development for the treatment of drug-induced diarrhea caused by irinotecan or non-steroidal anti-inflammatory drugs.

Description

Technical field [0001] The present invention belongs to the field of biomedical technology, particularly relates to the preparation of a diterpenoid isolated from the iron begonia and the application in the preparation of β - glucuronidase inhibitors, the application contributes to the treatment of irinotecan or nonsteroidal anti-inflammatory drugs caused by the development of drug-derived diarrhea drugs. Background [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 glucuronidin (SN-38G) in the liver, and then SN-38G is excreted into the intestine through the bile ducts, and is hydrolyzed into SN-38 by the intestinal bacteria β-glucuronidase, when SN-38 accumulates in the intestine, it will cause severe delayed diarrhea and intestinal damage, seriously affecting the process of chemotherapy. In addition, many NSAIDs containing carboxylic acids such as ketoprofen, diclofen...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/047A61K36/47A61P1/12
CPCA61K31/047A61K36/47A61P1/12Y02A50/30
Inventor 于航飞应优敏占扎君
Owner ZHEJIANG UNIV OF TECH