Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Application of diterpenoid compound in preparation of beta-glucuronidase activity inhibitor

An activity inhibitor, aldolidase technology, applied in the field of biomedicine

Active Publication Date: 2021-09-14
ZHEJIANG UNIV OF TECH
View PDF2 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of diterpenoid compound in preparation of beta-glucuronidase activity inhibitor
  • Application of diterpenoid compound in preparation of beta-glucuronidase activity inhibitor
  • Application of diterpenoid compound in preparation of beta-glucuronidase activity inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Preparation and Identification of Example 1 Compound 1

[0033] 1. Preparation of Compound 1

[0034] (1) After cutting and crushing the dried Tie Haitang (3kg), leaching with 18 liters of 95% ethanol at room temperature (25-30°C) for seven days, filtered, and repeated leaching of the filter cake twice (18 liters each time, seven days each time) , combined the extracts and concentrated to dryness under reduced pressure to obtain 364.5 g of extract extract;

[0035] (2) Dissolve 364.5 g of the extract extract from the above step (1) in 1 liter of chloroform, back-extract 3 times with water (3 liters each), take the organic phase and concentrate it to dryness under reduced pressure to obtain a chloroform extract (222 g) .

[0036] (3) step (2) chloroform extract is dissolved with 200mL dichloromethane, carries out open silica gel column chromatography (silica gel 200-300 order, silica gel column diameter d=13cm, height h=60cm), successively with volume ratio as 20: 1, ...

Embodiment 2

[0043] Example 2 The inhibitory effect of compound 1 on EcGUS

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

[0045] LB liquid medium: trypsin 10g / L, yeast extract 5g / L, sodium chloride 10g / L, solvent is water, pH7.0.

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

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

[0048] NTA-20 buffer: 20mM Tris-HCl, 0.5M sodium chloride, volume solubility 10% glycerol, 20mM imidazole, pH7.9.

[0049] NTA-250 buffer: 20mM Tris-HCl, 0.5M sodium chloride, volume solubility 10% glycerol, 250mM imidazole, pH7.9.

[0050] Inoculate Escherichia coli (Escherichia coli BL21 (DE3), stored at -80°C) into 200 mL of LB liquid medium containing 30 μg / mL kanamycin, and cultivate it at 200 rpm and 37°C until the OD600 reaches 0.5, then add Isopropyl-β-D-thiogalactopyranoside (IPTG) wit...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to application of a diterpenoid compound in preparation of a beta-glucuronidase activity inhibitor. The diterpenoid compound disclosed by the invention is euphominoid C; the compound has an obvious inhibition effect on the activity of beta-glucuronidase of escherichia coli; the IC50 value is 45.87 + / - 1.94 mu g / mL; and the diterpenoid compound has a wide application prospect in the aspect of research and development of medicines for treating drug-induced diarrhea caused by irinotecan or non-steroidal anti-inflammatory drugs.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a diterpenoid compound isolated and prepared from Tiegua and its application in the preparation of β-glucuronidase inhibitors. Development of drugs for drug-induced diarrhea caused by non-steroidal anti-inflammatory drugs. Background technique [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. In addition, taking many NSAIDs containing carboxylic acids such as ketoprofen, diclofenac, and indometh...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com